SUPER PHARMA TABLE

DRUG MOA and INDICATION ADVERSE EFFECTS NOTABLE PROPERTIES

1. AUTONOMIC DRUGS
Cholinomimetics
A. Direct Acting Choline Esters
Muscarinic agonist; activates M1
through M3 receptors in all CNS stimulation, miosis, cyclospasm,
peripheral tissues. Results to brochoconstriction, excessive GI and very short lived DOA: 5-30sec, apidly
i. Acetylcholine increased secretion, smooth muscle GU smooth muscle contraction, hydrolyzed by AChE; acts on both M
contraction (except in vascular increased secretory activity of sweat and N receptors
smooth muscles where it causes gland, airways etc, vasodilation
relaxation) and changes in heart rate
Results in smooth muscle
Muscarinic agonist; activates M1
Cylospasm, diarrhea, urinary contraction except in vascular
through M3 receptors in all
ii.Betanechol urgency, vasodilation, reflex smooth muscles where it causes
peripheral tissues (same as Ach) ; for
tachycardia, sweating relaxation; resistant to AChE, orally
Bladder and bowel atony
active, act on M receptors only
Nonselective muscarinic and
Cylospasm, diarrhea, urinary
nicotinic agonist; similar to acts on both M and N receptors,
iii. Carbachol urgency, vasodilation, reflex
betanechol; used topically for DOA: 30mins-2hrs
tachycardia, sweating
glaucoma treatment
B. Direct Acting Muscarinic Alkaloids
Partial muscarinic agonist; used for
good lipid solubility compared to
i. Pilocarpine treatment of Glaucoma, Sjogren's Miosis, blurring of vision
choline esters
syndrome and Sicca syndrome
C. Direct Acting Nicotinic Agonists
Agonist at both NN and NM
receptos; activates autonomic post
Generalized ganglionic stimulation
ganglionic neurons (both Able to enter the CNS and activates
i. Nicotine (hypertension, tachycardia, nausea,
sympathetic and parasympathetic) NN receptors ; DOA: 1-6h only
vomiting, diarrhea)
and skeletal muscle neuromuscular
end plates ; for Smoking Cessation
Selective partial agonist at nicotinic Generalized ganglionic stimulation
ii. Varenicline receptors; used exclusively for (hypertension, tachycardia, nausea, longer DOA than nicotine: 12-24h
smoking cessation vomiting, diarrhea)
D. Short Acting Cholinesterase Inhibitor (Alcohol)
Binds briefly to active site of
acetylcholinesterase (AChE) and
prevents access of acetylcholine
(Ach); Amplifies all actions of Ach; Miosis, salivation, nausea, vomiting, parenteral, very short lived DOA: 5-
i. Edrophonium
increases parasympathetic activity diarrhea, bradycardia 15min
and somatic neuromuscular
transmission ; for Myasthenia gravis
diagnosis (Tensilon test)
E. Intermediate Acting Cholinesterase Inhbitors (Carbamates)
Forms covalent bonds with AChE,
but is hydrolyzed and released;
Longer acting than Edrophonium ;
Miosis, salivation, nausea, vomiting, poor lipid solubility, oral, DOA:
i. Neostigmine for Myasthenia gravis treatment;
diarrhea, bradycardia 30min-2h
reversal of nondepolarizing
muscular blockade, Ogilvie
syndrome
Longer acting effect compared to Miosis, salivation, nausea, vomiting,
ii. Pyridostigmine poor lipid solubility, oral, DOA: 4-8h
Neostigmine diarrhea, bradycardia
Natural alkaloid tertiary amine, Miosis, salivation, nausea, vomiting, good lipid solubility: able to enter
iii. Physostigmine
similar to neostigmine diarrhea, bradycardia the CNS, DOA: 4-8h
F. Long Acting Cholinesterase Inhibitors (Organophosphates)
Similar to neostigmine but with Miosis, salivation, nausea, vomiting, moderate lipid solubiliy, DOA: 2-
i. Echothiophate
slower release diarrhea, bradycardia 7days
malathion: scabicide, parathion: Miosis, salivation, nausea, vomiting,
ii. Malathion, Parathion high lipid solubiliy, DOA: 7-30 days
insecticide diarrhea, bradycardia
Cholinoceptor Blocking Drugs
Drowsiness, blurring of vision, dry
Competitively blocks all muscarinic known as Hyoscine-N-Butyl-Bromide
i. Scopolamine eyes, constipation, dry mouth,
receptors, antagonizes histamine (Buscopan)
urinary retention

Page 1 of 56
 and serotonin ; for motion sickness,
dec. acid secretion in the GIT
Nonselective competitive
antagonism at all muscarinic
receptors in the CNS and peripheral
tissues; causes mydriasis and
cycloplegia; mandatory antidote for Tachycardia, mydriasis, cyloplegia,
DOC for organophosphate
severe cholinesterase inhibitor skin flushing, delirium,
ii. Atropine poisoning; notorious for causing
poisoning ; Mydriatic, cycloplegic, hallucinations, urinary retention,
hyperthermia
antidote for organophosphate constipation
poisoning (DOC), for bradycardia,
hypersalivation and to decrease
airway secretion during general
anesthesia
Similar to atropine but with a
shorter duration of action (12-24h) ;
iv. Homatropine Mydriatic, cycloplegic
Mydriatic, cycloplegic in eye
examinations
Similar to atropine but with a
shorter duration of action (3-6h),
v. Cyclopentolate Mydriatic, cycloplegic
Mydriatic, cycloplegic in eye
examinations
Similar to atropine but with the
shortest duration of action (15- shorter DOA among cholineceptor
vi. Tropicamide
60min); Mydriatic, cycloplegic in eye blockers (15-60min)
examinations
Competitive nonselective antagonist not as effective as SABAs but less
vii. Ipratropium at muscarinic receptors ; for BA and Dry mouth, cough, nasal dryness tachycardia and arrhythmia ; few
COPD muscarinic effects outside the lungs
not as effective as SABAs but less
Similar to Ipratropium but with
viii. Tiotropium Dry mouth, cough, nasal dryness tachycardia and arrhythmia ; few
longer duration of action
muscarinic effects outside the lungs
Nonselective muscarinic antagonist
Tachycardia, mydriasis, cyloplegia,
which reduces detrussor smooth
skin flushing, delirium, for urinary urgency and
ix. Oxybutinin muscle tone spasms ; for decreasing
hallucinations, urinary retention, incontinence
urgency in mild cystitis and dec.
constipation
bladder spasm after urologic surgery
Regenerates active Must be administered before 6-8
acetylcholinesterase; can relieve hours of organophosphate bond
x. Pralidoxime skeletal muscle and endplate block ; muscle weakness with cholinesterase occurs ; has
Usual antidote for early stage oxime group which has high affinity
cholinesterase inhibitor poisoning for phosphorus
Competitively blocks all Nn nicotinic Postural hypotension, dry mouth,
xi. Hexamethonium, first successful agents in treating
Ach receptors ; for Hypertensive blurred vision, constipation, sexual
Mecamylamine, Trimethaptan HTN
emergencies (obsolete) dysfunction
Sympathomimetics
Non-selective, direct acting
sympathomimetic; activates A and B
adrenergic receptors; A1 -
vasoconstriction and increased BP; DOC for Anaphylaxis ; inactive per
Hypertension, tachycardia, ischemia,
i. Epinephrine B1 - increased HR, conduction and orem ; do not enter CNS significantly
hyperglycemia
contractility; B2 - bronchodilatation ; short DOA
; used for Cardiac arrest,
anaphylaxis, asthma, COPD,
Hemostasis
Non-selective, direct acting
sympathomimetic; activates A and B Compensatory vagal reflexes tend to
adrenergic receptors; A1 - overcome the direct postive
Extreme vasospasm, tissue necrosis,
vasoconstriction and increased BP; chronotropic effects ; alpha activity
ii. Norepinephrine excessive BP increase, arrhythmias,
B1 - increased HR, conduction and > beta activity; inactive per orem ;
infarction, reflex bradycardia
contractility; B2 - bronchodilatation do not enter CNS significantly ; short
; used for Neurogenic shock, DOA
cardiogenic shock
Non-selective, direct acting
Cardiovascular disturbances, inactive per orem ; do not enter CNS
iii. Dopamine sympathomimetic; activates A, B
arrhythmias significantly ; short DOA; very
and D1 adrenergic receptors; A1 -

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 vasoconstriction and increased BP; effective in renal failure associated
B1 - increased HR, conduction and with shock
contractility; D1 - vasodilation in
splanchnic and renal blood vessels ;
for cardiogenic Shock and heart
failure
Beta nonselective
sympathomimetic; nonselectively
activates B adrenergic receptors; B1 Cardiovascular disturbances, synthetic catecholamine, not readily
iv. Isoproterenol
- increased HR, conduction and arrhythmias taken up into nerve endings
contractility; B2- bronchodilatation ;
for Asthma
A1 agonist used for short term
maintenance of BP in acute
Rebound nasal congestion (Rhinitis
hypotension; also used intranasally
vi. Phenylephrine medicamentosa), hypertension, Mydriasis without cycloplegia
to produce local vasoconstriction as
stroke, MI
a decongestant ; mydriatic, for drug-
induced hypotension, spinal shock
A2 agonist that inhibits adenylyl
cyclase and interacts with other
intracellular pathways; marked When taken per orem, there is initial
Sedation, rebound hypertension, dry
vii. Clonidine vasodilation by central inc in BP then will go down once the
mouth
sympatholytic effect ; for drug enters the CNS
Hypertension, Cancer pain, opioid
withdrawal
Central sympatholytics analogous to
viii. Methyldopa, Guanfacine and Sedation, positive Coomb's test Methyldopa - positive Coomb's test
clonidine ; Methyldopa is used for
Guanabenz (Hemolytic anemia) (Hemolytic anemia)
Pre-eclampsia
A2 agonist; reserved for
eye discomfort, hyperemia and
xi. Apraclonidine, Brimonidine ophthalmologic use in glaucoma for NONE
pruritus, blurred vision
reduction of intraocular pressure
B1 agonist that activates adenylyl
Tachyarrhythmia, Hypertension,
cyclase, increasing myocardial
Eosinophilic myocarditis, Premature
contractility; with positive inotropic
xii. Dobutamine ventricular beats, Angina, Dyspnea, Beta1 selective
effect ; Clinically used for
Fever, Headache, Nausea,
cardiogenic shock and acute heart
Palpitation
failure
B2 agonist with adenylyl cyclase
Nausea , Fever, Bronchospasm,
activation; results to bronchial Rapid development of tolerance;
xiii. Albuterol/Salbutamol Vomiting, Headache, Dizziness,
smooth muscle dilation ; for DOC as Asthma reliever
Cough, Allergic reactions
Bronchial Asthma
Angina, Cardiac dysrhythmia,
D1 agonist that activates adenylyl
Dizziness, Flushing, Heart failure,
xiv. Fenoldopam cyclase; results to vascular smooth D1 agonist
Hypotension, Myocardial infarction,
muscle relaxation ; for Hypertension
Tachycardia
D2 agonist that inhibits adenylyl
cyclase and interacts with other
Nausea, Hypotension, Headache,
xv. Bromocriptine intracellular pathways; restores D2 agonist
Dizziness
dopamine actions in the CNS for
Parkinson's disease, prolactinemia
Sympatholytics
Irreversibly blocks A1 and A2
receptors resulting to indirect
baroreflex activation. Decreases Orthostatic hypotension, Reflex
i. Phenoxybenzamine Irreversible blockade
blood pressure but increases heart tachycardia, GI irritation
rate due to baroreflex activation ;
for Pheochromocytoma
Reversible A1 and A2 receptor
antagonist with low half life ; for Orthostatic hypotension, Reflex
ii. Phentolamine Reversible blockade
Pheochromocytoma and Rebound tachycardia, GI irritation
hypertension
Blocks A1 but not A2 receptors; Dizziness, Drowsiness, Headache,
leads to reduction in blood pressure Weakness, Asthenia, Nausea, Used in patients with HTN and BPH
iii. Prazosin, Doxazosin, Terazosin
; for Benign Prostatic Hyperplasia, Palpitation, Edema, Orthostatic at the same time
Hypertension hypotension

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iv. Tamsulosin
vi. Labetalol
vii. Propranolol, Nadolol, Timolol
viii. Metoprolol, Atenolol,
Alprenolol, Betaxolol, Nebivolol
x. Pindolol, Acebutolol, Carteolol,
Bopindolol, Oxprenolol, Celiprolol,
Penbutolol
xi. Carvedilol, Medoxalol,
Bucindolol, Labetalol
xii. Esmolol
2. CARDIOVASCULAR-RENAL DRUGS
Antihypertensives
A. Diuretics
i.Thiazide: Hydrochlorothiazide,
Chlorthalidone, Metolazone,
Indapamide
ii. Loop: Furosemide, Torsemide,
Bumetanide, Ethacrynic Acid
B. Sympathoplegics
i.Sympathetic Outflow Blocker:
Clonidine, Methyldopa
Slightly selective A1a blockade
causing relaxation of prostatic
smooth muscles > vascular smooth
muscle ; for BPH
Beta blockade > A1 blockade; still
with BP depressant effects and
limited HR increase
Blocks B1 and B2 receptors; lowers
both HR and BP and reduces the
release of renin ; for Angina
prophylaxis, hypertension,
arrhythmias, migraine, performance
anxiety, hyperthyroidism
B1 > B2 blockade; lowers both HR
and BP, reduces the release of renin
BUT is considered safer for patients
with asthma ; for Angina
prophylaxis, hypertension,
arrhythmias, migraine, performance
anxiety, hyperthyroidism
B1, B2 with intrinsic
sympathomimetic (partial agonist)
effect; lowers BP with modest
reduction in HR
Beta blockade > A1 blockade; still
with BP depressant effects and
limited HR increase ; for Heart
Failure
B1 > B2 blockade; for rapid control
of BP and arrhythmias,
thyrotoxicosis and myocardial
ischemia intraoperatively ; for
Supraventricular tachycardia
lower BP by decreasing volume and
a direct vascular effect that is not
yet fully understood
Inhibit Na/Cl transporter in distal
convoluted tubule. Cause moderate
diuresis and reduced excretion of
calcium; for mild to moderate
hypertension (FIRST LINE), Heart
failure, Nephrogenic Diabetes
Insipidius, Renal calcium stones
Inhibit Na/K/2Cl transporter in thick
ascending limb of loop of Henle,
Cause powerful diuresis and
increased CA excretion; for heart
failure, hypertension, acute renal
failure, Pulmonary edema,
hypercalcemia, Anion overdose
decrease venous return, decrease
HR, decrease contractile force,
decrease cardiac output, decrease
TPR
activates a2 adrenergic receptors ;
for hypertensive urgency (clonidine),
pre eclampsia (methyldopa)
Headache, Orthostatic hypotension,
Rhinitis, Abnormal ejaculation,
Dizziness, Arthralgia, Infection
Bronchospasm, cardiac depression,
AV block, hypotension, dizziness,
headache; Use in caution with DM
Px: Masks symptoms of
hypoglycemia in diabetics
Hypokalemic metabolic alkalosis,
Dilutional hyponatremia, Potassium
wasting, hyperlipidemia,
hyperuricemia, sulfa allergy,
hyperglycemia, hypercalcemia
Hypokalemic metabolic alkalosis,
Potassium wasting, ototoxicity,
hyperuricemia, nephrotoxicity,
dehydration, hypomagnesemia,
sulfa allergy
dry mouth, sedation, rebound
hypertension, hemolytic anemia: (+)
Coomb's test (methyldopa),
sedation
Slightly selective A1a blockade
causing relaxation of prostatic
smooth muscles > vascular smooth
muscle
safe in pregnant patients
Propranolol has local anesthetic
effect
Nebivolol has vasodilating effect ;
metoprolol reduce moratlity in heart
failure
Pindolol is a partial agonist,
therefore safer in bronchial asthma
Carvedilol reduce mortality in heart
failure
Used in for perioperative thyroid
storm
causes hypercalcemia in contrast
with loop diuretics which cause
hypocalcemia ; FIRST LINE for mild
to moderate hypertension
causes hypocalcemia in contrast
with thiazide diuretics which cause
hypercalcemia
Taper use prior to discontinuation to
avoid rebound hypertension ;
readily enter the CNS
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ii. Ganglion blockers:
Hexamethonium,Trimethaphan
iii. Nerve terminal blockers:
Reserpine, Guanethidine,
Guanadrel
iv. Adrenergic antagonists:
Prazosin,Doxazosin, Terazosin,
Tamsulosin, Silodosin
C. Vasodilators
i. Oral Vasolidator: Hydralazine
Minoxidil
ii. Calcium Channel Blockers
Non-dihydropyridine calcium
channel blocker: Verapamil,
Diltiazem
Dihydropyridine calcium
channel blocker: Nifedipine,
Amlodipine, Nicardipine,
Nisoldipine, Isradipine, Felodipine
iii. Parenteral Vasodilators
Nitroprusside
Diazoxide
causes arteriolar vasolidation of the
afferent and efferent arterioles.
Fenoldopam
Increases renal blood flow; for
hypertensive emergency
D. Angiotensin antagonists and renin inhibitor
i. ACE inhibitors: Captopril,
Enalapril, Lisinopril, Benazepril
ii. Angiotensin receptor blocker:
Losartan, Valsartan, Irbesartan,
Candesartan
iii. Renin inhibitor: Aliskerin
Vasodilators and anti-Angina Pectoris
A. Nitrates
competetively blocks Nn nicotinic
Ach receptors; for hypertension
(obsolete), hypertensive
emergencies
Reserpine Irreversibly blocks the
vesicular monoamine transporter
(VMAT) while Guanethidine and
Guanadrel inhibit the vesicular
release of NE from the presynaptic
neuron; for Hypertension (obsolete)
selectively blocks a1 adrenergic
receptors; for hypertension, benign
prostatic hyperplasia
Release NO from endothelial cells,
Relaxes arteriolar smooth muscle,
causing vasolidation. Decreases
afterload ; for pre-eclampsia,
hypertension, heart failure
Opens K+ channels in vascular
smooth muscle, causing
hyperpolarization, muscle relaxation
and vasolidation; for alopecia / male
pattern baldness, hypertension
block voltage-gated L-type calcium
channels (cardiac > vascular); for
Angina, Supraventricular
tachycardia, migraine, hypertension
block voltage-gated L-type calcium
channels (vascular > cardiac); for
Angina, hypertension
relaxes venous and arteriolar
smooth muscle; for acute heart
failure, controlled hypotension,
cardiogenic shock, hypertensive
emergency
Opens K+ channels in vascular
smooth muscle, causing
hyperpolarization, muscle relaxation
and vasolidation; for hypertension
inhibit angiotensin converting
enzyme ; for hypertension, heart
failure
competetively blocks Angiotensin 1
receptor site ; for hypertension
inhibitor of renin's action on its
substrate angiotensinogen
Postural hypotension, blurred vision,
constipation, dry mouth, sexual
dysfunction
Sedation, suicidal ideation, severe
psychiatric depression
Reflex tachycardia (less chance), first
dose orthostatic hypotension
Edema, myocardial ischemia, drug
induced lupus (hydralazine), reflex
tachycardia
Edema, Angina, Reflex tachycardia,
Pulmonary hypertension,
Pericarditis, Hirsutism, salt and
water retention
Constipation, Nausea,
flushing,gingival hyperplasia, AV
block, sinus node depression,
Pretibial edema, dizziness
Nausea, Flushing, dizziness, pretibial
edema, constipation
hypotension, headache, CN toxicity
hypotension, headache
hypotension, hypokalemia
cough, hyperkalemia, rash,
hypotension, palpitations, renal
damage in patients with preexisting
renal vascular disease but is
protective for DM nephropathy ; CI
in pregnancy
fatigue / weakness, hypoglycemia,
anemia, diarrhea, cough, CI in
pregnancy
diarrhea, cough, rash, hyperkalemia,
increase in serum creatinine, renal
impairment, angioedema
NONE
NONE
Tamsulosin is most selective for
prostatic smooth muscle ; Doxazosin
and Terazosin has longer duration of
action than prazosin
combination treatment with ISDN
for heart failure is more effective
than ACEIs in blacks
require concomitant use of diuretics
and BBs to block compensatory
responses
excessive cardiac depression may
occur
greater vasodilator effect that
cardiodepressant effect
not commonly used because it is
very light sensitive, has short
Duration of action ; given as
continuous infusion
a thiazide derivative without a
diuretic effect ; also reduces insulin
release (can be used to treat
hypoglycemia in insulin-producing
tumors)
short duration of action: 10mins
slows down the progression of DM
nephropathy and cardiac
remodelling in heart failure
as effective as ACEi but less cough
no reproductive toxicity but is also
CI because of the toxicity of ACEi
and ARBs
Page 5 of 56

i. Ultrashort-acting nitrate: Amyl
Nitrite
ii. Short-acting nitrate:
Nitroglycerin, Isosorbide Dinitrate,
Isosorbide Mononitrate
B. Calcium Channel Blockers
i. Non-dihydropyridine calcium
channel blocker: Verapamil,
Diltiazem
ii. Dihydropyridine calcium
channel blocker: Nifedipine,
Amlodipine, Nicardipine,
Nisoldipine, Isradipine, Felodipine
Drugs used in Heart Failure
A. Cardiac Glycoside
i. Digoxin
Anti-Arrhythmics
A. Class 1 Antiarryhtmics
i. Class 1A: Procainamide,
Disopyramide, Quinidine,
ii. Class 1B: Lidocaine, Mexiletene,
Tocainide, Phenytoin
iii. Class 1C: Flecainide,
Propafenone, Encainide, Moricizine
B. Class 2 Antiarrythmics
i. Propranolol, Esmolol
releases nitric oxide (NO), relaxes
smooth muscle, especially vascular,
Reflex tachycardia, Orthostatic inhalational route, but now rarely
increases cGMP (cyclic guanosine
hypotension, methemoglobinemia used
monophosphate); for cyanide
poisoning
releases nitric oxide (NO), increases
cGMP (cyclic guanosine Dangerous hypotension with PDE
Reflex tachycardia, orthostatic
monophosphate) and relaxes inhibitors such as Sildenafil ; First
hypotension, headache, tolerance
smooth muscle especially vascular; Pass effect is ~90% (NTG), NTG also
(transdermal)
for Angina, acute coronary decrease platelet aggregation
syndromes
Commented [VET1]:
block voltage-gated L-type calcium Constipation, Nausea,
channels (cardiac > vascular); for flushing,gingival hyperplasia, AV excessive cardiac depression may
Angina, Supraventricular block, sinus node depression, occur
tachycardia, migraine, hypertension Pretibial edema, dizziness
block voltage-gated L-type calcium
Nausea, Flushing, dizziness, pretibial greater vasodilator effect that
channels (vascular > cardiac); for
edema, constipation cardiodepressant effect
Angina, hypertension
Other drugs for heart failure include
Diuretics (Furosemide is the DOC for
acute heart failure), Angiotensin
Antagonists (ACEi is the DOC for
chronic heart failure), Beta1
blockers (dopamine and
dobutamine), Non-selective Beta
Blockers (Carvedilol, Labetalol,
Metoprolol), PDEi (Inamrinone,
Milrinone), Vasodilators
(Nitroprusside, Nitroglycerin)
inhibits Na/K ATPase; increases
Narrow therapeutic index, Arrhythmogenesis increased by
intracellular Ca, increasing cardiac
Arrhythmias, diarrhea, vomiting, hypokalemia, hypercalcemia,
contractility; for heart failure, Nodal
visual changes hypomagnesemia
arrythmias
Use- and state-dependent block of
Arrhythmias, lupus-like syndrome
INa channels; some block of Ik
(procainamide), hypotension,
channels. Slowed conduction
cinchonism (quinidine),
velocity and pacemaker activity; Hyperkalemia exacerbates cardiac
thrombocytopenia (quinidine),
prolonged action potential duration toxicity
antimuscarinic effect
and refractory period; for atrial and
(disopyramide), quinidine reduces
ventricular arrhythmias especially
digoxin clearance
after myocardial infarction
highly selective use and state- Hyperkalemia, exacerbates cardiac
dependent INa block; minimal effect toxicity. Lidocaine is the least
in normal tissue; no effect on IK; CNS stimulation, Allergy, cardiotoxic among conventional
DOC for ventricular arrhythmia post- Arrhythmias, depression, anti-arrhythmics ; only affect
myocardial infarction, Digoxin- Agranulocytosis ischemic tissue; lidocaine is never
induced arrhythmia ; Mexilitine can given P.O due to significant first pass
be used for neuropathic pain effect
Selective use and state-dependent
Increased arrhythmias hyperkalemia exacerbates cardiac
block of INa; slowed conduction
(proarrhythmic effect), CNS toxicity contraindicated for post MI
velocity and pacemaker activity; for
excitation arrhythmias
refractory arrhythmias
Block of beta-receptors, decrease in
cAMP results to decreased Na and In CHF, reduces progression and
Ca current and suppression of decreases incidence of potentially
Bronchospasm, AV block,
cardiac pacemaker activity; for Post fatal arrhythmias. Sotalol is a beta-
Hypotension, Cardiac depression
MI prophylaxis against sudden blocker anti arrhythmic that has
death, thyrotoxicosis, acute class 3 properties
perioperative and thyrotoxic
Page 6 of 56

C. Class 3 Arrhythmics
i. Dofetilide, Ibutilide,
ii. Sotalol
iii. Amiodarone, Dronedarone
D. Class 4 Antiarrythmatics
i. Non-dihydropyridine calcium
channel blocker: Verapamil,
Diltiazem
E.Miscellaneous Antiarrythmics
i. Adenosine
Diuretics
A. Carbonic Anhydrase Inhibitors
i. Acetazolamide, Dorzolamide,
Brinzolamide, Dichlorphenamide,
Methanolamide
B. Loop Diuretic
i.Furosemide, Bumetanide,
Torsemide
C. Thiazide Diuretics
i. Hydrochlorothiazide,
Chlorthalidone, Indapamide,
Metolazone
D. Potassium-Sparing Diuretics
i. Spironolactone, Eplerenone
(Aldosterone Antagonist)
arrhythmias, Supraventricular
tachycardia
Group with the greatest risk for TDP
Selective Ik block ; prolonged action
potential and QT interval; for
Torsade de pointes NONE
treatment and prophylaxis of atrial
fibrillation
Ik block and beta-adrenoceptor
Dose-related torsade de pointes,
block; for ventricular arrhythmias,
excessive beta-blockade (sinus NONE
Supraventricular tachycardia, Atrial
bradycardia, asthma)
fibrillation
Strong Ik block produces marked
prolongation of action potential and
Amiodarone has Class 1, 2 3 and 4
refractory period. Group 1 activity Microcrystalline deposits in cornea
activity therefore is the MOST
slows conduction velocity; groups 2 and skin, paresthesias, Pulmonary
EFFICACIOUS of all anti-arrhythmics,
and 4 activity confer additional anti fibrosis, Tremor, Thyroid dysfunction
amiodarone has longest among all
arrhythmic activity; for refractory (hyper- or hypo-)
anti-arrhythmics (1-10 weeks)
arrhythmia, used off label in many
arrhythmia
Block voltage-gated L-type calcium
channels (cardiac >vascular),
Constipation, Pretibial edema,
decreased AV conduction velocity ;
Nausea, Flushing, Gingival should be avoided in Ventricular
for Angina, Hypertension,
hyperplasia, heart failure, AV block, tachycardia
Supraventricular tachycardia,
dizziness, sinus node depression
migraine, Raynaud's Phenomenon,
Vasospasm
Increase in diastolic Ik of AV node
that causes marked
DOC for paroxysmal supraventricular
hyperpolarization and conduction Flushing, Transient chest pain,
tachycardia, Duration of action is
block; reduced ICa; For AV nodal Dyspnea, Hypotension
only 15sec
arrhythmias, DOC for paroxysmal
supraventricular tachycardia
Inhibits carbonic anhydrase. In
proximal tubule, In glaucoma, Drowsiness, Sulfa Allergy, Renal
secretion of aqueous humor is calcium stones, Paresthesias,
reduced and in mountain sickness, hyperchloremic metabolic acidosis, diuresis is self-limiting after 2-3 days
metabolic acidosis increases hepatic encephalopathy in cirrhotic
respiration; for glaucoma, diuresis patients, potassium wasting
for edema with alkalosis.
Inhibit Na/K/2Cl transporter in thick
ascending limb of loop of Henle, Hypokalemic metabolic alkasis, Synergistic ototoxicity with
Cause powerful diuresis and dehydration, Ototoxicity, Potassium aminoglycosides. Efficacy decreased
increased Ca excretion; for Heart wasting, Sulfa allergy, by NSAIDs ; causes hypocalcemia in
failure, Hypertension, Pulmonary Hyperuricemia, Hypocalcemia, contrast with thiazide diuretics
Edema, Hypercalcemia, Acute renal Hypomagnesemia, Nephritis which cause hypercalcemia
failure, Anion overdose
Inhibit Na/Cl transporter in distal
convolutes tubes. Causes moderate Hypokalemic metabolic alkalosis, Synergistic effect with loop
diuresis and reduced excretion of Potassium wasting, dilutional diurectics. Efficacy decreased by
calcium; For hypertension hyponatremia, Hyperglycemia, NSAIDs ; causes hypercalcemia in
Hypercalciuria, Heart failure, hyperuricemia, sulfa allergy, contrast with loop diuretics which
Nephrogenic diabetes insipidius, hyperlipidemia cause hypocalcemia
renal calcium stones
Steroid inhibitors of cytoplasmic Hyperkalemia, impotence, Benign
aldosterone receptor in cortical prostatic hyperplasia, Eplerenone reduces progression of
collecting ducts. Reduce K excretion; Hyperchloremic metabolic acidosis, DM nephropathy and reduces
for Hyperaldosteronism, Heart anti-androgenic effect mortality post MI
failure, Hypokalemia, Hypertension (Spironolactione)
Page 7 of 56

ii. Amiloride, Triamterene (Na
channel Blocker)
E. Osmotic Diuretics
i. Mannitol, Glycerin, Isosorbide,
Urea
F. ADH Agonists/ Antagonists
i. Antidiuretic hormone,
Desmopressin, Vasopressin
G. ADH Antagonists: Conivaptan,
Tolvaptan, Lixivaptan,
Demeclocycline, Lithium
3. DRUGS WITH IMPORTANT ACTION ON SMOOTH MUSCLES
Histamine, Serotonin and the Ergot Alkaloids
A. H1 antagonists
i. 1st Generation:
Diphenhydramine, Dimenhydrinate,
Chlorpheniramine, Meclizine,
Promethazine
ii. 2nd Generation: Loratadine,
Desloratadine, Cetirizine,
Levocertirizine, Fexofenadine
B. H2 antagonists
i. Cimetidine, Ranitidine,
Famotidine, Nizatidine
Inhibitor of ENaC (Epithelial sodium
channels) in cortical collecting duct,
reduces Na reabsorption and K
excretion; for hypokalemia
Osmotically retains water in tubule
by reducing reabsorption in
proximal tubule, descending limb of
Henle's loop, and collecting ducts; in
the periphery, mannitol extracts
water from cells; for
Rhabdomyolysis, Hemolysis,
Increased intracranial pressure,
Acute glaucoma
Agonists at V1 and V2 ADH
receptors. Activate insertion of
aquaporin water channels in
collecting tubule. Vasoconstriction;
For central diabetes insipidus,
hemophilia, Nocturnal enuresis, von
Willebrand's disease
Antagonist at V1, V2 receptors; for
SIADH and Hyponatremia
diminish or abolish the major
actions of histamine in the body by
competitive, reversible blockade of
histamine H1-receptor sites on
tissues ; used primarily for the
alleviation of conditions such as
urticarial rashes and nasal allergy
that are characterised by type I
hypersensitivity ; are of value in
preventing urticaria and are used to
treat urticarial rashes and mild
angioedema
Reversible blockade of histamine
H1-receptor sites on tissues ; anti-
nausea and antiparkinsonism effect,
for allergic reactions, for sedation
and motion sickness
(Diphenhydramine Dimenhydrinate,
Cyclizine, Meclizine, Promethazine),
for chemotherapy-induced vomiting
(Diphenhydramine)
Reversible blockade of histamine
H1-receptor sites on tissues ; for
allergic reactions
Surmountable competitive
pharmacologic block of H2
receptors, reduction of nocturnal
acid secretion in gastirc and
duodenal ulcer, accelerate healing
Hyperkalemia, kidney stones,
metabolic acidosis, Acute renal
failure (with indomethacin), should
never be given with potassium
supplements
Transient volume expansion
(hyponatremia, pulmonary edema;
followed by hypernatremia) nausea,
headache, dehydration, vomiting
Hypertension, Hyponatremia
Infusion site reactions,
hyperkalemia, Nephrogenic diabetes
insipidus, Bone and Teeth
abnormalities(demeclocycline),
Renal failure (Lithium,
demeclocycline)
Sedation, should not be given to
neonates because they are more
susceptible to antimuscarinic effects
Anticholinergic effects, orthostatic
hypotension (promethazine),
sedation
headache, dry mouth, hyperkinesia,
malaise, may cause arrhythmia due
to blockade of cardiac potassium
channels (acrivastine, astemizole,
cetirizine, loratadine, and
terfenadine)
CYP450 inhibitor, antiandrogen
effects, decreased hepatic blood
flow (cimetidine), weak enzyme
inhibitory effect (Ranitidine)
should never be given with
potassium supplements
used to maintain high urine flow
Increases the factor VIII activity of
patients with mild hemophilia A or
von Willebrand disease
Central Pontine Myelinosis may
occur with rapid correction of
hyponatremia
Possess antimuscarinic, adrenaline-
antagonising, serotonin
antagonising, and local anaesthetic
effects. Some have calcium-channel
blocking activity ; Sedating
antihistamines may enhance the
sedative effects of CNS depressants
including alcohol, barbiturates,
hypnotics, opioid analgesics,
anxiolytic sedatives, and
antipsychotics ; all are PO but can be
given topical (nose and eyes) ;
negligible effect on H2 receptors
more likely to block autonomic
receptors, also has alpha1 blocking
and local anesthetic effect ; Cyclizine
(more anti-motion sickness action
less sedative and and autonomic
effects); Promethazine (less anti-
motion sickness, more sedative and
autonomic effects ; Usual half-life: 4-
12h
No sedation and antimuscarinic
effects ; usual half-life: 12-24h
No blocking action on H1 receptor
used in the ICU setting to prevent
gastric erosion and hemorrhage ;
usual half-life: 1-3h
Page 8 of 56

C. Serotonin Agonists
i. 5HT1D receptor agonist:
Sumatriptan, Naratriptan,
Almotriptan, Eletriptan,
Frovatriptan, Rizatriptan,
Zolmitriptan
D. Serotonin Antagonists
i. 5HT3 receptor antagonist:
Ondansetron, Granisetron,
Dolasetron, Alosetron
E. Ergot Alkaloids
i. Vasoselective: Ergotamine
ii. Uteroselective: Ergonovine
The Eicosanoids: Prostaglandins, Thromoboxanes, Leukotrienes and related compounds
A. Prostaglandin E1 analog
i. Misoprostol, Gemeprost
ii. Alprostadil
B. Prostaglandin E2 analog
i. Dinoprostone, Sulprostone
C. Prostaglandin F2a analog
i. Latanoprost, Arboprost,
Bimatoprost, Travoprost,
Unoprostone
D. Prostaglandin I2 analog
i. Epoprostenol, Beraprost,
Iloprost, Treprostinil
E. Leukotriene antagonists
i. Lipoxygenase inhibitor: Zileuton
ii. LT receptor blocker:
Montelukast, Zafirlukast
and prevent recurrences ; for PUD,
GERD and ZES
Agonist at the 5HT1D receptor in the all are per orem only except for
blood vessels causing Injection site reaction, paresthesia, Sumatriptan which can also be given
vasocontriction ; 1st line treatment dizziness, warm/hot sensation, chest intranasally, transdermal and IV ; All
for Acute migraine and cluster pain, coronary vasospasm has 2-27hrs DOA exc for sumatriptan
headache attacks DOA: 2-4h
Dolasetron can increase QRS and QT
Selectively block 5HT3 receptors ;
(proarrhythmic effect) duration so
For antiemesis in patients post- Constipation, headache, malaise
never use in patients with heart
chemotherapy or post-operation
disease
most are partial agonists at alpha
receptors and 5HT receptors but
some are potent agonist at
dopamine receptors
gangrene (secondary to ischemia) in
can cause epinephrine reversal due
Mixed partial agonist effects at 5- overdose, unusual hyperplasia of the
to partial agonist effect on alpha
HT2 and a-adrenoceptors, causes retroperitoneal, retropleural or
receptors (REMEMBER: All partial
vasoconstriction; For Migraine subendocardial cavity -->
agonist will act as antagonist in the
attacks (but 5HT1D are preferred) hydronephrosis, cardiac valvular and
present of a full agonist)
conduction system malfunction
uterus becomes more sensitive to
Mixed partial agonist effects at 5- ergots during pregnancy, produce
HT2 and a-adrenoceptors, causes marked uterine contraction, GI very powerful and long-lasting
vasoconstriction; For control of upset (nausea, vomiting, diarrhea) contraction leading to decreased
post-partum bleeding bleeding, Never give before delivery
of placenta
PGE1 analogue, activated EP
receptor, causes increased HCO3
Misoprostol's intended use is for
and mucus secretion in stomach and
Abdominal pain, Uterine cramping, NSAID-induced gastritis, may also be
uterine contraction; For prevention
teratogen, miscarriage used together with Mifepristone or
of ulcer in patients who take high
Methotrexate as safe abortifacient
doses of NSAIDs due to arthritis,
abortifacient
PGE1 analogue, causes vascular
smooth muscle relaxation and
Apnea, hypotension, priapism, given as injection into the cavernosa
vasolidation; For Maintenance of
lightheadedness, arrhythmia for erectile dysfunction
patent ductus arteriosus (PDA),
Erectile dysfunction
Low concentrations contract, higher
concentrations relax uterine and approved abortifacient in the 2nd
cervical smooth muscle, soften trimester, although effective in
Cramping, Fetal trauma
cervix at term before induction with inducing labor, it produces more SE
oxytocin; For cervical ripening, than other oxytocics
induction of labor, abortifacient
PGF2a analogue, increases outflow Latanoprost may cause changes in
vomiting, diarrhea, transient
of aqueous humor thus reduces the color of the iris and may
bronchoconstriction
intraocular pressure; For glaucoma lengthen eyelashes
PGI2 analogue, activates IP receptor,
causes vasolidation and reduces
platelet aggregation; For severe used primarily for pulmonary
Hypotension, headache, flusing
pulmonary Hypertension and hypertension (esp Treprostinil IV)
reducing platelet aggregation in
dialysis machines
see entry on Drugs used for Asthma
see entry on Drugs used for Asthma
Page 9 of 56
F. Corticosteroids
G. Non-steroidal anti-inflammatory
drugs
Drugs used in Asthma
A. Beta2-selective agonist (short-
acting)
i. Albuterol/Salbutamol,
Levalbuterol, Terbutaline,
Metaproterenol, Pirbuterol,
Procaterol, Fenoterol
B. Beta2-selective agonist (long
acting)
ii. Salmeterol, Formoterol,
Cleneterol, Bambuterol
C. Muscarinic receptor agonist
i. Ipratropium, Tiotropium
C. Methylxanthine
i. Theophylline, Aminophylline,
Pentoxifylline
D. Mast cell Stabilizer
i. Cromolyn, Nedocromil,
Lodoxamide
E. Corticosteroid
i. Fluticasone, Beclomethasone,
Budesonide, Flunisolide,
Mometasone, Triamcinolone,
Ciclosenide
F. Leukotriene synthesis inhibitor
i. Zileuton
see entry on Drugs used for Asthma
see entry on Analgesics
Activates beta2-receptors in
bronchial smooth muscle leading to
bronchodilation ; DOC for acute
asthma attacks
Activates beta2-receptors in
bronchial smooth muscle leading to
bronchodilation, potentiates
corticosteroid action; For Asthma
prophylaxis
Blocks muscarinic receptors in
bronchial smooth muscle and
prevent bronchoconstriction
mediated by vagal discharge; For
acute BA attack and COPD
Phosphodiesterase inhibitor,
Adenosine receptor antagonist,
causes bronchodilation and
increased strength of contraction of
diaphragm; For asthma especially in
nocturnal attacks, Intermittent
claudication (pentoxifylline), very
useful in COPD
Prevents calcium influx and
stabilizes mast cells, preventing
degranulation and release of
histamine, leukotrienes and
mediators; for Asthma prophylaxis
and allergies (oral, nasal and
ophthalmic drops)
Inhibit synthesis of arachidonic acid
by inhibiting Phospholipase A2,
Reduces expression of COX and LT,
inc responsiveness of Beta receptors
in the airway, bind to intracellular
receptors and activate
Glucocorticoid response elements in
the nucleus leading to synthesis of
substances that prevent full
expression of inflammation and
allergy ; DOC for Asthma
prophylaxis, First line treatment for
moderate to severe BA, COPD,
Allergic rhinitis, also used as anti-
inflammatory for other conditions
such as auto-immune diseases and
cancer, also for immune suppression
Inhibitor of 5-lipoxygenase. Reduces
synthesis of leukotrienes. Prevents
Tachycardia, Nervousness, tremors,
restlessness, arrhythmias when used
excessively, loss of responsiveness
(tolerance, tachyphylaxis)
Tachycardia, Nervousness, tremors,
restlessness, arrhythmia when used
excessively, loss of responsiveness
(tolerance, tachyphylaxis)
anti-muscarinic effects (dry mouth,
blurred vision etc.)
CNS stimulation (Insomnia, seizure,
Anorexia), Cardiac stimulation
(Arrhythmias), Tremors, increased
BP, diuresis, inc GI motility
Cough, Airway irritation
Oropharyngeal candidiasis, mild
growth retardation observed in
children, Minimal systemic steroid
steroid toxicity (eg, adrenal
suppression), Mild growth
retardation
Flulike syndrome, headache,
drowsiness, dyspepsia, hepatitis,
Increase toxicity when used for
COPD (May precipitate arrythmias)
and in patients with heart disease;
usual DOA: 2-4hrs, all are given
inhalational, Salbutamol and
terbutaline is also available PO,
terbutaline can also be given IV
Increase asthma mortality when
used alone; May precipitate
arrhythmias; usual DOA: 12hrs
More effective and less toxic than
beta agonists for COPD, Tiotropium
has longer DOA than Ipratropium,
Ipratropium given as aerosol has
little systemic effects, has no effect
on the chronic inflammation aspect
of BA
Antidote in overdosage is BB. Higher
clearance in adolescents and
smokers. Narrow therapeutic
window; usual DOA: 12hrs
No bronchodilator action but can
prevent bronchoconstriction caused
by antigens (both in the early and
late BA responses), unusually
insoluble chemicals so rarely used
For status asthmaticus: use IV
prednisolone or hydrocortisone ;
prednisolone is the active
metabolite of prednisone
No bronchodilator action, not
recommended for acute BA attack
Page 10 of 56

G. Leukotriene Antagonist
i. Montelukast, Zafirlukast,
Pranlukast
H. Anti-IgE antibody
i. Omalizumab
4. DRUGS THAT ACT ON THE CENTRAL NERVOUS SYSTEM
Sedative-Hypnotics
A. Short-acting benzodiazepines
i. Midazolam, brotizolam,
triazolam, oxazepam, etizolam
B. Intermediate-acting
benzodiazepines
i. Lorazepam, Alprazolam,
Estazolam, Clonazepam,
Lormetazepam, Nitrazepam,
Temazepam
C. Long-acting Benzodiazepine
i. Diazepam, chlorazepate,
chlordiazepoxide, flurazepam,
quazepam, flunitrazepam
D. Benzodiazepine antagonist
i. Flumazenil
E. Ultrashort-acting barbiturates
i. Thiopental, Methohexital,
Thiamylal
airway inflammation and
bronchoconstriction; For asthma
prophylaxis
Blocks leukotriene-1 receptor,
prevents airway inflammation and
bronchoconstriction; For asthma
prophylaxis
Binds IgE antibodies on sensitized
mast cells and prevents activation
by BA triggers and subsequent
release of inflammatory mediators;
For prophylaxis of severe, refractory
asthma not responsive to all other
drugs
bind GABA-A receptor subunits to
increase frequency of chloride
channel opening which causes
membrane hyperpolarization ; For
acute anxiety, panic attacks,
anesthesia induction and
preoperative sedation (esp
Midazolam), insomnia (Triazolam)
bind GABA-A receptor subunits to
increase frequency of chloride
channel opening which causes
membrane hyperpolarization; For
anxiety disorders even panic
disorders (Alprazolam and
Clonazepam), insomnia (Estazolam),
skeletal muscle relaxation, seizure
disorders (Clonazepam), status
epilepticus (Lorazepam),
tranquilizers, Bipolar disorder
(Clonazepam), infantile spasm
(Clonazepam)
bind GABA-A receptor subunits to
increase frequency of chloride
channel opening which causes
membrane hyperpolarization; For
anxiety disorders, insomnia
(Flurazepam), skeletal muscle
relaxation (e.g. cerebral palsy -
Diazepam), seizure disorders,
tranquilizers, for status epilepticus
(Diazepam), anesthesia (Diazepam),
alcohol withdrawal (Diazepam and
Chlordiazepoxide)
antagonist at benzodiazepine sites
on GABA-A receptor ; for
benzodiazepine overdose.
bind to GABA-A receptor sites
(distinct from benzodiazepines) to
increase duration of chloride
elevation of liver enzymes (more
than LT receptor blockers)
Gastrointestinal upset, Insomnia,
elevation of liver enzymes
Long term toxicity not yet well
documented
causes anterograde amnesia,
decreased psychomotor skills,
unwanted daytime sedation,
tolerance, dependence liability and
rebound insomnia or anxiety.
causes anterograde amnesia,
decreased psychomotor skills,
unwanted daytime sedation,
tolerance, dependence liability and
unwanted daytime sedation.
causes anterograde amnesia,
decreased psychomotor skills (esp
Diazepam and Flurazepam),
unwanted daytime sedation,
tolerance, dependence liability and
rebound insomnia or anxiety.
agitation, confusion, and
precipitates benzodiazepine
withdrawal syndrome for those with
benzodiazepine dependence.
dependence liability is greater than
benzodiazepine, acute intermittent
porphyria.
No bronchodilator action, not
recommended for acute BA attack
humanized murine monoclonal
antibody, very expensive and only
administered IV
additive CNS depression if used with
ethanol, antihistamines,
antipsychotics, opioids and TCAs,
decreased REM sleep, use lower
doses in the elderly when used for
insomnia
additive CNS depression if used with
ethanol etc, decreased REM sleep,
High dose BZD and Barbs may
suppress seizure but at the expenses
of marked sedation EXCEPT
Clonazepam and Phenobarbital,
Lorazepam is preferred over
Diazepam in Status Epilepticus due
to its long distribution halflife, use
lower doses in the elderly when
used for insomnia
additive CNS depression if used with
ethanol etc., decreased REM sleep,
Flunitrazepam is used as a date-rape
drug, use lower doses in the elderly
when used for insomnia
Seizures and arrhythmias may occur
when administered in patients who
took both TCAs and benzodiazepines
additive CNS depression if used with
ethanol etc., CYP450 inducer,
Page 11 of 56

F. Short and intermediate-acting
barbiturates
i. Pentobarbital, secobarbital,
amobarbital, butalbital,
butabarbital, talbutal, aprobarbital
G. Long-acting barbiturate
i. Phenobarbital, mephobarbital,
primidone
H. Imidazopyridine sedative-
hypnotics
i. Zolpidem, Zaleplon, Eszopiclone
I. Atypical Sedative-Hypnotics
i. Partial Serotonin Agonist:
Buspirone
ii. Melatonin receptor agonist:
Ramelteon
Antiseizure Drugs
i. Phenytoin, Fosyphenytoin,
Mephenytoin, Ethotoin
ii. Carbamazepine, Oxcarbazepine
channel opening, block glutamic acid
neurotransmission, at high doses
can block NA channels ; For
anesthesia induction (esp
Thiopental)
bind to GABA-A receptor sites
(distinct from benzodiazepines) to
increase duration of chloride
channel opening, block glutamic acid
neurotransmission, at high doses
can block Na channels ; For insomnia
and preoperative sedation
(Secobarbital), for status epilepticus
(Phenobarbital)
bind to GABA-A receptor sites
(distinct from benzodiazepines) to
increase duration of chloride
channel opening, block glutamic acid
neurotransmission, at high doses
can block Na channels ; For
insomnia, seizure disorders
(Phenobarbital), status epilepticus
(Phenobarbital)
bind selectively to a subgroup of
GABA-A receptors, acting like
benzodiazepines to enhance
membrane hyperpolarization, only
interact with GABA-A receptors with
alpha-1 subunit ; For insomnia and
sleep disorder esp. when sleep
onset is delayed
partial agonist at 5-HT1A receptors
and possibly D2 receptors, precise
MOA of anxiolytic effect is unkown ;
For generalized anxiety disorders
activates melatonin receptors (MT1
and MT2 receptors) in the
suprachiasmatic nuclei in the CNS --
> decreased latency of sleep onset
block voltage-gated Na channel ;
DOC for generalized tonic-clonic
seizures, DOC for partial seizures,
status epilepticus, arrhythmias,
migraine
block voltage-gated Na channels and
decreases glutamate release ; DOC
for trigeminal neuralgia, DOC for
generalized tonic-clonic seizures,
dependence liability is greater than
benzodiazepine, acute intermittent
porphyria.
dependence liability is greater than
benzodiazepine, acute intermittent
porphyria, severe respiratory and
cardiovascular depression
day-after psychomotor depression,
few amnestic effects; tolerance,
dependence liability and withdrawal
symptoms is less than that of
benzodiazepines
non-specific chest pain, tachycardia,
palpitations, dizziness, nervousness,
tinnitus, GI distress, paresthesias,
dose-dependent pupillary
constriction
Dizziness, fatigue, decreased
testosterone, increased prolactin
nystagmus, diplopia, sedation,
gingival hyperplasia, hirsutism,
anemias, peripheral neuropathy
(absent DTRs), osteoporosis, fetal
hydantoin syndrome, abnormalities
in Vit D metabolism
diplopia, cognitive dysfunction,
drowsiness, ataxia, blood dyscrasias,
Stevens-Johnson syndrome,
erythematous rash, teratogen (spina
Thiopental has highest lipid
solubility
additive CNS depression if used with
ethanol etc., CYP450 inducer
additive CNS depression if used with
ethanol, CYP450 inducer,
Phenobarbital may be excreted
unchanged in the urine, High dose
BZD and Barbs may suppress seizure
but at the expenses of marked
sedation EXCEPT Clonazepam and
Phenobarbital
lack anti-convulsant, anti-anxiety
and muscle relaxant effects, effects
are reversed with Flumazenil, very
rapid onset of action, may dec. REM
sleep, rebound inc on withdrawal
from chronic use, increasing use due
to rapid onset with minimal effects
on the sleep pattern and cause less
daytime cognitive impairment as
compared to BZD
minimal abuse liability, minimal CNS
depressant effects, tolerance and
withdrawal ; no anticonvulsant or
muscle relaxant property ; slow
onset of action (>1week),
metabolized by CYP3A4, safe for
pregnant patients
minimal rebound insomnia or
withdrawal symptoms, minimal
abuse liability, metabolized by
CYP450 (increased levels in the
presence of CYP1A2 or CYP2D6
inhibitors
CYP450 inducer , metabolism is non-
linear (elimination shift from 1st
order to zero order at moderate to
high dose levels) , Fosphenytion is a
water-soluble prodrug of phenytoin
; phenytoin is preferred in prolonged
therapy for status epilepticus
because it is less sedating.
CYP450 inducer, Oxcarbazepine has
less drug interactions, metabolism
may be inhibited by other drugs
such as Propoxyphene and valproic
acid ; may be used for acute manic
Page 12 of 56
 DOC for partial seizures, for bipolar bifida and craniofacial anomalies), phase and as prophylaxis in the
disorders hyponatremia (Oxcarbazepine) depressive phase
blocks high-frequency firing of
CYP450 inhibitor ; also have the
neurons which modifies amino acid
same effect on Ca currents like
metabolism ; DOC for bipolar
drowsiness, nausea, tremor, Ethosuximide ; Other MOA include
disorder (acute mania), DOC for
iii. Valproic acid alopecia, weight gain, hepatotoxicity enhancing K channel permeability ;
generalized tonic-clonic seizures and
(esp in infants), neural tube defects BZDs are commonly required at
absence seizure, partial seizures,
initiation therapy of valproic acid ;
myoclonic seizures, also used for
DOC for acute manic illness
Bipolar disorders
May also act on Na channels and as
antagonist at some glutamate
see notes above ; For status
iv. Phenobarbital cognitive dysfunction, dependence receptors ; primary anticonvulsant in
epilepticus in children
infants, children and pregnant
patients
inhibit low threshold (T-type) Ca
v. Ethosuximide, Phensuximide, GI distress, lethargy, headache and
currents esp in thalamic neurons ; Long half-life
Methsuximide behavioural changes.
DOC for absence seizure
vi. Diazepam see entry on Sedative-Hypnotics
eliminated in the kidneys in their
blocks Ca++ channels, increases unchanged form ; structural
GABA release ; For neuropathic pain dizziness, sedation, ataxia, analogues of GABA but does not
vii. Gabapentin, Pregabalin
such as postherpetic neuralgia, nystagmus, tremor activate GABA receptor directly ;
partial seizures, migraine also have the same effect on Ca
currents like Ethosuximide
blocks Na and Ca++ channels and
decreases glutamate , Zonisamide
primarily undergoes glucuronidation
only blocks Na channels ; For dizziness, ataxia, nausea, rash, SJS /
reaction ; Lamotrigine may be used
viii. Lamotrigine, Zonisamide generalized tonic-clonic seizures, TEN (lamotrigine), severe skin
for acute manic phase and as
DOC for partial seizures, myoclonic reaction (Zonisamide)
prophylaxis in the depressive phase
seizures, absence seizures, bipolar
disorder.
Bind synaptic protein selectively
inhibiting hypersynchronization of It is not metabolized by CYP450
dizziness, sedation, weakness,
ix. Levetiracetam epileptiform burst firing ; For enzymes, eliminated in the kidneys
irritability, hallucinations, psychosis
generalized tonic-clonic seizures, in their unchanged form
partial seizures
multiple actions on synaptic
function, probably via actions on
drowsiness, dizziness, ataxia, Antiseizure drugs with the most
phosphorylation (Na, Ca, GABA,
psychomotor slowing, memory number of MOA, undergo both
AMPA-glutamate, carbonic
impairment, paresthesias, weight hepatic and renal metabolism,
anhydrase), Felbamate also facilitate
loss, acute myopia, glaucoma, Topiramate can also block Na
x. Topiramate, Felbamate the inhibitory actions of GABA but
myopia, urolithiasis ; felbamate channels and potentitae action of
its exact MOA is still unknown ; For
causes hepatic failure and GABA and block glutamate receptor,
generalized tonic-clonic seizures,
hematotoxic (can cause ITP, aplastic Felbamate may also block glutamate
partial seizures, absence seizures,
anemia) receptors
migraine ; Felbamate is only for
severe refractory seizure states
Irreversibly inactivates GABA
aminotransaminase (GABA-T) which
xi. Vigabatrin visual field defects None
terminates the action of GABA ; For
GTC seizure
Inhibits GABA transporter (GAT-1) in
neurons and glia thus inhibiting its
xii. Tiagabine asthenia or weakness, dizzines None
reuptake, leading to prolongation of
GABA effects ; For partial seizures
General Anesthetics
This group in general increase the
A. Inhalational General Anesthetics
threshold for firing of CNS neurons
Facilitates GABA-mediated Lowest Potency (highest MAC) and
inhibition, block brain NMDA and megaloblastic anemia on prolonged least cardiotoxic; additive CNS
i. Nitrous Oxide Ach-N receptors; used as anesthesia exposure; Euphoria (laughing gas), depression with many agents
for minor surgery and dental bronchodilation especially opioids and sedative-
procedures hypnotics
Facilitates GABA-mediated bronchospasm, peripheral additive CNS depression with many
ii. Desflurane
inhibition, block brain NMDA and vasodilation agents especially opioids and

Page 13 of 56

iii. Sevoflurane
iv. Isoflurane
v. Enflurane
vi. Halothane
vii. Methoxyflurane
B. Intravenous General Anesthetics
i. Barbiturates: Thiopental,
Methohexital, Thiamylal
ii. Benzodiazepine: Midazolam,
Brotizolam, Triazolam, Oxazepam,
Etizolam
iii. Phencyclidine derivative:
Ketamine
iv. Imidazole derivative:
Etomidate
v. Opioid analgesics: Fentanyl,
morphine, alfentanil, remifentanil
vi. Propofol, Fospropofol
Local Anesthetics
A. Ester Local Anesthetics
i. Procaine
Ach-N receptors ; For general
anesthesia
Facilitates GABA-mediated
inhibition, block brain NMDA and
Ach-N receptors; For general
anesthesia
Facilitates GABA-mediated
inhibition, block brain NMDA and
Ach-N receptors ; For general
anesthesia
Facilitates GABA-mediated
inhibition, block brain NMDA and
Ach-N receptors ; For general
anesthesia
Facilitates GABA-mediated
inhibition, block brain NMDA and
Ach-N receptors ; For general
anesthesia
Facilitates GABA-mediated
inhibition, block brain NMDA and
Ach-N receptors ; For general
anesthesia
see notes above
see notes above
Blocks excitation by glutamate at
NMDA receptors; For dissociative
anesthesia (analgesia, amnesia and
catatonia but with retained
consciousness)
Modulates GABA-A receptors
containing beta3 subunits; For
general anesthesia to patients with
limited cardiac or respiratory
reserve
Interacts with mu, sigma, kappa
receptors for endogenous opioid
peptides ; For high risk patients who
might not survive general anesthesia
Potentiates GABA-A receptors,
blocks Na channels; For prolonged
sedation esp in ICU patients and also
in OPD surgeries
Blockade of Na channels slows
which prevents axon potential
propagation; For local anesthesia
peripheral vasodilation, renal
insufficiency (due to Flourine
release), bronchodilation
catecholamine-induced arrhythmias,
peripheral vasodilation,
bronchodilation
spike-and-wave activity in EEG,
muscle twitching, breath-holding,
myocardial depression, renal
insufficiency (due to Flourine
release), dec cardiac output,
bronchodilation
catecholamine-induced arrhythmias,
myocardial depression, post-
operative hepatitis, dec cardiac
output, bronchodilation
renal insufficiency (due to Flourine
release), bronchodilation
are respiratory and circulatory
depressants --> dec cerebral blood
flow --> dec ICP
see notes above
CV stimulation, hypertension,
increased ICP, delirium, Dissociative
anesthesia, post-op effects:
disorientation, hallucination,
excitation
pain at injection site, myoclonus,
postoperative nausea and vomiting,
adrenocortical suppression (on
prolonged administration)
respiratory depression, chest wall
rigidity (which may cause impaired
ventilation) and constipation
bradycardia, vasodilation,
hypotension, negative inotropism,
pain at injection site, anterograde
amnesia, dystonia, priapism,
paresthesia (Fospropofol)
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression
sedative-hypnotics ; all inhaled
anesthetcis cause bronchodilation
except Desflurane
additive CNS depression with many
agents especially opioids and
sedative-hypnotics
additive CNS depression with many
agents especially opioids and
sedative-hypnotics
additive CNS depression with many
agents especially opioids and
sedative-hypnotics ; has pungent
odor which limits its use
additive CNS depression with many
agents especially opioids and
sedative-hypnotics
Highest potency and lowest MAC
(very slow onset and recovery);
additive CNS depression with many
agents especially opioids and
sedative-hypnotics
rapid entry into the brain (<1min)
Midazolam is a usual adjunct with
inhalational anesthetics and IV
opioids, has a slow onset but longer
DOA
Reduces delirium by pretreatment
with benzodiazepine, congener of
Phencyclidine / angel dust
Minimal effects on CV and
respiratory functions, no analgesic
properties, short DOA
Antidote is Naloxone / Naltrexone ;
Neuroleptanesthesia (analgesia +
amnesia) happens when Fentanyl,
Droperidol and Nitrous oxide are
given together ; faster recovery with
remifentanil ; these drugs have fast
onset of action
"milk of anesthesia", additive effects
with sedative-hypnotic drugs ; as
rapid as thiopental and also with
fast recovery ; antiemetic action ;
Fospropofol is the water-soluble
prodrug form of propofol but with
slower onset and recovery
this group can cause antibody
formation in some patients
Shortest half-life among local
anesthetics
Page 14 of 56
 Blockade of Na channels slows
which prevents axon potential
ii. Benzocaine
propagation; For local anesthesia,
topical anesthesia
Blockade of Na channels slows
which prevents axon potential
iii. Cocaine propagation, with intrinsic
sympathomimetic activity; For local
anesthesia, topical anesthesia
Blockade of Na channels slows
which prevents axon potential
propagation; For local anesthesia,
iv. Tetracaine
spinal anesthesia, epidural
anesthesia, topical ophthalmic
anesthesia
B. Amide Local Anesthetics
Blockade of Na channels slows
which prevents axon potential
propagation; For local anesthesia,
i. Lidocaine
antiarrhythmia (group 1B activity),
used for post-MI and for digitalis
toxicity
Blockade of Na channels slows
which prevents axon potential
ii. Prilocaine
propagation; For local anesthesia,
dental anesthesia
Blockade of Na channels slows
which prevents axon potential
iii. Bupivacaine propagation; For local anesthesia,
epidural anesthesia, intrathecal
anesthesia
Blockade of Na channels slows
which prevents axon potential
iv. Ropivacaine
propagation; For local anesthesia,
epidural anesthesia
Skeletal Muscle Relaxant
A. Depolarizing Neuromuscular
Blocker
Agonist at Ach-N receptors causing
initial twitch then persistent
i. Succinylcholine depolarization ; For skeletal muscle
relaxation during intubation and
general anesthesia
B. Non-Depolarizing Neuromuscular
Blocker
Competitive antagonists at skeletal
muscle nicotinic acetylcholine
i. Mivacurium (short-acting: 10-
receptors; For skeletal muscle
20mins DOA)
relaxation during intubation and
general anesthesia
ii. Atracurium (intermediate-
acting)
iii. Vecuronium (intermediate-
acting)
iv. Rocuronium (intermediate-
acting)
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression, abuse
liability, severe hypertension,
cerebral hemorrhage, cardiac
arrhythmia, MI
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression, severe
CV toxicity, hypotension and
arrhythmias
light-headedness, sedation,
restlessness, nystagmus, seizures,
respiratory, CV depression,
cardiotoxicity
muscle pain, hyperkalemia,
increased intragastric pressure
leading to regurgitation (aspiration),
increased intraocular pressure,
malignant hyperthermia
a common SE for this group is
Histamine release
respiratory paralysis, apnea, and
moderate histamine release
respiratory paralysis, apnea, and
moderate histamine release and
bronchospasm
respiratory paralysis and apnea
respiratory paralysis and apnea,
hypersensitivity
Use cautiously in sunburns, Topical
only
with intrinsic sympathomimetic
activity so it does not need an alpha
agonist (like epinephrine) to limit its
systemic absorption; causes mood
elevation due to action on dopamine
receptor ; All local anesthetics are
vasodilators EXCEPT cocaine ;
Topical only
also available as Ophthalmic
solution
Frequently administered with
Epinephrine to avoid systemic
absorption
causes methemoglobinemia
(antidote: methylene blue)
Use with caution in pregnant
women and patients with cardiac
disease (may cause heartblock,
arrhyhtmia and hypotension)
Longest half-life among local
anesthesia
Metabolized by
pseudocholinesterase ; may cause
malignant hyperthermia if given
together with inhaled anesthetics
effects are easily reversed by giving
AChE inhibitors such as Neostigmine
Metabolized by
pseudocholinesterase; reverse
effects with Neostigmine
Undergoes Hoffman elimination
(rapid spontaneous breakdown);
reverse effects with Neostigmine ;
converted to Laudanosine which can
cause seizures
Undergoes elimination in bile;
reverse effects with Neostigmine
reverse effects with Neostigmine;
Suggamadex is a novel reversal
agent for rocuronium; most rapid
onset time (60-120 sec)
Page 15 of 56

v. Tubocurarine (long-acting)
vi. Pancuronium (long-acting)
Anti-Parkinsonism and other drugs
for movement disorders
A. Dopamine Precursor
i. Levodopa-carbidopa
B. Dopamine Agonist
i. Bromocriptine, Pergolide
ii. Pramipexole, Ropinirole
iii. Apomorphine
C. MAO type B inhibitor
i. Selegiline, Rasagiline
D. COMT inhibitor
i. Entacapone, Tolcapone
E. Antiviral
i. Amantadine
F. Anticholinergic
i. Benztropine, Biperiden,
Trihexyphenidyl, Orphenadrine
Competitive antagonists at skeletal
muscle nicotinic acetylcholine
receptors; For skeletal muscle
relaxation during intubation and
general anesthesia, euthanasia,
lethal injection, strychnine poisoning
Levodopa is a dopamine precursor,
carbidopa inhibits peripheral
metabolism via dopa decarboxylase;
Drug of choice for parkinsons
disease
Partial agonist at dopamine D2
receptors in brain; For Parkinsons
disease which is levodopa
intolerance, hyperprolactinemia
Partial agonist at dopamine D3
receptors in brain, Roprinole is a D2
agonist; For Parkinsons disease
Partial agonist at dopamine D3
receptors, antagonist at 5-HT and
alpha adrenoceptors; For off-periods
of Parkinsons disease, alcoholism,
opiate addiction, erectile
dysfunction, alzheimers disease
Selective inhibitors of MAO type B
leading to decreased degradation of
dopamine, increases response to
levodopa/carbidopa; Only as adjunct
to levodopa for parkinsons disease
but Rasigiline can be given alone
(more potent)
Block L-dopa metabolism by
inhibiting catechol-O-
methyltransferase in periphery and
CNS, prolongs response to levodopa;
used in the wearing-off phenomena
of parkinsons disease, as adjuncts
to levodopa
enhances dopaminergic
transmission by unknown
mechanism, maybe by influencing
the synthesis, release or reuptake of
dopamine; For Parkinsons disease
and influenza
Decrease the excitatory actions of
cholinergic neurons on cells in the
striatum by blocking muscarinic
respiratory paralysis, apnea,
hypotension and recurarization
respiratory paralysis, apnea,
tachycardia, hypertension,
recurarization
GI upset (emesis), dyskinesia
(choreoathetosis), behavioural
changes (anxiety, agitation,
confusion, delusion), on-off
phenomena, wearing-off
phenomena, postural hypotension,
tachycardia
anorexia, nausea, vomiting,
dyskinesia, postural hypotension,
behavioural changes,
erythromelalgia (Bromocriptine),
pulmonary infiltrate (Bromocriptine)
anorexia, nausea, vomiting,
dyskinesia, postural hypotension,
behavioural changes (more
prominent compared to levodopa)
severe nausea, dyskinesia,
hypotension, drowsiness and
sweating
insomnia, mood changes,
dyskinesias, GI distress and
hypotension
dyskinesias, GI distress, postural
hypotension, sleep disturbance,
orange discoloration of urine,
hepatotoxicity (tolcapone only),
neuroleptic malignant syndrome,
rhabdomyolysis
behavioural changes (restlessness,
agitation, insomnia, hallucination,
psychosis), livedo reticularis, GI
disturbances, urinary retention,
postural hypotension, peripheral
edema
drowsiness, inattention, confusion,
delusions, hallucinations, atropine-
like effects
Relatively contraindicated in
myocardial ischemia; reverse effects
with neostigmine
Reverse effects with Neostigmine,
may cause heart block
Contraindicated in patients with
history of psychosis; hypertensive
crisis occurs when used with MAO
inhibitors, ameliorates signs of
parkinsonism and decreases
mortality rate ; patient response
decreases with time but is improved
when given together with COMT
inhibitors
Ergot alkaloids
Contraindicated for patients with
active peptic ulcer disease, psychotic
illnesss or recent MI ; decrease dose
in renal dysfunction ;
Neuroprotective ; Ropirinole is
metabolized by CYP1A2
Premedicate with
Trimethobenzamide to prevent
severe nausea
serotonin syndrome occurs when
used with SSRI and Meperidine ;
Selegiline is hepatically metabolized
into desmethyl selegiline (which is
neuroprotective) and amphetamine
Entacapone only acts in the
periphery while Tolcapone acts both
in the periphery and CNS.
May improve bradykinesia, rigidity
and tremor ; has antimuscarinic
action
Exacerbate tardive dyskinesias that
result from prolonged use of
antipsychotic drugs; improve tremor
Page 16 of 56

Antipsychotics and Lithium
A. Typical Antipsyhotics
i. Phenothiazine: Chlorpromazine
ii. Other Phenothiazines:
Thioridazine, Fluphenazine,
Perphenazine, Prochlorperazine,
Trifluoperazine
iii. Butyrophenol: Haloperidol,
Droperidol
B. Atypical Antipsychotics
i. Clozapine
ii. Olanzapine
iii. Quetiapine
iv. Risperidone
v. Ziprasidone
vi. Aripiprazole
vii. Lithium (mood stabilizer)
receptors; as adjunct for parkinsons
disease and extrapyramidal
symptoms caused by antipsychotics
may also be used for pruritus and as
sedatives
Blocks D2 receptors >> 5-HT2
receptors; For schizophrenia and
other psychotic disorders
Blocks D2 receptors >> 5-HT2
receptors; For schizophrenia and
other psychotic disorders,
antiemesis (prochlorperazine)
Blocks D2 receptors >> 5-HT2
receptors; For schizophrenia and
other psychotic disorders,
huntingtons disease and tourettes
syndrome
may be used for mania and
psychotic symptoms in Alzheimer's
dementia and Parkinsons disease
Blocks 5-HT2 receptors >> D2
receptors; For schizophrenia
(refractory, suicidal) and other
psychotic disorders
Blocks 5-HT2 receptors >> D2
receptors; For schizophrenia, bipolar
disorders, anorexia nervosa and
depression
Blocks 5-HT2 receptors >> D2
receptors; For schizophrenia, bipolar
disorders (manic)
Blocks 5-HT2 receptors >> D2
receptors; For schizophrenia, bipolar
disorders, depression, intractable
hiccups, tourette syndrome
Blocks 5-HT2 receptors >> D2
receptors; For schizophrenia, bipolar
disorders (acute mania)
Blocks 5-HT2 receptors >> D2
receptors; For schizophrenia, bipolar
disorders, depression, autism,
cocaine dependence
Uncertain MOA but the proposed
MOA is by inhibiting the enzyme
involved in the recycling of neuronal
membrane phosphoinositides which
causes depletion of
phosphatidylinositol bisphosphate,
thus consequently decreasing IP3
and DAG --> decrease in
neurotransmission ; For bipolar
and rigidity with little effect on
bradykinesia
has no effect on negative symptoms
extrapyramidal dysfunction, tardive
dyskinesia, hyperprolactinemia,
atropine-like effects, failure of
prototype of all typical
ejaculation, postural hypotension,
antipsychotics
marked sedation, corneal and lens
deposits, neuroleptic malignant
syndrome, contact dermatitis
Thioridazine has the Strongest
extrapyramidal dysfunction, tardive
autonomic effects; only
dyskinesia, hyperprolactinemia,
antipsychotic with fatal overdose ;
atropine-like effects, failure of
Fluphenazine and Trifluoperazine
ejaculation, postural hypotension,
have very significant parkinson-like
retinal deposits (thioridazine),
effect ; Fluphenazine has less
cardiotoxicity (arrhythmias -
sedation compared to other anti-
thioridazine)
psychotics
causes the most extrapyramidal
extrapyramidal dysfunction, tardive
symptoms of all typical anti-
dyskinesia, hyperprolactinemia,
psychotics ; has the weakest
neuroleptic malignant syndrome
autonomic effects
cure both negative and positive
symptoms
Extrapyramidal dysfunction (less),
hyperprolactinemia (less), postural Only antipsychotic that reduces the
hypotension, weight gain, risk of suicide ; may be effective for
hyperglycemia, hyperlipidemia, drug-resistant types ; weight gain,
myocarditis, agranulocytosis, agranulocytosis, seizure and
seizures, ileus, hypersalivation hyperglycemia is prominent
(sialorrhea)
Extrapyramidal dysfunction (less),
hyperprolactinemia (less), postural weight gain and hyperglycemia is
hypotension, weight gain, prominent, safe in pregnancy
hyperglycemia, hyperlipidemia
Extrapyramidal dysfunction (less),
hyperprolactinemia (less), postural
hypotension, weight gain,
can cause TDP, safe in pregnancy
somnolence, fatigue, sleep paralysis,
hypnagogic hallucinations, cataracts,
priapism, QT prolongation (TDP)
Extrapyramidal dysfunction (less),
Only antipsychotic approved for
hyperprolactinemia (marked),
schizophrenia in the youth
insomnia, photosensitivity
Extrapyramidal dysfunction (less), Increased mortality in elderly
postural hypotension, QT patients with dementia-related
prolongation (TDP) psychosis ; can cause TDP
Extrapyramidal dysfunction (less), GI
Least sedating atypical
upset, tremor, hypersensitivity
antipsychotics
(rare)
Tremor, sedation, ataxia, aphasia, Contraindicated in sick sinus
thyroid enlargement, syndrome; treat overdose with
hypothyroidism, reversible hemodialysis ; high volume of
nephrogenic diabetes insipidus, distribution ; clinical benefit is seen
edema, acneiform skin eruption, only after weeks of use ;
leukocytosis, teratogen (ebsteins antipsychotic agents or BZDs are
anomaly), bradycardia, some drugs commonly required at initiation
(NSAIDs, ACEi, diuretis etc) can therapy of Li and valproic acid ;
increase Lithium toxicity while Contraindicated in lactation ;
Page 17 of 56

Antidepressants
A. Tricyclic Antidepressants
i. Imipramine, Clomipramine,
Desipramine, Amitryptyline,
Nortryptiline
B. SSRI
i. Fluoxetine, Paroxetine,
Citalopram, Escitalopram,
Sertraline, Fluvoxamine
C. SNRI
i. Venlafaxine, Duloxetine,
Desvenlafaxine
D. Serotonin antagonist
i. Trazodone, Nefazodone
E. Tetracyclics
i. Amoxapine
ii. Mirtazapine
iii. Bupropion
F. MAO Inhibitors
disorder, recurrent depression,
schizoaffective disorder
Block NE and 5-HT transporters
leading to potentiation of NT action
at postsynaptic receptors; For MDD
(most effective), bipolar disorder,
acute panic attacks, ADHD, chronic
pain states, as sleeping aid, OCD
(Clomipramine) ; this group is very
useful for patients with
psychomotor retardation, sleep
disturbance, poor appetite and
weight loss
Inhibits neuronal reuptake of
serotonin by inhibiting Serotonin
Transporter (SERT); DOC for OCD,
for MDD, anxiety, panic attacks,
phobias, PTSD, GAD, bulimia,
premenstrual dysphoric disorder,
alcohol dependence
Inhibits neuronal reuptake of
serotonin and norepinephrine by
binding to transporters for both 5HT
and NE; For MDD, fibromyalgia,
neuropathic pain, menopausal
symptoms
Blocks 5-HT2A receptors, weak
inhibitor of NE and 5HT
transporters; For MDD, as sleeping
aid (trazodone)
Strong norepinephrine reuptake
inhibitor and weak serotonin
reuptake inhibitor, blocks dopamine
D2 receptors; For MDD
Increases amine release from nerve
endings by antagonism of
presynaptic a2 adrenoceptors, also
blocks serotonin 5-HT2A receptors;
For MDD, appetite stimulation, as
sleeping aid
Inhibits neuronal reuptake of
dopamine and norepinephrine,
increase dopamine and
norepinephrine activity; For MDD
and smoking cessation, alcohol
dependence
caffeine and theophylline can
decrease its toxicity
excessive sedation, fatigue,
confusion, sympathomimetic
effects, atropine-like effects,
orthostatic hypotension,
cardiomyopathies, arrhythmias,
tremors, paresthesias, weight gain ;
3Cs of overdose: Coma,
Cardiotoxicity, Convulsions
nausea, vomiting, headache,
anxiety, agitation, drowsiness,
insomnia, erectile dysfunction, EPS,
QT prolongation (citalopram),
withdrawal syndrome
dizziness, insomnia, sedation, GI
distress, hypertension (venlafaxine),
hepatotoxicity (duloxetine),
withdrawal syndrome even in just
one missed dose, CNS stimulation
(Venlafaxine), liver dysfunction
(Duloxetine)
sedation, GI disturbance, orthostatic
hypotension, priapism,
hyperprolactinemia, liver
dysfunction (nefazodone)
autonomic effects, akathisia,
parkinsonism (due to dopamine
receptor blockade), seizures,
cardiotoxicity
weight gain, marked sedation,
dizziness, blurred vision and
nightmares
weight loss, agitation, anxiety,
dizziness, dry mouth, aggravation of
psychosis, seizures, priapism
Natriuresis stimulates reflex
increase in the reabsorption of Li
and Na in the PCT
Additive depression of the CNS with
other central depressants ;
Imipramine is metabolized to
desipramine while amitriptyline is
metabolized to nortriptyline ;
longterm use may lead to down-
regulation of Beta receptors leading
to a decrease in BP and depression
of cardiac conduction ; has
significant muscarinic receptor
blocking effect esp Amitriptyline ;
lower seizure threshold ; may
interfere with antihypertensive
action of Clonidine
Serotonin syndrome when used with
MAOIs ; minimal inhibitory effect on
cholinergic or adrenergic receptors ;
lower seizure threshold ; this group
can decrease appetite leading to
weight loss ; Increased risk for
suicide in children and adolescents ;
Fluoxetine, Fluvoxamine and
Paroxetine are CYP450 inhibitors
venlafaxine has less affinity for NE
transporter than desvenlafaxine and
duloxetine ; differ from TCA in
lacking blockade of H1, M and alpha
receptors ; Increased risk for suicide
in children and adolescents
May cause arrhythmias in px with
pre-existing cardiac disease ; short
t1/2 so given BID to TID, has
significant muscarinic receptor
blocking effect esp Nefazodone ;
CYP450 inhibitors ; Trazodone also
has significant alpha1 and H1
blocking effect
Increased risk for suicide in children
and adolescents
Lowers seizure threshold, has
significant muscarinic receptor
blocking effect
has significant muscarinic receptor
and alpha2 blocking effect
Lowers seizure threshold, for
smoking cessation ; no effect on 5HT
or NE receptors or amine
transporters ; CYP450 inhibitor
Page 18 of 56
 Inhibits MAO type A and type B,
increases CNS levels of NE and
serotonin, Phenelzine and
Tranylcypromine are nonselective
i. Phenelzine, tranylcypromine, MAO inhibitors while Selegiline is a
selegiline MAO-B selective inhibitor; For MDD
unresponsive to other agents ;
useful in patients with significant
anxiety, phobic features and
hypochondriasis
Opioid Analgesics and Antagonists
A. Full Agonist
Strong agonist at u receptors; For
i. Morphine severe pain, pain associated with
acute MI, for pulmonary edema
Strong agonist at u receptors; For
severe pain, adjunct in anesthesia,
ii. Fentanyl
chronic pain and breakthrough
cancer pain
Strong agonist at u and k receptors,
inhibits pain neurotransmission,
muscarinic blocking actions; For
iii. Meperidine
moderate to severe pain, labor
analgesia, spasmodic pain (biliary,
renal), preoperative sedation
Strong agonist at u receptors,
inhibits pain neurotransmission,
binds NMDA receptors and
iv. Methadone antagonizes the effects of
glutamate; For moderate to severe
pain, opioid dependence, opioid
withdrawal
B. Partial Agonist / Moderate
Agonist
Strong agonist at u receptors,
inhibits pain neurotransmission,
binds NMDA receptors and
i. Hydrocodone, oxycodone antagonises the effects of
glutamate; For moderate to severe
pain, opioid dependence, opioid
withdrawal
Decreases sensitivity of cough
receptors, depressing the medullary
ii. Dextrometorphan, codeine cough center through sigma
receptors stimulation; For cough
suppression
C. Weak Agonist
Weak agonist at u receptors, inhibits
i. Propoxyphene,
pain neurotransmission; For mild to
levopropoxyphene,
moderate pain, restless leg
dextropropoxyphene
syndrome
D. Mixed Agonist-Antagonist
Strong agonist at k receptors, weak
antagonist activity at u receptors;
i. Nalbuphine, buprenorphine, For moderate to severe pain, opioid
butorphanol, pentazocine dependence, alcohol dependence,
balance anesthesia, for opioid
withdrawal states (buprenorphine)
dizziness, insomnia, orthostatic
hypotension, blurred vision,
arrhythmia, diarrhea, hyperthermia,
CNS stimulation, seizure
TRIAD: miosis, coma, respiratory
depression
miosis, restlessness, respiratory
depression, increased ICP, postural
hypotension, urinary retention,
pruritus, addiction liability
restlessness, respiratory depression,
increased ICP, postural hypotension,
urinary retention, pruritus, addiction
liability
restlessness, respiratory depression,
increased ICP, postural hypotension,
urinary retention, pruritus, addiction
liability, seizures
miosis, restlessness, respiratory
depression, increased ICP, postural
hypotension, urinary retention,
pruritus, addiction liability
miosis, restlessness, respiratory
depression, increased ICP, postural
hypotension, urinary retention,
pruritus, addiction liability
hallucination, confusion, excitation,
increased or decreased pupil size,
nystagmus, seizures, coma,
respiratory depression, addiction
liability
miosis, respiratory depression,
increased ICP, postural hypotension,
urinary retention, pruritus, addiction
liability, fatal arrythmias
sedation, dizziness, sweating,
nausea, anxiety, hallucinations,
nightmares, respiratory depression
(less), tolerance, dependence
liability
Hypertensive crisis when taken with
tyramine-rich food, serotonin
syndrome when taken with SSRI ;
this group is structurally related to
amphetamine ; CYP450 inhibitors ;
longterm use may lead to down-
regulation of Beta receptors (leading
to decrase in BP) ; lower seizure
threshold ; selegiline may be given
as skin patch
Additive CNS depression with other
depressants
Exerts hemodynamic effects on the
pulmonary circulation ; significant
first-pass effect ; metabolized in the
body to morphine-6-glucuronide
which has equal analgesic activity as
morphine
May be given transdermally or via
lollipop; ohmefentanyl is the most
potent opioid
Only opioid that does not cause
miosis and biliary contraction ;
opioid of choice for pain relief in
pancreatitis ; metabolized to
normeperidine which can cause
seizure therefore contraindicated in
patients with seizure disorder ; if
given with MAOi --> Hyperpyrexic
coma, if given with SSRI -->
Serotonin syndrome
Used in methadone maintenance
therapy (MMT) for opioid
dependence; currently being
investigated as a novel treatment
for leukemia
there is genetic variation in the
metabolism of codeine and its
derivatives
codeine is metabolized by CYP2D6
to morphine
Withdrawn because of fatal
cardiotoxicity
Buprenorphine reduces craving in
alcohol dependence, buprenorphine
and nalbuphine is resistant to
Naloxone
Page 19 of 56
E. Opioid Antagonist
i. Naloxone, naltrexone,
nalmefene
F. Dual-acting
i. Tramadol
5. DRUGS USED TO TREAT DISEASES OF THE BLOOD, INFLAMMATION, & GOUT
Agents Used in Anemias and Hematopoietic Growth Factors
A. Hematopoietic growth factor
i. Ferrous sulfate, Ferrous
gluconate, Ferrous Fumarate, Iron
dextran, Sodium Ferric Gluconate
complex, Iron sucrose
B. Heavy metal chelator
i. Deferoxamine, Deferasirox
C. Hematopoietic growth factor
i. Cyanocobalamin,
Hydroxocobalamin
D. Hematopoietic growth factor
i. Folic acid, Folacin
(Pteroylglutamic acid), Folinic acid
E. Hematopoietic growth factor
i. Epoetin Alfa, Darbepoetin alfa, expressed by red cell progenitors;
Methoxy Polyethylene Glycol-
Epoetin Beta
F. Myeloid growth factor
i. (G-CSF) Filgrastim, Sargamostim Accelerates neutrophil recovery and
(GM-CSF), Pegfilgrastim
G. Megakaryocyte growth factor
i. Oprelvekin(IL-11),
Thrombopoietin
Agents Used in Dyslipidemia
A. HMG-CoA Reductase Inhibitors:
Simvastatin, Atorvastatin,
Rosuvastatin, Fluvastatin,
Competitively blocks u, sigma and k
receptors, rapidly reverses effects of
opioid agonists; For opioid
overdose, opioid and alcohol
dependence (naltrexone)
Weak agonist at u receptors, inhibits
neuronal reuptake of serotonin and
norepinephrine; For moderate pain,
chronic pain syndrome, neuropathic
pain
Required for the biosynthesis of
heme and heme containing proteins,
including hemoglobin and
myoglobin; For Iron deficiency
anmia, iron supplementation
Chelates excess iron; For acute and
chronic iron poisoning
Cofactor required for essential
enzymatic reactions that form
tetrahydrofolate, convert
homocysteine to methionine and
metabolize methylmalonyl-CoA; For
vitamin B12 deficiency,
megaloblastic anemia
Precursor of an essential donor of
methyl groups used for synthesis of
amino acids, purines and
deoxynucleotide; For Megaloblastic
anemia, prevention of neutral tube
defects (spina bifida), prevention of
coronary artery disease
Agonist of erythropoietin receptors
For Anemia, associated with chronic
renal failure, cancer, HIV infection
and prematurity
Binds receptors on myeloid
progenitors and stimulates cell
maturation and proliferation ;
reduces incidence of infection; For
neutropenia associated with
chemotherapy, myelodysplasia, and
aplastic anemia
Recombinant form of an
endogenous cytokine; activates IL -
11 receptors ; For secondary
prevention of thrombocytopenia in
patients undergoing chemotheraphy
Inhibits rate-limiting enzyme in
cholesterol biosynthesis (HMG-CoA
reductase), Increased hepatic
pruritus, nausea, vomiting
seizures, nausea, dizziness, pruritus,
constipation
Black stools, shock, lethargy,
dyspnea, abdominal pain,
necrotizing gastroenteritis, death,
organ failure, hemochromatosis,
metabolic acidosis
Hypotension, Neurotoxicity, ARDS,
Increased susceptibility to infections
No significant toxicity
No significant toxicity
Hypertension, Thrombosis, Pure red
cell aplasia
Edema, Fever, Arthralgia
fatigue, headache, anemia, fluid
accumulation in the lungs, dizziness,
transient atrialarrythmias
Hepatoxicity, Myopathy,
Rhabdomyolysis, Gastrointestinal
distress, Teratogen
Precipitates abstinence syndrome in
Px with opioid dependence ;
Naloxone and Nalmefene is IV (DOA:
12-24 hrs) while Naltrexone is PO
(DOA: 48h)
Lower seizure threshold ; CI in Px
taking SSRI and those with history of
seizure
None
None
Hydroxocobalamin has a longer t1/2
than cyanocobalamin ; has a storage
of up to 5yrs in the liver
only modest amounts are stored in
the body
Performance-enhancing drug in
athletes ; darbepoietin is once a
week administration, while Methoxy
Polyethylene Glycol- Epoetin Beta is
1-2x per month administration
Pegfilgrastim has longer t1/2
given SC OD
has direct anti-atherosclerotic
effect, and can prevent bone loss ;
Increased risk of myopathy and
Page 20 of 56
Pravastatin, Lovastatin,
Pitavastatin, Cerivastatin,
B. Bile Acid Binding Resin:
Colesevelam, Colestipol,
Cholestyramine
C. NPC1L1 transporter inhibitor:
Ezetimibe
D. Sterol absorption blocker:
Sitosterol
E. Nicotinic Acid derivatives: Niacin
F. Fibrates: Gemfibrozil,
Fenofibrate, Bezafibrate
Drugs for Coagulation
A. Antiplatelet
i. Aspirin
cholesterol uptake, Increased high
affinity LDL receptors which leads to
decreased LDL levels ; DOC for
hypercholesterolemia (high LDL),
decreases risk of acute coronary
syndromes, ischemic stroke
non-absorbable polymers that bind
bile acids and similar steroids in the
intestines preventing their
reabsorption, increases cholesterol
utilization for replacement,
modestly lowers LDL levels by
increasing hepatic LDL receptors ;
For hypercholesterolemia (high LDL),
pruritus in cholestasis, digitalis
toxicity
Selective inhibitor of the NPC1L1
transporter decreasing intestinal
absorption of cholesterol and other
phytosterols, decreases cholesterol
hepatic pool, increases hepatic LDL
receptors ; For
Hypercholesterolemia (High LDL),
phytosterolemia
Cholesterol analog, takes the place
of dietary and billiary cholesterol,
decreasing intestinal absorption of
cholesterol and other phytosterols ;
For Hypercholesterolemia (high
LDL), phytosterolemia
Decreases VLDL synthesis and LDL
cholesterol concentrations,
decreases hormone-sensitive lipase
activity leading to decreased LDL
levels, Increases HDL cholesterol by
decreasing its catabolism ; DOC for
increasing HDL levels, for
Hypercholesterolemia (low HDL,
high LDL/VLDL),
hypertriglyceridemia
Activates PPAR- and increases
expression of lipoprotein lipase and
apolipoproteins (apoA-I, apoA-II)
leading to enhanced clearance of
TG-rich lipoproteins, Lowers
triglycerides, Increases HDL ; DOC
for hypertriglyceridemia
For arterial thrombosis only
Nonselective, irreversible COX 1&2
inhibitor. Reduces platelet
production of thromboxane A2,
temporarily inhibit Prostacyclin
synthesis ; For prevention or arterial
thrombosis (MI, TIA, CVD),
Inflammatory disorders (rheumatic
Constipation, Bloating, Gritty taste,
Gallstone formation, steatorrhea,
malabsortion of fat soluble
substances (vitamin k, folate)
Hepatoxicity (increased with statin
use), Myositis
Gastrointestinal upset, bloating,
impotence (rare), coronary events
Flushing, nausea, vomiting, Pruritus,
Acanthosis nigricans, Rashes,
Gastrointestinal irritation,
Hepatoxicity (mild), Hyperuricemia,
Impaired glucose tolerance,
Arrhythmias, Ambylopia
rhabdomyolysis when used with
Nausea, Rashes, Leukopenia,
nausea, vomiting, increased risk of
cholesterol gallstones
Gastrointestinal toxicity,
nephrotoxicity, tinnitus,
hyperventilation, hypersensitivity,
HAGMA, Increased bleeding time,
Nephrotoxicity (AKI and Interstitial
Nephritis)
rhabdomyolysis when used with
fibrates ; Given before bedtime
because cholesterol synthesis
predominantly occurs at night ;
simvastatin and lovastatin are
prodrugs, all the rest are in their
active form already ; Rosuvastatin,
Atorvastatin and Simvastatin have
greater maximal effect than other
statins ; if given together with resins
give at least 1hr before or 4hrs after
resin administration (resins decrease
the absorption of statins) ; has
CYP450 dependent metabolism
Increases TGs and VLDL in patients
with high TGs and combined
hyperlipidemia ; Treat constipation
with fiber supplements/psyllium ;
Avoid in patients with diverticulitis
Synergistic LDL-lowering effect with
statins ; is a prodrug
NONE
decreases fibrinogen and increases
t-PA ; NSAIDs pre-treatment reduces
flushing ; Avoid in patients with
peptic ulcer disease ; Potentiates
effects of antihypertensives
(vasodilators, ganglion blockers)
Increased risk of myopathy and
statins ; Avoided in patients with
hepatic or renal dysfunction ; may
increase LDL in patients with familial
combined hyperlipoproteinemia ;
has little or no effect on LDL ; higher
risk of gallstone formation if given
together with resins
Uncoupler of oxidative
phosphorylation, associated with
Reye syndrome in children ; Do not
use as NSAID for gout
Page 21 of 56

ii. GPIIb-IIIa inhibitor: Abciximab,
Eptifibatide,Tirofiban
iii. PDE III inhibitor: Dipyridamole,
Cilostazol
iv. ADP inhibitor:
Clopidogrel,Ticlopidine, Prasugel
B. Anticoagulant
i. Heparin (indirect thrombin
inhibitor)
ii. LMWH: Enoxaparin, Dalteparin,
Tinzaparin, Fondaparinux
iii. Direct Thrombin Inhibitors:
Lepirudin, Desirudin, Bivalirudin,
Argatroban, Dabigatran
iv. Direct Oral Factor Xa inhibitor:
Rivaroxaban, Apixaban
v. Warfarin, Dicumarol
fever, juvenile rheumatoid arthritis,
kawasaki disease)
Reversbily inhibits the binding of
fibrin and other ligands to the
platelet GPIIb-IIIa receptor ; For
Bleeding, Thrombocytopenia Adjunct to thrombolysis
antithrombosis during PCI, Acute
coronary syndromes (unstable
angina, NSTEMI)
Inhibits phosphodiesterase III and
increases cAMP in platelets and
blood vessels, Inhibits platelet
additional MOA: inhibit uptake of
aggregation and causes vasolidation
adenosine by endothelial cells and
; For prevention of thromboembolic
RBC, thus increasing adenosine
complications of cardiac valve Headache, palpitations
levels leading to inhibition of
replacement (as adjunct to
platelet aggregation ; Cilostazol is
warfarin), secondary prevention of
contraindicated in heart failure
ischemic stroke (with aspirin),
Intermittent claudication (Cilostazol
only)
Irreversibly inhibits binding of ADP
to platelet receptors,thus reducing
Bleeding, nausea, hematologic
platelet aggregation ; For prevention GI & Hematologic SE are more
(neutropenia, leukopenia),
and treatment of arterial thrombosis common with ticlopidine. Additive
thrombotic thrombocytopenic
(stroke, TIA, unstable angina), Acute effects with aspirin
purpura (Ticlopidine), dyspepsia
coronary syndromes, Prevention of
re-stenosis after PCI
For both venous and arterial
thrombosis
Activates antithrombin III which
Inactivates thrombin or factor IIa,
factor IXa & factor Xa by forming
stable complexes with them ; For
deep venous thrombosis, myocardial
dysfunction, Pulmonary embolism, DOC for anticoagulation during
Bleeding, transient Heparin-induced
adjuvant to percutaneous coronary pregnancy ; administered IV or SC ;
thrombocytopenia, Osteoporosis
intervention (PCI) and Monitor with aPTT, Antidote:
with chronic use
thrombolytics, Atrial fibrillation, Protamine Sulfate
Pulmonary embolism, given with
thrombolytics for revascularization
procedures, given with GPIIb-IIIa
inhibitors for angioplasty and stent
placement
Binds and potentiates effect of
antithrombin III on factor Xa (more Does not require aPTT monitoring,
selective for Xa); For Deep venous Protamine sulfate is only partially
thrombosis, Pulmonary embolism, Bleeding, less risk of effective in reversing effects ;
unstable angina, myocardial thrombocytopenia advantage over regular heparin is
infarction, adjuvant to percutaneous higher bioavailability and t1/2 ;
coronary intervention (PCI) and Fondaparinux is given SC OD
thrombolytics, Atrial fibrillation
Binds to thrombin's ative site and
Monitor with aPTT. No reversal
inhibits its enzymatic action; For
agents exist ; Dabigatran is PO while
anticoagulation in patients with Bleeding, Anaphylactic reactions,
all the rest are parenteral ;
heparin induced thrombocytopenia Effect-prolonging antibodies
Bivalirudin also inhibits platelet
(HIT), percutaneous coronary
activation
angioplasty (Bivalirudin with aspirin)
bind to free and bound factor Xa ;
For prevention of Venous
bleeding No reversal agent
thrombosis, in stroke patients with
Afib
Inhibits vitamin K epoxide reductase
(responsible for y-carboxylation of Bleeding, Teratogen (bone defects, Monitor effects with PT-INR.
the vitamin K- dependent clotting hemorrhage), warfarin-induced skin Antidote is vitamin K or FFP. Narrow
(factors II, VII, IX, X, Protein C & necrosis (transient therapeutic window ; 99% protein-
Protein S) ; For chronic hypercoagulability) bound
anticoagulation (DVT, atrial
Page 22 of 56

C. Antidote
i. Protamine Sulfate
ii. Endogenous Vitamin: Vitamin
K1, K2, K3 (Phytonadione,
Menaquinone, Menadione)
D. Thrombolytic: Alteplase,
Anistreplase, Reteplase,
Streptokinase, Tenecteplase,
Urokinase
E. Antiplasmin drug: Tranexamic
acid
F. ADH agonist: Desmopressin
Non-steroidal Anti-Inflammatory
Drugs, Disease-Modifying Anti-
rheumatic Drugs, Non-opioid
Analgesics & Drugs Used in Gout
A.Non-selective NSAID
i. Aspirin, Sodium Salicylate
ii. Ibuprofen, Diclofenac,
Diflunisal, Etodolac, Fenoprofen,
Flurbiprofen, Ketoprofen,
Meloxicam, Nabumetone,
Naproxen, Oxaprozin, Piroxicam,
Sulinidac, Tolemtin, Mefenamic
acid, Ketorolac
iii. Indomethacin
fibrillation, valve replacement)
EXCEPT in pregnancy
Chemical antagonist of heparin.
Reverses excessive anticlotting
activity of unfractionated heparin;
For heparin overdosage
Increases supply of reduced vitamin
K, which is required for synthesis of
functional vitamin K-dependent
clotting and anticlotting factors ; For
Vitamin K deficiency, Antidote to
warfarin, prevention of hemorrhagic
diatheses in newborns
Tissue plasminogen activator analog.
Converts plasminogen to plasmin,
which degrades the fibrin and
fibrinogen, causing thrombolysis ;
For acute myocardial infarction,
pulmonary embolism, Ischemic
stroke
Competitively inhibits plasminogen
activation thus inhibiting fibrinolysis
; For prevention and treatment of
acute bleeding episodes in patients
with high risk of bleeding
(hemophilia, intracranial aneurysms,
menstrual, obstetrics, thrombolytics,
postperative)
Vasopressin V2 receptor agonist,
Increases factor VIII activity of
patients with mild hemophilia A or
VWD; For hemophillia A, von
Willebrand's disease, central
diabetes insipidus
See entry on Drugs for caogulation
Disorder
Nonselective reversible COX-1 and
COX-2 inhibitor. Inhibits
prostaglandin and thromboxane
synthesis ; For analgesia, fever and
as anti inflammatory
Nonselective reversible COX-1 and
COX-2 inhibitor. Inhibits
prostaglandin synthesis and inhibit
crystal phagocytosis by
macrophages ; For anti
inflammatory (gout arthritis,
ankylosing spondylitis), for closing
PDA
hypotension, flushing, bradycardia,
dyspnea, hypersensitivity
Severe infusion reaction when
administered at a fast rate (dyspnea,
chest and back pain)
Bleeding, Reperfusion, Cerebral
hemorrhage, Arrhythmias ; Loss of
effectiveness (on 2nd use) and
allergic reactions (streptokinase)
Thrombosis, hypotension,
Myopathy, Diarrhea
headaches, nausea, flushing,
seizures, hyponatremia
See entry on Drugs for caogulation
Disorder
Gastrointestinal bleeding (less than
aspirin), Nephrotoxicity (AKI and
Interstitial Nephritis),
Hypersensitivity reaction
Gastrointestinal toxicity,
pancreatitis, Nephrotoxicity, Serious
hematologic reactions, BM
suppression
Partially reverses effect of LMWHs
Vit K1 may be given PO or IV
Tx should be done within 6 hrs,
better if within 3hrs ; Antidote is
AMINOCAPROIC ACID ;
Streptokinase forms a complex with
endogenous plasminogen, thus
catalyzing the conversion of
plasminogen to plasmin ; tPA is
selective for fibrin-bound
plasminogen
Contraindicated in disseminated
intravascualr coagulation (DIC) and
genitourinary bleeding
may cause immunologic reactions
and infections
low doses undergo first order
kinetics while high doses undergo
zero order reaction ; Long term use
reduces the risk of colon cancer
Ibuprofen and Indomethacin can be
used to close PDA ; Ibuprofen and
naproxen have moderate
effectiveness ; Ibuprofen is relatively
safe but with short half-life of 2hrs ;
Naproxen and Piroxicam have longer
half-lives ; Ketorolac has significant
analgesic effect but not anti-
inflammatory effect ; use Ketorolac
only for 72hrs due to GI and renal
damage ; NSAIDs may interfere with
ASA's antithrombotic action
Indomethacin has greater anti-
inflammatory effect compared to
other NSAIDs
Page 23 of 56
 Selective COX-2 inhibitor. Inhibits Gastrointestinal bleeding,
Rofecoxib and Valdecoxib
B. COX-2 Selective NSAID: prostaglandin synthesis ; For Nephrotoxicity (same risk as
withdrawn due to incereased
Celecoxib, Etoricoxib, Parecoxib Analgesia, Anti inflammatory, nonselective NSAIDs), Myocardial
incidence of thrombosis
Antipyretic infarction and stroke
Selectively inhibits COX-3 in the CNS,
Hepatoxicity (antidote: NAC), Renal
C. Non-opioid Analgesic (COX3 Weak COX-1 and COX-2 inhibitor in Preferred antipyretic in children
papillary necrosis and Interstitial
inhibitor) Paracetamol the periphery, Inhibits prostaglandin (does not cause reye's syndrome) ;
nephritis, Methemoglobinemia,
(Acetaminophen) synthesis ; For Analgesia and t1/2 is only 2-3h
Hemolytic anemia
antipyretic
D. Disease Modifying Anti-
Rheumatic Drug
Inhibits AICAR transformylase and
thymidylate synthase, with
Nausea, Mucosal ulcers,
secondary effects on DMARD of choice for Rheumatoid
hepatoxicity, hypersensitivty,
i. Methotrexate polymorphonuclear chemotaxis ; For arthritis, Rescue agent: Leucovorin
Pseudolymphomatous reaction,
rheumatoid arthritis, SLE, JRA, (Folinic acid)
teratogen, hematotoxicity
psoriatic arthritis, Ankylosing
spondylitis, Polymyositis
Bacterial infections (URTIs),
reactivation of latent tuberculosis,
lymphoma, Demyelination,
Binds or inhibits to TNF-a ; For
ii. TNF-alpha inhibitor: Infliximab, Reactivation of Hepatitis B, Auto Synergistic effects with
Crohn's disease, rheumatoid
Adalimumab, Etanercept antibody formation (ANA, anti methotrexate
arthritis, other rheumatic disease
dsDNA), infusion reactions,
hepatoxicity, hematotoxicity,
cardiotoxicity
Forms 6-thioguanine, suppressing
Cannot give allopurinol with
inosinic acid synthesis, B-cell and T-
Bone marrow supression, increased azathioprine (allopurinol reduces
cell function, Immunoglobulin
risk of infections, increased xanthine oxidase catabolism of
iii. Azathioprine production and interleukin-2
incidence of lymphoma, Fever, rash, purine analogs, increasing 6-
secretion ; For rheumatoid arthritis,
hepatotoxicity, allergic reactions thioguanine nucleotides, leading to
psoriatic arthritis, reactive arthritis,
severe leukopenia)
polymyositis, SLE
Suppression of T-lymphocyte leading
to decreased leukocyte chemotaxis,
Ocular toxicity, Dyspepsia, Nausea,
stabilization of lysosomal enzymes,
iv. Chloroquine, vomiting, abdominal pain, rashes,
inhibition of DNA and RNA synthesis, safe for pregnant women
Hydroxychloroquine nightmares, myopathy, neuropathy,
trapping of free radicals ; For
ocular toxicity
rheumatiod arthritis, SLE, Sjogren's
syndrome, Malaria
Forms phospharamide mustard,
which cross links DNA to prevent cell
replication, Supresses T-cell and B-
Hemorrhagic cystitis, Rescue agent
v. Cyclophosphamide cell function ; For Rheumatoid Hemorrhagic cystitis
is Mesna
arthritis, SLE vasculitis, Wegener's
granulomatosis, severe rheumatic
diseases
Inhibits interleukin-1 and iterleukin-
2 receptor production and
Nephrotoxicity, hypertension,
secondarily inhibits macrophage-T-
vi. Cyclosporine hyperkalemia, hepatoxicity, Gingival NONE
cell interaction and T-cell
hyperplasia, hirsutism
responsiveness ; For rheumatoid
arthritis, SLE, Tissue transplantation
active product inhibits inosine
monophosphate dehydrogenase and
Gastrointestinal disturbances,
inhibits T-cell lymphocyte
vii. Mycophenolate Mofetil headache, hypertension, reversible NONE
proliferation ; For SLE nephritis,
myelosupression
vasculitis, Wegener's
granulomatosis, rheumatoid arthritis
Nausea, vomiting headache,rash,
active metabolite inhibits the hemolytic anemia,
release of inflammatory bowel methemoglobinemia, neutropenia,
viii. Sulfasalazine cytokines; For rheumatoid arthritis, leukopenia, thrombocytopenia, anti-IBD drugs
inflammatory bowel disease, JRA, pulmonary toxicity, autoantibody
ankylosing spondylitis formation (anti dsDNA), Reversible
infertility in men

Page 24 of 56
E. Antigout drugs
i. Microtubule assembly inhibtor:
Colchicine
ii. Uricosuric agent: Probenecid,
Sulfinpyrazone
iii. Xanthine oxidase inhibitor:
Allopurinol, Febuxostat
Inhibits microtubule assembly and
LTB4 production leading to
decreased macrophage migration
and phagocytosis ; For gout
are weak acids that compete with
uric acid for reabsorption in the PCT
leading to increased uric acid
excretion ; For gout
Active metabolite (alloxanthine)
irreversibly inhibits xanthine oxidase
and lowers production of uric acid;
1st line treatment of chronic gout,
tumor lysis syndrome
Diarrhea, nausea, vomiting,
a general mitotic poison, may also
abdominal pain, hepatic necrosis,
be used for Familial Mediterranean
acute renal failure, disseminated
Fever ; diarrhea is the adverse effect
intravascular coagulation, seizures,
which signals toxicity from
hair loss, bone marrow depression,
colchicine
peripheral neuritis, myopathy
May precipitate acute gout during
early phase of drug action (prevent
by coadministering with colchicine
Gastrointestinal irritation, rashes,
or indomethacin) ; may be given
nephrotic syndrome, aplastic
together with antimicrobial agents
anemia ; sulfa allergy
(particularly Penicillins) to prolong
therapeutic effect by inhibiting renal
tubular secretion of antibiotics
Inhibits metabolism of
mercaptopurine and azathioprine.
Witheld for 1-2 wk after an acute
Gastrointestinal upset, Rash,
episode of gouty arthritis
Peripheral neuritis, Vasculitis, bone
(coadministered with colcichine or
marrow dysfunction, Aplastic
indomethacin to avoid an acute
anemia, liver dysfunction
attack) ; Feboxustat is a newer non-
(Febuxostat)
purine inhbitor of Xanthine Oxidase ;
Febuxostat is more effective than
Allopurinol

6. ENDOCRINE DRUGS
Hypothalamic and Pituitary
Hormones
Recombinant Growth hormone,
Increases release of IGF-1 in the liver
and carilage, stimulates skeletal
muscle growth, amino acid
transport, protein synthesis and cell
proliferation ; For GH deficiency in
children and genetic disease
i. Somatropin associated with short stature
(Turner syndrome, Prader-Willi
syndrome), failure to thrive due to
chronic renal failure or SGA, AIDS
wasting, improve GI function in
patients who underwent intestinal
resection that led to malabsorption
syndrome
Recombinant IGF-1 ; For children
ii. Mecasermin
unresponsive to GH therapy
Somatostatin analog, suppresses the
release of growth hormones,
glucagon, insulin, gastrin, IGF-1,
iii. Octreotide, Lanreotide serotonin and gastrointestinal
peptides ; For Acromegaly, pituitary
adenoma, carcinoid, gastrinoma,
glucagonoma, variceal bleeding
GH receptor antagonist ; For
iv. Pegvisomant
acromegaly
Gonadotropin analog (FSH analog);
activates FSH receptors and mimics
v. Follitropin alfa, Follitropin beta, effects of endogenous FSH ; For
Urofollitropin Controlled ovarian hyperstimulation,
infertility due to hypogonadism in
men
Gonadotropin analog (LH analog);
vi. Menotropins, Human chorionic
activates LH receptors and mimics
gonadotropin (HCG),
effects of endogenous LH ; For
Choriogondaotropin alfa, Lutropin
Controlled ovarian hyperstimulation
Peripheral edema, Myalgia,
Arthralgia, Intracranial
used as Performance enhancing
hypertension, pseudotumor cerebri,
drug since it increases muscle mass ;
slipped capital femoral epiphysis,
given SC
progression of scoliosis,
hyperglycemia
Hypoglycemia, increased LFT, remedy to hypoglycemia: give
intracranial HTN patient some snacks prior to dose
regular release: given BID-QID SC, if
GI upset, gallstone, cardiac slow release: every 4wks IM ; are
condution abnormality long-acting synthetic analogs of
somatostatin
Diarrhea, nausea, flu-like syndrome,
onset of action is expected within
elevated LFTs, hypesensitivity
2wks of use
reaction
Headache, depression, edema,
Follitropin alfa and beta are
ovarian hyperstimulation syndrome
recombinant FSH forms while
(ovarian enlargement, ascites,
Urofollitropin is a purified
hypovolemia, shock), multiple
preparation from urine of
pregnancies in women,
postmenopausal women
gynecomastia in men
Headache, depression, edema,
menotropins are mixtures of FSH
ovarian hyperstimulation syndrome,
and LH from postmenopausal
multiple pregnancies in women,
women ; Choriogondaotropin alfa is
gynecomastia in men
Page 25 of 56

vii. Leuprolide, Gonadorelin,
Goserelin, Histrelin, Nafarelin,
Triptorelin
viii. Ganirelix, Cetrorelix,
Degarelix
ix. Bromocriptine, Carbegoline
x. Oxytocin
xi. Desmopressin, Vasopressin
xii. Conivaptan, Tolvaptan,
Lixivaptan
Thryoid & Antithyroid Drugs
i. Levothyroxine (T4), Liothyronine
(T3)
ii. Propylthiouracil (PTU)
iii. Methimazole, Carbimazole
(ovulation induction),
hypogonadotripic hypogonadism
GnRH analog, increased LH and FSH
secretion with intermittent
administration , reduced LH and FSH
secretion with prolonged continuous
administration (due to
downregulation of GnRH receptors
in the pituitary cells that normally
release LH and FSH ; For Controlled
ovarian hyperstimulation,
endometriosis, myoma uteri,
precocious puberty, prostate CA
GnRH antagonist, blocks GnRH
receptors, reduces endogenous
production of LH and FSH ; For
Controlled ovarian hyperstimulation
(prevents premature LH surge),
advanced prostate CA
Dopamine agonist, partial agonist at
dopamine D2 receptors in brain,
inhibits prolactin release ; For
Hyperprolactinemia, Pituitary
adenoma, acromegaly, Parkinson's
disease
Activates oxytocin receptors,
stimulates uterine contraction and
labor, stimulates mammary glands,
lactation and milk let-down ; For
Labor induction, labor
augmentation, control of uterine
hemorrhage post-delivery
ADH agonist, Vasopressin V2
receptor agonist which causes
insertion of water channels in the
collecting duct leading to more
water reabsoprtion, also regulates
the release of factor VIII and VWF ;
For Central DI, Hemophilia A, von
Willebrand's disease, Variceal
bleeding, colon diverticula, primary
nocturnal seizures
ADH antagonist, Antagonist at V1a
and V2 receptors ; For SIADH,
Hyponatremia, offset fluid retention
in acute heart failure and SIADH
which causes hyponatremia
(dilutional)
Thryoid hormone, activation of
nuclear receptors results in gene
expression with RNA formation and
protein synthesis ; For
Hypothyroidism, myxedema coma
Inhibits thyroid peroxidase
reactions, blocks iodine
organification, inhibits peripheral
conversion of T4 into T3 ; For
Hyperthyroidism, thyroid storm
Inhibits thyroid peroxidase
reactions, blocks iodine
Hot flushes, sweats, headaches,
osteoporosis, gynecomastia,
reduced libido, decreased
hematocrit
Nausea, headache, hypersensitivity,
hot flushes, gynecomastia,
decreased libido, decreased
hematocrit, osteoporosis
Nausea, headache, lightheadedness,
orthostatic hypotension, fatigue,
behavioral changes,
erythromelalgia, Raynaud's
phenomenon, pulmonary infiltrates
Fetal distress, placental abruption,
uterine rupture, fluid retention,
hyponatremia, heart failure,
seizures, hypotension
Headaches, flushing, nausea,
hyponatremia, seizures
Infusion site reactions, hyperkalemia
Dry skin, sweatng, tachycardia,
nervousness, tremor, weight loss,
weakness, heat intolerance
Maculopapular pruritic rash,
gastrointestinal distress, fulminant
hepatitis, agranulocytosis, urticaria,
vasculitis, lupus-like syndrome,
lymphadenopathy,
hypoprothrombinemia, Exfoliative
dermatitis, polyserositis, arthralgia,
hypothyroidism
Maculopapular pruritic rash,
gastrointestinal distress, fulminant
a recombinant hCG while Lutropin is
a recombinant LH ; hCG given IM
there is exacerbation of symptoms
in males with prostate CA and
children with precocious puberty
during the first few weeks of
therapy (remedy: co-administer
Flutamide, an androgen receptor
antagonist) ; Gonadorelin is a
synthetic human GnRH ; Leuprolide
has a long agonist activity
Does NOT cause tumor flare-up whe
used for treatment of advanced
prostate cancer, also less likely to
cause ovarian hyperstimulation
syndrome ; Degarelix is used for
prostate CA while Ganirelix prevent
LH surge in controlled ovulation
Slightly inhibits GH release if given in
high doses ; CI in patients with
history of psychotic illness
ATOSIBAN - an oxytocin antagonist
used in preterm labor
also contracts vascular smooth
muscles via V1 receptor leading to
vasoconstriction, used as treatment
for esophageal varices or colon
diverticula
Central pontine myelinolysis may
occur with rapid correction of
hyponatremia, tolvaptan is more
selective for V2 receptors
T4 dose must be lowered in patients
with cardiovascular disease or
longstanding hypothyroidism
(increased cardiosensitivity) ;
Liothyronine has a faster onset but
shorter half-life
Drug of choice for pregnant
hyperthyroid patients (does not
eneter placenta and breastmilk);
slow onset of action (3-4 weeks for
full effect)
Methimazole and Carbimazole are
teratogens (causes Aplasia Cutis
Page 26 of 56

iv. Lugol Solution (Iodine in
Potssium Iodide), Potassium Iodide
v. Propranolol, Esmolol,
Metoprolol, Atenolol
vi. Radioactive Iodine
Adrenocorticosteroids &
Adrenocortical Antagonists
i. Low Potency: Desonide
ii. Med Potency: Fluticasone,
Mometasone
iii. High Potency:
Desoximetasone, Clobetasol
iv. Synthetic GCs: Prednisone,
Prednisolone, Methylprednisolone,
Meprednisone, Dexamethasone,
Betamethasone, Triamcinolone,
Beclomethasone, Budesonide
v. Mineralocorticoid:
Fludrocortisone,
Deoxycorticosterone
organification ; For Hyperthyroidism,
thyroid storm
Inhibit iodine organification and
hormone release leading to reduced
size and vascularity of thyroid gland
; For Hyperthyroidism, thyroid
storm, preparation for surgical
thyroidectomy to reduce the size
and vascularity of the thyroid gland,
radiation prophylaxis
Beta blocker control HR and other
cardiac abnormalities of severe
thyrotoxicosis, slows pacemaker
activity; inhibits peripheral
conversion of T4 into T3 ; For
Hyperthyroidism, thyroid storm,
post MI prophylaxis, hypertension
Iodide, emits beta rays causing
destruction of thyroid parenchyma ;
For hyperthyroidism, permanent
cure of thyrotoxicosis without
surgery and no effect on other
tissues
Glucocorticoid, activates
glucocorticoid receptors, leading to
altered gene transcription,
Suppresses inflammation, Replaces
cortisol when deficient ; For Acute
adrenal insufficiency associated with
life-threatening shock, chronic
adrenal insufficiency (Addison's
disease), congenital adrenal
hyperplasia, insect bites, contact
dermatitis, status asthmaticus,
thyroid storm
Glucocorticoid; For supressession of
inflammation and immune
response, hematopoeitic cancers,
transplant rejection, collagen and
rheumatic disease, lung maturation
in preterm labor (betamethasone
and dexamethasone), bronchial
asthma, chemotherapy-induced
vomiting, hypercalcemia, mountain
sickness
strong agonist of mineralocorticoid
receptors and moderate activation
of glucorticoid receptors, Increases
Na reabsorption, K and H excretion ;
For Chronic adrenal insufficiency
hepatitis, dose-dependent,
agranulocytosis, urticaria, vasculitis,
lupus-like syndrome,
lymphadenopathy,
hypoprothrombinemia, Exfoliative
dermatitis, polyserositis, arthralgia,
hypothyroidism
Iodism, acneiform rash, swollen
salivary glands, mucous membrane
ulcerations, conjunctivitis,
rhinorrhea, drug fever, metallic
taste, bleeding disorders,
anaphylactoid reactions
Bronchospasm, cardiac depression,
AV block, hypotension
Permanent hypothyroidism, sore
throat
Adrenal suppression, growth
inhibition, DM, muscle wasting,
osteoporosis, salt retention, glucose
intolerance, behavioral changes
Adrenal suppression, growth
inhibition, muscle wasting,
osteoporosis, salt retention, glucose
intolerance, behavioral changes
(psychosis)
Salt and fluid retention,
Hypokalemia, Congestive heart
failure, muscle wastng,
osteoporosis, glucose intolerance,
behavioral changes
Congenita) ; given as once daily
dosing
onset is more rapid (2-7 days) but
effect is transient (thyroid gland
escapes iodide block after several
weeks of treatment) ; Should not be
used alone (escape in 2-8 weeks);
prevents radiation induced thryoid
damage; prenatal exposure causes
fetal goiter
Esmolol may be used to treat
thyrotoxicosis-related arrhythmias;
causes clinical improvement
WITHOUT altering thyroid hormone
levels
Preferred treatment for most
patients due to ease of
administration, effectiveness, low
expense and absence of pain;
contraindicated in pregnant women
or nursing mothers
Effects: stimulate gluconeogenesis,
increased fat deposition, muscle
protein and bone catabolism,
lymphoid connective tissue fat and
skin wasting inhibit cell-mediated
immunologic functions,
lymphotoxic, increased neutrophils,
decreased lymphocytes eosinophils
basophils and monocytes, inhibit
leukocyte migration, inhibit PLA2,
delay rejection in transplant
patients, increased GI acid secretion
(ulcer) ; Biochemical effects: induced
synthesis of an inhibitor of PLA2,
decreased mRNA for COX2, decrease
in IL-2 and IL-3 and decrease in
Platelet Activating Factor (PAF)
prednisolone is the active
metabolite of prednisone ; this
group has a long t1/2, reduced salt-
retaining effect and better
penetration of lipid barriers
Additive hypokalemia with loop
diurectics and thiazides ;
Deoxycorticosterone is the
precursor of aldosterone ;
Fludrocortisone also has significant
Page 27 of 56

Corticosteroid Antagonists
vi. Aminoglutethimide
vii. Ketoconazole
viii. Metyrapone
ix. Mifepristone (RU486)
x. Spironolactone, Eplerenone
Gonadal Hormones and Inhbitors
A. Estrogen compounds
i. Ethinyl Estradiol, Mestranol,
Estradiol cypionate, Premarin
ii. Diethylstilbestrol
B. Progestins
(Addison's disease), Congenital
adrenal hyperplasia, adrenal
replacement therapy post-
adrenalectomy
Glucorticoid synthesis inhibitor,
inhibits desmolase activity, blocking
conversion of cholesterol to
pregnenolone ; For Breast CA,
Cushing syndrome
Glucorticoid synthesis inhibitor;
azole antifungal; inhibits cholesterol
side chain cleavage, cytochrome
P450 enzymes and other enzymes
necessary for synthesis of all
steroids ; For Adrenal CA, Hirsutism,
Breast CA, steroid-responsive
metastatic Prostate CA, Cushing's
syndrome, Fungal infections,
hirsutism
Glucorticoid synthesis inhibitor,
selective inhibitor of steroid-11
hydroxylation, interfering with
cortisol and corticosterone synthesis
; As diagnostic test for adrenal
function
competitive inhibitor at the GC
receptor as well as progesterone
receptor ; For Cushing's syndrome
Aldoesterone antagonist ; For
hypokalemia due to other diuretics,
for post-MI, hyperaldoteronism- see
entry -
Activates etrogen receptors, leads to
changes in rates of trasncription of
estrogen-regulated genes ; For
Primary hypogonadism,
Postmenopausal hormonal
replacement therapy, Osteoporosis
and prevention of bone loss,
Contraception, Intractable
dysmenorrhea
Synthetic estrogen (nonsteroid);
activates estrogen receptors; leads
to changes in rates of transcription
of estrogen-regulated genes ; For
Atrophic vaginitis, hormone
replacement therapy, prevention of
adverse pregnancy outcomes,
metastatic prostate CA
Skin rash, hepatotoxicity,
hypothyroidism
Hepatotoxicity, many drug
interactions, androgenic effect
Dizziness, GI disturbances
abdominal pain and cramping,
uterine cramping, nausea,
headache, vomiting, diarrhea,
dizziness, vaginal bleeding
Hyperkalemia, gynecomastia
(spironolactone) - see entry -
breakthrough bleeding, nausea,
breast tenderness, migraine,
thromboembolism (DVTs),
gallbladder disease,
hypertriglyceridemia, hypertension,
premature closure of the epiphysis
in young females, increased risk of
breast and endometrial cancer
(remedy: add progesterone to the
preparation)
breakthrough bleeding, nausea,
breast tenderness, migraine,
thromboembolism (DVTs),
gallbladder disease,
hypertriglyceridemia, hypertension,
premature closure of the epiphysis
in young females, increased risk of
breast and endometrial cancer
(remedy: add progesterone to the
preparation)
glucocorticoid activity ; Aldosterone
is implicated in myocardial and
vascular fibrosis and baroreceptor
dysfunction
Also inhibits synthesis of all
hormonally active steroids
Potent inhibitor of CYP450 enzymes
DOC for pregnant patients with
Cushing's syndrome
also used as an approved
abortifacient for medical abortion
(usually together with misoprostol)
also with weak antagonist effect at
the androgen receptor
Increases risk of endometrial cancer
and breast cancer ; Ethinyl Estradiol
has low bioavailability,
PO/TD/IM/Intravaginal ; Estradiol
cypionate is IM with longer t1/2 ;
Premarin is a mixture of conjugated
estrogen used in HRT ; Ethinyl
estradiol undergoes enterohepatic
recirculation ; Effects of Estrogen:
growth of genital structures and
secondary sexual characteristics,
modifies serum protein levels and
decrease bone resorption, enhances
coagulability of blood, increases TG
and HDL levels while decreasing LDL
levels, if given as continuous
infusion will inhibt FSH and LH
release
associated with Infertility, ectopic
pregnancy, clear cell vaginal
adenocarcinoma in daughters of
women treated with DES
Page 28 of 56

i. Norgestrel,
Medroxyprogesterone,
Norethindrone, Norgestimate,
Desogestrel, Megestrol
C. Combined Hormonal
Contraceptives
i. Estradiol + Norethindrone
ii. Ethinyl Estradiol + Desogestrel
iii. Ethinyl Estradiol +
Drospirenone
iv. Ethinyl Estradiol +
Noregistmate
v. Medroxyprogesterone Acetate
vi. Levonorgestrel
D. Selective Estrogen Receptor Modulators (SERMs)
i. Tamoxifen, Torimefene
ii. Raloxifene
iii. Clomiphene
activates progesterone receptors,
changes rate of transcription of
progesterone-regulated genes ; For
Hormone replacement therapy
(given together with Estrogen, to
prevent estrogen-induced
endometrial cancer), contraception,
assisted reproduction (for
maintenance of pregnancy),
anovulation induction (given in high
doses to suppress FSH and LH)
Combined oral contraceptive,
activates estrogen and progesterone
receptors, inhibits ovulation, effects
on cervical mucus gland, uterine
tubes and endometrium lead to
decreased fertility, inhibit ovulation
when given before the LH surge ; For
Contraception, hypogonadism, acne,
hirsutism, dysmenorrhea,
endometriosis
Progestin-only contraceptive,
activates progresterone receptors,
Prevents conception by altering
cervical mucus and creating a hostile
endometrium ; For Contraception,
hormone replacement therapy
Postcoital contraceptive, activates
estrogen and/or progesterone
receptors, thickens cervical mucus,
inhibits ovulation ; For Emergency
contraception
Estrogen antagonist actions in
breast tissue and CNS, Estrogen
agonist effects in uterus, liver and
bone ; For Hormone responsive
breast CA, prophylaxis of breast CA
esp. in those with high risk
Estrogen antagonist actions in
breast tissue, uterus, and CNS,
Estrogen agonist effects in liver and
bone. Increases bone mineral
density ; For Osteoporosis esp on
post menopausal women, breast CA
prevention
Partial agonist in pituitary, reduces
negative feedback by estradiol,
increases FSH and LH output ; For
Induction of ovulation in women
who want to become pregnant
Hypertension, decreased HDL,
weight gain, reversible decrease in
bone mineral density, delayed
resumption of ovulation after use
breakthrough bleeding, nausea,
breast tenderness, migraine,
thromboembolism (DVTs), breast
cancer (earlier onset), headache,
skin pigmentation, depression,
weight gain acne and hirsutism for
older OCPs
Breakthrough bleeding, hair loss,
dysmenorrhea, delayed return of
fertility, osteoporosis
Severe nausea, vomiting, breast
tenderness, irregular bleeding,
headache, dizziness (fewer SE
compared to estrogen alone and
combi contraceptives)
Hot flushes, thromboembolism,
endometrial hyperplasia,
endometrial cancer
Hot flushes, thromboembolism
Hot flushes, afterimages, headache,
constipation, reversible hair loss,
ovarian enlargement
Prevents estrogen induced
endometrial cancer when used in
combination with estrogens;
Megesterol is used as an appetite
stimulant ; given PO or as vaginal
cream ; Medroxyprogesterone has a
better oral bioavilability ; L-
Norgestrel and Norethindrone has
more androgenic effect ; Norgestrel
undergoes enterohepatic
recirculation ; Effects of
progesterone: induces secretory
changes in the endometrium,
stabilize the endometrium, affect
carbohydrate metabolism and
stimulate deposition of fat, high
doses suppress FSH and LH secretion
maybe PO/IM/TD/vaginal rings/IUD
Lifetime risk of breast cancer is NOT
changed; Norethindrone is a
testosterone derivative while
Drospirenone is a spironolactone
derivative that is antiandrogenic ;
Norgestimate and Desogestrel are
newer progestins ; combined OCPs
may be used for androgen-induced
hirsutism ; Mestranol (Estrogen)
may also be used in OCPs
IM depot preparation
Must be taken within 72 hours of
unprotected sexual intercourse
prevent osteoporosis in post-
menopausal women ; Torimefene is
structurally related to Tamoxifen
No estrogenic effect on endometrial
tissue unlike tamoxifen
may cause multiple pregnancies ;
FULVESTRANT: pure estrogen
receptor anatgonist in all tissues
used in breast CA resistant to
tamoxifen
Page 29 of 56

Reduces estrogen synthesis by
iv. Anastrozole, Letrozole,
inhibiting aromatase ; For breast CA,
Exemestane
precocious puberty
Ovarian inhibitor, weak cytochrome
P450 inhibitor and partial agonist of
progestin and androgen receptors ;
v. Danazol
For Endometriosis, Fibrocystic
disease, Hemophilia, Angioneurotic
edema
Glucocorticoid receptor antagonist,
progesterone receptor antagonist ;
vi. Mifepristone (RU486)
For Medical abortion, Cushing's
syndrome
vii. Leuprolide and Ganirelix see entry
E. Androgens
Activates androgen receptors,
promotes development of male
characteristics, increases body
i. Testosterone, Fluoxymesterone, muscle bulk and RBC production ;
Methyltestosterone For Male hypogonadism, delayed
puberty, wasting syndromes (for
weight gain), certain types of
anemias
Activates androgen receptors,
promotes development of male
ii. Oxandrolone, Stanozolol, characteristics, increases body
Nandrolone muscle bulk and RBC production;
increased ratio of anabolic-to-
androgenic activity in animals
For benign and malignant prostate
F. Anti-androgens disease, precocious puberty, hair
loss and hirsutism
Competitive antagonist at androgen
i. Flutamide, Bicalutamide,
receptor ; For Prostate CA, surgical
Nilutamide
castration
Antagonist at androgen receptor.
Marked progestational effect that
suppresses the feedback
ii. Cyproterone enhancement of LH and FSH ; for
Hirsutism, component of combined
oral contraceptives, decreased
sexual drive in men
Androgen synthesis inhibitor,
inhibits 5a reducase enzyme that
iii. Finasteride, Dutasteride converts testosterone to
dihydrotestosterone ; For BPH, Male
pattern baldness. Hirsutism
iv. GnRH agonist and antagonists see entry
v. Spironolactone for treatment of hirsutism in women
inhibit gonadal and adrenal steroid
vi. Ketoconazole
synthesis
Pancreatic Hormones & Antidiabetic Drugs
A. Insulins
Activates insulin receptors leading to
a reducting of circulating glucose:
i. Rapid Acting Insulin: Lispro, promotes glucose transport and
Aspart, Glulisine oxidation; glycogen, lipid, protein
synthesis and regulation of gene
expression ; For Diabetes mellitus,
Hot flushes, musculoskeletal
disorders, osteoporosis, joint pains
Acne, hirsutism, weight gain,
menstrual disturbances, hepatic
dysfunction
Vaginal bleeding, abdominal pain, GI
upset (vomiting, diarrhea), uterine
cramping, nausea, vomiting,
headache, dizziness, diarrhea
see entry
Virilization and menstrual
irregularities in females, paradoxical
feminization in males, cholestatic
jaundice, elevated LFTs
Virilization in females, paradoxical
feminization in males; cholestatic
jaundice, elevated liver enzymes,
hepatocellular CA
Gynecomastia, hot flushes,
impotence, hepatotoxicity
Hepatotoxicity, Adrenal suppression,
depression, gynecomastia,
galactorrhea, thromboembolism
Impotence, gynecomastia,
depression
see entry
see entry
Hypoglycemia (antidote: sugar or
candy, IV glucose, IM glucagon),
insulin allergy, immune insulin
resistance, lipodystrophy at injection
site
Effective against brest CA that have
become tamoxifen-resistant ;
Exemestane is an IRREVERSIBLE
inhibitor
May also act on Glucocorticoid
receptors
Combined with misoprostol results
in abortion of 95% of early
pregnancies ; as abortifacient in
early pregnancy (may be used up to
49days after menses) ; complication:
failure to induce complete abortion
see entry
may be given IV or as TD
Effects of androgen: secondary
sexual characteristics, fertility and
libido, male pattern baldness,
increases muscle mass, increased
RBC production, decreased urea
nitrogen excretion, maintains
normal bone density ; used illegally
by atheletes as performance
enhancer
this group is called "anabolic
steroids"
GnRH analogs must be
coadministered with flutamide to
prevent acute flareups of prostate
CA ; Bicalutamide and Nilutamide
have less heaptotoxicity
Orphan drug status
Dutasteride is newer with longer
t1/2 ; this group is less likely to
cause impotence, infertility and
decreased libido
see entry
see entry
Effects of insulin: increased glycogen
and protein synthesis, decreased
protein catabolism, increased TG
storage ; rapid acting insulins are
injected a few mins prior to meals
and they are the preferred insulin
Page 30 of 56

ii. Short Acting Insulin: Regular
iii. Intermediate Acting: NPH,
Lente
iv. Long Acting Insulin: Detemir,
Glargine, Ultralente, Lantus
B. Sulfonylureas
i. Glipizide, Glibenclamide,
Glimepiride, Gliclazide, Glyburide
ii. Tolazamide, Tolbutamide,
Chlorpropamide
C. Meglitinides
i. Repaglinide
ii. Nateglinide
D. Biguanides
i. Metformin
E. Alpha Glucosidase Inhibitors
i. Acarbose, Miglitol
F. Thiazolidinediones
i. Pioglitazone
diabetic emergencies like DKA, HHS
(rapid-acting), Hyperkalemia
2nd generation sulfonylurea, acts as
an insulin secretagogue, increases
insulin secretion from pancreatic
beta cells by closing ATP sensitive K+
channels leading to depolarization
of the B cell; For Type 2 Diabetes
Mellitus
1st generation sulfonylurea, acts as
an insulin secretagogue; increases
insulin secretion from pancreatic
beta cells by losing ATP sensitive K+
channels ; for Type 2 Diabetes
Mellitus
Insulin Secretagogue, similar to
sulfonylureas with some overlap in
binding sites, reduces circulating
glucose, increases glycogen, fat and
protein formation and gene
regulation ; For Type 2 Diabetes
Mellitus
Insulin Secretagogue, similar to
sulfonylureas with some overlap in
binding sites, reduces circulating
glucose, increases glycogen, fat and
protein formation and gene
regulation ; For Type 2 Diabetes
Mellitus
Reduced hepatic and renal
gluconeogenesis with decreased
endogenous glucose production,
activates AMP-stimulated protein
kinase leading to inhibition of
gluconeogenesis ; For Type 2 DM,
Diabetes prevention, PCOS
Inhibits intestinal alpha-glucosidases
, reduces conversion of starch and
disacchardies to monosaccharidea,
reduces post prandial hyperglycemia
; For Type 2 DM, Diabetes
prevention
Regulates gene expression by
binding to PPAR-gamma and PPAR-
alpha which increases tissue
sensitivity, increases glucose uptake
in muscle and adipose tissue,
inhibits hepatic gluconeogenesis,
effects on lipid metabolism and
Less hypoglycemia, weight gain,
photosensitivity, cholestatic
jaundice (glibenclamide)
Hypoglycemia, weight gain,
disulfiram reaction, hyperemic flush,
dilutional hyponatremia,
hematologic toxicity
Least hypoglycemia, headache, URTI
Least hypoglycemia, headache, URTI
GI disturbance, weight loss, lactic
acidosis (esp in renally and
hepatically impaired patients), Vit
B12 malabsorption
GI disturbance, hypoglycemia,
increased liver enzymes, flatulence,
diarrhea, abdominal pain
Fluid retention, weight gain,
congestive heart failure, fractures
esp in women, cardiovascular
events, hepatotoxicity
(Troglitazone), macular edema,
dyslipidemia, increased risk of MI
(Rosiglitazone)
for continuous SC infusion devices ;
short-acting insulins are injected
more than an hour before a meal ;
intermediate acting insulins are
often combined with regular and
rapid acting insulins ; long acting
insulins are called "peakless" insulins
Not effective in patients with
functional B cells
tolbutamide and chlorpropamide
are highly protein bound drugs,
which may also cause allergic
reactions and rash
Least Hypoglycemia, rapid onset and
short DOA
Has least incidence of hypoglycemia,
may be used in CKD patients ; rapid
onset and short DOA
DOC for obese diabetics ; may also
cause slowing of glucose absorption
from GIT, decreased plasma
glucagon ; causes a decrease in
endogenous insulin production by
increasing insulin sensitivity of
tissues "Insulin Sparing Effect"
therefore does not have weight gain
as a SE ; do NOT cause hypoglycemia
relatively minor glucose lowering
effects ; impaired absoprtion of
sucrose ; taken immediately before
a meal
binds to PPAR-gamma and PPAR-
alpha ; PPAR regulates transcription
of genes encoding proteins involved
in carbohydrate and lipid
metabolism ; may increase risk for
developing Bladder Cancer
Page 31 of 56

ii. Rosiglitazone
G. Novel Antidiabetic Agents
i. Exenatide
ii. Sitagliptin, Linagliptin
iii. Pramlintide
iv. Colesevelam hydrochloride
Agents That Affect Bone Mineral Homeostasis
A. Vitamin D Metabolites and
Analogs
i. Cholecalciferol, Ergocalciferol
ii. Calcitriol, Doxercalciferol,
Paricalcitol, Calcipotriene
B. Bisphosphonates
i. Alendronate, Risedronate,
Ibandronate, Pamidronate,
Zoledronate, Etidronate,
Tiludronate, Zoledronic acid
distribution of body fat, control of
fasting and postprandial glucose,
decreased risk of DM in high-risk
patients ; For Type 2 DM, Diabetes
prevention
Regulates gene expression by
binding to PPAR-gamma ONLY ; for binds to PPAR-gamma ONLY
Type 2 DM, Diabetes prevention
Analog of GLP-1, Binds to GLP-1
receptors which leads to reducetion
of post-meal glucose excursions,
Hypoglycemia, acute pancreatitis, GI usually combined with SU or
increases glucose-mediated insulin
upset, nausea, vomiting metformin ; long-acting injectables
release, lowers glucagon levels,
slows gastric emptying time,
produces satiety ; For Type 2 DM
Dipeptidyl Peptidase-4 Inhibitors,
blocks degradation of GLP-1, raises
circulating GLP-1 levels, reduces
post-meal glucose excursions,
Headache, nasopharyngitis, URTI often combined with metformin
increases glucose mediated insulin
release, lowers glucagon levels,
slows gastric emptying time,
decreases appetite ; For Type 2 DM
Analog of amylin, Binds to amylin
receptors, reduce post-meal glucose
used with insulin to control post-
excursions, lowers glucagon levels, Hypoglycemia, GI disturbances
prandial glucose
slows gastric emptying, decreases
appetite ; For Type 2 DM
Bile acid binder, lowers glucose
constipation, dyspepsia, myalgia,
through unknown mechanisms ; For None
asthenia
Type 2 DM
INACTIVE Vitamin D; Regulates gene
tanscription via the vitamin D
receptor; stimulates intestinal
calcium absorption, bone
resorption, renal calcium and
given topically for psoriasis ; given
phosphate reabsorption, decreases Hypercalcemia, hyperphosphatemia,
with calcium supplements for
PTH, promote innate immunity ; For hypercalciuria
osteoporosis
Vitamin D deficiency states
(intestinal osteodystrophy, CKD,
chronic liver disease,
hypoparathyroidism, nephrotic
syndrome) osteoporosis, psoriasis
The active form Calcitriol is
ACTIVE Vitamin D; Regulates gene preferred in patients with CKD,
tanscription via the vitamin D chronic liver disease and
receptor; stimulates intestinal hypoparathyroidism ;
Hypercalcemia, hyperphosphatemia,
calcium absorption, bone Doxercalciferol is a prodrug that is
hypercalciuria ; Doxercalciferol,
resorption, rena calcium and converted in the liver to 1,25-
Paricalcitol and Calcipotriene cause
phosphate reabsorption, decreases dihydroxyvitaminD ; Paricalcitol,
less hypercalcemia and
PTH, promote innate immunity ; For Calcipotriene are analogs of calcitriol
hypercalciuria
Secondary hyperparathyroidism in and are used topically for psoriasis
CKD, hypocalcemia in and are being investigated for
hypoparathyroidism, psoriasis malignancies and inflammatory
disorders
Suppress the activity of osteoclasts Adynamic bone, Esophagitis, Pamidronate, Zoledronic acid and
in part via inhibition of farnesyl Osteonecrosis of the Jaw, renal Etidronate are used IV for
pyrophosphate synthesis, inhibit impairment, GI irritation (remedy: hypercalcemia in Paget's disease
resorption and formation of bone by take lots of water and keep patient and cancer ; all other preparations
acting on the basic hydroxyapatite in an upright position for 30mins and Etidronate can be given PO but
crystal structure ; For Paget's after intake of drug) with low bioavailability (<10%) ;
Page 32 of 56

C. Hormones
i. Teriparatide
ii. Calcitonin
D. Selective Estrogen Receptor
Modulators (SERMs)
i. Raloxifene
E. Rank Ligand (RANKL) Inhibitor
i. Denosumab
F. Calcium Receptor Antagonist
i. Cinacalcet
7. CHEMOTHERAPEUTIC DRUGS
Beta-Lactam & Other Cell Wall-Active & Membrane-Active Antibiotics
A. Penicillin
i. Natural Penicillins: Penicillin G,
Penicillin V (narrow spectrum
penicillin)
ii. Anti-Staphylococcal Penicillins:
Methicillin, nafcillin, oxacillin,
cloxacillin (very narrow spectrum)
iii. Extended Spectrum Penicillin:
Ampicillin, Amoxicillin
disease of the bone, Hypercalcemia
esp in malignancies, Osteoporosis
Recombinant PTH, Acts via cognate
G protein coupled receptors,
stimulates bone formation when
given in low intermittent doses
Acts via cognate G protein coupled
receptors; suppresses bone
resorption ; For Paget's disease of
the bone, hypercalcemia,
osteoporosis, tumor marker for
thyroid CA
Interacts selectively with estrogen
receptors, inhibits PTH-stimulated
bone resorption without stimulating
breast or endometrial hyperplasia,
delay bone loss in post-menopausal
women
Monoclonal antibody, binds to
RANKL and prevents it from
stimulating osteoclast
differentiation and function, blocks
bone resorption ; For
postmenopausal osteoporosis
Activates the calcium sensing
receptors in the parathyroid gland,
inhibits PTH secretion ; For
secondary hyperparathyroidism in
CKD, hypercalcemia in patients with
parathyroid CA
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; DOC for syphillis, for
streptococcal, meningococcal, G+
bacilli, spirochete infection
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls; For staphylococcal
infections
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; For enterococci, Listeria,
E. coli, Proteus, H. influenza,
Moraxella
hypercalcemia, arthralgia, rhinitis,
nausea, weakness, dizziness,
pharyngitis, dyspepsia, rash
Rhinitis, Nausea, vomiting, facial
flushing
see entry
increased risk of infection
hypocalcemia, adynamic bone
disease (profound decreae in bone
cell activity)
hypersensitivity, GI disturbances
hypersensitivity, GI disturbances,
interstitial nephritis (methicillin),
neutropenia (nafcillin)
hypersensitivity, GI disturbances,
pseudomembranous colitis
(ampicillin), rash (ampicillin)
Treatment regimen: oral OD
(alendronate, risedronate,
ibandronate), weekly PO
(alendronate, risedronate), monthly
PO (ibandronate), quarterly injection
(ibandronate), annual IV
(zoledronate)
used IV for osteoporosis
given as injection or as nasal spray ;
used for osteoporosis but is less
effective than bisphosphonates and
teriparatide
see entry
as potent as bisphosphonates ; given
SC every 6months which avoid the
GI SE
considered a Calcimimetic
(decreases PTH)
Bactericidal ; excreted unchanged in
the urine ; capable of entering the
blood brain barrier
Inactivated by beta-lactamase
(penicillinase) ; given IM but Pen V
can be given PO ; increased activity
against enterococci when given
together with aminoglycosides
Resistant to inactivation by beta-
lactamase (penicillinase) ; all
penicillins are excreted unchanged
in the urine EXCEPT for Nafcillin
which is excreted in the bile
Inactivated by beta-lactamase
(penicillinase), enhanced effect
when used with beta-lactamase
inhibitors (clavulanic acid,
sulbactam) ; ampicillin undergoes
enterohepatic recirculation ;
synergistic effect with
aminoglycosides
Page 33 of 56

iv. Antipseudomonal Penicillin:
Piperacillin, ticarcillin, carbenicillin
B. Cephalosporins
i.First Generation: Cefazolin,
cefadroxil, cephalothin, cephapirin,
cephradine, cephalexin
ii. Second Generation:
Cefamandole, cefaclor, cefonicid,
cefuroxime, cefprozil, loracarbef,
ceforanide, cefoxitin, cefmetazole,
cefotetan
iii. Third Generation:
Cefoperazone, cefotaxime,
ceftizoxime, ceftriaxone, cefixime,
cefpodoxime proxetil, cefdinir,
ceftibuten
iv. Fourth Generation: Cefipime,
Ceftaroline
C. Other Beta-Lactams
i. Carbapenems: Imipenem-
cilastatin , ertapenem, meropenem
ii.Monobactam: Aztreonam
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; For Pseudomonas,
Enterobacter, Klebsiella
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; For surgical prophylaxis,
bone infections, infections due to
staph and strep, E. coli, Klebsiella,
G+ cocci
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; For surgical prophylaxis,
bone infections, infections due to
staph strep and E. coli, Enterobacter,
Neisseria, infections against
anaerobes (Bacteroides), sinus ear
and respiratory infections by
Klebsiella andHemophilus
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; decreased gram +
coverage, increased gram activity
(pseudomonas, bacteroides), against
Providencia, Serratia, Neiserria,
Haemophilus ; DOC for gonorrhea
(Ceftriaxone and Cefixime)
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; wide coverage against
gram + and gram - bacteria
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls, wide coverage against
gram + gram - bacteria and
anaerobes ; For infections resistant
to other antibiotics EXCEPT MRSA,
DOC for Enterobacter, Citrobacter
and Serratia
Binds to penicillin-binding proteins,
inhibits transpeptidation in bacterial
cell walls ; used against Gram like
klebsiella, pseudomonas and
Serratia
hypersensitivity, GI disturbances
hypersensitivity, injection site
reactions, phlebitis, GI upset
hypersensitivity, injection site
reactions, phlebitis, GI upset,
Hypoprothrombinemia and
Disulfiram rection (cefamandole,
cefotetan)
hypersensitivity, GI upset,
Hypoprothrombinemia and
Disulfiram rection (cefoperazone)
hypersensitivity, GI upset
hypersensitivity, GI upset, CNS
toxicity (confusion, encephalopathy,
seizures)
GI upset, superinfection, vertigo,
headache, skin rash and
hepatotoxicity
Inactivated by beta-lactamase
(penicillinase), enhanced effect
when used with beta-lactamase
inhibitors (clavulanic acid,
tazobactam)
Bactericidal ; mostly IV ; all have
renal excretion EXCEPT
Cefoperazone and Ceftriaxone
Increases nephrotoxicity of
aminoglycosides ; do not cross the
BBB ; minimal activity against G-
cocci, enterococci, MRSA and most
G- rods
Increases nephrotoxicity of
aminoglycosides ; do not cross the
BBB ; slight less activity against G+
but extended G- activity ;
Cefuroxime has improved action
against pneumococcus and H.
influenzae ; Cefotetan and Cefoxitin
have good activity against B. fragilis
and thus are used for abdominal and
pelvic infections
Synergistic effect with
aminoglycosides ; all have renal
excretion EXCEPT Cefoperazone and
Ceftriaxone ; all can penetrate the
BBB EXCEPT Cefoperazone and
Cefixime ; Ceftriaxone and
Cefotaxime are the most active
Cephs against Penicillin resistant
Streptococcus pneumoniae ;
Ceftizoxime is commonly used
against Bacteroides ; should be
reserved against serious infection
EXCEPT ceftriaxone and cefixime ;
Ceftriaxone has very good CNS
penetration ; Ceftazidime has very
good action on Pseudomonas
More resistant to beta-lactamase
produced by Enterobacter,
Haemophilus, Neisseria and
Pneumococcal ; Has improved
stability to chromosomal lactamase ;
Ceftaroline used for MRSA
Reserved for serious ife-threatening
infections; cilastatin inhibits renal
metabolism of imipenem ; given IV ;
low susceptibility to B-lactamases ;
active against Pseudomonas and
Acinetobacter EXCEPT Ertapenem ;
Imipenem given with Cilastatin
which acts as Dehydropeptidase
enzyme inhibitor ; Partial cross-
allergenicity with Penicillins ;
Ertapenem has longer t1/2 but less
active against Enterococci and
Pseudomonas
Resistant to beta-lactamase, no
activity against gram + bacteria or
anaerobes ; given IV ; synergistic
with AG ; renal excretion ; No cross-
allergenicity with Pens
Page 34 of 56

iii. Beta-Lactamase Inhibitors:
Clavulanic acid , sulbactam,
tazobactam
D. Other Cell Wall Synthesis
Inhibitors
i. Glycopeptides: Vancomycin,
teicoplanin, telavancin, dalbavancin
ii. Peptide Antibiotic: Bacitracin
iii. Antimetabolite: Cycloserine
iv. Antimetabolite: Fosfomycin
v. Cyclic lipopeptide: Daptomycin
Tetracyclines, Macrolides, Clindamycin, Chloramphenicol, Streptogramins & Oxazolidinones
A. Chloramphenicol (broad
spectrum protein synthesis
inhibitor)
B. Tetracyclines: Tetracycline,
doxycycline, minocycline,
tigecycline, demeclocycline
Inhibits inactivation of penicillins by
bacterial beta-lactamase
(penicillinase); used against beta-
lactamase producing gonococci,
streptococci, E. coli and H. influenza
Inhibits cell wall synthesis by binding
to the D-Ala-D-Ala terminus of
nascent peptidoglycan --> inhibit
transglycosylation --> prevent
elongation and cross-linking of
peptidoglycan chain ; For MRSA,
PRSP, as alternative for
pseudomembranous colitis
Interferes with a late stage oin cell
wall synthesis in gram + organisms ;
For gram + bacteria
Blocks incorporation of D-Ala into
the pentapeptide side chain of the
peptidoglycan ; For drug-resistant TB
inhibits cytosolic enolpyruvate
transferase --> prevents formation
of N-acetylmuramic acid (a
peptidoglycan precursor molecule)
same spectrum of activity as
Vancomycin ; For VRE, VRSA, for G+
acitivity, against endocarditis and
sepsis
Inhibits transpeptidation (catalyzed
by peptidyl transferase) by blocking
the binding of aminoacyl moiety of
the charged tRNA to the acceptor
site o mRNA at 50S subunit,
basteriostatic ; For meningitis (Strep
pneumonia, H influenza, Neisseria
meningitides), back up for
Salmonella, Rickettsia, Bacteroides,
Wide spectrum antibiotic
Binds 30s ribosomal subunit thus
preveting the binding of tRNA to
mRNA, bacteriostatic ; Broad/Wide
Spectrum (G+ and G-), For infections
caused by Mycoplasma pneumonia,
Chlamydia, Rickettsia, Vibrio,
Spirochetes such as Leptospira,
Peptic ulcer disease, Lyme disease,
Malaria prophylaxis, Amoebiasis,
Acne, Doxycycline is an alternative
to macrolides as initial treatment of
CAP, Alternative in syphilis,
treatment of respiratory infection
caused by susceptible organism,
prophylaxis against infection in
chronic bronchitis ; Selective uses:
Tetracycline (H. Pylori PUD),
Doxycycline (Lyme disease and
malaria prevention), Minocycline
hypersensitivity and cholestatic
jaundice
red man syndrome, nephrotoxicity,
ototoxicity, chills, fever, phlebitis
nephrotoxicity
neurotoxicity (tremors, seizures and
psychosis)
Diarrhea
myopathy
GI disturbance, aplastic anemia, gray
baby syndrome
GI disturbances (enetrocolitis,
nausea, diarrhea, vomiting),
teratogen (tooth enamel
dysplasia/discoloration),
hepatotoxicity, nephrotoxicity,
photosensitivity n(esp.
demeclocycline), vestibulotoxicity,
candidiasis, bacterial superinfection
with S. aureus and C. difficile,
Fanconi syndrome
Most active against plasmid
encoded B lactamases (Gonococci,
Streptococci, E coli and H. Influenzae
; not good inhibitor of inducible
chromosomal B lactamases
(Enterobacter,Pseudomonas,
Serratia)
Narrow spectrum Treat red man
syndrome by slowing the rate of
infusion ; VRSA and VRE are due to
D-Ala-D-Lactate formation ;
teicoplanin and telavancin are not
absorbed in the GIT thus used for
bacterial enterocolitis, they are also
eliminated unchanged in the urine ;
decrease dose for renally impaired
patients ; Dalbavancin has very long
t1/2 (6-11 days) which permits once-
weekly dosing and is more active
than Vancomycin
Reserved for topical use only due to
marked nephrotoxicity
only used as a second-line agent in
TB
renal excretion ; resistance emerges
rapidly ; synergistic with Beta lactam
and quinolones
monitoring of CPK is needed, NOT
Bactericidal (only destabilizes
bacterial cell membrane)
given PO and IV ; able to cross the
placenta and BBB ; Inhibits hepatic
drug-metabolizing enzymes causing
many drug interactions ; resistance
is due to the formation of
acetyltransferase that inactivates
drug ; usually used as topical agent
Tigecycline has the broadest
spectrum and has the longest t1/2
(30-36hrs); do not drink with milk
(decreased absorption with divalent
cations like calcium) ; high Vd, cross
the placenta, enterohepatic
recycling ; all are excreted renally
EXCEPT Doxycycline (bile) ;
Resistance is due to development of
efflux pumps for active extrusion of
tetracyclines and the formation of
ribosomal protection proteins that
interfere with tetracycline binding
(but not present with Tigecycline
EXCEPT in Proteus and
Pseudomonas) ; Tigecycline is given
IV only and is unaffected by
common tetracyclie resistace
mechanisms
Page 35 of 56

C. Macrolides
i. Erythromycin, azithromycin,
clarithromycin, telithromycin
ii. Fidaxomicin
iii. Telithromycin
D. Lincosamides: Clindamycin,
lincomycin
E. Streptogramin: Quinupristin-
Dalfopristin
F. Oxazolidinone: Linezolid
Aminoglycosides & Spectinomycin
A. Gentamycin, tobramycin
(Meningococcal carrier state),
Demeclocycline (SIADH), Tigecycline
(more broad spectrum - MRSA, VRE,
B-lactamase producing G- bacteria,
anaerobes, Chlamydiae,
Mycobacteria)
Binds 30s ribosomal subunit, inhibit
transpeptidation, bacteriostatic ; For
good oral bioavilability but
community-acquired pneumonia,
azithromycin absoprtion is impeded
pertussis, diphtheria, chlamydial
by food ; All macrolides inhibit
infections ; Eryhthromycin
CYP450 except azithromycin;
(Campylobacter, Chlamydia,
azithromycin has highest Vd and
Mycoplasma, Legionella,
slowest elimination; telithromycin is
Corynebacterium, Chlamydophila,
used for macrolide-resistance ; Half-
Legionella, Ureaplasma, Bordetella, GI disturbance, cholestatic hepatitis,
lives: Erythromycin (2hrs),
G+ cocci, some G-), Clarithromycin QT prolongation, drug interaction
Clarithromycin (6hrs), Azithromycin
and Azithromycin (coverage of
(24-48hrs) ; Resistance is due to
Erythromycin plus greater activity
development of efflux pumps and
against Chlamydia, Mycobacterium
production of methylase enzyme ;
avium, Toxoplasma, Helicobacter,
Cross-resistance among macrolides:
Haemophilus, Moraxella, Neiserria) ;
complete or partial resistance with
Azithromycin is used as an
drugs acting on the 50S
alternative Ceftriaxone in Gonorrhea
and to Pen G in syphilis
a narrow spectrum macrolide, for GI upset, rashes, eosinophilia, acute as effective as Vancomycin as
G+ and anaerobe, low oral cholestatic hepatitis, enzyme treatment for C. difficile possibly
bioavailability inhibitor with lower relapse rate
Ketolide, structurally related to
macrolide, same MOA and spectrum For CAP including multi-drug
QT prolongation, enzyme inhibitor,
as erythromycin but macrolide- resistant organisms, A ketolide not a
hepatic dysfunction
resistant organisms are susceptible macrolide in chemical structure
to telithromycin ; For CAP
Binds 30s ribosomal subunit, inhibit
Cross-resistance between
transpeptidation, bacteriostatic ; For
clindamycin and macrolides is
anaerobic infections (Bacteroides), GI disturbance, skin rash,
common ; Resistance is due to
alternative against gram + cocci neutropenia, hepatic dysfunction,
methylation of binding sites and
(MRSA), endocarditis prophylaxis possible superinfection
enzymatic inactivation ; G- aerobes
esp in those allergic to Pens, PCP (Pseudomembranous colitis - C.
are resistant because of poor
pneumonia, toxoplasmosis (+ difficile overgrowth)
penetration through th eouter
Pyrimethamine), skin and soft tissue
membrane
infection
Binds 50s ribosomal subunit,
constricting the channel where
polypeptides are extruded thus
Inhibits CYP450 enzymes causing
tRNA synthetase is also inhibited --> Injection site reaction, anthralgia-
multiple drug interactions ;
decreased free tRNA ; For infections myalgia syndrome
BACTERICIDAL
caused by drug-resistant gram +
cocci (MRSA, VRSA, PRSP, resistant
E. faecium)
Binds 23S rRNA of 50s ribosomal
subunit, inhibit initiation by blockin
Inhibits CYP450 enzymes causing
formation of the tRNA-ribosome-
Thrombocytopenia, neutropenia, multiple drug interactions ;
mRNA ternary complex,
serotonin syndrome, neuropathy, Resistance is due to
bacteriostatic ; Reserved for
optic neuritis decreasedaffinity of drug to binding
infections caused by drug-resistant
site
gram + cocci (MRSA, VRE, PRSP),
Listeria, Corynebacteria
General MOA of all aminoglycosides nephrotoxicity (reversible - Acute AG are given IM or IV only, have
(AG) is by inhibiting protein Tubular Necrosis esp in elderly, if concentration dependent killing, is
synthesis by binding to 30s subunit: given with Amphotericin B, not capabale of penetrating the
(1) block formation of the initiation Cephalosporin and Vancomycin)), blood brain barrier, low tissue
complex (2) cause misreading of the ototoxicity (irreversible), penetration, SYNERGISTIC effect
code on the mRNA template (3) neuromuscular blockade (Curare- with cell wall synthesis inhibitors
inhibit translocation, bactericidal ; like block --> respiratory paralysis. due to enhancement of transport to
Page 36 of 56

B. Amikacin
C. Streptomycin
D. Neomycin, kanamycin,
paromomycin
E. Spectinomycin
F. Netilmicin
Sulfonamides, Trimethoprim & Quinolones
A. Sulfonamides: Silver sulfadiazine,
mafenide acetate
i. Short acting: Sulfisoxazole
ii. Intermediate acting:
Sulfamethoxazole
iii. Long acting: Sulfadoxine
B. Combination: Co-trimoxazole
(Sulfamethoxazole + Trimethoprim)
For serious infections caused by
aerobic gram bacteria (E.coli,
Enterobacter, Klebsiella, Proteus,
Providencia, Pseudomonas, Serratia,
Haemophilus, Moraxella, Shigella),
endocarditis, ocular infections ; If
given together with Pens, may be
used for Listeria, Enterococcus and
G+ cocci
Inhibits protein synthesis by binding
to 30s subunit, bactericidal ; For
serious infections caused by aerobic
gram bacteria (E.coli,
Enterobacter, Klebsiella, Proteus,
Providencia, Pseudomonas, Serratia,
Haemophilus, Moraxella, Shigella),
endocarditis, ocular infections,
multidrug resistant TB (2nd line) ; If
given together with Pens, may be
used for Listeria, Enterococcus and
G+ cocci
Inhibits protein synthesis by binding
to 30s subunit, bactericidal ; For TB,
tularaemia, bubonic plague,
brucellosis
Inhibits protein synthesis by binding
to 30s subunit, bactericidal ; For skin
infections, bowel preparations for
elective surgeries, hepatic
encephalopathy, visceral
leishmaniasis (paromomycin)
Inhibits protein synthesis by binding
to 30s subunit, bactericidal ; For
drug-resistant gonorrhoea,
gonorrhoea in penicillin allergic
patients
Inhibits protein synthesis by binding
to 30s subunit, bactericidal ; For
serious infections caused by aerobic
gram bacteria
Inhibits dihydropteroate synthase,
bacteriostatic ; For burn infections,
for G=, G-, Chlamydia and Nocardia,
Simple oral sulfas (UTI),
Sulfacetamide (ocular infection,
topical), Mafenide and Silver
sulfadiazine (burn infection, topical),
Sulfasalazine (Ulcerative colitis and
RA, oral), Sulfadizaine +
Pyrimethamine + Folinic acid
(Toxoplasmosis, oral)
Sequential blockade of
dihydropteroate synthase
Remedy: Calcium, Neostigmine and
Mechanical Ventilator) ; S.
pneumoniae is resistant to
Gentamicin, Enterococci is resistant
to amikacin, gentamicin, tobramycin
but NOT streptomycin
nephrotoxicity (reversible),
ototoxicity (irreversible),
neuromuscular blockade
hypersensitivity, nephrotoxicity
(reversible), ototoxicity
(irreversible), neuromuscular
blockade, teratogen (congenital
deafness), injection site reactions
hypersensitivity, nephrotoxicity
(reversible), ototoxicity
(irreversible), neuromuscular
blockade
nephrotoxicity (reversible),
ototoxicity (irreversible),
neuromuscular blockade
hypersensitivity, nephrotoxicity
(reversible), ototoxicity
(irreversible), neuromuscular
blockade
GI upset, mild hepatic dysfunction,
acute hemolysis in G6PD deficiency,
nephrotoxicity (precipitate in the
urine at acidic pH --> crystalluria,
hematuria), hypersensitivity (cross-
allergenicity with other related
drugs such OHAs and diurectics),
exfoliative dermatitis, polyarteritis
nodosa, SJS, hematotoxicity
(granulocytopenia,
thrombocytopenia, aplactis anemia),
kernicterus ; Drug Interactions:
warfarin, methotrexate, bilirubin
GI upset, acute hemolysis in G6PD
deficiency, nephrotoxicity,
the inside of the bacterial cell ;
mechanism of resistance of AG:
plasmid-mediated formation of
inactivating enzymes "group
transferase" --> catalyze the
acetylation of amine functions and
the transfer of phosphoryl or
adenylyl groups to the oxygen atoms
of the hydroxyl groups of AG, For
Streptomycin, resistance is due to
changes in the ribosomal binding
site ; Gentamicin and tobramycin
are the most vestibulotoxic and
nephrotoxic
Least resistance and narrowest
therapeutic window ; used for
streptomycin-resistant TB
Administered intramuscularly ; if
given together with Pens can be
used for enterococcal endocarditis,
TB plague and tularemia
Limited to topical and oral use due
to nephrotoxicity, kanamycin is most
ototoxic ; Neomycin has the most
skin reactions (allergic reactions,
contact dermatitis)
Ototoxcity of AG's can be increased
by loop diuretics
For Treatment of serious infections
caused by organisms resistant to
other aminoglycosides
low solubility in acidic urine causing
formation of stones ; Resistance is
due to plasmin-mediated (decreased
intracellular accumulation of the
drug, increased production of PABA
by bacteria, decreased sensitivity of
dihydropteroate synthetase to sulfas
and production of dihydrofolate
reductase that has decreased affnity
for the drug ; sulfonamides are
formulated in a 5:1 ratio with
trimethoprim
Sulfonamides are weakly acidic
while Trimethroprim is a weak base ;
Page 37 of 56

C. Fluoroquinolones
i. First Generation
Fluoroquinolones: Norfloxacin,
Nalidixic acid
ii. Second Generation
Fluoroquinolones: Ciprofloxacin,
ofloxacin, Enoxacin Norfloxacin
iii. Third Generation
Fluoroquinolones: Levofloxacin,
Gemifloxacin, Moxifloxacin,
Sparfloxacin
(sulfamethoxazole) and
dihydrofolate reductase
(trimethoprim), bactericidal ; For
UTI, respiratory, ear and sinus
infections (Hemophilus, Moraxella,
Aeromonas), DOC for P. jiroveci
pneumonia and Nocardiosis,
toxoplasmosis, Back-up for cholera
typhoid fever shigellosis, G- sepsis,
MRSA, Listeria
Avoid in pregnancy due to absence
of safety data
Inhibits DNA replication by binding
to DNA gyrase and topoisomerase IV
(G+) and Topoisomerase II (G-),
bactericidal, inhibition of
Topoisomerase II results in blockade
of relaxation of supercoiled DNA
that is catalyzed by DNA gyrase
while inhibition of Topoisomerase IV
interferes with the separation of
replicated chromosomal DNA during
cell division ; General use of FQs: For
infections of the urogenital and GI
tract by G- (gonococci, E. coli,
Klebsiela, Campylobacter,
Enterobacter, Pseudomonas,
Salmonella, Shigella), respiratory
tract, skin and soft tissue infection ;
may be used against meningococcal
carrier state, for treatment of TB
and prophylaxis in neutropenic
patients
Inhibits DNA replication by binding
to DNA gyrase and topoisomerase IV
(G+) and Topoisomerase II (G-),
bactericidal, bactericidal ; For UTI
and GIT infections (gram rods,
gonococci, gram + cocci), atypical
pneumonia (Mycoplasma,
Chlamydophila), Mycobacteria ;
increased activity against G-
Inhibits DNA replication by binding
to DNA gyrase and topoisomerase IV
(G+) and Topoisomerase II (G-),
bactericidal, bactericidal ; For lung
infections caused by gram + cocci,
atypical pneumonia (Chlamydia,
mycoplasma) ; less G- activity
compared to 2nd gen but increased
activity against G+ cocci,
enterococci, MRSA
hypersensitivity, hematotoxicity,
kernicterus ; trimethoprim toxicity:
antifolate effects (megaloblastic
anemia, leukopenia,
granulocytopenia)
General SE: GI distress, skin rashes,
HA, dizziness, insomnia, increased
LFT, phototoxicity, CNS effects
(dizziness, headache), tendinitis and
tendon rupture, opportunistic
infection by Candida and
Streptococci ; CI in pregnancy and in
children (damage growing cartilage -
-> arthropathy), enhance toxicity of
methylxanthines (theophylline) ;
Mechanism of resistance for
Quinolones: decreased intracellular
accumulation via efflux pumps,
change in porin structure, chnages
in sensitivity of target enzyme svia
point mutations in the antibiotic
binding region, mutations in the
quinolone resistance determining
region of the gyrA gene that
encodes for DNA gyrase
GI distress, skin rashes, HA,
dizziness, insomnia, increased LFT,
phototoxicity, CNS effects (dizziness,
headache), tendinitis and tendon
used as alternative to Ceftriaxone
rupture, opportunistic infection by
Candida and Streptococci ; CI in
pregnancy and in children (damage
growing cartilage --> arthropathy)
GI distress, skin rashes, HA,
dizziness, insomnia, increased LFT,
phototoxicity, CNS effects (dizziness,
headache), tendinitis and tendon
rupture, opportunistic infection by
Candida and Streptococci ; CI in
pregnancy and in children (damage
growing cartilage --> arthropathy)
remedy for antifolate effects: Folinic
acid supplement
General properties of quinolones:
good oral bioavailability, high Vd,
t1/2 3-8hrs, absorption is impeded
by antacids, elimination is via
kidneys by tubular secretion (may
compete with probenecid for
excretion) EXCEPT for
MOXIFLOXACIN ; Norfloxacin does
not achieve adequte plasma levels
for use in systemic infections
high resistance esp for C. jejuni,
gonococci, G+ cocci like MRSA,
Pseudomonas and Serratia ; are
and Cefixime in gonorrhea ;
Ofloxacin can be used against C.
trachomatis
"Respiratory Quinolones" ;
Moxifloxacin and Gemifloxacin are
the newest members of this family
and are condisered to have the
broadest spectrum of activity with
increased activity aginst anaerobes
ang atypical agents ; FQ elimination
is via kidneys by tubular secretion
(may compete with probenecid for
excretion) EXCEPT Moxifloxacin ;
NEVER use moxifloxacin in UTI ;
Levofloxacin is used in CAP caused
by Chlamydia, Mycoplasma and
Legionella ; Gemifloxacin,
Levofloxacin and Moxifloxacin can
prolong QT ; Levofloxacin has
superior activity against G(+)
bacteria including S. pneumoniae ;
All have relatively long t1/2
permitting once daily dosing ; Oral
absorption is impaired by cations ;
Gatifloxacin can cause
hyperglycemia in DM Px and
hypoglycemia in patients also
Page 38 of 56

iv. Fourth Generation
Fluoroquinolones: Trovafloxacin,
Alatrofloxacin
D. Miscellaneous agents
i. Metronidazole, tinidazole
ii. Nitrofurantoin
Antimycobacterial Drugs
A. Isoniazid (nicotinic acid
derivative)
B. Rifamycin derivatives:
Rifampicin, rifabutin, rifapentine,
rifamixin
C. Ethambutol (butanol derivative)
D. Pyrazinamide (pyrazine
derivative)
Inhibits DNA replication by binding
to DNA gyrase and topoisomerase IV
(G+) and Topoisomerase II (G-),
bactericidal, bactericidal ; has broad
spectrum activity (gram and gram
+), enhanced activity against
anaerobes
Reactive reduction by ferredoxin
forming free radicals that disrupt
electron transport chain,
bactericidal ; For anaerobic or mixed
intra-abdominal infections, vaginitis
(trichomonas, gardnerella),
pseudomembranous colitis, brain
abscess, protozoal infections
Forms multiple reactive
intermediates when acted upon by
bacterial nitrofuran reductase,
bactericidal ; For UTI (except
Proteus and Pseudomonas)
Inhibits mycolic acid synthesis,
bactericidal ; For TB, for latent
infection, given as a sole drug for
prophylaxis of close contacts and
skin test converters
Inhibits DNA-dependent RNA
polymerase, bactericidal ; For TB,
leprosy, prophylaxis for
meningococcal and staphylococcal
carrier states, drug-resistant
infections (MRSA, PRSP) when given
together with Vancomycin, can be
used as sole drug in the treatment
of latent TB in INH-intolerant patient
or in close contact of patients with
INH-resistant strains of the organism
Inhibits arabinosyl transferases
involved in the synthesis of
arabinogalactan in mycobacterial
cell wall, bacteriostatic ; For TB
Unknow MOA, bacteriostatic but
can be bactericidal on actively
dividing mycobacteria, is
metabolozed to pyrazinoic acid, t
1/2 is increased in liver and kidney
disease ; For TB
GI distress, skin rashes, HA,
dizziness, insomnia, increased LFT,
phototoxicity, CNS effects (dizziness,
headache), tendinitis and tendon
rupture, opportunistic infection by
Candida and Streptococci ; CI in
pregnancy and in children (damage
growing cartilage --> arthropathy)
QT prolongation
GI irritation, metallic taste,
headache, dark urine, leukopenia,
dizziness, ataxia, neuropathy,
seizures and disulfiram reaction
GI irritation, skin rashes, pulmonary
infiltrates, phototoxicity,
neuropathies, hemolysis in patients
with G6PD deficiency
hepatotoxicity, neurotoxicity
(seizures, peripheral neuritis,
insomnia, restlessness, muscle
twitching), acute hemolysis in G6PD
deficiency, drug-induced lupus
red-orange urine, light chain
proteinuria, skin rash,
thrombocytopenia, nephritis,
hepatotoxicity, flulike syndrome,
anemia, impair antibody response
dose-dependent visual disturbances
(decreased visual acuity, red green
color blindness, retrobulbar neuritis,
retinal damage, optic neuritis),
headache, confusion,
hyperuricemia, peripheral neuritis
hepatotoxicity, nongouty
polyarhtralgia, asymptomatic
hyperuricemia, myalgia, GIT
irritation, maculopapular rash,
porphyria, photosensitivity ; CI in
pregnancy
receiving OHA and was withdrawn
from the market in 2006 (USA)
additional SE: diabetes (gatifloxacin),
hepatotoxicity (trovafloxacin)
DOC for amoebiasis, giardiasis and
Pseudomembranous colitis
single OD dose can prevent
recurrent UTI ; acidification of urine
enhances activity ; adjust dose in
renal patients
Most impt drug in TB, prevent
neurotoxicity by giving pyridoxine
(vit B6) ; structural congener of
pyridoxine ; high level resistance
due to deletion of KatG gene whichh
codes for catalase-peroxidase
enzyme involved in bioactivation of
INH, low level resistance due to
deletion og inhA gene which
encodes the target enzyme which is
an acyl protein reductase ; Potent
CYP450 inhibitor
Potent CYP450 inducer ; rapid
development of resistance if used
alone ; resistance is due to changes
of drug sensitivity of the polymerase
enzyme; undergoes enterohepatic
recirculation ; orange-colored
metabolites ; delay emergence of
resistance to dapsone ; Rifabutin is
equally effective as anti-
mycobacterial agent with less drug
interaction and it is the preferred
anti-TB for AIDS patients ; Rifamixin
is not absorbed in the GIT and is
used for traveler's diarrhea
Resistance is due to mutation in
emb gene ; dose adjustment id
needed in renal patients ; always
used in combination with other
drugs for TB
Most hepatotoxic anti-TB drug, also
known as sterilizing agent ; require
metabolic conversion via
pyrazinamidases in MTb ; resistance
is via mutation in pncA gene which
codes for pyrazinamidases and
increased efflux systems ; decrease
dose in hepatic and renal patients
Page 39 of 56

E. Streptomycin (aminoglycoside)
Drugs for Leprosy
A. Sulfones: Dapsone, acedapsone
B. Clofazimine
Antifungal Agents
A. Polyene antifungal:
Amphotericin B
B. Flucytosine
C. Azole Antifungals
i. Ketoconazole (Imidazole)
ii. Fluconazole (Triazole)
iii. Itraconazole (Triazole)
for MDRTB (TB meningitis, miliary
TB, severe organ TB)
Inhibition of folic acid synthesis,
bacteriostatic ; For leprosy,
alternative for PCP pneumonia
Binds to guanine bases in bacterial
DNA, bactericidal ; For leprosy
Binds to ergosterol in fungal cell
membranes, forming artificial pores,
fungicidal, WIDEST antifungal
spectrum ; For systemic fungal
infections (aspergillus, blastomyces,
candida, Cryptococcus, histoplasma,
mucor), for initial induction before
followup treatment with azoles, can
be used topically in mycotic corneal
ulcers and keratitis
Accumulated in fungal cells by the
action of permease and converted
by cytosine deaminase to 5-FU,
which inhibits thimidylate synthase,
pyrimidine antimetabolite,
fungistatic ; given together with
ampho B and Triazoles - For
cryptococcal infection, systemic
candidal infections,
chromoblastomycosis
Inhibit 14-demethylase -->
decreased ergosterol production -->
increased permeability of cell
membrane, Inhibits fungal P450-
dependent enzymes blocking
ergosterol synthesis, fungistatic ; For
chronic mucocutaneous candidiasis,
dermatophytosis
Inhibit 14-demethylase -->
decreased ergosterol production -->
increased permeability of cell
membrane, Inhibits fungal P450-
dependent enzymes blocking
ergosterol synthesis, fungistatic ;
DOC for candidiasis (esophageal,
oropharyngeal, vulvovaginitis),
coccidioidomycosis, cryptococcal
meningitis (treatment and
prophylaxis)
Inhibit 14-demethylase -->
decreased ergosterol production -->
increased permeability of cell
membrane, Inhibits fungal P450-
dependent enzymes blocking
ergosterol synthesis, fungistatic ;
DOC for blastomycosis,
sporotrichosis, dermatophytosis esp
onchomycosis,
chromoblastomycosis ; alternative
for infections due to Aspergillus,
Coccidioides, Cryptococcus and
see entry
GI irritation, fever, skin rashes,
methemoglobinemia, acute
hemolysis in G6PD deficiency
patients
GI irritation, skin discoloration
infusion reactions (chills, fever,
muscle spasms, vomiting,
hypotension), dose limiting
nephrotoxicity (decreased GFR, ATN
with magnesium and potassium
wasting, decreased erythropoietin),
neurotoxicity (seizure, neuronal
damage)
reversible myelosuppresion,
alopecia, hepatotoxicity
Limited to topical use because of
GI disturbances (vomiting, diarrhea),
rash, hepatotoxicity, drug
interaction, gynecomastia,
menstrual irregularities and
infertility
GI disturbances (vomiting, diarrhea),
rash, hepatotoxicity
GI disturbances (vomiting, diarrhea),
rash, hepatotoxicity
see entry
Most active drug against M. leprae ;
used in combination with rifampicin
and clofazimine ; Acedapsone is a
repository form of dapsone which
has drug action that can last for
several months
a phenazine dye
Control infusion reactions by
slowing the rate of infusion and
premedication with antihistamines,
additive nephrotoxicity with other
nephrotoxic drugs (aminoglycosides)
; highly lipid soluble, poorly
absorbed in the GIT ; high Vd except
in the CNS with a t1/2 of 2weeks ;
resistance is due to decreased level
of ergosterol or change in
membrane structure ; has the
WIDEST antifungal spectrum
decrease dose in renal patients ;
resistance is due to decreased
activity of fungal permease and
deaminase ; has synergistic effect
when given with ampho B and
Triazoles.
systemic toxicity ; narrow antifungal
spectrum ; resistance is due to
chnages in the sensitivity of target
enzyme ; Potent CYP450 inhibitor ;
Ketoconazole is rarely used due to
drug interactions and narrow
spectrum
alternative to Ampho B in the
treatment of C. neoformans, as
effective as Ampho B in candidemia
may also be used for subcutaneous
chromoblastomycosis
Page 40 of 56

iv. Voriconazole (Triazole)
v. Posaconazole (Triazole)
vi. Clotrimazole, miconazole,
ketoconazole
D: Echinocandins: Caspofungin,
anidulafungin, micafungin
E. Griseofulvin
F. Terbinafine
G. Nystatin (polyene)
Antiviral Agents
A. Anti-Herpes
i. Acyclovir, valacyclovir,
penciclovir, famciclovir, docosanol
Histoplasma , for esophageal
candidiasis resistant to fluconazole
Inhibit 14-demethylase -->
decreased ergosterol production -->
increased permeability of cell
membrane, Inhibits fungal P450-
GI disturbances (vomiting, diarrhea),
dependent enzymes blocking
rash, hepatotoxicity, blurring of
ergosterol synthesis, fungistatic ; co- wider specturm azole
vision in 30% of patients, CI in
DOC for invasive aspergillosis,
pregnancy
alternative in candidemia, for
fluconazole-resistant organisms, for
candidal esophagitis and stomatitis
in AIDS patients
Inhibit 14-demethylase -->
decreased ergosterol production -->
increased permeability of cell
membrane, Inhibits fungal P450-
BROADEST spectrum triazole ; the
dependent enzymes blocking
GI disturbances (vomiting, diarrhea), only azole with activity against
ergosterol synthesis, fungistatic ; For
rash, hepatotoxicity Rhizopus sp. (mucormycosis) ;
Candida and Aspergillus, as
Potent CYP450 inhibitor
prophylaxis of fungal infection
during cancer chemotherapy,
salvage therapy in invasive
aspergillosis
Inhibit 14-demethylase -->
decreased ergosterol production -->
increased permeability of cell
membrane, Inhibits fungal P450-
Limited to topical use because of
dependent enzymes blocking None when administered topically
systemic toxicity
ergosterol synthesis, fungistatic ; For
mucocutaneous candidiasis,
dermatophytosis, seborrheic
dermatitis, pityriasis versicolor
Inhibit beta-glucan synthase which
produces (1-->2) glycan which is a
cellwall component, thus decreasing
fungal cell wall synthesis, headache, GI distress, rash, fever, all are given IV ; micafungin can
fungostatic ; For disseminated and flushing (histamine release), increase levels of cyclosporine and
mucocutaneous candidiasis who fail elevated liver enzymes tacrolimus
to respond to amphoB, for
mucormycosis, salvage therapy for
invasive aspergillosis
headache, mental confusion, GI given PO ; Accumulates in keratin ;
Interferes with microtubule function irritation, photosensitivity, potent CYP450 inducer ; absorption
in dermatophytes, inhibits synthesis hepatotoxicity, disulfiram reaction, is increased by intake of fatty meal ;
and polymerization of nucleic acids, drug interactions (decreases resistance is due to decreased
fungistatic ; For dermatophytosis bioavialability of warfarin) ; transport of drug into the fungal cell
contraindicated in porphyria wall
Inhibits withg ergosterol synthesis
by inhibiting fungal squalene given PO and topical, also
oxidase leading to increased GI upset, rash, headache, taste accumulates in keratin, more
squalene which interferes with disturbances effective than griseofulvin in
ergosterol synthesis, fungicidal ; For onchomycosis
dermatophytosis, onchomycosis
Binds to ergosterol in fungal cell
membranes, forming artificial pores,
fungicidal ; For candidiasis Minimal mucocutaneous absorption,
((oropharyngeal, esophageal and nephrotoxicity (severe) available as swish and swallow
vaginal), for GI fungal infections in preparation
patients with impaired defense
mechanisms
Activated by viral thymidine kinase nausea, diarrhea, headache, given PO, topical and IV ; dose
(TK) to forms that inhibit viral DNA delirium, tremor, seizures, adjustment in renal patients ; No
polymerase, guanosine analog, hypotension, nephrotoxicity activity against strains of HSV with
Page 41 of 56
 competitive substrate for DNA
polymerase, causes chain
termination after its incorporation
into the viral DNA ; For infections
due to HSV1, HSV2, VZV
(mucocutaneous and genital herpes,
prophylaxis in AIDS and in other
Immunocompromised states such as
organ transplant patients, herpes
encephalitis, neonatal HSV infection
etc.
Inhibits fusion between the HSV
envelope and plasma membrane,
ii. Docosanol
prevents viral entry and subsequent
replication
Inhibits viral DNA polymerase
causing chain termination,
guanosine derivative ; For infections
iii. Ganciclovir, valganciclovir
due to CMV, HSV1, HSV2, VZV ; For
(anti-CMV)
prohylaxis and treatment of CMV
retinitis and other CMV infections in
the immunocompromised patients
Inhibits viral DNA polymerase
causing chain termination ; For CMV
retinitis, mucocutaneous HSV
iv. Cifodovir (anti-CMV)
infections, acyclovir-resistance,
ganciclovir-resistance, genital warts
and molluscum contangiosum
Inhibits viral RNA polymerase, DNA
polymerase, and HIV reverse
transcriptase, binds to
pyrophosphate binding site ; as
v. Foscarnet (anti-CMV) alternative for prophylaxis and
treatment of CMV retinitis,
gancyclovir-resistant strains of CMV,
HSV infection in patients with AIDS,
also used in organ transplantation
vi. Vidarabine adenine analog ; For HSV, VZV, CMV
pyrimidine analogs ; For herpes
vii. Idoxuridine, trifluridine
keratitis (HSV-1)
antisense oligonucleotide that binds
to mRNA of CMV causing inhibition
viii. Fomivirsen
of early protein synthesis ; For CMV
retinitis
B. Drugs for HIV
Inhibit HIV reverse transcriptase
after phosphorylation by cellular
enzymes, acts as chain terminators
i. NRTI:
via insertion into the growing DNA
chain ; For HIV infection, prevention
of maternal-fetal HIV transmission
a. Abacavir guanosine analog
b. Didanosine (ddI) NRTI
nausea, diarrhea, headache,
delirium, tremor, seizures,
hypotension, nephrotoxicity
leukopenia, thrombocytopenia,
mucositis, hepatotoxicity, seizures,
neutropenia
nephrotoxicity
nephrotoxicity, electrolyte
abnormalities (hypocalcemia), GU
ulcerations, CNS effects (headache,
hallucination, seizures)
GI irritation, paresthesia, tremor,
convulsion, hepatic dysfunction, CI
in pregnancy
irritation, blurred vision,
photophobia
iritis, vitritis, increased IOP, changes
in vision
see specific drugs below
hypersensitivity reaction
acute pancreatitis, peripheral
neuropathy, diarrhea, hepatic
dysfunction, hyperuricemia, CNS
effects
absent thymidine kinase activity ;
resistance is due to changes in viral
DNA polymerase ; Valacyclovir is a
prodrug that is converted to
Acyclovir and reached plams levels
3-5x (longer t1/2) more than
acyclovir ; Penciclovir does not
cause chain termination ;
Famciclovir is a prodrug which is
converted to Penciclovir in vivo
topical preparation shortens healing
time
given as IV or intraocular implant
(for CMV retinitis) ; No activity
against strains of HSV with absent
thymidine kinase activity ; CMV
resistance is due to mutation in viral
DNA polymerase and in the genes
that code for the activating viral
phosphotransferase ; Valganciclovir
is a prodrug of ganciclovir with
increased oral bioavialability
Active against strains of HSV with
absent thymidine kinase activity ;
resistance is due to mutation in
DNA polymerase ; dose adjustment
in renal patients
Active against strains of HSV with
absent thymidine kinase activity ;
does not require phosphorylation
for antiviral activity ; resistance is
due to mutations in DNA
polymerase gene ; dose adjusment
in renal patients
used topically only because it is
rapidly metabolized into the inactive
form and because it has a toxic
potential
topical only because it is too toxic fo
systemic use
injected intravitreally ; concurrent
systemic use of anti-CMV in threapy
is recommended to protect against
extraocular and contralateral retinal
CMV disease
these are prodrugs converted by
host cell kinases tp triphosphates
causing competitive binding of
natural nulecotides to the dNTP-
binding site of Reverse Transcriptase
; resistance is due to mutation in pol
gene
good oral bioavailability, T1/2 is 12-
24hrs, resistance is slow
oral bioavailability is decreased by
food and chelating agents ; dose
adjustment in renal patients
Page 42 of 56
 aesthenia, GI upset, headache,
hyperpigmentation of palms of per orem once a day treatment,
c. Emtricitabine NRTI
soles, CI in pregnancy, children, dose adjustment in renal patients
renal and hepatic and patients
80% oral bioavailability ;may also be
GI upset, headache, fatigue,
d. Lamivudine (3TC) NRTI used for Hepa B infection ; HAART,
insomnia
dose adjustment in renal patients
peripheral neuropathy esp if given
good oral bioavailability, dose
e. Stavudine (d4T) NRTI together with Zalcitabine, lactic
adjustment in renal patients
acidosis with hepatic steatosis
a nucleotide but acts as NRTI,
competitively inhibits RT, cause GI upset, asthenia, headache, oral bioavailabilty is 25-40% ; halflife
f. Tenofovir
chain termination after Fanconi syndrome, AKI is 60hours ; also used against HBV
incorporation into DNA
peripheral neuropathy, pancreatitis,
increased oral bioavailability, dose
g. Zalcitabine (ddC) NRTI esophageal ulceration, stomatitis,
adjustment in renal patients
arthralgias
BM suppression (anemia,
neutropenia, thrombocytopenia), dose adjustment in uremic patients
h. Zidovudine (ZDV) Azidothymidine or AZT acute cholestatic hepatitis, agitation, and cirrhosis ; affected by enzymes
insomnia, myalgia, headache, GI inducers and inhibitors
upset
Delavirdine and Nevirapine (rash,
Inhibits HIV reverse transcriptase,
increased AST/ALT, Efavirenz binds to a different binding site ;
ii. NNRTI: Delavirdine, efavirenz, no phosphorylation required, do not
(teratogenicity), Etravirine resistance is due to mutations in pol
etravirine, nevirapine compete with nucleoside
(increased cholesterol and gene
triphosphate ; For HIV infection
triglycerides)
metabolized by CYP3A4 and CYP2D6,
a. Delavirdine NNRTI rashes, teratogenic affected by enzyme inducer and
inhibitor
CNS dysfunction, skin rash,
enhanced absorption by fatty meals,
b. Efavirenz NNRTI increased plasma cholesterol,
drug interactions are common
teratogenic
nausea, vomiting, diarrhea,
c. Etravirine NNRTI, for drug-resistant HIV increased cholesterol, triglycerides NEWEST NNRTI
and LFTs
used as a singledose to prevent HIV
good oral bioavailability,t1/2 is
d. Nevirapine vertical transmission at the onset of rash, SJS, TEN
>24hours
labor and also given to the neonate
General SE: hyperglycemia, insulin
resistance, hyperlipidemia, altered
cleaves precursor polyprotein to body fat distribution (buffalo hump,
iii. Protease Inhibitor: Atrazanavir,
form the final structural protein of gynecomastia, truncal obesity, facial Resistance is due to mutation in pol
Darunavir, Fosamprenavir,
the mature virion core, inhibits viral and peripheral lipodystrophy) due to gene ; are potent CYP3A4 inhibitor
Indinavir, Nelfinavir, Lopinavir-
protein processing ; For HIV the inhibition of lipid-regulating esp Ritonavir
Ritonavir, Saquinavir, Tipranavir
infection proteins which have active sites with
structural homology to that of HIV
protease
per orem absorption requires acidic
environment ; can penetrate CSF
peripheral neuropathy, skin rash, and seminal fluid ; is not associated
a. Atazanavir Protease Inhibitor
hyperbilirubinemia, QT prolongation with dyslipidemia, fat deposition or
metabolic syndrome ; CYP3A4 and
2C9 inhibitor
rash, hepatotoxicity, hypersensitivity Given together with Ritonavir in
b. Darunavir Protease Inhibitor
; CI in patients with sulfa allergy patients resistant to other PIs
GI upset, paresthesia, rash, CI in
pregnant patients and children if
a prodrug that is converted to the
drug uses propylene glycol as
active drug Amprenavir ; absorption
c. Fosamprenavir Protease Inhibitor solvent ; does not have risk for
is impaired by fatty food ; used with
hyperlipidemia, fat maldistribution,
lowdose Ritonavir
hyperglycaemia and insulin
resistance
decreased bioavailability in the
nausea, vomiting, diarrhea,
d. Indinavir Protease Inhibitor presence of food ; affected by
thrombocytopenia,
enzyme inhibitors and inducers
Page 43 of 56

e. Lopinavir-Ritonavir
f. Nelfinavir
g. Ritonavir
h. Saquinavir
i. Tipranavir
iv. Entry inhibitors:
a. Fusion Inhibitor: Enfuvirtide,
Docosanol
b. CCR5 receptor antagonist:
Maraviroc
C. Drugs for Influenza
i. Uncoating inhibitors:
Amantadine, rimantadine
ii. Neuraminidase inhibitors:
Oseltamivir, Zanamivir, Peramivir
D. Drug for HBV and HCV
i. Interferon-
used as a combination drug: uses
subtherapeutic dose of ritonavir
which inhibits CYP3A4 mediated
metabolism of lopinavir
Protease Inhibitor
Protease Inhibitor ; subtherapeutic
doses inhibit CYP3A4-mediated
metabolism of other Pis (Indnavir,
Lopinavir, Saquinavir) which permits
lower dose of the other PI
Protease Inhibitor ; given together
with low dose Ritonavir to improve
compliance and decrease GI upset
Protease Inhibitor ; given with
Ritonavir for PI-resistant HIV
Binds to gp41 subunit of viral
envelope glycoprotein, preventing
fusion of viral and cellular
membranes ; For previously drug-
treated patients with persistent HIV
replication despite ongoing therapy
Blocks viral attachment by blocking
CCR5, a transmembrane protein
involved in the attachment of HIV to
host cell ; For HIV infection
Inhibit early step replication and
prevent uncoating by binding to M2
proton channels ; For influenza A
and rubella
Inhibits neuraminidase which
cleaves sialic acid residues from viral
proteins and surface proteins of
infected cells , decrease release of
progeny virus ; For influenza A and
B, shortens duration of symptoms
cytokine, increased activity of JAKS
leading to phosphorylation of signal
transducers and activation of
transcription (STATS) which causes
increased formation of antiviral
proteins , also increases NK cells
that destroy infected liver cells,
hearing loss, neutropenia ;
Degrades viral RNA via activation of
host cell RNAse (ribonuclease) ; For
chronic HBV, HCV infection, Kaposi
sarcoma, genital warts, prevents
dissemination of HZV in cancer
patients and decreased CMV
shedding after renal transplantation
hyperbilirubinemia, nephrolithiasis,
insulin resistance
GI upset (well-tolerated side effects)
Diarrhea
GI upset, bitter taste, paresthesia,
increased LFT's
nausea, vomiting, diarrhea,
dyspepsia, rhinitis
GI upset, rash, hepatotoxicity
injection site reaction,
hypersensitivity reaction, increased
incidence of bacterial pneumonia
cough, diarrhea, muscle and joint
pains, increased LFTs
GI irritation, dizziness, cerebellar
dysfunction (ataxia, dysarthria),
livedo reticularis
GI effects (Oseltamivir),
bronchospasm in asthmatics and
cough with throat discomfort
(Zanamivir )
alopecia, myalgia, severe
depression, flu-like syndrome,
thyroid dysfunction, reversible
Contraindications include
autoimmune disease, history of
cardiac arrhythmia and pregnancy
there is increased compliance with
this drug ; Ritonavir has boosting
effect on other PI due to enzyme
inhibitory effect
absorption is increased by food,
short half-life ; has the most
favorable safety profile for
pregnancy
good oral bioavailability esp when
taken with meals ; affected by
enzyme inducer and inhibitors
affected by enzyme inducers and
inhibitors
newer drug ; induces P-glycoprotein
transporters which leads to
alteration of GI absorption of other
drugs
subcutaneous and usually given
together with other HIV agents
good tissue penetration ; affected by
enzyme inhibitors and inducers
Amantadine is also used in treating
parkinsonism ; should be given
within 48hrs of exposure ;
Rimantadine has longer halflife and
doe snot need dose-adjustment for
renally-impaired Px ; there is
increased resistance observed with
amantadine
DOC for influenza (including H1N1) ;
Oseltamivir is PO while Zanamivir is
intranasal ; Peramivir has been given
temporary emergency use
authorization by US FDA for H1N1 in
2009 but has not yet been licensed
by the US FDA
slow absorption, given IM or SC
once a day 3x week but the PEG-
form is only given once a week,
given topically for genital warts
Page 44 of 56

Inhibits HBV DNA polymerase
causing chain termination after
incorporation into the viral DNA ;
ii. Adefovir, Dipivoxil, Telbivudine,
For lamivudine-resistant Hepatitis B
Tenofovir
infection, suppresses HBV
replication and improves liver
histology and fibrosis
guanosine nucleoside, inhibits DNA
iii. Entecavir
polymerase
see entry, also active for HBV,
iii. Lamivudine (3TC)
rapidly suppresses HBV replication
Inhibits guanosine triphosphate
formation, prevents capping of viral
mRNA, blocks RNA-dependent RNA
polymerase, inhibit replication of
many DNA and RNA viruses like
iii. Ribavirin
Influenza A and B, parainfluenza,
paramyxo viruses, HCV and HIV ; For
HCV infection (with IFN-) and RSV
infection, decreases mortality in
viral hemorrhagic fevers
Antiprotozoal Drugs
A. Antimalarial drugs
accumulates in the food vacuole of
plasmodia > Prevents
polymerization of heme into
hemozoin > inc heme
concentration which is toxic to the
parasite, Blood schizonticide ; For
malaria (non-falciparum,
i. Chloroquine,
chloroquine-sensitive), DOC for
hydroxychloroquine
acute attacks of non-Falciparum and
sensitive Falciparum malaria, used
as chemoprophylaxis except in
regions where P. falciparum is
resistant, for autoimmune diseases
such as rheumatoid arthritis,
amoebic liver abscess
Complexes with double stranded
DNA to prevent strand separation
> blocks DNA replication and
transcription to RNA, blood
schizonticide ; For malaria
ii. Quinine, Quinidine gluconate
(chloroquine-resistant) and severe
falciparum malaria (quinidine), given
together with Doxycycline and or
Clindamycin to shorten duration of
disease
Unknown MOA, blood schizonticide
; For chemoprophylaxis
(chloroquine-resistant areas) ; 1st
line drug (weekly administration) for
iii. Mefloquine prophylaxis in all areas with
Chloroquine resistance), alternative
to quinine in acute attacks and
uncomplicated infections from
falciparum malaria
8-aminoquinoline, Forms quinoline-
quinone metabolites which are
iv. Primaquine
electron-transferring redox
compounds that act as cellular
Lactic acidosis, renal toxicity, severe
hepatomegaly with steatosis
headache, dizziness, fatigue, nausea
see entry
haemolytic anemia, conjunctival and
bronchial irritation, teratogen
is NOT effective
May precipitate porphyria ;
GI irritation, skin rash, headache,
severe skin lesions, peripheral
neuropathies, myocardial
depression, retinal damage, auditory
impairment, psychosis
cinchonism (headache, tinnitus,
vertigo), hemolysis in G6PD
deficiency, blackwater fever,
blurring of vision, GI upset,
disturbance n cardiac conduction ; CI
in pregnancy
GI distress, skin rash, headache,
dizziness, cardiac conduction
defects, psychiatric disorders
(psychosis), neurologic symptoms,
seziures
GI distress, pruritus, headaches,
methemoglobinemia, hemolysis in
G6PD deficient patients ; CI in
pregnancy
Dipiroxil is a prodrug of Adefovir ;
Telbivudine is a newer drug
(nucleoside analog) but
develpoment of resistance is rapid,
it is as effective as lamivudine ;
Tenofovir is an anti-RT drug that is
also effective in chronic HBV, it is
active against lamivudine and
entecavir-resistant strains
is as effective as lamivudine, longer
t1/2 of 12hrs
Coinfection between HBV and HIV
may increase the risk of pancreatitis
with lamivudine use ; longer t1/2 in
HBV infected cells than in HIV (lower
dose required in HBV than in HIV)
given PO, IV or aerosol, avoid
concomitant administration of
anatcids ; Early IV administration of
ribavirin decreases mortality in viral
hemorrhagic fevers ; monotherapy
Chloroquine is 4-aminoquinoline
derivative, can be given PO and has
high Vd, absorption is decrease by
antacids ; resistance is due to dec.
intracellular accumulation via inc
activation of membrane pumps, dec
intravacuolar accumulation via
transporter encoded by pfcrt gene
Quinine is commonly used with
doxycycline or clindamycin to limit
toxicities, PO and IV (in severe
infection) ; NEVER use as prophylaxis
is a 4-quinoline derivatives, PO
Eradicates hypnozoites in the liver,
preventing malarial relapse, PO ,
should be used with a blood
Page 45 of 56

v. Atovaquone-proguanil
vi. Sulfadoxine-pyrimethamine
(Fansidar)
vii. Doxycycline
viii. Halofantrine , lumefantrine
ix. Artemsinin, artesunate,
artemether, dihydroartemsinin
x. Amiodaquine
B. Anti-amoebiasis
i. Diloxanide Furoate
ii. Emetine, dehydroemetine
ii. Iodoquinol
oxidants, tissue schizonticides, schizonticide, 14-day course of Tx
gametocides ; For malaria, after Tx with choloroquine
eradicates liver stages of P. vivax
and P. ovale (radical cure of P. vivax
and P. ovale), alternative as primary
prevention, terminal prophylaxis
(vivax, ovale), PCP pneumonia
Atovaquone disrupts mitochondrial
electron transport, blood and tissue
also effective against Mefloquine-
schizonticide, proguanil inhibits
abdominal pain, nausea, vomiting, resistant Falciparum infection ;
folate synthesis, sporonticide ; For
diarrhea, headache, rash, increased Proguanil has a t1/2 12-16h ;
treatment and chemoprophylaxis of
liver enzymes Atovaquone is an alternative for P.
chloroquine-resistant falciparum,
jiroveci infection
protective vs. Mefloquine-resistant
falciparum
Sequential blockade of folic acid
synthesis (sulfadoxine blocks GI disturbances, teratogen (enamel
Dihyrodpteroate synthetase, dysplasia and discoloration), t1/2 is usually >100h, PO, highly
Pyrimethamine blocks Dihydrofolate hepatotoxicity, nephrotoxicity, protein bound ; pyrimethamine is a
reductase, blood schizonticide and photosensitivity, vestibulotoxicity, sporonticide
sporonticide ; For malaria (for hemolysis
Chloroquine-resistant)
Impairs progeny of malarial
GI disturbances, teratogen (enamel
apicoplast genes, resulting in
dysplasia and discoloration), Do not drink with milk (decreased
abnormal cell division, blood
hepatotoxicity, nephrotoxicity, absorption), PO
schizonticide ; For chemoprophylaxis
photosensitivity, vestibulotoxicity
in multi-drug resistant strains
Lumefantrine used in combination
Unknown MOA, active vs the with artemether (Co-arthem) for
erythrocytic stage of all 4 strains abdominal pain, diarrhea, vomiting, uncomplicated falciparum infection ;
including Chloroquine-resistant, cough, rash, headache, pruritus, Halofantrine is never used for
blood schizonticide ; For elevated liver enzymes, prophylaxis because of
chloroquine-resistant malaria and cardiotoxicity, teratogen cardiotoxicity and embryogenecity,
severe falciparum malaria Lumefantrine has minimal
cardiotoxicity
Co-artem is the DOC for
uncomplicated falciparum malaria in
the Philippines ; Combination
therapy of artemesinins with one or
two long-acting antimalarial drugs
is metabolized in the food vacuole of
(amodiaquine, mefloquine,
protozoa > Forms toxic free
nausea, vomiting, diarrhea ; SAFE in sulfadoxine/pyrimethamine or
radicals in malarial food vacuole,
pregnancy lumefantrine) is favored to retard
blood schizonticide ; For malaria
the development and progression of
(falciparum and MDR strains)
drug resistance in P. falciparum ; not
given as Prophylaxis due to short
t1/2 (1-3h) ; the only reliably
effective meds vs Quinine-resistant
strains
MOA same as chloroquine (inhibits
low-cost, given as combination with
the digestion of hemoglobin) ; For agranulocytosis, aplastic anemia
Artesunate
chloroquine-resistant falciparum
Unknown MOA, converted to
Diloxanide freebase (active
flatulence, nausea, abdominal converted in vivo into Diloxanide
amobecide), luminal amebicide ;
cramps freebase which is the amoebicide
DOC for asymptomatic cyst carrier
of E. histolytica
Inhibits protein synthesis by
blocking ribosomal movement along Reserved only for situations where
messenger RNA, tissue amebicide ; GI distress, muscle weakness, CV metronidazole cant be used , given
back up drug for severe intestinal, dysfunction (arrhythmias and CHF) SC or IM , usually given together
hepatic and extraintestinal with luminal amebicides
amebiasis
halogenated hydroxyquinoline, GI distress, thyroid enlargement, Usually used in combination with
Unknown MOA, luminal amebicide ; skin reactions due to iodine toxicity, metronidazole, PO
Page 46 of 56
 Alternative to Diloxanide for mild to
severe intestinal amebiasis
Reactive reduction by ferredoxin
forming free radicals that disrupt
electron transport chain, tissue
amebicide ; DOC for severe
intestinal wall disease and in hepatic
iii. Metronidazole, Tinidazole,
abscess and other extra intestinal
Secnidazole
amebic disease, DOC for
trichomoniasis, also used for
giardiasis, bacterial vaginosis
(Gardnerella vaginalis), anaerobic
infections, H. pylori PUD
An aminoglycoside, Inhibits protein
synthesis, binds to 16S ribosomal
iv. Paromomycin subunit, luminal amebicide ; For
intestinal amebiasis,
cryptosporidiosis
Reactive reductions by ferredoxin
forming free radicals that disrupt
electron transport chain, tissue
v. Nitazoxanide
amebicide ; For metronidazole-
resistant amebiasis, giardiasis,
cryptosporidiosis (DOC)
C.Drugs for Pneumocystis and Toxoplasmosis
Sequential blockade of
dihydropteroate synthase
(sulfamethoxazole) and
dihydrofolate reductase
i. Co-trimoxazole
(trimethoprim), bactericidal ; DOC
for prophylaxis and treatment of
Pneumocystosis, prophylaxis (T.
gondii, I. belli)
Unknown MOA but may involve
inhibition of glycolysis or
interference with NA metabolism of
ii. Pentamidine Protozoans and Fungi ; For
prophylaxis and treatment of
pneumocystosis and
trypanosomiasis
Sequential blockade of
dihydropteroate synthase
(sulfadiazine) and dihydrofolate
iii. Pyrimethamine-sulfadiazine
reductase (pyrimethamine) ; DOC
for prophylaxis and treatment of
toxoplasmosis
Atovaquone disrupts mitochondrial
electron transport ; For mild to
iv. Atovaquone moderate PCP, as chemoprophylaxis
for Chloroquine resistant malaria
(with Proguanil)
D. Drugs for Trypanosomiasis
Unknown MOA but may involve
inhibition of glycolysis or
interference with NA metabolism of
Protozoans and Fungi ; For
i. Pentamidine
hemolymphatic stage of T.
gambiense and T. rhodiense, For
prophylaxis and treatment of
pneumocystosis
Polyanionic compound, Unknown
MOA ; DOC for early hemolymphatic
ii. Suramin stages of African sleeping sickness,
Alternative to Ivermectin in
onchocerciasis
neurotoxicity (peripheral
neuropathy, visual dysfunction)
given PO, IV or topical,
Metronidazole t1/2 is 6-8h,
GI irritation, metallic taste, Tinidazole t1/2 is 12-14h; dose
headache, dark urine, leukopenia, adjustment in renal patients, well
dizziness, ataxia, neuropathy, distributed even in CSF ; active
seizures, disulfiram reaction, against protozoan and bacteria
opportunistic infections, (Bacteroides and Clostridium, DOC
parestheisa, CI in pregnancy for Pseudomembranous colitis) ;
causes potentiation of warfarin
action ; bets taken with meals
may be given together with
tetracycline in mild intestinal
headaches, dizziness, rashes,
disease ; superior to Diloxanide in
arthralgia
asymptomatic carries but SE limits
its use
may also be used in helminthic
GI distress
infections
GI upset, acute hemolysis in G6PD
deficiency, nephrotoxicity, Recommended at CD4 count < 200,
hypersensitivity, hematotoxicity, given daily, PO or IV
kernicterus
respiratory stimulation followed by
Administered by nasal
depression, hypotension,
spray/aerosol, given once a month if
hypoglycaemia, anemia,
used for prophylaxis, IV or IM for 21
neutropenia, hepatitis, pancreatitis,
days if for Tx of active disease
inhalant route has minimal SE
gastric irritation, glossitis, neurologic
an alternative drug for
symptoms (headache, insomnia,
Toxoplasmosis is Clindamycin ,give
tremors, seizures), hematotoxicity
daily for 3-4 weeks if for Tx of active
(megaloblastic anemia,
toxoplasmosis , if for Toxoplasma
thrombocytopenia),
encephalitis, give for at least 6
pseudomembranous colitis
weeks
(clindamycin)
abdominal pain, nausea, vomiting,
has increased absorption in the
diarrhea, fever, increased liver
presence of food, PO
enzymes
respiratory stimulation followed by
depression, hypotension, do not use for latter stages because
hypoglycaemia, anemia, it does not cross the BBB, also used
neutropenia, hepatitis, pancreatitis, for Kala-azar and PCP
inhalant route has minimal SE
fatigue, nausea, vomiting, seizures,
Do not cross blood brain barrier ,
shock fever, rash, headache,
Used in combination with
paresthesia, neuropathies, renal
melarsoprol
abnormalities (proteinuria), chronic
Page 47 of 56
 diarrhea, haemolytic anemia and
agranulocytosis
Suicide inhibitor of ornithine diarrhea, vomiting, anemia,
iii. Eflornithine decarboxylase ; DOC for advanced thrombocytopenia, leukopenia, Crosses blood brain barrier, PO, IV
west African sleeping sickness seizures
Organic arsenical, inhibits enzyme
Crosses BBB, administered
sulfhydryl (-SH) groups in GI irritation, reactive
iv. Melarsoprol parenterally because it causes GI
trypanosomes ; DOC for African encephalopathy
upset
sleeping sickness
Nitrofurazone derivative, Inhibits
trypanothione reductase which is
unique to the parasite ; DOC for
nausea, vomiting, fever, rash,
Chagas disease / American Sleeping
v. Nifurtimox restlessness, insomnia, Does not cross BBB
sickness (Trypanosoma cruzi),
neuropathies, seizures
alternative for African sleeping
sickness, also for mucocutaneous
leishmaniasis
Drugs for Leishmaniasis
IV ; alternative for leishmaniasis are
as follows: Pentamidine or
Pentavalent antimony, Inhibits GI symptoms, fever, rash, arthralgia, Miltefosine (for visceral
vi. Sodium Stibogluconate glycolysis or effects on NA healdache, myalgia, sterile leishmaniasis), Fluconazole or
metabolism ; DOC for Leishmaniasis abscesses, cardiotoxicity Metronidazole (for cutaneous
leishmaniasis) and Amphotericin B
(for mucocutaneous leishmaniasis)
Anthelmintics
Selectively inhibits microtubule
synthesis and glucose uptake in
Greatly affected by enzyme inducers
nematodes, ovicidal ; Whipworm
and inhibitors ; Contraindicated in
infections (drug of choice), Also a GI irritation, agranulocytosis,
A. Mebendazole pregnancy, Use cautiously in
primary drug (together with alopecia, Elevated liver enzymes
patients with Cirrhosis and children
albendazole) for ascariasis,
<2y.o.
pinworm, Trichinosis, Visceral larval
migrans (backup)
Inhibits microtubule assembly,
larvicidal and ovicidal ; DOC for
"primary drug for ascariasis,
Ascariasis, Hookworm, Pinworm,
ancylostomiasis, trichuriasis ; safety
Hydatid disease ; Also used for reversible leukopenia, alopecia,
in pregnant and children is not yet
B. Albendazole Whipworm infections, Cutaneous & elevation of liver function tests,
established ; Improved penetration
Visceral Larva migrans, Cysticercosis bone marrow suppression
(> Praziquantel) of the subarachnoid
(larval stages of T. solium),
space in Neurocysticersosis
Angiostrongylus cantonensis,
Capillaria philippinensis
Should not be given to patients
with Cirrhosis"
Immobilizes microfilariae by an
headache, malaise, weakness,
unknown mechanism > inc
anorexia, filarial fever (fever, rashes, May cause mazzotti reaction when
C. Diethylcarbamazine susceptibility to host defense
ocular damage, joint and muscle used for onchocerciasis
mechanism ; DOC for filariasis and
pain, lymphangitis)
eye worm disease (Loa-Loa)
Intensifies GABA-mediated
Antidote for Mazzoti reaction:
neurotransmission in nematodes Mazzotti reaction (fever, headache,
antihistamine and NSAIDs ; CI in
> immobilizes parasites > removal dizziness, rashes, pruritus,
pregnancy, children 5 y.o. and Avoid
D. Ivermectin by reticuloendothelial system ; Used tachycardia, hypotension, pain in
concomitant use with other drugs
for Strongyloidiasis (drug of choice), muscles and joints and lymph
that enhance GABA activity
Onchocerciasis, Cutaneous larva glands), corneal opacities
(Barbituraates, BZDs etc)
migrans, Filariasis (back up)
Stimulates nicotinic receptors at
NMJ of nematodes >
depolarization-induced paralysis,
Contraindicated in patients with
Causes release of ACh and inhibition
GI distress headache, weakness, hepatic dysfunction (may cause an
E. Pyrantel pamoate of Cholinesterase, Kills adult worms
dizziness, insomia, rash, fever, increase in LFT) ; No study on
not eggs ; DOC for pinworm, may be
pregnant and children <2y.o.
used also for Hookworm,
Trichostrongylus and Ascaris
infections

Page 48 of 56
 Structural congener of
Mebendazole, same MOA as
Gastrointestinal irritation,
Mebendazole, Selectively inhibits
Headache, Dizziness, Drowsiness,
microtubule synthesis and glucose
Leukopenia, Hematuria,
uptake in nematodes, Inhibits CI in renal and liver disease and in
F. Thiabendazole Hypersensitivity reactions (SJS),
fumarate reductase. Ovicidal, has pregnancy
Hepatotoxicity (intrahepatic
anti-inflammatory and
cholestasis, liver failure), Reactions
immunosuppressive action in the
caused by dying parasites
host ; Used for Trichinosis (drug of
choice), Strongyloidiasis (backup)
Increases membrane permeability to
calcium > contraction of
trematode and cestode muscle >
muscle paralysis, vacualization and Used with steroid when treating
death ; DOC for trematodes neurocysticercosis to dec swelling ,
headache, dizziness, nausea,
(schistosoma, paragonimus, contraindicated in ocular
malaise, Inc ICP, seizure
G. Praziquantel clonorchis, opistorchis, Fasciolopsis, cysticercosis (may cause irreparable
(neurocystecercosis) ; CI in
Heterophyes) and cestodes (taenia, eye damage) ; May be used as an
pregnancy
diphyllobothrium, Hymenopelsis) adjunct to Albendazole in Hydatid
together with Niclosamide ; for disease
infection by small and large
intestinal flukes ; alternative to
Albendazole in Cysticerci
Uncouples oxidative
phosphorylation or by activating
ATPases, scoleces and segments are
killed but NOT Ova ; alternative drug
to Praziquantel for cestode infection Avoid ethanol consumption for 48
(Taenia, Diphyllobotrium), not hours upon drug consumption ;
H. Niclosamide GI distress, headache, rash, fever
effective in cystecercosis (use Safety in children <2y.o. and
Albendazole or Praziquantel instead) pregnanct not yet established
or Hydatid disease (use
Albendazole), effective in the Tx of
infections from small and large
intestinal flukes
GABA agonist > paralyze ascaris
Contraindicated in pregnancy,
> expelled by normal peristalsis ,
impaired renal or hepatic function
I. Piperazine block ACh at the myoneural junction GI upset
or with a history of epilepsy or
--> expulsion via normal peristalsis ;
chronic neurologic disease
As alternative for ascariasis
Unknown MOA ; co-DOC (with
Nausea,vomiting, diarrhea,
Triclabendazole) for Tx of
J. Bithionol abdominal cramps, phototoxicity, do not use in Px <8y.o.
Fascioliasis (sheep liver fluke), as
rash
alternative for paragonimiasis
an organophosphate prodrug >
Dichlorvos (AchE inhibitor) -> muscle Excess cholinergic stimulation
K. Metrifonate CI in pregnancy
contraction > paralysis ; Active vs (DUMBBELSS)
Schistosoma haemoatobium
GI upset, pruritus, eosinophilia,
effective solely in Schistosoma
urticaria, pulmonary infiltrates,
mansion (intestinal bilharziasis) - on
fever, orange-red discoloration of Px is not allowed to drive within
L. Oxamniquine male immature forms and adult
urine ; CI in pregnancy and seizure 24hrs after intake of Oxamniquine
schistosomal forms ; MOA is
disorder, proteinuria, microscopic
unknown
hematuria,
Cancer Chemotherapy
all are Cell-cycle non-specific ;
Universal MOA: form reactive
molecular species that alkylate Resistance is due to increased DNA
nucleophilic groups on DNA bases, repair, decreased drug permeability
A. Alkylating agents
particularly the N-7 of guanine and production of trapping agents
leading to cross-linking of bases, such as thiols
abnormal base pairing and DNA
strand breakage
i. Nitrogen Mustards: Forms DNA cross-links, resulting in bone marrow suppression, Rescue therapy is MESNA and
Cyclophosphamide, Chlorambucil, inhibition of DNA synthesis and hemorrhagic cystitis, hepatotoxicity, hydration; metabolite is acrolein
Mechlorethamine function, Cell-cycle nonspecific, alopecia, SIADH, pulmonary toxicity, which is important for

Page 49 of 56

ii. Platinum Analogs: Cisplatin,
Carboplatin, oxaliplatin
iii. Alkyl sulfonate: Busulfan
iv. Nirtosoureas: Carmustine,
lomustine
v. Others: Procarbazine,
Dacarbazine
B. Antimetabolites
i. Folate antagonist: Methotrexate
ii. Purine antagonist: 6-
Mercaptopurine, 6-thioguanine,
fludarabine, cladribine
iii. Pyrimidine antagonist: 5-
Fluorouracil
iv. Pyrimidine antagonist:
Cytarabine (ARA-C)
Mechlorethamine has additional
MOA: converts to a reactive
cytotoxic product ; For non-
hodgkins lymphoma, breast cancer,
ovarian cancer, neuroblastoma, CLL
Forms DNA cross-links, resulting in
inhibition of DNA synthesis and
function, Cell-cycle nonspecific ;
component of regimen For testicular
cancer, ovarian cancer, bladder
cancer and lung cancer ; Oxaliplatin
is used also for advanced colon CA
Forms DNA cross-links, resulting in
inhibition of DNA synthesis and
function, Cell-cycle nonspecific ; For
CML
Forms DNA cross-links, resulting in
inhibition of DNA synthesis and
function, Cell-cycle nonspecific ; For
brain tumors, melanoma, skin
cancer
a reactive agent which forms
hydrogen peroxide, which generates
free radicals that cause DNA strand
scission, cell cycle non-specific ;
component of reigned For Hodgkins
lymphoma, non-hodgkins
lymphoma, brain tumors
all are cell-cycle specific , they also
have immunosuppressant action
Inhibits dihydrofolate reductase,
decreases synthesis of thymidylate,
amino acids, purine nucleotides >
interfere with NA and CHON
metabolism ; cell cycle specific ; For
choriocarcinoma, acute leukemia,
non-hodgkin, primary CNS
lymphoma, breast cancer, head and
neck cancer, bladder cancer ; also
for psoriasis, rheumatoid arthritis,
ectopic pregnancy
are activated by hypoxanthie-
guanine phosphoribosyltransferase
(HGPRT) to toxic nucleotides which
inhibit enzymes in purine
metabolism > Inhibits de novo
purine nucleotide synthesis , cell
cycle specific ; For acute leukemia
(AML, ALL), CML
converted to 5-fluoro-2-
deoxyuridine-5-monophosphate (5-
FdUMP) which Inhibits thymidylate
synthase, incorporation inhibits
DNA synthesis and function, cell
cycle specific ; For bladder cancer,
breast cancer, colorectal cancer,
anal cancer, head and neck cancer,
liver cancer and ovarian cancer,
topically for keratoses and
superficial basal cell skin cancer
a cytosine arabinoside, activated by
kinases to Ara-Cytidine Triphosphate
(AraCTP) which Inhibits DNA
polymerase > inhibition of DNA
synthesis and repair, inhibits
cardiac dysfunction ;
Mechorethamine SE include marked
vesicant action, sterility,
myelosuppresion, alopecia
nausea, vomiting, nephrotoxicity,
neurotoxicity (peripheral neuritis),
ototoxicity (acoustic nerve damage),
hematotoxicity
pulmonary fibrosis, adrenal
insufficiency, skin pigmentation
CNS toxicity (dizziness, ataxia),
nausea and vomiting, bone marrow
suppression, skin flushing
bone marrow suppression,
pulmonary toxicity, hemolysis,
disulfiram reaction,skin reactions,
peripheral neuropathy, CNS
dysfunction
bone marrow suppression,
pulmonary infiltrates and fibrosis,
mucositis, crystalluria, hepatotoxic
bone marrow suppression, hepatic
dysfunction (necrosis, jaundice,
cholestasis)
bone marrow suppression, GI
irritation, alopecia
GI irritation, bone marrow
suppression, neurotoxicity
Cyclophosphamides anti-cancer
effect and also its toxicity
IV, Rescue therapy is Amifostine,
decreased nephrotoxicity by giving
mannitol with forced hydration ;
Carboplatin is less nephrotoxic but
has more myelosuppression
Spares the bone marrow
Highly lipophilic allowing ease of
passage through BBB into the CNS
PO, can pemetrate the CSF,
LEUKEMOGENIC, CPY450 inhibitor,
Dacarbazine is phototoxic
PO, IV, Rescue therapy is Leucovorin
(Folinic acid) ; cytotoxic due to
formation of polyglutamate
derivatives ; resistance is due to
decreased drug accumulation,
changes in drug sensitivity or activity
of DHF reductase and decreased
formation of polyglutamates ;
clearance is dependent on renal
function therefore adequate
hydration is important to prevent
crystallization into stones
6-MP metabolism inhibited by
allopurinol and febuxostat ,
Resistance is due to decreased
activity of HGPRT, increased alkaline
phosphatase activity (which
inactivates the toxic nucleotide) ,
undergo significant FPE (by xanthine
oxidase)
IV, can distribute to CSF, causes
thymineless death of cells,
Resistance is due to decreased
activation of 5-FU, increase
thymidylate synthase activity and
decreased sensitivity of this enzyme
; another metabolite is 5-
florouridine-5triphosphate (FUTP)
which incorporates into RNA >
interfere with RNA processing and
function
Most specific for the S-phase of the
cell cycle, Resistance is due to
decreased uptake and decreased
conversion to AraCTP, a cytosine
arabinoside
Page 50 of 56

v. Pyrimidine antagonist:
Gemcitabine
C. Natural Anticancer Drugs
i. Vinca alkaloid: Vincristine,
Vinblastine, Vinorelbine
ii. Podophyllotoxin: Etoposide,
Teniposide
iii. Camptothecins: Topotecan,
Irinotecan
iv. Taxanes: Paclitaxel, Docetaxel
Docetaxel (neurotoxicity, bone
marrow suppression)"
D. Antitumor antibiotics
i. Anthracycline: Doxorubicin,
Daunorubicin, Idarubicin,
Epirubicin, Mitoxantrone
ribonucleotide reductase with
reduced formation of dNTPs, cell
cycle specific ; For AML, ALL, CML
a deoxycytidine analog, converted to
Gemcitabine diphosphate which
inhibits ribonucleotide reductase
with reduced formation of
deoxyribonucleotide triphosphate
required for DNA synthesis, bone marrow suppression,
a deoxycytidine analog
Gemcitabine triphosphate is neutropenia, pulmonary toxicity
incorporated into DNA causing chain
termination, cell cycle specific ; For
pancreatic cancer, bladder cancer,
non-small cell lung cancer, non-
Hodgkins lymphoma
all are cell-cycle specific
Prevents assembly of tubulin dimers
into microtubule assembly blocking
the formation of mitotic spindles,
causes cell arrest at metaphase, cell IV, highly distributed except in CSF,
cycle specific ; For acute leukemias, Acts primarily in M phase of cancer
Neurotixicity (areflexia, peripheral
lymphomas, wilms tumor and cell cycle, Resistance is due to
neuritis, paralytic ileus)
neuroblastoma ; Vinblastine For increased efflux of drugs via
lymphomas, neuroblastomas, membrane drug transporter
testicular carcinoma and Kaposi
sarcoma ; Vinorelbine For non-small
cell lung cancer and breast cancer
Induces DNA breakage by inhibiting
DNA topoisomerase II, inhibits
mitochondrial electron transport,
PO, high Vd ; dose adjustment in
cell cycle specific ; Combination bone marrow suppression, alopecia,
renal patients ; Act on the Late S and
regimen For lung cancer, prostate GI distress
early G2 phase
cancer, testicular cancer, non-
hodgkins lymphoma, germ cell and
gastric cancer
Inhibits DNA topoisomerase I which
cute and relegates single DNA
strands during normal DNA repair,
Irinotecan can be used for
cell cycle specific; For advanced bone marrow suppression, diarrhea
metastatic colorectal cancer
ovarian cancer (2nd line), small cell
lung cancer, Irinotecan For
metastatic colorectal cancer
Interferes with mitotic spindle
synthesis by preventing microtubule
disassembly into tubulin monomers,
"Paclitaxel (neutropenia,
cell cycle specific ; For solid tumors -
thrombocytopenia, peripheral
advanced breast and ovarian cancer,
neuropathy, hypersensitivity),
lung cancer, gastroesophageal
cancer, prostate cancer, bladder
cancer, head and neck cancer
Act on M phase
Intercalates between base pairs,
inhibits topoisomerase II, generates
free radicals, blocks synthesis of
RNA and DNA causing DNA strand
scission, causes membrane
disruption, cell cycle non-specific ; alopecia, nausea, vomiting,
Rescue therapy is Dexrazoxane and
Doxorubicin For Hodgkins and Non- Cardiotoxicity (dilated
liposomal formulation of the drug
Hodgkins lumphoma, myelomas, cardiomyopathy, CHF)
sarcomas, breast cancer,
endometrial cancer, lung cancer,
ovarian cancer and thyroid cancer ;
Daunorubicin For acute leukemias
Idarubicin For AML, Epirubicin For
Page 51 of 56

ii. Bleomycin
iii. Actinomycin D
iv. Mitomycin C
E. Miscellaneous Anticancer Drugs
i. TK inhibitor: Imatinib, Dasatinib,
Nilotinib
ii. Growth Factor Receptor
Inhibitor
a. Her-2-neu inhibitor:
Trastuzumab
b. EGFR inhibitor: Cetuximab,
Panitumumab, Gefitinib, Erlotinib
c. VEGF Inhibitor: Bevacizumab,
Sorafenib, Sunitinib, Pazopanib
iv. Rituximab
breast cancer and gastroesophageal
; Mitoxantrine For acute myeloid
leukemias, Non-Hodgkins
lymphoma, breast and
gastroesophageal cancer
Generated free radicals which bind
to DNA and causes DNA strand
breaks leading to inhibition of DNA
IV, inactivated by tissue
synthesis, intercalates with DNA, cell pneumonitis, pulmonary fibrosis,
aminopeptidases, Most specific for
cycle specific ; Component of alopecia, mucocutaneous reactions,
the G2 phase of cell cycle, a
regimens in Hodgkins lymphoma hypersensitivity reactions
glycopeptide
and testicular cancer, lymphomas
and squamous cell cancer, head and
neck cancer, skin cancer
Binds to double stranded DNA,
inhibits DNA-dependent RNA
bone marrow suppression, skin
synthesis, cell cycle non-specific ; None
reactions, GI irritation
For melanoma, wilms tumor,
choriocarcinoma, Kaposi sarcoma
Metabolized into an alkylating agent
that cross-links DNA ; In
severe myelosuppression, toxic the
combination regimens for IV, used for hypoxic tumor cells
heart, liver, lungs and kidneys
adenocarcinoma of the cervix,
stomach, pancreas and lungs
Tyrosine kinase inhibitor of the
diarrhea, myalgia, fluid retention, Resistance is due to mutation is bcr-
protein product of bcr-abl oncogene
CHF abl gene
in CML ; For CML, GIST
recognizes a surface protein in
breast CA cells that overexpress Her- nausea, vomiting, chills, fever,
None
2-neu receptors for epidermal headache, cardiotoxicity (CHF)
growth factor
EGFR (Epidermal Growth Factor
Receptor) regulate signaling
involved in cellular proliferation,
invasion and metastasis and
angiogenesis, it also inhibits
cytotoxic activity of some anti-
cancer and radiation treatment,
Gefitinib and Erlotinib are capable of folliculitis, diffuse hair loss, dry skin, Erlotinib can also be used for
inhibiting EGFRs Tyrosine Kinase paronychia advanced pancreatic cancer
domain ; Cetuximab (+ Irinotecan
and Oxalipatin) For metastatic colon
cancer and Head and Neck cancer ;
Panitumumab For refractory
colorectal cancer ; Gefitinib and
Erlotinib as second-line agents for
non-small cell lung cancer
VEGF (Vascular Endothelial Growth
Factor) has a role in angiogenesis
required for metastasis, Inhibits
binding of VEGF to VEGFR leading to
inhibition of VEGF signalling, inhibits
tumor vascular permeability but hypertension, arterial thrombosis,
may also be used in non-small cell
enhances tumor blood flow and impaired wound healing,
lung CA and renal CA
drug delivery ; Sorefenib Sunitinib proteinuria, GI perforation
and Pazopanib inhibits multiple
receptor Tyrosine Kinase including
those associated to VEGF ; For
metastatic colorectal cancer, breast
cancer, diabetic retinopathy
Binds to a surface protein in NHL
hypersensitivity reaction, bone
cells, induces complement-mediated None
marrow suppression
lysis, direct cytotoxicity and
Page 52 of 56

v. Interferon alpha
vi. Asparaginase
vii. All-Trans retinoic acid
viii. Protease Inhibitor:
Bortezomib
F. Hormonal Anticancer Agents
i. Prednisone
ii. SERM: Tamoxifen, Toremifene
iii. Androgen antagonist:
Flutamide
iv. GnRH analog: Leuprolide,
Goserelin Nafarelin
v. Aromatase inhibitor:
Anastrazole, Letrozole
induction of apoptosis ; For Non-
Hodgkins lymphoma and other
lymphomas
Endogenous glycoproteins with
antineoplastic, immunosuppressive
and antiviral actions ; For hairy cell
leukemia, early CML, T-cell
lymphoma
Depletes serum asparagine ; For ALL,
T-cell auxotrophic CA (leukemia and
lymphomas) that require asparagine
for growth
Allows DNA transcription and
differentiation of immature
leukemic promyelocytes into mature
granulocytes ; For acute
promyelocytic leukemia
a reversible inhibitor of 26s
proteasome in mammalian cell ; For
multiple myeloma
Suppresses inflammation and
immune response, may trigger
apoptosis and work on nondividing
cancer cells ; For CLL, Hodgkins
lymphoma, leukemia, lymphoma
Estrogen antagonist actions in
breasts tissue and CNS, estrogen
agonist effects in uterus, liver and
bone ; For hormone-responsive
breast cancer, Toremifene For
advanced breast cancer
Androgen antagonist ; For prostate
cancer
Increased LH, FSH secretion with
intermittent administration,
reduced LH and FSH secretion with
prolonged continuous
administration ; For prostate cancer
Reduces estrogen synthesis by
inhibiting aromatase; For advanced
breast cancer
alopecia, myalgia, depression,
thyroid dysfunction, hearing loss, None
bone marrow suppression
acute pancreatitis, bleeding, severe
None
hypersensitivity reaction
retinoic acid syndrome (dyspnea, Only vitamin that can cure cancer,
fever, weight gain, peripheral treat retinoic acid syndrome with
edema) dexamethasone
peripheral neuropathy,
thrombocytoppenia
adrenal suppression, growth
inhibition, muscle wasting, see entry
osteoporosis, salt retention
hot flushes, thromboembolism,
Prevents osteoporosis and decrease
endometrial hyperplasia,
risk of atherosclerosis
endometrial cancer
GnRH analogs (leuprolide) must be
gynecomastia, hot flushes,
co-administered to prevent acute
impotence
flare-up of prostate cancer
hot flushes, sweats, headache,
osteoporosis, gynecomastia,
see entry
gynecomastia, testicular atrophy,
impotence, bone pain
nausea, diarrhea, hot flushes, bone
Effective againsts breast cancer that
and back pain, dyspnea, peripheral
have become resistant to tamoxifen
edema

Drugs Used in the Treatment of Gastrointestinal Diseases [Divided into 2 classes: agents that reduce intragastric acidity and
agents that promote mucosal defense
Neutralize stomach acid by reacting
A. Antacids: Magnesium-Aluminum
with protons in the lumen ; For
Hydroxide, Calcium carbonate,
peptic ulcer disease,
Sodium bicarbonate
Gastroesophagal reflux
Competitive pharmacologic block of
B. H2 receptor antagonist:
H2 receptors ; For peptic ulcer
Cimetidine, Ranitidine, Famotidine,
disease, Zollinger-Ellison syndrome,
Nizatidine
Gastroesophagal reflux, dyspepsia
Sodium bicarbonate: Belching,
metabolic alkalosis. Calcium
carbonate: hypercalcemia, renal
insufficiency, metabolic alkalosis
(milk-alkali syndrome) exc for
Aluminum Magnesium Hydroxide
Gynecomastia (cimetidine only),
Diarrhea, headache, fatigue,
Myalgias, constipation, Nosocomial
pneumonia, Mental status changes,
Bradycardia, Hypotension, Blood
dyscrasias
Impairs absorption of tetracyclines,
flouroquinolones,itraconazole and
iron --> should not be given within 2
hours with these drugs ; When used
regularly in large doses needed to
significantly raise the stomach pH,
antacids, decrease recurrence rate
of peptic ulcers ; Aluminum and
Magnesium are always given
together to cancel out each other's
adverse effects ; Avoid in renally
impaired patients ; DOA: 1-2 hours
Cimetidine is a potent inhibitor of
CYP450. Highly effective in
suppressing nocturnal acid secretion
but only modest effect on meal-
stimulated secretion ; avoid in
renally and hepatically (severe)
impaired patients ; are highly

Page 53 of 56

C. Proton Pump Inhibitor:
Omeprazole, Lansopraole,
Rabeprazole, Pantoprazole,
Esomeprazole
D. Mucosal Protective Agent:
i. Sucralfate
ii. Bismuth Salicylate
iii. Misoprostol
E. Prokinetics
i. Metoclopramide, Domperidone,
Erythromycin, Neostigmine
F. Laxatives
i. Bulk-forming: Psyllium,
Methylcellulose, Polycarbophil
ii. Stool-softener: Docusate,
Glycerine, Mineral oil
iii. Osmotic: Lactulose,
Magnesium oxide, Magnesium
hydroxide, Sorbitol, Magnesium
citrate, Sodium phosphate,
Polyethylene Glycol
selective and does not affect H1 and
H3 receptors, may also reduce
seceretion of pepsin ; DOA: 6-10hrs ;
Reduces acid secretion by 60-70%
usually enetric coated, t1/2 is 1-2hrs
but DOA of is around 24hrs, needs 3-
4 days treatment to achieve full
Irreversible blockade of H/K ATPase
effectiveness ; decreases
in active gastric parietal cells, Long Diarrhea, headache, abdominal pain,
bioavailability drugs that require
lasting reduction of meal stimulated Malabsorption syndrome (Vit B12,
acidity for GI absorption ; when used
and nocturnal acid secretion ; For Ca, Fe, Zn, Digoxin, Ketoconazole),
for PUD together with 2 antibiotics,
Peptic ulcer disease(DOC), Zollinger- Infections (respiratory, enteric),
achieve 90% cure ; Reduces acid
Ellison syndrome, Gastroesophageal Hypergastrinemia, Atrophic gastritis
secretion by 90-98% ; should be
reflux, dyspepsia
taken on an empty stomach since
food decreases its bioavailability by
50%
polymerizes in acidic environmet
> polymers bind to injured tissue
and forms a protective covering over Highly insoluble, requiring frequent
constipation, dizziness, flatulence,
ulcer bed, Accelerates healing of dosing (QID) ; chemically: Aluminum
dry mouth
peptic ulcers and reduces Sucrose Sulfate
recurrence rate ; For Peptic ulcer
disease
forms a protective coating on
ulcerated tissue, stimulates mucosal
protective mechanisms, direct Black stools, darkening of tongue,
Reduces stool frequency and
antimicrobial effects and Encephalopathy (Atraxia,
liquidity in infectious diarrhea
sequestration of enterotoxins ; For headaches, confusion, seizures)
Peptic ulcer disease, Dyspepsia,
Infectious diarrhea
PGE1 analog, Activates EP receptors,
causes increased HCO3 and mucus
secretion and inhibits acid secretion
in the stomach, causes uterine Abdominal pain, Diarrhea, Uterine see entry, decreases ulcer in NSAIDs
contraction ; For Peptic ulcer cramping, Miscarriage induced ulceration
disease, Prevention of NSAID-
induced gastric mucosal injury,
Abortifacient
Metoclopramide and domperidone
block D2 receptors, Erythromycin
stimulates motilin receptor,
Increases gastric emptying and Domperidone does not cross the
Parkinsonism, Extrapyramidal
intestinal motility ; As Antiemetic for BBB (less toxic) ; Increases LES
effects, Hyperprolactinemia
post operative/chemotherapy pressure (helpful in GERD)
vomiting, Diabetic gastroparesis
(drug of choice), Neostigmine for
acute large bowel distention
Indigestible, hydrophilic colloids that
absorb water, forming a bulky
emollient gel that distends the colon Diarrhea None
and promotes peristasis ; For
constipation
Soften stool material, Permitting Diarrhea, Aspiration,(Lipid
water and lipids to penetrate the pneumonitis), Malaabsorption of None
stool ; For constipation fat-soluble vitamins (A, D, E, K)
Soluble but nonabsorbable
compound that result in increased
Diarrhea, Flatus, Abominal cramps,
stool liquidity due to an obligate
Electrolyte abnormalities
increase in fecal fluid ; For
(hyperphosphatemia, hypocalcemia, None
Constipation, Hepatic
hypernatremia, hypokalemia,
encephalopathy (lactulose),
hypermagnesemia)
Preparation for endoscopy
(polyethylene glycol)
Page 54 of 56

iv. Stimulant: Bisacodyl, Aloe,
Senna, Cascara, Castor oil
v. Miscellaneous: Lubiprostone,
Methylnaltrexone, Alvimopan
G. Anti-diarrheals: Diphenoxylate,
Loperamide, Kaolin+Pectin,
Colloidal Bismuth
H. Drugs for IBS
i. laxatives, antidiarrheals and
low-dose TCA
ii. Anticholinergics: Dicylomine,
Hyoscyamine
iii. 5HT3 antagonist: Alosteron
iv. Lubiprostone
I. Anti-emetics
i. Ondansetron, Granisetron,
Dolasetron, Palonosetron
ii. Aprepitant
iii. Scopoloamine
J. Drugs for IBD
i. Aminosalicylates: Mesalamine,
Balsalazine, Olsalazine,
Sulfasalazine
ii. Other agents: Antibiotics,
Immunosuppressibe
antimetabolites (Azathioprine, 6-
MP, Methotrexate), anti-TNF
(Infliximab), Natalizumab
K. Miscellaneous Agents
i. Pancreatic lipase: Pancreatin or
Pancrealipase
ii. Drugs that inhibit formation of
Gallstones: Ursodiol
Unknown. Directly stimulate enteric
nervous system and colonic Diarrhea can cause melanosis coli
electrolyte and fluid secretion
Lubiprostone is a Chloride channel
activator which stimulates Cl
secretion into the intestines leading
to increased fecal fluid content, mild nausea, stomach pain, mild
NONE
Methylnaltrexone and Alvimopan diarrhoea, bloating, headache
are Opioid receptor antagonist that
block intestinal mu receptors, but
not the CNS
Activates opioid receptors in enteric
Do not use in children less than 4
nervous system. Slows motility with
years of age (increased chance of
negligible CNS effects, Kaolin Drowsiness, Nausea, Paralytic ileus,
causing paralytic ileus), Reverse ileus
(+pectin) absorbs bacterial toxin and interfere with absorption of other
by administering Betanechol. Direct
fluid leading to decreased stool drugs
m-agonist, Kaolin is hydrated
liquidity ; for Diarrhea (nonspecific,
Magnesium Aluminum Silicate
noninfectious)
see entry see entry see entry
see entry ; antispasmodic for
abdominal pain, for IBS with see entry see entry
prominent diarrhoea
see entry ; For IBS with severe
severe constipation, ischemic colitis see entry
diarrhoea
see entry ; activate type2 chloride
channels in small intestines ; For IBS see entry see entry
with predominant constipation
Blocks chemoreceptor trigger zone
Headache, Dizziness, Constipation,
and enteric nervous system 5-HT3
QRS and QT prolongation see entry
receptors ; For Vomiting (Post
(Dolasetron only)
chemothereaphy, postoperative)
antagonist of the Neurokinin-1
receptor in the areas postrema that
is activated by substance P and fatigue, dizziness, diarrhea an enzyme inhibitor
other tackykinins ; For post-
chemotherapy nausea and vomiting
see entry ; For motion sickness
see entry see entry
emesis
Unknown. Probably inhibits
production of eicosanoid Gastrointestinal upset,Headaches,
inflammatory mediators (PG and LT) Arthralgias, Myalgias, Bone marrow Not useful for treating active flare
and interfering with cytokines ; For suppression, Malaise, ups of disease
Inflammatory bowel disease (mild to Hypersensitivity reactions ( severe)
moderate)
see entry ; Natalizumab is a Mab
that blocks intergrins in circulating
multifocal leukoencephalopathy see entry
leukocytes, restricted to severe
refractory Crohns disease
For pancreatic enzyme replacement,
improve digestion of fats proteins
and carbohydrates ; For pancreatic hyperuricemia Taken with every meal
insufficiency due to Cystic Fibrosis,
pancreatitis and pancreatectomy
a bile acid derivative that decreases
cholesterol content of bile by
decreasing hepatic cholesterol headache, dizziness, mild stomach
secretion and other effects on pain, rhinorrhea, sore throat, rash None
hepatocyte canalicular membrane ; hair loss
For gallstone in patients refusing or
not eligible for surgery
Page 55 of 56
Drugs Used For Cough
A. Mucolytics : N-acetylcysteine,
Carbocysteine, Ambroxol
B. Expectorants: Guiafenesin
C. Antitussives
i. Centrally-acting: Opioid
antitussives (codeine,
dextromethorphan)
ii. Centrally-acting: Non-opioid
(butamirate citrate)
iii. Peripherally-acting:
Levodropropizine
decrease sputum activity ; Usually
derivatives of cysteine; reduce
disulfide bridges that bind
glycoproteins to other proteins such
as albumin ; Also act as antioxidants
& may reduce airway inflammation ;
Orally available drugs are well-
tolerated; but of little benefit in
acute respiratory condition
may act as an irritant to gastric vagal
receptors, and recruit efferent
parasympathetic reflexes that cause
glandular exocytosis of a less viscous
mucus mixture.
Used for dry painful cough of
neoplasia or pleural disease ;
Irritative cough in inflammation of
the respiratory tract (epiglottitis); in
hemoptysis
decreased sensitivity of the
medullary/ CNS cough centers to
peripheral stimuli and decreased
mucosal secretion
act through receptors in the
brainstem to inhibit cough
Non-opoid drug with a peripheral
action by inhibiting the afferent
pathways that generate the cough
reflex (modulates C-fibre activity)
Chest tightness, Disagreeable odor,
Drowsiness, Fever, Hemoptysis,
Increased volume of bronchial
secretions, Irritation of tracheal or
bronchial tract, Nausea, Rhinorrhea,
Stomatitis, Vomiting"
Drowsiness, Incomplete or
Infrequent Bowel Movements,
Inducing of a Relaxed Easy State,
Stomach Cramps, dizziness or
headache, a rash, or. nausea,
vomiting, or stomach upset
Decreases secretions in the
bronchioles, thickens sputum &
inhibits ciliary activity, reducing
clearance of thickened sputum,
Constipation
Somnolence, nausea, vomiting,
diarrhea, dizziness and hypotension
Nausea, vomiting, heartburn,
diarrhea, fatigue, weakness,
drowsiness, dizziness, headache,
palpitations
available as IV, PO, IM and
inhalational forms
Are often emetics (ipecac,
guaifenesin)
DO NOT suppress in bacterial lung
infections, asthma, bronchiectasis
(suppurating bronchial
inflammation) or chronic bronchitis
where antitussives can cause
harmful sputum thickening &
retention
Morphine may be effective but
indicated only in intractable cough
from bronchial carcinoma ;
Dextromethorphan has no addictive
potential, no analgesic effect,
produces less constipation and
inhibition of mucociliary clearance
Centrally acting antitussive but is
neither chemically or
pharmacologically related to opioids
does not cause side effects such as
constipation or respiratory
depression which can be produced
by opioid antitussives
Page 56 of 56