Escolar Documentos
Profissional Documentos
Cultura Documentos
Eicosanoids
NSAIDs
Immunopharmacology
Adrenergic Agonists
Adrenergic Antagonists
PsNS Agents
Anti-Hypertensives
Antibiotics
Cancer Drugs
Movement Disorders
Anti-Convulsants
Anxiolytics
Anti-Psychotics
Anti-Depressants
Alcoholism
Opioids
General Anesthetics
Local Anesthetics
GI Drugs
Anti-Virals
Anti-Virals: HIV
Anti-Arrhythmics
Cardiotonics
Diuretics
Alternative Medications
Pituitary Hormones
Estrogens/Progestins
Thyroid/Parathyroid/Adrenal Hormones
Anti-Malarials
Anti-Parasitics
Pulmonary Drugs
Caloric Regulation
Diabetes Drugs
Lipid Drugs
Dermatology Drugs
Gout Drugs
S. Carr
Drug
Eye
Clotting
PGI
PGE1
PGE2
PGF2
plt aggregation
intraocular
pressure
intraocular
pressure
intraocular
pressure
TXA
plt aggregation
plt aggregation
plt aggregation
LTC
LTD
Epoprostenol (PGI)
Treprostinil
Misoprostol
(PGE1)
Alprostadil
(PGE1)
Dinoprostone
(PGE2)
Latanoprost
(PDF2 )
Carboprost
(PGF2 )
Zileuton
(lipoxygenase)
Zafirlukast (LTR)
Montelukast
Indomethacin
(COX inh.)
Vasculature
Lungs
GI
vasodilation
( cAMP)
vasodilation
( cAMP)
vasodil + vasocx
( IP3 & Ca2+)
vasocx
( IP3 & Ca2+)
vasocx
( IP3 & Ca2+)
permeability
( BP)
permeability
( BP)
vasodilation
( cAMP)
bronchodilation
( cAMP)
bronchodilation
( cAMP)
bronchodilation
( cAMP)
bronchocx
( IP3 & Ca2+)
bronchocx
( IP3 & Ca2+)
bronchocx
( IP3 & Ca2+)
bronchocx
( IP3 & Ca2+)
acid, mucus,
blood
acid, mucus,
blood
acid, mucus,
blood
tone
(+ oxy CX)
CX
( oxytocin)
body temp
NE
body temp
NE
acid, mucus,
blood
Dinoprostone
Kidney: blood
CX
( oxytocin)
bronchodilation
(blocks LT synth)
bronchodilation
(blocks LT synth)
Treats
Primary pulmonary
HTN
Misoprostol
Alprostadil
Latanoprost
Carboprost
CX
( oxytocin)
vasocx
( PG synth)
CNS
Zileuton
Zafirlukast
Montelukast
tone
CX
tone
Organs
Kidney: blood,
diuresis
Kidney: blood,
diuresis, ADH
Kidney: blood,
diuresis, ADH
Reproductive
CX
( oxytocin)
Primary pulmonary
HTN
NSAID-ulcer
Abortifacient
Impotence
Maintain PDA
Abortifacient
Labor induction
Open angle
glaucoma
Abortifacient
(inhibits leukotrienes)
Asthma
Asthma
Close PDA
Drug
Inhibits
Aspirin
COX-1
COX-2
Non-acetylated
COX-1
COX-2
salicylates
Ibuprofen
Diclofenac
Etodolac
Indomethacin
Ketoprofen
Naproxen
Sulindac
Celecoxib
Rofecoxib
Valdecoxib
Acetaminophen
NSAID Effects
NSAID Side Effects
Metabolism
Duration
Side Effects
Treats
Low = 15 min
High = 4 h
High = 13 h
RA
Chronic inflm
RA
Chronic inflm
COX-1
COX-2
Liver
CYP2C8
Short
(2hr)
RA
Chronic inflm
COX-1
COX-2
Liver
CYP3A4
CYP2C9
Short
(2hr)
Typical NSAID
RA
Chronic inflm
Intermediate
(5 hr)
Less GI
RA
Chronic inflm
RA
Chronic inflm
COX-1
COX-2
COX-1
COX-2
COX-1
COX-2
1) Short (2 hr)
2) Slow release
Typical NSAID
RA
Chronic inflm
COX-1
COX-2
Long
(12 hr)
Typical NSAID
RA
Chronic inflm
COX-1
COX-2
Long
(12 hr)
1) serum aminotransferases
2) Treats familial intestinal polyposis
RA
Chronic inflm
COX-2
RA
Chronic inflm
COX-2
RA
Chronic inflm
COX-1
COX-2
RA
Chronic inflm
Analgesia
(low grade pain)
Anti-pyretic
(PG inhibition)
Anti-inflamatory
(MSK, RA, OA)
Anti-coagulant
(other NSAIDs can block long-lasting ASA)
COX-2 Pro-coagulant
( COX-2 PGI but not COX-1 TXA)
GI irritation
(ASA espclly)
bleeding time
(inhib. TXA)
Kidney effects
Pregnancy
(delayed onset of labor from PGE & PGF)
Hypersensitivity
( COX arachidonate lipoxygenase)
Drug
Cytotoxic
T-cell Inhibitor
Prednisone
Prednisolone
Cyclosporine
Tacrolimus
Sirolimus
Azathioprine
Mycophenolate
FTY720
Antithymocyte Ig
Immunoglobulins
Immune globulin
Anti-CD3 Ig
Basiliximab
Daclizumab
Infliximab
Etanercept
Rho Immune Ig
Bacillis CalmetteGuerin
Thymic Factors
Interleukin-2
GM-CSF
G-CSF
Action
Response
Treats
Down-regulate inflammation
Immunosuppression
Anti-inflammatory
T-cell response
Converted to thioinosinate
Myelosuppression
Coadministration w/allopurinol is toxic
Transplant rejection
Rheumatoid arthritis
Transplant rejection
Transplant rejection
Ig against T-cells
Human plasma Ig
Replaces missing Ig
Immunodeficiencies
Lymphocytic leukemia
Kawasake disease
Transplant rejection
Ig against TNF-
Rheumatoid arthritis
Crohn's disease
Bladder cancer
SCID
Natural cytokine
AIDS
Cancer
WBC recovery
in pts with hematopoiesis
Natural cytokine
Cancer
Congenital
Autoimmune disease
Transplantation inflm
Hypersensitivity
GVHD (bone marrow trxpnt)
Aplastic anemia (ineligible)
Autoimmune disease
Transplant rejection
GVHD
Autoimmune disease
Drug
Epinephrine
Phenylephrine
Levarterenol
Norepinephrine
Dopamine
Amphetamine
Arbutamine
-methyl-DOPA
Tyramine
Guanethidine
Ephedrine
Clonidine
Brimonidine
Tizanidine
Isoproterenol
Dobutamine
Metaproterenol
Salmeterol
Formoterol
Terbutaline
Albuterol
Receptors
Heart
Vasculature
1 [high]
2 [high]
1 [low]
2 [low]
1
Reflex bradycardia
DBP ( MSK)
HR, CX, CO
GI
mucus congestion
SBP (indirect)
DBP ( MSK)
Reflex bradycardia
Lungs
Treats
Eye: intraocular
pressure
Metabolism:
Asthma
Anaphylaxis
Cardiac arrest
uterine CX
ACh (2A)
motility
bronchodilation
Organs
Reproductive
motility
uterine CX
Nasal deconges.
1
2
1
D1 [low]
1 [high]
1 [ high]
Reflex bradycardia
DBP (vasocx)
HR, CX, CO
SBP (indirect)
HR, CX, CO
SBP (indirect)
Shock
Kidney: renin
vasodilation
Kidney: renin
DBP (vasocx)
1) displaces NE from vesicles.2) competitively inhibts NE reuptake.3) inhibits MAO activity NE lingers
1
1
2
1
2
1
1
1
2
1
HR, CX, CO
SBP (indirect)
Narcolepsy
Kidney: renin
1) shock caused by
CO & renal fxn
2) Parkinson's
(Experimental)
HTN during
pregnancy
SNS outflow
BP
Reflex bradycardia
DBP (vasocx)
HR, CX, CO
SBP (indirect)
Kidney: renin
1) displaces NE from vesicles.2) competitively inhibts NE reuptake.3) inhibits MAO activity NE lingers (acts like amphetamine)
2
2
2
1
2
1 [high]
1 [low]
2
2
2
2
2
SNS outflow
SNS outflow
SNS outflow
BP
BP
HTN
humor production & uveoscleral outflow
OA glaucoma
MSK spasticity
HR, CX, CO
SBP (indirect)
cardiac efficiency
DBP vasodilation
cardiac efficiency
DBP (vasocx)
HR, CX, CO
SBP (indirect)
Multiple sclerosis
Kidney: renin
bronchodilation
motility
Kidney: renin
Bronchodilator
Cardiac arrest
Decompensated
heart failure
M = medium
bronchodilation
Bronchospasm
bronchodilation
Bronchospasm
Bronchospasm
F = fast
bronchodilation
T = tachycardia
bronchodilation
Minimal tachycardia
Bronchospasm
A = acute
bronchodilation
Bronchospasm
Drug
Receptors
-methyl-paratyrosine
Reserpine
binds VMAT-2 irreversibly inhibits vesicular concentration of NE & DA transient at receptors SNS depletion
Cocaine
reversibly inhibits NET & DAT (CNS) anesthetic, CNS stimulant, sympathomimetic
Phenoxybenzamine
Carvedilol
Heart
Anti 1
Reflex tachycardia
Anti 2
SNS outflow
Vasculature
Lungs
GI
Reproductive
Organs
vasocx
Treats
Pheochromocytoma
Anti 1
Anti 1
Heart failure
Anti 2
Prazosin
Tamsulosin
Anti 1
Reflex tachycardia
vasocx
Anti 2B
Reflex tachycardia
vasocx
Anti 1A
Reflex tachycardia
vasocx
Alfuzosin
Anti 1
Yohimbine
Anti 2
Propranolol
Anti 1
Anti 1 [low]
Hypertension
HR, CX, CO
SBP
Kidney: renin
bronchocx
HR, CX, CO
SBP
Kidney: renin
Anti 1
HR, CX, CO
SBP
Acebutolol
Anti 1
HR, CX, CO
SBP
Timolol
Anti 1
HR, CX, CO
SBP
Anti 2
Anti 1
Kidney: renin
Hypertension
HR, CX, CO
SBP
Hypertension
Hypertension
Kidney: renin
bronchocx
Anti 2
Sotalol
Hypertension
Migraine
bronchocx
Atenolol
Anti 1
BPH
Male impotence
Anti 2 [high]
Labetalol
Hypertension
BPH
smooth muscle RX
Anti 2
Metoprolol
smooth muscle RX
Kidney: renin
Open angle
glaucoma
Hypertension
bronchocx
HR, CX, CO
SBP
Anti 2
Kidney: renin
Arrhythmia
Atrial fibrillation
Carbachol
ACh musc Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Pilocarpine
ACh musc Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Physostigmine
AChE inhib Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Echothiophate
AChE inhib Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Brimonidine
Latanoprost
2
PDF2
OA glaucoma
OA glaucoma
Cholinomimetics
Drug
Bethanechol
Carbachol
Pilocarpine
Parasympathetic Antagonists
Atropine
Scopalamine
Heart
Vasculature
Lungs
GI
GU
Organs
Treats
Choline Ester
PsNS agonist
M1, M2, M3
M2
[Lo] = reflx tach
[Hi] = AV block
M3
vasodil (B & C)
secretions
bronchoCX
M1
motility (B)
secretions
M1
Detrussor CX
(B & C)
Eye : M1
Circular M. CX
Ciliary M. CX
C: OA glaucma
B: GI/GU retentn
Natural alkaloid
M1, M2, M3
Muscarinic blockade
(M1, M2, M3)
Muscarinic blockade
(M1, M2, M3)
Pirenzepine
M1 antagonist
Tolterodine
Trospium
Oxybutynin
Anti-muscarinic
Ipratropium
Tiotropium
Edrophonium
Physostigmine
Neostigmine
Cholinesterase Inhibitors
Mechanism
M3 (ant)
vasocx
secretions
bronchodil
M1 (ant)
motility
secretions
M1 (ant)
Detrussor RX
Urine retention
Eye: M1 (ant)
Circular M. RX
Ciliary M. RX
Used w/H-2 blockers to reduce gastric acid secretion to promote gastric ulcer healing
Reversible ChE
inhibitor (competitive)
Physo : block nACh?
DFP
Irreversible ChE
inhibitor
(phosphorylate ChE)
GI spasms
Eye exams
ChEI toxicity
Anesth adjunct
Motion sickness
Overax bladder
Gastric ulcer
Overactive
bladder
secretions
bronchodil
COPD
Reversible ChE
inhibitor
Diagnosis of MG
PAT
Direct:
M2
HR
Indirect:
M3
vasodil
reflex tachy
M3
NO-cGMP
vasodil
secretions
bronchoCX
M1
motility
secretions
M1
Detrussor CX
Trigone RX
Ex. sphincter RX
micturition
Parathion
Eye : M1
Circular M. CX
Ciliary M. CX
~
Skel Muscle :
Nm
fasciculations
~
CNS :
Stimulation
depression
Atropine toxicity
(crosses BBB)
Paralytic ileus
Treatment of MG
Xerostomia
Caused by
exposure to
toxins
*Atropine can
reverse
*Pralidoxime can
reverse
Soman
Tacrine
Donepezil
Tubocurarine
Mivacurium
Vecuronium
Rocuronium
Succinylcholine
Ganglion blockers
Botulinum toxin
Varenicline
Reverses ChEI
toxicity
Splits covalent bond forming oxime-phosphonate splits off leaves regenerated ChE
Pralidoxime
M2 (ant)
[Lo] = brady
[Normal] = HR
M2 (ant)
[Lo] = brady
[Hi] = HR
Muscarinic blockade
(M1, M2, M3)
[No cilia motility]
Echothiophate
Malathion
Treats OA glaucoma: (1) pupillary CX, (2) spasm of accom., (3) transient IOP persistent IOP, (4) impaired night vision
Non-competitive
reversible ChE inhib.
(centrally-acting)
Steroid nucleus
competitive NMJ
blocker (NmX)
Isoquinoline
competitive NMJ
blocker (NmX)
Depolarizing NMJ
blocker
( open freq. & dur.)
Competitive /
Depolarizing Nn
blockers
Prevent ACh release
from the motor nerve
terminal
Partial nicotine agonist
at 42 Nn
Also: (1) blocks DA, NE, 5-HT uptake (2) MAO inhibitor (3) block Na+ & K+ channelshepatotoxicity
Alzheimer's
disease
AChE selectivity in CNS (minimal peripheral activity)no hepatotoxicity
Nm (ant)
HR
(PsNS + rx tach)
Nm (ant)
BP
(SNS + hstmne)
Resp. paralysis
BronchoCX
(histamine)
Used during
procedures that
require muscle
paralysis
Nn
BP
(SNS)
Nn (ant)
BP
Resp. paralysis
Slight histamine
Nn (ant)
Urinary reten
impotence
Eye : mydriasis
Skin : sweat
Surg: bleeding
SCI: reflexia
Cleaves synaptobrevin & SNAP to prevent ACh vesicle fusion & release
Dystonia
Spasticity
Hyperhidrosis
Nicotine addiction
Drug
SNS Inhibitors
Guanethidine
Reserpine
-methyl DOPA
Clonidine
Blockers
K+
Thiazide
Sparing
Diuretic
Diuretic
Direct on VSM
Hydralazine
Minoxidil
Sodium
nitroprusside
Hydrochlorothiazide
Chlorthalidone
Amiloride
Spironolactone
Proproanolol
Atenolol
Acebutolol
ReninPDE5
1
Ca2+ Channel Blockers Angiotensin
inhib
Antag
Inhibitors
Labetalol
Prazosin
Captopril
Enalapril
Losartan
Nifedipine
Verapamil
Diltiazem
Sildenafil
Mechanism
Duration
Renin
Side Effects
Treats
Depletes NE
SNS
Long lasting
w/residual
Initial:
Eventual:
HTN (?)
Stimulate NTS
2 receptors
Post-syn 2A
NTS SNS
Initial:
Eventual: ?
Common+...hemolytic anemia,
sedation, imp, lactation, EP signs
Moderate HTN
(LVH)
Stimulate NTS
2 receptors
Initial:
Eventual: ~
HTN (?)
NO
K+ permeability
Initial:
Eventual: ?
Severe HTN
K+ permeability
Initial:
Eventual: ?
Same as hydralazine
(should use w/-blocker & diuretic)
Severe HTN
w/ renal disease
Initial:
Eventual: ?
HTN Crisis!
Na+ reabsorption
in DCT urine
Initial:
Eventual: ~
Hypokalemia, hyperglycemia,
hyperuricemia, chol & TAG
Mild HTN
Aldosterone
antagonist
Initial: ?
Eventual: ?
Not anti-HTN by
themselves
Metabolized to NO
cGMP
Very short
Mild-Moderate
HTN
Initial:
CX, CO, renin
pre-syn. (+) fdbk
Same as above
(+ partial agonist)
Initial:
1/1/2 blocker
Initial:
t1/2 = 3-4 hr
Initial:
Prevent A1 A2
conversion
(ACE inhibitors)
Short
Long (prodrug)
Initial: ?
Eventual: ?
Vasculature A-2
receptor blocker
Initial: ?
Eventual: ?
DHP Ca2+
channel blocker
Initial: ?
Eventual: ?
Reflex tachycardia
Adverse cardiac events
Initial: ?
Eventual: ?
Cardiodepression: HR & CO
Initial: ?
Eventual: ?
Initial: ?
Eventual: ?
PDE-5 inhibitor
cGMP
Mild-Moderate
HTN
HTN Crisis!
Block 1
(& some 2B)
Should use
long-acting
L-type Ca2+ channel
(short acting
blocker
toxicities)
Ca2+ channel
blocker
Mild-Moderate
HTN
Mild-Moderate
HTN
Moderate HTN
(LVH)
HTN (?)
HTN (?)
(Not first-line)
impotence
Pulm. Art. HTN
Fluoro
quinolones
Resistance
Pharmacodynamics
Adverse Reactions
1) Target modification
2) Altered uptake/efflux
3) Plasmid-mediated modification by
quinolone transacetylase
Administer: oral or IV
Drug Intrxn: antacids oral avail.
Administer: oral or IV
Distribution: great, CNS, intracellular
Metronidazole
Produces compounds
toxic to DNA
Administer: oral or IV
Distribution: great, CNS
Sulfanilamide
Administer: oral or IV
Sulfa & trimethoprim given together
(TMX-SMX = Bactrim)
Sulfa given w/silver ions in cream
Allergy
Not given to: G6P or folic acid
deficiency, or pregnant
HIV: prophylaxis neutropenia &
exfoliative dermatitis
1) Altered transpeptidases
2) permeability
3) -lactamases
Administer: oral or IV
Distribution: good bioavailability
Crosses BBB
Allergy
(Can be desensitized)
1) Altered transpeptidases
2) permeability
3) -lactamases
Administer: oral or IV
Distribution: good bioavailability
Crosses BBB
Allergy
(Can be desensitized)
Administer: IV
Distribution: good, CNS (inflam.)
Administer: topical
(often w/neomycin & polymyxin B)
Allergy (rare)
Ciprofloxacin
Levofloxacin
Sulfa
Drugs
Trimethoprim
Dapsone
Penicillins
w/-lactamase
inhibitors
Poly Glyco
peptide peptide
Penicillin G/V
Artificial penicillin
TicaricillinClavulanic Acid
Amoxicillin1) Bind transpeptidase & prevent
Clavulanic Acid
cross-linking
Piperacillin2) Bind & inhibit -lactamase
Tazobactam
Ampicillin-Sulbactam
Vancomycin
Bacitracin
Cephalosporins
Cephalexin
Carba Mono
penem bactam
Action
Rifampin
Penicillins
Drug
Cefotaxime
Bind transpeptidase & prevent
cross-linking
Allergy
(5-10% PCN-allergy crosshypersensitivity)
Aztreonam
No PCN-allergy crosshypersensitivity
Imipenem-Cilastatin
Ertapenem
Ceftazidime
Ceftriaxone
Allergy
(PCN-allergy cross-hypersen.)
Drug
Action
Resistance
Pharmacodynamics
Adverse Reactions
Administer: IM or IV
Post-ABX Effect: persistent
suppression after drug removal
Conc.-Dependent Killing:
concentrations better killing
Nephrotoxicity
Ototoxicity
(Particularly Streptomycin)
Administer: oral or IV
Distribution: good, including CNS
Drug Intx: food absorption
Antagonizes -lactams
Nausea
Photosensitivity
Can discolor teeth
(not given to children or pregnant)
Tetracyclines
Aminoglycosides
Streptomycin
Neomycin
Gentamycin
Tobramycin
Tetracycline
Doxycycline
Tigecycline
Macrolides
Erythromycin
Azithromycin
Clarithromycin
1) Methylation of ribosomes
(most common )
2) Efflux pumping
Administer: oral or IV
Distribution: good
Azithromycin: long intracellular
half-life, given to children, pregnant
Miscellaneous
Strepto
gramin
Oxazoli Linco
dinone samide
Telithromycin
Severe hepatotoxicity
Clindamycin
Linezolid
Chloramphenicol
QuinupristinDalfopristin
Polymyxins
Daptomycin
Nitrofurantoin
Mupirocin
Allergy
Administer: oral or IV
Distribution: good
Thrombocytopenia
Contraindication: SSRI
Administer: oral or IV
Administer: IV
Arthralgias
Myalgias
Administer: Topical or IM or IV
(often w/neomycin & bacitracin)
Few
Administer: IV
liver fx tests
muscle weakness & pain (CPK)
Administer: oral
(drug concentrated in urine)
Radiomimetic
(IC enzymatic redctn required)
Disrupts protein synthesis
1) rRNA methylation/adenylation
2) altered ribosomal proteins
Drug
MOA
Treats
Toxicity
Hodgkin lymphoma
Bone marrow
GI
Interesting N-(CH2-CH2-Cl)2
structure activates to ring
Non-Hodgkin Lymphoma
Breast/Ovary Carcinoma
Brain tumors
Insulin shock
Nephrotoxicity
Hepatotoxicity
CML
Pulmonary fibrosis
Mechlorethamine
Cyclophosphamide
Alkylating Agents
(Phase non-specific)
Ifosfamide
Carmustine
Lomustine
Streptozocin
Dacarbazine
Temozolomide
Procarbazine
Cis-platinum
Carboplatin
Oxaliplatin
Methotrexate
6-Mercaptopurine
Antimetabolites
(S phase specific)
6-Thioguanine
Fludarabine
Hodgkin/Non lymphoma
SCLC, Melanoma
Brain tumors
CURES: testicular tumor
Ovarian cancer
Also: SCLC & bladder CA
ALL
Leukemia
Converted to 5FdUMP
thymidylate synthetase
TMP DNA synthesis
Breast cancer
Colorectal cancer
Basal cell carcinoma
Acute leukemia
(w/6-TG)
Thiopurine methyltransferase
mutation 6-MP metabolism
MP controls ALL
Pentostatin
5-Fluorouracil
Cytarabine
Gemcitabine
Vincristine
Vinblastine
Vinorelbine
Antimitotics
Busulfan
Paclitaxel
Peripheral neuropathy
Etoposide
Teniposide
Inhibit topoisomerase II
DNA replication
Teniposide =
topoisomerase II
Teniposide = ten year-olds
Topotecan =
topoisomerase I
Both "tecans" do the same
ALL
Topotecan
Irinotecan
Actinomycin D
Inhibit topoisomerase I
DNA replication
Doxorubicin
Daunorubicin
Antibiotics
Mnemonic
Epirubicin
Plicamycin
Bleomycin
Mitomycin
Cross-links DNA DNA synthesis
Specific to osteoclasts
[Ca2+] in hypercalcemic
patients
Protea
some
Inhib.
Drug
L-asparaginase
Tretinoin
Gefitinib
Specialty Antibodies
ALL
CML
(Well tolerated!)
Diarrhea, acne-like rash
RCC (adv.)
GI stromal tumors
Fatigue, anorexia
Nausea, diarrhea, mucositis, stomatitis
RCC (adv.)
Multiple myeloma
Colorectal cancer
EGFR is overexpressed in
colorectal cancer
Antiviral activity
Sunitinib
Sorafenib
Bortezomib
Rituximab
Cetuximab
Bevacizumab
Interferons
Biological Response
Modifiers
Treats
Imatinib mesylate
Trastuzumab
Interleukin-2
G-CSF
GM-CSF
Diethylstilbesterol
Ethinyl Estradiol
Tamoxifen
Toremifene
Fulvestrant
Aminoglutethimide
Hormones
MOA
Prednisone
Leuprolide
Goserelin
Flutamide
Hypersensitivity, hyperglycemia,
Coagulation defects, hypoalbuminemia
due to normal protein
Nasty drug.retinoic acid syndrome:
fever, wt gain, SOB, heart, photosens.,
skin, hearing, diarrhea, liver enzymes,
Mnemonic
ALL disparaging
Melanoma (malig.)
RCC
Chemotherapy-induced
neutropenia
Bone pain
Bone marrow
transplantation
Fever
Bone pain
Block production of LH
testosterone
Hypercalcemia
Vaginal carcinomas in offsprings
Breast cancer
(Post-men; in ER+ tumors)
osteoporosis
serum & LDL cholesterol
apolipoprotein A1
Breast cancer
(Pre-men; in ER+ tumors)
Breast cancer
(Post-men; in ER+ tumors)
CNS depression
(drowsiness, blurry vision, ataxia)
Breast cancer
(Post-men; in ER+ tumors)
Breast cancer
(Post-men; in ER+ tumors)
Nausea
Musculoskeletal pain
ALL, CLL
Hodgkin/Non-H lymphoma
Breast cancer
Cushing's syndrome
Immunosuppression
Prostate cancer
Sexual dysfunction
Converted to dihydroxyflutamide
blocks DHT binding to receptors
Prostate cancer
GI distress
Anastrozole
Letrozole
Toxicity
Drug
Metabolism
Toxicity
L-DOPA DA (AADC)
DA (MAO-B, DBH, COMT)
Dopamine agonist
Bromocriptine
Pergolide
B: D2 agonist / D1 antagonist
P: D2 agonist / D1 agonist
B: short half-life
P: better w/L-DOPA (D1 & lipophilic)
D2 agonist
Selegiline
Deprenyl
Anticholinergic
Apomorphine
Treats
Amantadine
COMT
Inhibitors
Dopamine Agonists
Levodopa
Carbidopa
Mechanism
Tolcapone
Entacapone
Anti
Anti
Psychotics Depressant
MAO
Inhibitors
Pramipexole
Ropinirole
No effect on tremor
May
SSRI
Block 5-HT reuptake
Anxiolytics
Butyrophenone
Block DA receptors (D2)
Phenothiazine
Reserpine
Clonidine
Guanfacine
Miscellaneous
Parkinson's Disease
Antipsychotics
Bromocriptine
Primidone
Baclofen
Riluzole
2 agonists
Tourette's Syndrome
Tardive Dyskinesia
Anticonvulsant
Abuse potential
Congener of phenobarbital
Amyotrophic Lateral
Sclerosis
Miscellaneous
Generalized
Seizures
Drug
Mechanism
Metabolism
Toxicity
Treats
Phenytoin
Partial seizures
Gen. tonic-clonic seizures
Status epilepticus
(not absence)
Carbamazepine
Partial seizures
Gen. tonic-clonic seizures
Trigeminal neuralgia
Bipolar Disorder
(not absence)
Partial seizures
Gen. tonic-clonic seizures
(not absence)
Partial seizures
Generalized seizures
Absence seizures
Myoclonic seizures
Felbamate
NMDA antagonist
Enhance GABA
Aplastic anemia
Severe hepatitis
Gabapentin
GABA analog
( release of GABA?)
Topiramate
Tiagabine
Pregabalin
GABA analog
Phenobarbital
Vigabatrin
Lamotrigine
Enhance GABA
Ethosuximide
Valproic Acid
No liver involvement!
Partial seizures
Neuropathic pain
Alcoholism
Partial seizures
Gen. tonic-clonic seizures
Partial seizures
Neuropathic pain
Absence seizures
Absence seizures
Myoclonic seizures
Atonic seizures
Partial seizures
Diazepam
Clonazepam
Partial seizures
(poorly controlled)
Status epilepticus
Absence seizures
Myoclonic seizures
Infantile spasms
Drug
Mechanism
Alprazolam
Chlordiazepoxide
Benzodiazepines
Oxazepam
Lorazepam
Anxiolytics
(Non-Benzo/Non-Barb)
Barbiturates
Anxiety
Alcohol withdrawal
Rapidly absorbed
Long acting
Slowly absorbed
Short acting
Slowly absorbed
Short acting
Midazolam
Meprobamate
Carisiprodol
Short acting
Long acting
Thiopental
Methohexital
Phenobarbital
Ramelteon
Anxiety
Status epilepticus
Anxiety
Anxiety
Insomnia
Status epilepticus
Palpitations, tachycardia
GI distress
Miosis, BP
Muscle relaxant
Short acting
Eszoplicone
Pentobarbital
Secobarbital
Insomnia
Zolpidem
Zaleplon
REM suppression
REM rebound upon W/D
Tolerance
~
Sedation, lethargy, fatigue, mental
clouding, fine motor incoord, ataxia,
W/D, convulsions
~
Physio/Psycho dependence
~
Anterograde amnesia
Paradoxical hostility
~
Toxicity reversed by flumazenil
-BZ-1 & BZ-2 antagonist
-Not effective w/other agents
-Short acting
-Must be given IV
Long acting
?: 5-HT1A or DA receptor
Major metabolite blocks 2
(Not GABA receptor)
Treats
Rapidly absorbed
Short acting
Long acting
Buspirone
Anxiety
Depression
Flurazepam
Clonazepam
Toxicity
Short acting
Rapidly absorbed
Short acting (very )
Triazolam
Diazepam
Metabolism
Short-intermediate acting
Long acting
Insomnia
Anesthesia adjuct
Drugs of abuse
Anticonvulsant
Insomnia
(sleep onset problems)
Atypical Antipsychotics
Typical
Antipsychotics
Drug
Chlorpromazine
Haloperidol
Fluphenazine
Clozapine
Metabolism
Toxicity
Treats
Jaundice, photosensitivity,
Parkinsonism, NMS, TD
IM preparation
Schizophrenia
Schizoaffective D/O
Bipolar D/O
Mania
Tourette's syndrome
Causes sialorrhea
Have to keep their mouth clozed
Risperidone
Olanzapine
Schizophrenia
Schizoaffective D/O
Bipolar D/O
Mania
Tourette's syndrome
Less SE's
Aripiprazole
Lithium
Mood Stabilizers
Mechanism
Valproic Acid
Anti-convulsant
Block Na+, enhance GABA
Carbamazepine
Lamotrigine
Anti-convulsant
Block Na+
Clonazepam
Benzodiazepine
Mania
Sedation, GI
Hepatotoxicity
Birth defects
Mania
(early)
Diplopia, ataxia, GI
Aplastic anemia, birth defects
Agranulocytosis
Mania
Miscellaneous
MAO Inhibitors
SSRIs
Tricycic Antidepressants
Drug
Mechanism
Metabolism
Imipramine
Metabolized to desipramine
Amitriptyline
Metabolized to nortriptyline
Desipramine
Inhibits NE reuptake
Nortriptyline
Buproprion
CV SE's
sexual complications
seizure threshold
Venlafaxine
CV SE's
BP
Trazodone
Nefazodone
Phenelzine
Tranylcypromine
Moclobemide
Sedation
Orthostasis
Cardiotoxicity
Anti-cholinergic effects
Hypomania
Rash, photosensitivity
seizure threshold
1: hypotension reflex SNS
Tachycardia
Arrhythmia
Angina, infarct
Suicide
Impotence
Fluoxetine
Sertraline
Paroxetine
Fluvoxamine
Toxicity
Long acting
Active metabolite
Inhibits P450 system
Shorter acting (than fluox)
No active metabolites (like fluox)
No inhibition of P450 system
Akathisia
Behaviorally activating
Nervousness, insomnia, N/V
Headache, anorgasmia
Suicide
MAOI Interax: serotonin syndrome
Photosensitivity
Induces liver enzymes
Treats
Depression
~
Enuresis
(anti-ACh)
Pain
ADHD
Psychomotor activation
Depression
Nicotine withdrawal
Depression
Depression
(Nef>Traz)
Depression
OCD
Bulimia
Depression
Narcolepsy
Phobia anxiety D/O
OCD
Depression?
Substance P
antagonist
Needs confirmation
Depression?
Mifepristone
Psychotic major
depression
Alcoholism Treatment
Drug
Mechanism
Metabolism
Toxicity
Disulfiram
Acetaldehyde syndrome
alcohol flush reaction
Naltrexone
Opiate OR antagonist
Blocks alcohol reinforcement
Acamprosate
Topiramate
Tiapride
Toxic Alcohols
Ondansetron
Methanol
Ethylene glycol
Treats
Reduces craving
Reduces relapse rates by 50%
Reduces hyperexcitability during
withdrawal
Taurine derivative
Alcoholism
D2 dopamine antagonist
Alcoholism
(early-onset)
5-HT effects
Toxic
Metabolic acidosis
Renal failure (oxalate deposits)
Antifreeze
Mixed Opioid
Agonist-Antagonists
Moderate Opioid
Agonists
Drug
Mechanism
Morphine
Fentanyl
Su & Alfentanil
Toxicity
Treats
Mod-severe pain
Myocardial infarction
Dyspnea, anxiety
Less nausea
Sufentanyl = fentanyl
Alfentanyl = fentanyl
Post-op pain
Anesthetic (w/droperidol)
Meperidine
No cough suppression
Less constipation
No labor prolongation
OB/Surg analgesia
Mod-severe pain
Methadone
No euphoria
Prevents W/D signs
Mod-severe pain
Opioid addiction
Codeine
Propoxyphene
Pentazocine
Butorphanol
KOR agonist
MOR antagonist
Nalbuphine
Mild-moderate pain
Cough
Few SE
Oxycodone
Mild-moderate pain
Abuse
Combined w/tripelennamine
("T's & blues") heroin-like
Sedation (KOR)
Sweating, dizziness
Psychotomimetic effects
Anxiety, nausea, vomiting
Moderate pain
Mod-severe pain
(acute)
Less psychotomimetic effects
Less MOR antagonist activity
Mod-severe pain
Buprenorphine
Opioid
Antagonists
Metabolism
Naloxone
Fast onset
Competitive opioid antagonist
(MOR)
Naltrexone
Tramadol
Opioid overdose
Opioid addiction
(highly motivated)
Less potential for abuse &
respiratory depression
Dental pain
Acute MSK pain
Cancer pain
Drug
Mechanism
General Anesthetics
(Inhalation)
Halothane
Enflurane
Toxicity
Halo = Heart
Intermediate induction
Intermediate potency
Isoflurane
Thiopental
Diazepam
Loraz/Midaz
Morphine
Fentanyl
Mnemonic
NO potency
Benzodiazepines
Slower onset
Long acting
Respiratory depression
Analgesic
Only anesthetic @ doses
Rapid onset
Rapid recovery
Anti-emetic
Respiratory depression
Hypotension
Analgesic
Amnesia
Catatonia
Ketamine = catatonic
Analgesia
Pt. can respond to commands
(no loss of consciousness)
Not analgesic
He tummy ache
Barbiturate
Propofol
Ketamine
Droperidol
Antipsychotic
Etomidate
Nitrous oxide
Metabolism
Rapid onset
Rapid recovery
Drug
Cocaine
Procaine
Tetracaine
Benzocaine
Mechanism
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
~
Quickly metabolized by PChE
Local Anesthetics
(Amides)
Lidocaine
Mepivacaine
Bupivacaine
Procainamide
Metabolism
Toxicity
Use
Produces vasoconstriction
(All other LA's produce vasodilation)
Topical LA
Short acting
(metabolized by plasma ChE)
Given w/EPI
Infiltration
Nerve block
Spinal anesthesia
Spinal anesthesia
Topical LA
Dusting powder
Ointment
(burns/ulcerations)
LA
Cardiac arrhythmias
Drowsiness
Lassitude in neonate
Cardiotoxic
OB LA
Particularly long acting
(some nerve blocks last 24+ hrs!)
Analgesia + abdominal muscle control
Cyto
Protect
Mucosal
Protectants
Proton
Pump
Inhibitor
H2 Receptor Antagonists
Second Generation
H1 Receptor Antagonists
First Generation
H1 Receptor Antagonists
Degranulation
Inhibitors
Drug
Mechanism
Metabolism
Toxicity
Treats
Bronchial asthma
(prophylaxis)
Cromolyn Sodium
Inhibit immunologically triggered mast
cell degranulation
Nedocromil
Chlorpheniramine
Diphenhydramine
Promethazine
Terfenadine
Fexofenadine
Loratadine
Allergies
Motion sickness
Sedation
Allergies
Long acting
Little to NO sedation
Cyproheptadine
Allergies
Cimetidine
Ranitidine
Competitive inhibitor of histamine (H2)stimulated gastric HCl secretion
Famotidine
Nizatidine
Gastric/duodenal ulcers
ZE syndrome
GERD
Absorbed in alkaline SI pH
Use >2 months not advisable
Diarrhea, nausea
Dizziness, headache
Gastric/duodenal ulcers
ZE syndrome
GERD
Sucralfate
Short acting
Drug interax: blocks tetracycline & PO4
absorption
Constipation
Nausea
Duodenal ulcer
Colloidal bismuth
Gastric/duodenal ulcers
Prostaglandin E1 analog H+
mucus & bicarbonate secretion
Nausea, diarrhea
Abortion in preggos
Omeprazole
Misoprostol
Sulfasalazine
Hydrocortisone
Azathioprine
Mercaptopurine
Nausea, vomiting
Headache
Allergy
Corticosteroid inflammation
Cytotoxins
Cyclosporine
Infliximab
Gastric/duodenal ulcers
NSAID-induced damage
Nausea
Serum sickness
Infections, autoimmunity, cancer
Crohn's disease
Drug
Acyclovir
Valacyclovir
Ganciclovir
Valganciclovir
Famciclovir
Penciclovir
Metabolism
Valacyclovir (rapidly) acyclovir
Toxicity
Trifluridine
Pyrimidine analog
Cornea inflammation
Fomivirsen
Antisense oligonucleotide
Docosanol
Idoxuridine
CMV (retinitis)
HSV
(acyclovir resist.)
CMV (retinitis)
(in HIV patients unresp)
For herpes, tri giving
acyclovir, doc (or
dox)!
Orally inhaled
Used once taily to prevent flu
Oseltamivir
HSV
(keratitis)
Reduces duration & severity of influenza
infection
90% of influenza is resistant!
Influenza A
Parkinson's disease
Influenza A & B
Dexamethasone
Interferons
Croup
Imquimod
Nephrotoxicity
IM or SC injection
Hepatitis B
(chronic)
HPV
Hepatits B & C
Kaposi's sarcoma, MS
Renal dysfunction
Myopathy ( CK)
Hepatitis B
Hepatitis C
RSV , Influenza, HIV
Parainflu, Paramyxo
HPV
Telbivudine
Ribavirin
HSV
Metabolized by liver
Zanamivir
Adefovir
HSV
(Keratoconjunctivitis)
(Epithelial keratitis)
CMV (retinitis)
CMV
(retinitis)
Metabolized by kidney
Treats
HSV
VZV
Cidofovir
Rimantadine
Mnemonic
Nausea, diarrhea
Headache
Tumors, testicular toxicity
Foscarnet
Amantadine
Viral Respiratory Infections
Mechanism
Drug
Mechanism
Metabolism
Toxicity
Didanosine
Zalcitabine
Non-Nucleoside
RT Inhibitors
Zidovudine
Mnemonic
Treats
HIV
HIV
(AZT resistant)
Resistance: mutated RT
Peripheral neuropathy
Lactic acidosis, hepatic steatosis,
lipoatropy, central fat, lipids
Stavudine
Lamivudine
Emtricitabine
HIV
HIV
HIV
Hepatitis B
Hyperpigmentation
Abacavir
HIV
Tenofovir
Flatulence
Renal toxicity
HIV
Hepatitis B
Efavirenz
Rash
Delavirdine
Nevirapine
HIV
HIV
Binds enfulope
HIV
Indinavir
Diarrhea, nausea, vomiting, lipodystrophy,
hyperglycemia
Protease Inhibitors
Saquinavir
Ritonavir
Lopinavir
Administered together:
Ritonavir inhibits CYP3A4
Lopinavir
Nelfinavir
Inhibits CYP34A (Rx toxicity)
Rifampin induces CYP3A4
Amprenavir
Atazanavir
Fusion
Inh.
Fosamprenavir
Enfuvirtide
Metabolism
Toxicity
Treats
Quinidine
Chronic SVT
Procainamide
automaticity
refractory period
conduction velocity
Ventricular tachycardia
SVT
Seizures
Nystagmus, tremor, dysarthria, altered
sernsorium
Lidocaine
Flecainide
Propafenone
Class II - Blockers
Class 1B
Na+ blocker
(Rapid )
Mechanism
Class 1C
Na+ blocker
(Very long )
Class 1A
Na+ blocker
(Intermediate )
Drug
Mexiletine
Propranolol
Non-selective blocker
Na+ blocker at dose
(membrane stabilization)
Metoprolol
1 blocker
Carvedilol
Non-selective blocker
blocker
Amiodarone
Atrial arrhythmia
(if no other strx disease)
Atrial arrhythmia
Antioxidant properties
Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Angina
Longer acting
Esmolol
Class IV Miscellaneous Ca2+ channel Class III - K+ channel blockers
blockers
Lupus-like syndrome
1 blocker
Orally active
Acebutolol
Atenolol
Ventricular tachycardia
Ventricular fibrillation
Blocks K+ channels
Blocks Na+ & Ca2+ channels
Non-competitive SNS blocker
Atrial tachycardia
Ventricular tachycardia
Sotalol
Blocks K+ channels
Non-selective blocker
Ibutilide
Blocks K+ channels
Non-selective blocker
IV use only
Delays repolarization,
action potential
Torsades
Contraindicated in hypokalemia
IV use only
Atrial arrhythmias
(acute)
Blocks K+ channels
(rapid delayed rectifier K+ current)
Torsades
Rx Interax: [Dofetilide]
Interfere w/cation trx in kidney, prolong QT
interval, use liver metab.
Atrial arrhythmias
(chronic)
Dofetilide
Verapamil
Diltiazem
Digoxin
Adenosine
CX ( Ca2+)
Vagal: atrial AP & AV refractory
Arrhythmias
Nausea
CNS effects
Transient: asystole, dyspnea, bronchoCX
Atrial fibrillation
Flushing
Atrial arrhythmias
(chronic)
SVT
(acute or chronic)
SVT
(acute or chronic)
CHF ( CO)
Atrial tachycardia
Atrial fibrillation
Produce controlled hypotension
Miscellaneous
Inotropes
Digitalis
Glycosides
Drug
Toxicity
Treats
Heart failure
Simulate 1 receptors CX
Inhibits phosphodiesterase-III
vasodilation & CX
Nausea, vomiting
Thrombocytopenia, liver damage
Arrhythmia
Short acting
Very potent
Hyponatremia, hypokalemia,
hypocalcemia, hypomagnesemia,
hypophosphatemia
Hyrdochlorothiazide
Chlorothiazide
Diuresis
Hyponatremia, hypokalemia,
hypocalcemia, hypophosphatemia
Heart failure
(mild)
Spironolactone
Diuresis
Avoids K+ wasting
Heart failure
Digoxin
Digitoxin
Dopamine
Dobutamine
Amrinone
Diuretics
Furosemide
Bumetamide
Captopril
Enalapril
Lisinopril
Mechanism
Metabolism
Vasodilators
Isosorbide dinitrate
Nitroglycerin
Isosorbide 5-mononitrate
Hydralazine
Carvedilol
Metoprolol
Bisoprolol
Verapamil
Diltiazem
Nifedipine
Heart failure
Sodium nitroprusside
Heart failure
(serious)
Heart failure
Cyanide thiocyanate
(eliminated kidneys)
No tolerance (different NOS from NG)
Heart failure
Angina
Hypotension
Reflex SNS activity
Heart failure
Heart failure
Carbonic
Anhydrase
Inhibitors
Drug
Acetazolamide
Dorzolamide
Mechanism
Metabolism
Toxicity
Topical application
Minimal
Loop Diuretics
Furosemide
Bumetanide
Shorter acting
50% liver elimination
(50% kidney elimination)
Longer acting
Faster absorption
80% liver elimination
Torasemide
Hyponatremia/dehydration
Hypocalcemia
Hypokalemia
Metabolic alkalosis
Hypomagnesemia
Hyperuricemia
Ototoxicity
Allergy
Thiazide Diuretics
Shorter acting
Potassium-Sparing Diuretics
Chlorthalidone
Hyponatremia/dehydration
Hypokalemia
Metabolic alkalosis
Hypercalcemia
Hyperglycemia
Hyperuricemia
Allergy
Weakness
Epoxy-spironolactone derivative
Lithium
Cirrhosis (ascites)
Hyperaldosteronism
Hypertension
Heart failure
Shorter acting
Metabolized in liver into kidney lumen
insoluble & ppts out
Photosensitivity
Must be given IV
flow urea excretion
ability to concentrate urine
Intracranial pressure
Renal excretion of toxins
Nephrotoxic
Tetracycline antibiotic
SIADH
Bipolar disorder
(~SIADH)
Nesiritide
Tolvaptan
Hypertension
CHF
Idiopathic hypercalciuria
(renal stones)
Nephrogenic diabetes insipidus
Edema
Hypertension
Miscellaneous
Pulmonary edema
Edema (CH, renal, cirrhosis)
Hypercalcemia
Hyperkalemia
Demeclocycline
Conivaptan
Glaucoma
Longer acting
Triamterene
Mannitol
Longer acting
Longer acting
Excellent oral absorption
Eliminated via liver
Indapamide
Amiloride
Chlorothiazide
Eplerenone
Hydrochlorothiazide
Spironolactone
Treats
Ethacrynic Acid
Metolazone
Hypotension
CHF
Heart failure
ADH V2 receptor antagonist
free H2O excretion &
urea & Na+ reabsorption
Drug
Toxicity
Treats
URI or "Colds"
Ephedra
Contains ephedrine
(sympathomimetic)
Weight loss
Energy
Feverfew
Contains melatonin
Does work, but not better than
traditional treatment
Migraines
Arthritis
Hypertension
As effective as antihistaminics in
nausea
Motion sickness
Morning sickness
Echinacea
Mechanism
Metabolism
Contraind: anti-coagulants
(may inhibit platelet aggregation)
Garlic
Ginger
Effective anti-nausea
Inhibit thromboxane synthase
Contraind: anti-coagulants
(may inhibit platelet aggregation)
Ginseng
Contraind: anti-coagulants
(may inhibit platelet aggregation)
Phenelzine
Dementia
Ginko biloba
ACh activity
Effects 5-HT & NE
VasoRX.Antioxidant...coag
Contraind: anti-coagulants
Dementia
Circulatory disorders
Kava
Saw Palmetto
Valerian
Glucosamine
Creatine
Androstenedione
Anxiety
Insomnia
BPH
Photosensitivity
Depression
Insomnia
Gi discomfort, nausea,
photosensitivity, systolic HTN,
proteinuria
Osteoarthritis
Wound healing
Athletic performance
Weight loss
Drug
HPA Axis
Growth Hormone
Somatropin
Somatotropin
IGF
Mecasermin
GHRH
Sermorelin
Hexa/Capromorelin
Somatostatin
Octreotide
Pegvisomant
Bromocriptine
Cabergoline
Pergolide
ACTH
Cosyntropin
CRH
HPT Axis
Corticorelin
TSH
Thyrotropin-
TRH
Protirelin
hCG
Choriogonadotropin-
hMG
Gonadotropins
Menotropin
FSH
Urofollitropin
rFSH
Clomiphene
GnRH
Gonadorelin
Leuprolide, Goserelin
Post.
Pituitar
y
Ganirelix
Cetrorelix
Vasopressin
Desmopressin
Mechanism
Metabolism
Toxicity
Children: few
Adults: per. edema, arthralgia,
myalgia, carpal tunnel syndrome
Childhood deficiency
Adult deficiency
SPIGFD: mutations in GH receptor,
post GHR defect, IGF-1 defects
Dx pituitary defect
Hypothalamic GH deficiency
Acromegaly
Carcinoid tumors
VIPomas
PEGylated to t1/2,
immunogenicitybut affinity
(8 AA substitutions fix that)
hepatic aminotransferase
(otherwise well-tolerated)
Acromegaly
Somatroph adenomas
Dx adrenal insufficiency
Treats
Dx ACTH-secreting tumor
location
Dx residual thyroid
carcinoma
Dx 2 hypothyroidism
Measure PRL reserves
Male infertility
Cryptorchidism
Dx Leydig cell failure
Male infertility
Female infertility
IM
Urofollitropin: IM/subQ
rFSH: subQ
Induce ovulation
Dx gonadotropin secr'n
Hypogonadism, bone
mineralization, lipids
GnRH deficiency
Delayed/precoc. Puberty
Gn-depen. Disease
subQ
VasoCX
GI muscle, uterine muscle
Female infertility
Drug
Mechanism
Estrogens
Ethinyl estradiol
Mestranol
Admin: IM
Admin: PO
first pass metabolism (ethinyl)
Synthetic steroidal estrogens
Admin: IM (x1/month)
Insoluble in water
Estradiol cypionate
Diethylstilbesterol
Methallenestril
Toxicity
Endometrial hyperplasia
Endometrial cancer
Breast tenderness
Feminization in males
Cholestasis (GB disease)
Hepatic adenomas
plasma TAG
Thromboembolic disease/MI
Headache, migraine
BC Interax: ABX, phenytoin,
barbiturates
17 -estradiol
Esterified estradiol
Metabolism
Admin: PO
As potent as estradiol
Longer t1/2 than estradiol
Treats
Hormone replacement
(Primary hyogonadism)
Prostate cancer
Oral contraceptive
Hormone replacement
(Primary hypogonadism)
Advanced prostate
carcinoma
Anti
Progestin
Estrogen
Synthesis
Inhibitors
Estrogen Receptor
Modulators
Progestins
Progesterone
Admin: IM
>oral activity than progesterone
Medroxyprogesterone
Norethindrone
Norgestrel
Levonorgestrel
Endometriosis
Dys/amenorrhea
Oral contraceptive
Suppress gonadotropins
Fulvestrant
Tamoxifen
Raloxifene
total cholesterol
risk of breast cancer
Osteoporosis
(in post-menopausal)
Exemestane
Anastrozole
Mifepristone
Admin: IM (x1/month)
As effective as anastrozole
Breast cancer
(unresponsive to
tamoxifen)
Abortifacient
Cushing syndrome
Thyroid
Drug
Mechanism
Metabolism
Levothyroxine
Identical to endogenous T4
Converted to T3
Propylthiouracil
Methimazole
Radioactive iodine
Sodium Iodide
Calcium Homeostasis
PTH
Teriparatide acetate
Vitamin D
Calcitriol
Etidronate
Alendronate
Risedronate
Glucocorticoids
Hydrocortisone
Cortisone
Dexamethasone
ACTH
Corticosteroid Antagonists
Fludrocortisone
Ketoconazole
Spironolactone
Drospirenone
Propyl: Preggos
Methim: longer duration
Graves disease
Thyrotoxicosis
Hypothyroidism
Hyperthyroidism
Thyrotoxic crisis
Hypocalcemia, hypophosphatemia
Upper GI distress
Hypoparathyroidism
Dx pseudohyperPTH
Osteoporosis
HypoPTH, pseudohypoPTH
Rickets, osteomalacia
Osteoporosis
Hypervitaminosis D: hypercalcemia
Short-acting
4x anti-inflammatory
Intermediate-acting
5x anti-inflammatory
5x topical
Long-acting
30x anti-inflammatory
10x topical
susceptibility to infx
Inhibits growth in kids
Myopathy
Osteoporosis
Cataracts
Adrenocortical atrophy
Iatrogenic Cushing's
Inhaled
Cosyntropin
Aminoglutethimide
Hypercalcemia
HyperPTH, VitD, Bone mets
Osteoporosis, Paget's Dz
Paget's Dz
Osteoporosis
Malignancy Ca2+
Short-acting
Betamethasone
Metyrapone
Treats
Triamcinolone
Traps thyroid iodide & blocks thyroid Coadmin: -blockers & Ca2+ channel
hormone release
blockers & thionamide
Calcitonin
Prednisone
Prednisolone
Toxicity
Addison's disease
Dx of hypercortisolism
Congenital adrenal
hyperplasia
Asthma
Dx of adrenal insufficiency
Primary adrenocortical
deficiency
Cushing's syndrome
Primary hyperaldosteronism
Drug
Miscellaneous
ABX
Folate
Inhib.
Main Drugs
Chloroquine
Quinine
Quinidine
Mechanism
Metabolism
Toxicity
Unknown
Mefloquine
Schizonticide
Used as prophylaxis
GI
Neuropsychiatric
Cardiac & blood dyscrasias
Primaquine
Synthetic 8-aminiquinoline
Absorbed GI
Half-life: 3-8 hours
GI, methemoglobinemia
Hemolysis in G6PD
Cardiac & blood dyscrasias
GI
Pruritus
Pyrimethamine
Proguanil
Tetracycline
Doxycycline
Clindamycin
Atovaquone
GI
Treats
PF malaria
Hepatic amebic abscess
PF malaria
PF malaria
(chloroquine resistant)
Only agent active against dormant
hypnozoite liver form
(P. vivax & P. ovale)
Malaria
Halofantrine
Artemisin
PF malaria
(drug-resistant)
Drug
Mechanism
Suramin
Melarsoprol
Eflornithine
Nifurtimox
Stibogluconate
Metronidazole
Other Protozoa
Anti-Helminths
Toxicity
Treats
Admin: IV
Does not cross BBB
GI
Neurological
Cardiovascular, blood dyscrasias
Early hemolymphatic
African trypanosomiasis
Admin: IV
Does cross BBB
Reactive encephalopathy
Renal & cardiac toxicity
Hypersensitivity
Admin: IV
GI
Blood dyscrasias
Nitrofuran structure
Admin: oral
GI
CNS
Acute American
trypanosomiasis
Pentavalent antimonial
Admin: IM or IV
(daily)
GI
Fever, arthralgias
T wave changes, QT prolong
Admin: oral
Giardiasis
Entamebiasis
Trichomoniasis
Coadmin: metronidazole
GI
Pruritis
Little GI absorption
Renal excretion
GI
Paromomycin
Emetine
CNS advanced
African trypanosomiasis
Iodoquinol
Anti-Trematodes
Metabolism
Entamebiasis
Heart failure
Hypotension
Cardiovascular
Pancreatic, hepatic, renal, blood
Bronchospasm, dyspnea
Injectable (trypanosomatid)
Inhalation (pneumocystis)
Trypanosomes
P. carinii
Giardiasis
Cryptosporidiasis
(+ tapeworms)
Pentamidine
Admin: IM or IV
Half-life: ~6 hr
Accumulates in tissues (12 days)
Nitazoxanide
Piperazine
Admin: oral
Excretion: w/in 24 hrs
GI
Ascariasis
Pyrantel pamoate
Tetrahydropyrimidine derivative
NMJ blocking agent paralyzes & expels
Admin: oral
Poorly absorbed from GI (good!)
GI
Insomnia
Ascariasis
Pinworm
Hookworm
Mebendazole
Admin: oral
Poorly absorbed from GI
(effect w/fatty meal)
Hypersensitivity reactions
Alopecia
Wide-spectrum
Ascariasis
Trichuriasis
Pin & Hookworm
Albendazole
Admin: oral
Metabolized in liver to active form
Mild GI
Long-term use (hydatid):
liver enzyme & blood dyscrasia
Cysticercosis
Hydatid disease
Round, Pin, Hook
Niclosamide
Salicylamide derivative
Inhibits oxidative phosphorylation
Admin: oral
Mild GI
Praziquantel
Isoquinoline-pyrazine derivative
cell membrane permeability to Ca2+
paralysis
Admin: oral
[]: cimetidine or carbs
[]: steroids or antiepileptics
Admin: oral
GI
Skin rash
Admin: oral
Half-life: 2-3 hrs (acidic urine)
10 hrs (alkaline urine)
Bithionol
Diethylcarbamazepine
Tapeworm
Schistosomiasis
Hydatid disease
Neurocysticercosis
Trematodes & Cestodes
Fascioliasis
Give w/antihistaminics
(allergic reactions)
Filariasis
Noradrenergic Targets
Drug
Phentermine
Diethylproprion
Phendimetrazine
Benzphetamine
Phenylpropanolamine
Mixed
Fat
Target
Metab.
s
Ephedra
Sibutramine
Orlistat
Mechanism
Amphetamine derivative
Inhibits NE reuptake
Inhibit NE reuptake
Metabolism
Coadmin: fenfluramine
(Pulmonary HTN & valve problems)
Interax: MAOI, guaneth, stim, EtOH,
sibutramine, TCA
NE target
Toxicity
Interax: cyclosporine
Treats
Obesity
Obesity
Asthma
URI
Obesity
Drug
Lispro insulin
Insulin
Regular insulin
Mechanism
Metabolism
Short-acting
Admin: IV or subQ
(30-60 min before meal)
NPH insulin
Lente insulin
Intermediate-acting
Peptides
Type 1 diabetes
Ultra-long-acting
Delayed onset of action
Pramlintide
Insulin-induced severe
hypoglycemia
N/V, diarrhea
Glipizide
First generation:
Longest acting (60 hours)
Intermediate potency
Bind SUR receptors associated w/
ATP-sensitive K+ channels
K+ current insulin secretion
Second generation:
Glimepiride
Highest potency
Once daily dosing
Meglitinides
Biguanides
Glyburide
Repaglinide
Phenformin
Nateglinide
Metformin
TZDs
Rosiglitazone
Pioglitazone
Contraind: hypersensitivity,
gastroparesis, hypoglycemia
unawareness
Type 1 diabetes
Type 2 diabetes
Type 2 diabetes
First generation:
Shortest acting
Least potent
Chlorpropamide
Sulfonylureas
Hypoglycemia
(Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
Glargine insulin
Exenatide
inhib.
Treats
Long-acting
Tolbutamide
Dipep
Ultralente insulin
Hyperglycemic
Pptdase glcsdase
s
4 inhib
Toxicity
gluconeogenesis
insulin-stimulated GLUT4
trafficking to membrane
cAMP-act. protein kinase
(Increase tissue sensitivity to
insulin)
Metabolized by liver
Half-life: 1 hour
Severe hypoglycemia
(chlorpropamide & glyburide)
Weight gain
Skin reactions & erythema
Blood dyscrasias
Hepatic dysfunction
(All are liver metabolized)
GI disturbances
Type 2 diabetes
Hypoglycemia
Weight gain
Type 2 diabetes
Lactic acidosis
(Even less with 2nd generation)
Cardiovascular disorders
Type 2 diabetes
(obese)
Troglitazone: hepatotoxicity
Heart failure
Angina, MI
Type 2 diabetes
Type 2 diabetes
Metabolized by liver
Half-life: even shorter & rapider
Acarbose
Miglitol
Sitagliptin
Diazoxide
Metabolized in liver
Half-life: 48 hours
Nausea/vomiting
Fluid & salt retention
Insulinoma
Glucagon
Severe hypoglycemia
Shock & GI RX
Dx pheochr-cytoma
Type 2 diabetes
Drug
Mechanism
Metabolism
Toxicity
Treats
Half-life: 1 hour
Used w/: bile acid binding resin
Used w/: HMG CoA reductase inh.
Flushing, pruritis
Nausea, diarrhea, peptic ulcer
Hepatotoxic, glucose intol., gout
HyperTAG
Familial hyperTAG
FC hyperTAG
Gemfibrozil
Fenofibrate
Clofibrate
GI disturbances
Rash, myopathy, arrhythmia
Fatigue
Cholestipol
Cholestyramine
HyperTAG
GI (constipation)
Familial HyperTAG
FC hyperTAG
Statins
Myopathy (CK)
Renal dysfx (myoglobinuria)
Rhabdomyolysis (w/gemfribrozil)
BMP-2 osteoblasts
fracture risk
Hypercholesterolemia
(& familial)
Enterohepatic recycling
Half-life: 22 hours
Low systemic bioavailability
Hypercholesterolemia
Triglycerides
Niacin
Cholesterol
Ezetimibe
Estrogen
replacement
lipid oxidation
TAG, HDL
LDL, cholesterol
Plant stanol
esters
Omega-3 fatty
acids
Ethanol
HyperTAG
Dysbetalipoproteinemia
FC hyperTAG
endothelial inflammation
LDL & TAG
Drug
Mechanism
Metabolism
Toxicity
Ointment
Used w/neomycin or polymyxin
Absorbed through skin
Intranasal preparation
Impetigo
(S. aureus & S. pyogenes)
Topical
Bacterial Infections
Bacitracin
Mupirocin
Treats
P. aeruginosa
E. coli, enterobacter
Klebsiella
Polymyxin B
Sensitization
Cross-sensitivity to streptomycin,
kanamycin, gentamycin
Neomycin
Gentamycin
10% of topical application is
absorbed
Clindamycin
Bloody diarrhea
Pseudomembranous colitis
Acne Vulgaris
Acne vulgaris
Erythromycin
Naftifine
Terbinafine
Allylamines
Inhibit ergosterol synthesis
Oral
Antifungals
Ketoconazole
Pencyclovir
Dermatophytes
Diarrhea
Photosensitivity
Headaches
Gynecomastia
Hepatitis
Ventricular dysfx
Tinea infections
Cream
Applied at first sign of infection
Shampoo or lotion
~Absorbed via skin, in fatty tissue,
excreted in urine in 5 days
Skin staining
Unpleasant odor
Inhibit tyrosinase melanin
skin hyperpigmentation
Hydroquinone = temporary
Monobenzone = permanent
Scabies
Local irritation
Allergy
Retinoic acid
Tretinoin (ATRA)
epidermis cohesion
cell turnover
Erythema
Dryness
Sunlight sensitivity
Adapalene
Admin: topical
Applied to dry skin only
Pediculosis capitis
Pediculosis pubis
Scabies
Hematotoxicity
Neurotoxicity
Skin cancer
Cataracts
Admin: oral
Similar to hypervitaminosis A:
dryness, itching, IBS
IBS, muscle pain, teratogen
Admin: topical
Skin irritation
Vitiligo
May appear worse in the first month,
as quiescent comedones emerge &
rupture
Acne vulgaris
Admin: oral
Anti-inflammatory
Antiproliferative
Synthetic vitamin D3
Skin dryness
Itching
Corticosteroids
Anti-inflammatory
Antimitotic
Tar compounds
Irritant folliculitis
Allergic contact dermatitis
Anaphylactic shock
Irritation & inflammation
Salicylism
Salicylic acid
Produce repigmentation of
depigmented macules
Psoralens intercalate w/DNA
Calcipotriene
Superficial candidiasis
Trioxsalen
Methoxsalen
Tazarotene
Ointment
Sulfur
Hydroquinone
Monobenzone
Dermatophytes
Candida
P. obiculare
Lindane
Acne
Psoriasis
Seborrheic dermatitis
Candidiasis
Use in onychomycosis only effective
in ~10% of patients
Acitretin
Antiinflammatory
Well tolerated
Benzoyl peroxide
Keratolytics
Acne rosacea
Amphotericin B
Nystatin
Isotretinoin
Pruritis
Possible carcinogen
Contraind: pregnancy & lactation
Well tolerated
Acyclovir
Tricogenics
Acne vulgaris
Acne rosacea
Tolfnaftate
Griseofulvin
Antiparasites
Ciclopiroxolamine
Topical
Antivirals
Topical Antifungals
Azoles
Burning
Irritation
Topical
Alone or with sulfur preparation
Sulfacetamine
Metronidazole
Skin
Pigmentation
Effective against
Propionibacterium acnes
Propylene glycol
Urea
Psoriasis
Doxepin
Minoxidil
Admin: topical
Finasteride
Admin: oral
Atopic dermatitis
Lichen simplex chronicus
Drug
Misc.
Colchicine
Urate
Inhib.
Uricosuric
Agents
Indomethacin
Mechanism
Metabolism
Toxicity
Admin: oral
Accumulates in WBCs
Deacetylated in liver
GI
Blood dyscrasias
CNS depression, shock
Admin: oral
Half-life: 6-12 hours
Interax: PCN, ASA, sulfa, allopurinol
Sulfinpyrazone
GI
Dermatitis
Nephrotic syndrome
Treats
Gouty arthritis attacks
Pseudogout
Familial Med. fever
Anti-inflammatory
Probenecid
Allopurinol
Drug
Albuterol
Terbutaline
Metaproterenol
Salmeterol
Formoterol
Mechanism
2-agonists Gs cAMP
bronchoRX
Metabolism
Toxicity
Treats
Long-acting
Salmeterol = slow-acting
Formoterol = fast-acting
Theophylline
Admin: IV
Low therapeutic index
Ipratropium
Tiotropium
Cromolyn
Nedocromil
Prednisone
Methylprednisone
Methylprednisone
Hydrocortisone
Beclomethasone
Flunisolide
Triamcinolone
Troleandomycin
Gold salts
Methotrexate
Admin: oral
Inhibit late-phase reactions of
inflammation
Decrease bronchial reactivity
Most potent anti-asthma agents
available
Admin: IV
Admin: inhalation
Nocturnal asthma
Chronic bronchitis
Limited in asthma
Asthma
(maintenance)
Acute asthma
Steroid-sparing therapy
Asthma
(maintenance)
Montelukast
Omalizumab
Iodinated glycerol
Chronic bronchitis