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 Vasculature Lungs GI Reproductive Organs CNS Treats
PGI vasodilation bronchodilation ↓ acid, ↑ mucus, Kidney: ↑ blood, Primary pulmonary
↓ plt aggregation ↓ tone
(↑ cAMP) (↑ cAMP) ↑ blood ↑ diuresis HTN
PGE1 ↓ intraocular vasodilation bronchodilation ↓ acid, ↑ mucus, Kidney: ↑ blood, ↑ body temp Misoprostol
↓ plt aggregation ↓ tone
pressure (↑ cAMP) (↑ cAMP) ↑ blood ↑ diuresis, ↓ ADH ↓ NE Alprostadil
PGE2 ↓ intraocular vasodil + vasocx bronchodilation ↓ acid, ↑ mucus, ↓ tone Kidney: ↑ blood, ↑ body temp
↓ plt aggregation Dinoprostone
pressure (↑ IP3 & ↑ Ca2+) (↑ cAMP) ↑ blood (+ ↑ oxy CX) ↑ diuresis, ↓ ADH ↓ NE
PGF2α ↓ intraocular vasocx bronchocx ↑ CX Latanoprost
pressure (↑ IP3 & ↑ Ca2+) (↑ IP3 & ↑ Ca2+) (↑ oxytocin) Carboprost
TXA vasocx bronchocx Kidney: ↓ blood
↑ plt aggregation ↑ CX
(↑ IP3 & ↑ Ca2+) (↑ IP3 & ↑ Ca2+)
LTC ↑ permeability bronchocx
Zileuton
(↓ BP) (↑ IP3 & ↑ Ca2+)
Zafirlukast
LTD ↑ permeability bronchocx
Montelukast
(↓ BP) (↑ IP3 & ↑ Ca2+)
Epoprostenol (PGI) vasodilation Primary pulmonary
(Epopro = IV / Trepro = subQ) (vasculature = vasodilates to relieve pulmonary HTN)
Treprostinil (↑ cAMP) HTN
Misoprostol ↓ acid, ↑ mucus, ↑ CX NSAID-ulcer
(GI = cytoprotective at low doses, ↓ acid at high doses) (during pregnancy = dinoprostone)
(PGE1) ↑ blood (↑ oxytocin) Abortifacient
Alprostadil vasodilation Impotence
(male = erection injection) (vasculature = vasodilates to maintain PDA until surgical correction)
(PGE1) (↑ cAMP) Maintain PDA
Dinoprostone ↑ CX Abortifacient
(administered vaginally, uterine contractions & ↑ collagenase activity)
(PGE2) (↑ oxytocin) Labor induction
Latanoprost ↓ intraocular Open angle
(stable, long acting, SE: brown pigmentation, dry eyes)
(PDF2 α) pressure glaucoma
Carboprost ↑ CX
(administered vaginally, uterine contractions & ↑ collagenase activity) Abortifacient
(PGF2 α) (↑ oxytocin)
Zileuton bronchodilation
(inhibits leukotrienes) Asthma
(↓lipoxygenase) (blocks LT synth)
Zafirlukast (↓LTR) bronchodilation
(blocks leukotriene receptors) Asthma
Montelukast (blocks LT synth)
Indomethacin vasocx
(NSAID indole derivative) (vasculature = vasoconstricts to close PDA in premies) Close PDA
(COX inh.) (↓ PG synth)
Drug Inhibits Metabolism Duration What Makes it Unique Side Effects Treats
Aspirin Low = 15 min 1) binds serum proteins (depends on dose) 1) salicylism, respirary alkalosis, met. acid
COX-1 RA
High = 4 h 2) irreversibly acetylates COX-1&2, 3) 2) NSAID-asthma
COX-2 Chronic inflm
↑ High = 13 h irreversibly inhibits platelet aggregation 3) Reyes syndome
Non-acetylated COX-1 Less side effects, no renal toxicity, RA
Less effective at COX inhibition than ASA
COX-2 no NSAID-asthma Chronic inflm
salicylates
Ibuprofen COX-1 Liver Short Low dose = analgesic (no anti-inflam) GI, rash, tinnitis, fluid retention RA
COX-2 CYP2C8 (2hr) High dose = analgesic & anti-inflam kidney failure, hepatitis Chronic inflm
Diclofenac Liver
COX-1 Short 1)↑ serum aminotransferase activity in liver RA
CYP3A4 Typical NSAID
COX-2 (2hr) 2) Renal dysfx doesn't impair clearance Chronic inflm
CYP2C9
Etodolac COX-1 Intermediate RA
Affects COX-2 > COX-1 by 10:1 Less GI
COX-2 (5 hr) Chronic inflm
Rofecoxib RA
COX-2 Most COX-2 selective → CV problems Still contraindicated in pts w/GI ulcers
Chronic inflm
Valdecoxib
Acetaminophen 1) COX inhibitory effects primarily in CNS
COX-1 1) Less GI irritation & bleeding RA
2) Best anti-pyretic/analgesic in children
COX-2 2) Liver toxicity (↓ glutathione) Chronic inflm
3) No anti-inflammatory or anti-coagulant
Analgesia Anti-pyretic Anti-inflamatory Anti-coagulant COX-2 Pro-coagulant
NSAID Effects (low grade pain) (PG inhibition) (MSK, RA, OA) (other NSAIDs can block long-lasting ASA) (↓ COX-2 PGI but not COX-1 TXA)
GI irritation ↑ bleeding time Pregnancy Hypersensitivity
NSAID Side Effects (ASA espclly) (inhib. TXA)
Kidney effects
(delayed onset of labor from ↓ PGE & PGF) (↓ COX → arachidonate → ↑ lipoxygenase)
Drug Action Response What Makes it Unique Treats
Prednisone Autoimmune disease
Immunosuppression Chronic use associated with: ↑infections, ulcers,
Down-regulate inflammation Transplantation inflm
Prednisolone Anti-inflammatory hyperglycemia, osteoporosis
Hypersensitivity
GVHD (bone marrow trxpnt)
T-cell Inhibitor
Converted to thioinosinate
S phase inhibitor Coadministration w/allopurinol is toxic Rheumatoid arthritis
Mycophenolate Inhibits inosine monophosphate Inhibits T-cell & B-cell cell cycle & Coadminister: cyclosporine & corticosteroids
Transplant rejection
dehydrogenase proliferation Do not coadminister: antacids
Antithymocyte Ig
Ig against T-cells Removes T-cells from system Coadminister: azathioprine & corticosteroids Transplant rejection (kidney)
Kawasake disease
Anti-CD3 Ig
Ig against CD3 on T-cells Blocks antigen recognition site Toxicity: cytokine release syndrome Transplant rejection
Rho Immune Ig Administered to Rh- mother pregnant with Rh+ Hemolytic disease of the
Ig against anti-D antibodies Blocks anti-Rh antibodies
fetus newborn (prevention)
Biological Response Modifiers
Bacillis Calmette-
Strain of myobacterium bovis Stimulates T-cells & NK cells Toxicity: severe hypersensitivity & shock Bladder cancer
Guerin
Thymic Factors
Promotes T-cell differentiation Enhanced T-lymphocytic function Stem cells rushed through boot camp SCID
β2
α-methyl-DOPA α1 some activity, but less effective than NE SE: hepatotoxicity & autoimmune hemolytic anemia HTN during
α2 ↓ SNS outflow ↓ BP pregnancy
Tyramine α1 Reflex bradycardia ↑ DBP (vasocx) If MAO inhib: 1) displaces NE from vesicles, 2) competes w/NE for reuptake
β1 ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Initially potentiates NE effects, then eventually depletes NE Kidney: ↑ renin
Guanethidine α1 Depletes NE in the SNS (but does not cross the BBB)
α2
β1
Ephedrine 1) displaces NE from vesicles….2) competitively inhibts NE reuptake….3) inhibits MAO activity → NE lingers (acts like amphetamine)
Clonidine α2 ↓ SNS outflow ↓ BP HTN
Brimonidine α2 ↓ SNS outflow ↓ BP ↓ humor production & ↑ uveoscleral outflow OA glaucoma
Tizanidine α2 ↓ SNS outflow ↓ MSK spasticity Multiple sclerosis
Isoproterenol β1 ↑HR, ↑CX, ↑CO ↑ SBP (indirect) Kidney: ↑ renin Bronchodilator
β2 ↓ cardiac efficiency ↓DBP vasodilation bronchodilation ↓ motility Cardiac arrest
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
Anti β2
Prazosin Anti α1 Reflex tachycardia ↓ vasocx smooth muscle RX Hypertension
BPH
Anti α2B Reflex tachycardia ↓ vasocx
Tamsulosin Anti α1A Reflex tachycardia ↓ vasocx Hypertension
Alfuzosin Anti α1 smooth muscle RX BPH
Yohimbine Anti α2 Male impotence
Propranolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP Kidney: ↓ renin Hypertension
Migraine
Anti β2 bronchocx
Metoprolol Anti β1 [low] ↓HR, ↓CX, ↓CO ↓SBP Kidney: ↓ renin
Hypertension
Anti β2 [high] bronchocx
Atenolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP Long-lasting, specific, reduced CNS activity, no bronchocx Kidney: ↓ renin Hypertension
Acebutolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP β1 specific, partial agonist → less exercise intolerance Hypertension
Timolol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP ↓ intraocular pressure w/o affecting pupil or ciliary body Kidney: ↓ renin Open angle
glaucoma
Anti β2 bronchocx
Labetalol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP Kidney: ↓ renin
Hypertension
Anti β2 bronchocx
Sotalol Anti β1 ↓HR, ↓CX, ↓CO ↓SBP anti-arrhythmic, anti-atrial fibrillation Kidney: ↓ renin Arrhythmia
Atrial fibrillation
Anti β2 bronchocx
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 α2 Inhibits aqueous humor production OA glaucoma
Latanoprost PDF2α Enhance uveoscleral outflow OA glaucoma
Cholinomimetics
Drug Mechanism Heart Vasculature Lungs GI GU Organs Treats
Bethanechol Choline Ester M2 M1 M1 Eye : M1
M3 ↑ secretions C: OA glaucma
PsNS agonist [Lo] = reflx tach ↑ motility (B) Detrussor CX Circular M. CX
vasodil (B & C) bronchoCX B: GI/GU retentn
Carbachol M1, M2, M3 [Hi] = AV block ↑ secretions (B & C) Ciliary M. CX
Natural alkaloid
Pilocarpine Treats OA glaucoma: (1) pupillary CX, (2) spasm of accom., (3) transient ↑ IOP → persistent ↓ IOP, (4) impaired night vision
M1, M2, M3
M2 (ant) GI spasms
Muscarinic blockade
Atropine (M1, M2, M3)
[Lo] = brady
M1 (ant) M1 (ant) Eye: M1 (ant)
Eye exams
[Normal] = ↑ HR M3 (ant) ↓ secretions ChEI toxicity
Parasympathetic Antagonists
Pirenzepine M1 antagonist Used w/H-2 blockers to reduce gastric acid secretion to promote gastric ulcer healing Gastric ulcer
Tolterodine
Overactive
Trospium Anti-muscarinic
bladder
Oxybutynin
Atropine toxicity
Physostigmine Reversible ChE (crosses BBB)
Eye : M1
inhibitor (competitive) Circular M. CX Paralytic ileus
Physo : block nACh? Ciliary M. CX
Neostigmine Direct: Treatment of MG
~ Xerostomia
M2 M1
Cholinesterase Inhibitors
Skel Muscle :
Echothiophate ↓HR M3 Detrussor CX
M1 Nm
Indirect: NO-cGMP ↑ secretions Trigone RX
↑ motility ↓ Caused by
DFP M3 ↓ bronchoCX Ex. sphincter RX
↑ secretions fasciculations exposure to
vasodil vasodil ↓
Irreversible ChE ~ toxins
↓ micturition
Malathion inhibitor CNS : *Atropine can
reflex tachy
(phosphorylate ChE) Stimulation reverse
Parathion ↓ *Pralidoxime can
depression reverse
Soman
Reverses ChEI
Pralidoxime Splits covalent bond → forming oxime-phosphonate → splits off → leaves regenerated ChE
toxicity
Tacrine Non-competitive
Also: (1) blocks DA, NE, 5-HT uptake (2) MAO inhibitor (3) block Na+ & K+ channels…hepatotoxicity
Alzheimer's
reversible ChE inhib.
disease
(centrally-acting)
Donepezil ↑ AChE selectivity in CNS (minimal peripheral activity)…no hepatotoxicity
α-methyl DOPA Stimulate NTS Post-syn α2A Initial: ↓ Metabolized to α-methyl NE (false NT) and Common…+...hemolytic anemia, Moderate HTN
α2 receptors ↑ NTS → ↓ SNS Eventual: ? acts mostly α2, little α1 centrally sedation, ♂ imp, ↑ lactation, EP signs (LVH)
Minoxidil Initial: ↑ Preference for resistance (over capacitance) Same as hydralazine Severe HTN
↑ K+ permeability
Eventual: ? vessels….↓ venous pooling (should use w/β-blocker & diuretic) w/ renal disease
Hydrochlorothiazide
Diuretic
Amiloride Aldosterone Initial: ? Used with thiazide diuretic to avoid Hyperkalemia (in renal disease) Not anti-HTN by
K+
Mild-Moderate
Initial: ↓
↓ Heart, bronchial CX, hypoglycemia, HTN
W/D rebound, exercise intol.
Acebutolol Same as above Partial agonist activity: ↑ TAG & ↓ HDL Mild-Moderate
Initial: ↓
(+ partial agonist) less ↓ HDL & less exercise intolerance HTN
Labetalol
α1/β1/β2 blocker Initial: ↓ HTN Crisis!
Prazosin
Antag
Sildenafil
PDE5
inhib
PDE-5 inhibitor Initial: ? Requires ACh to initiate process: Rx interaction: (in cardiac pts) ♂ impotence
→ ↑ cGMP Eventual: ? M3 → NOS → GMP cyclase → ↑ cGMP Nitrates → ↑ NO → hypotension Pulm. Art. HTN
Drug Action Resistance Pharmacodynamics Adverse Reactions
Ciprofloxacin 1) Target modification
quinolones
Inhibitors of Nucleic Acid Synthesis
Fluoro
Inhibit DNA gyrase & topo IV 2) Altered uptake/efflux Administer: oral or IV Arthopathy (no preg or children)
Levofloxacin (Bactericidal) 3) Plasmid-mediated modification by Drug Intrxn: antacids ↓ oral avail. QT interval prolongation
quinolone transacetylase
Rifampin Inhibit RNA polymerase Administer: oral or IV Liver problems, induces cyt p450
Target site mutation in rpoB subunit
(Bactericidal) Distribution: great, CNS, intracellular (HIV meds), turns fluids orange
Metronidazole Produces compounds Administer: oral or IV ↓ elimination of lithium & ergot
(Rare, unknown mechanisms)
toxic to DNA Distribution: great, CNS derivatives...(no alcohol!)
Sulfanilamide PABA analog that binds DHP
synthetase → ↓ folic acid Allergy
Administer: oral or IV
Target site mutation, up-regulation, Not given to: G6P or folic acid
Drugs
Sulfa
Trimethoprim DHF acid analog that binds DNF Sulfa & trimethoprim given together
new genes, altered uptake/efflux deficiency, or pregnant
acid reductase → ↓ folic acid (TMX-SMX = Bactrim)
(Plasmid/Chromosomal) HIV: prophylaxis → neutropenia &
Sulfa given w/silver ions in cream
Dapsone PABA analog that binds DHP exfoliative dermatitis
synthetase → ↓ folic acid
Penicillin G/V
Penicillins
Ticaricillin-
Clavulanic Acid
w/β-lactamase
Amoxicillin-
Penicillins
inhibitors
Vancomycin
Poly Glyco
Binds D-alanine dimer in cross- Transposon: enzymes use D-serine or Administer: IV Red man syndrome: histamine
linking peptide in peptidoglycan D-lactate to make cell wall Distribution: good, CNS (inflam.) mediated w/rapid IV admin.
Bacitracin Binds membrane lipid carrier Administer: topical
Allergy (rare)
molecule → ↓ cell wall comp. (often w/neomycin & polymyxin B)
Cephalexin
Cephalosporins
Cefotaxime
Allergy
Bind transpeptidase & prevent
(5-10% PCN-allergy cross-
Ceftazidime cross-linking
hypersensitivity)
Ceftriaxone
penem bactam
Aztreonam
Carba Mono
Tetracycline
Inhibitors of Bacterial Protein Synthesis
Tetracyclines
Erythromycin
More nausea & ↑ QT prolongation
Macrolides
Telithromycin
Severe hepatotoxicity
dinone samide
Clindamycin Block protein synthesis by bacterial 1) rRNA methylation/adenylation Administer: oral or IV or topical
Oxazoli Linco
Allergy
ribosomes 2) altered ribosomal proteins Distribution: good, but no CNS
Linezolid Block protein synthesis by bacterial Administer: oral or IV Thrombocytopenia
ribosomes Distribution: good Contraindication: SSRI
Chloramphenicol Block protein synthesis by bacterial 1) acetylation (most common ) Aplastic anemia, BM suppression
Administer: oral or IV
ribosomes 2) efflux pumping Gray syndrome (shock, coma)
Strepto
Quinupristin-
gramin
Dacarbazine Active metabolite monomethyl triazeno Dcarb: Hodgkin lymphoma Bone marrow (immunosupp)
methylates DNA Temozo: malignant glioma Nausea
Temozolomide
Procarbazine Hodgkin/Non lymphoma Bone marrow (immunosupp)
Drinking, driving, & drugs
Inhibits DNA/RNA/protein synthesis SCLC, Melanoma Neurotoxic & leukemia
don't mix!
Brain tumors Contraindx: EtOH/Drugs
Cis-platinum Forms intrastrand & interstrand DNA CURES: testicular tumor Ototoxicity Testes & ovaries are
cross-links → ↓ DNA/RNA synthesis Ovarian cancer Nephrotoxicity precious, & platinum is a
Carboplatin Produces DNA breaks Also: SCLC & bladder CA Electrolyte disturbances precious metal!
Oxaliplatin Bone marrow (immunosupp)
Forms platinum-DNA cross-links → Colorectal cancer (malig.) CRC: w/5-FU & Leucovorin Good for ovaries & your
Nausea/diarrhea/fatigue
↓ DNA synthesis Ovarian cancer (adv.) Ovary C: w/Cisplatin & Paclitaxel o-ring
Neurotoxicity (glutathione helps)
Methotrexate CURES: osteosarcoma & Bone marrow (immunosupp) Develops resistance via DHFR ,
Inhibits DHFR → ↓ thymidylate, ↓ Luke to the rescue
choriocarcinoma GI transport, MPs
purines, ↓ methionine, ↓ serine (meth lab)!
ALL, Burkitt's, Non-H, Blad Nephro & Hepatotoxicity Also treats RA & psoriasis
6-Mercaptopurine Converted to 6-MPRP by HGPRT → Bone marrow (immunosupp) Thiopurine methyltransferase
ALL MP controls ALL
↓ purine synthesis 6-MP can → gout (give Allopurinol) mutation → ↓ 6-MP metabolism
Pentostatin
that….Epi)!
Epirubicin
HER2/neu receptor → ↓ growth signal breast cancer heart with her new pistol
Respiratory problems
Rituximab Antibody that blocks CD20 antigen on Fever & chills Does not deplete stem cells Ritu has 20 CD's which will
Non-H B-cell lymphoma
B-cells → ↓ B-cells in blood Nausea w/first infusion (which lack CD20) be selled.
Cetuximab Antibody that blocks (amplified) EGFR is overexpressed in Can see (C) Colorectal
Colorectal cancer Acne-like skin rash
EGF receptor → ↓ growth signal colorectal cancer cancer in situ (Cetu)
Bromocriptine B: D2 agonist / D1 antagonist B: short half-life Bromo only works in L-DOPA Pergolide
Pergolide P: D2 agonist / D1 agonist P: better w/L-DOPA (D1 & lipophilic) allows ↓ L-DOPA dose
Nausea, somnolence, dry mouth, edema,
insomnia, postural/OH
Peak-dose, on-off,
depr., anxiety, hallucinations Reduce on-off in late PD
Pramipexole Parkinson's Disease
D2 agonist Pramipexole can delay L-DOPA by 2
Ropinirole years
Inhibitors
MAO
SSRI
Anti
Anxiolytics
Fatigue, restlessness, hyperexcitability,
tardive dyskinesia
Butyrophenone Huntington's Disease
Anti
Phenothiazine
Partial seizures
Block Na+ channel Acute: stupor, coma, convulsions, irritability Accelerates metabolism: phenytoin, Gen. tonic-clonic seizures
Induces liver microsomes
Carbamazepine (prolong inactive state)
Produces active 10,11 epoxide metabolite
Chronic: diplopia, ataxia, GI, sedation, fluid reten primadone, ethosuximide, valproate, BC Trigeminal neuralgia
Enhance GABA activity Major: aplastic anemia, agranulocytosis Congener (oxcarb) less toxic, less potent Bipolar Disorder
(not absence)
Partial seizures
(prolong inactive state) Sedation, ataxia, respiratory depression, rash,
Phenobarbital Prolongs GABA-A channel activity nystagmus, porphyria, tolerance, withdrawal
Congeners (mephobarbital & primidone) Gen. tonic-clonic seizures
(not absence)
Block AMPA receptor
Partial seizures
Block Na+ channel
Generalized seizures
Lamotrigine (prolong inactive state) Headache, diplopia, rash, nausea, dizziness, ataxia Life-threatening rash in 1-2% of patients
Absence seizures
May block Ca2+ channel
Myoclonic seizures
Partial seizures
GABA analog
Gabapentin (↑ release of GABA?)
Renal excretion of unchanged drug Somnolence, dizziness, ataxia No liver involvement! Neuropathic pain
Alcoholism
Block T-type Ca2+ channel (↓ threshold) Good absorption orally (stomach irritation)
Generalized
Ethosuximide GI, lethargy, fatigue, rash, bone marrow suppression Phensuximide & methsuximide not as good Absence seizures
Seizures
Absence seizures
Clonazepam Sedation, tolerance, withdrawal Myoclonic seizures
Infantile spasms
Drug Mechanism Metabolism Toxicity What makes it unique Treats
Anxiety
Alprazolam Short acting
Depression
REM suppression
Rapidly absorbed
Triazolam Short acting (very )
REM rebound upon W/D Insomnia
Tolerance
Bind α1γ2 on GABA-A receptor ~
→ ↑ GABA binding freq. Rapidly absorbed Sedation, lethargy, fatigue, mental Don't induce their own metabolism Anxiety
Diazepam → ↑ Cl- conductance Long acting clouding, fine motor incoord, ataxia, (MDOS) Status epilepticus
Benzodiazepines
Thiopental
Ultra short acting Thio huxtable was ultra short Anesthesia adjuct
Methohexital Induce own metabolism (MDOS)
Barbiturates
Antipsychotics
High dose, low potency DA: EPS, ↑ prolactin, wt gain
Blocks: α1=5-HT2A > D2 Jaundice, photosensitivity, Schizophrenia
Chlorpromazine Liver metabolized mACh: "anti-cholinergic effects"
Typical
Agranulocytosis
Low doses → ↓EPS
Blocks: 5-HT2A > D2 Schizophrenia
Risperidone (potent @ D2…looks typical)
Therapeutic doses → EPS & DA: EPS, ↑ prolactin, wt gain
prolactin Schizoaffective D/O
Bipolar D/O
Weight gain prominent Especially good for negative SX of Mania
Olanzapine Blocks: 5-HT2A > D2 > α
(Metabolic syndrome) schizophrenia Tourette's syndrome
Less SE's
Na+ or Mg2+ replacement Oral absorption Acute: fatigue, weakness, tremor Only drug that ↓suicide
Lithium ↓IP3/DAG, ↓cAMP Kidney excretion (↑ in preggo) Chronic: ↓thyroid, diabetes insipidus, Breast milk (Ebstein anomaly) Mania
↓NT release Narrow therapeutic window nephritis, edema ↑ dietary sodium can ↓ effect
Sedation, GI
Used for early mania Mania
Valproic Acid Hepatotoxicity As effective as lithium in early mania
Mood Stabilizers
Anti-convulsant
Lamotrigine Used as lithium adjunct Mania
Block Na+
Sedation
Clonazepam Benzodiazepine Amnesia
Abuse, dependence
Drug Mechanism Metabolism Toxicity What makes it unique Treats
↓CV SE's
2nd & 3rd Generation
Depression
Buproprion Inhibits DA reuptake (?) ↓sexual complications Psychomotor activation
Nicotine withdrawal
↓seizure threshold
↓CV SE's
Venlafaxine Inhibits NE & 5-HT reuptake
↑BP
Depression
Trazodone Trazodone: Sedation (in a tranz) Trazodone can cause priapism & Depression
Nefazodone Nefazodone: Hypnotic orgasms w/yawning (Nef>Traz)
amitriptyline
Substance P
Needs confirmation Depression?
antagonist
Psychotic major
Mifepristone Glucocorticoid receptor antagonist
depression
Drug Mechanism Metabolism Toxicity What makes it unique Treats
Alcoholism
Ondansetron 5-HT effects
(early-onset)
Toxic Alcohols
Enflurane
Nonspecific interactions w/ lipid bilayer Fluranes (fluoride) can be nephrotoxic
Intermediate induction Fluranes fluoride floppy
Block K+ channels → hyperpolarization ↓minute volume
Intermediate potency muscles
Activate or facilitate GABA Muscle relaxation
Isoflurane
Morphine Analgesic
High potency opioid Can be reversed w/naloxone Respiratory depression
Fentanyl Only anesthetic @ ↑ doses
Rapid onset
Respiratory depression
Propofol Rapid recovery
Hypotension
Most popular IV anesthetic Be proper, don't puke
Anti-emetic
CV stimulation: ↑HR, ↑BP, ↑CO Analgesic
Ketamine Blocks NMDA receptors ↑cerebral blood flow, ↑ICP Amnesia Ketamine = catatonic
Disorientation, illusions, vivid dreams Catatonia
Analgesia
Can talk to the patient from
Droperidol Antipsychotic Given w/opioid (fentanyl) Pt. can respond to commands
behind the drape
(no loss of consciousness)
Nausea & vomiting
Rapid onset
Etomidate Rapid recovery
Pain Not analgesic He tummy ache
(Minimal CV/repspiratory Depression)
Drug Mechanism Metabolism Toxicity What makes it unique Use
Local Anesthetics (Esters)
Absorb via mucous membranes Produces vasoconstriction
Cocaine Block V-G Na+ channels Topical use
CNS stimulation & euphoria (abuse)
(All other LA's produce vasodilation)
Topical LA
in high frequency pain fibers
(spend lots of time "open") Short acting Infiltration
~ Aunt Ester had allergies
Procaine (metabolized by plasma ChE)
…but she was a peach! (PChE)
Nerve block
Weak bases (pKa=8-9) Given w/EPI Spinal anesthesia
1) uncharged into axoplasm
2) ionized & trapped inside More lipophilic than Pro/Coke:
Spinal anesthesia
Tetracaine 3) binds open Na+ channel Rapider onset, potenter Most commonly used drug for Spinals
Topical LA
~ Longer acting
Dusting powder
Quickly metabolized by PChE So poorly water soluble that systemic toxicity
Benzocaine Poorly water soluble
potential is zero.
Ointment
(burns/ulcerations)
LA
Lidocaine More lipophilic than Pro/Coke:
Drowsiness Used in ester-allergic individuals
Cardiac arrhythmias
Block V-G Na+ channels
Local Anesthetics
Degranulation
Cromolyn Sodium
Inhibitors
Inhibit immunologically triggered mast Bronchial asthma
Ineffective after asthma attack has started
cell degranulation (prophylaxis)
Nedocromil
Rapidly absorbed orally Ineffective in bronchial asthma (mediated by Seasonal allergic rhinitis
Chlorpheniramine Allergies Metabolized by CYP3A4 more than just ol' histamine) Urticaria
First Generation
Motion sickness
Sedation Strong sedation! Allergies
Diphenhydramine Antiparkinsonian effects Ototoxicity Motion sickness
Promethazine Anti-cholinergic effects (newborns or ABX) Sedation
Anti-serotonergic effects
α receptor blocking Drug interax: cardiotoxic w/ conazoles or Metabolized to fexofenadine (not cardiotoxic),
Terfenadine Local anesthetic effects macrolides if CYP3A4 inhibited, terfenadine accumulates
Allergies
H1 Receptor Antagonists
Loratadine Block H1 receptor → ↓ histamine ax Long acting Little to NO sedation No significant side effects Allergies
4-10x more effective than cimetidine Less side effects than cimetidine
Ranitidine Does not interfere with P450 No antiandrogenic effects Gastric/duodenal ulcers
Competitive inhibitor of histamine (H2)-
Ci me, I ran ti dine with my family & my nizce ZE syndrome
stimulated gastric HCl secretion
GERD
Famotidine Not metabolized by P450 Don't use in renal disease
Gastric/duodenal ulcers
Proton
Pump
Active form irreversibly binds & inhibits Absorbed in alkaline SI pH Diarrhea, nausea Heals duodenal ulcers more rapidly than H2
Omeprazole proton pump in parietal cells Use >2 months not advisable Dizziness, headache blockers
ZE syndrome
GERD
Aluminum salt of sucrose sulfate → Short acting
Constipation Additionally: inhibits pepsin & bile aciton
Protectants
Sucralfate binds plasma proteins in crater → Drug interax: blocks tetracycline & PO4 Duodenal ulcer
Mucosal
Nausea
Monoclonal antibody against TNF-α → ↓
Infliximab inflammatory action
Single IV infusion → remission Serum sickness Crohn's disease
Infections, autoimmunity, cancer
Drug Mechanism Metabolism Toxicity What makes it unique Mnemonic Treats
Resistance: altered/deficient viral
Acyclovir Nausea, vomiting, diarrhea HSV
Valacyclovir −(rapidly)→ acyclovir thymidine kinase or
Valacyclovir Guanine nucleoside analog Headache, renal dysfx VZV
viral DNA polymerase
Viral thymidine kinase produces analog →
binds viral DNA polymerase & inactivates Myelosuppression, neutropenia vision CMVertables are fos
Ganciclovir CMV
disturbances, carcinogenic More toxic than acyclovir cars, cid so you ganci
Valganciclovir (retinitis)
CNS effects the road fomi
Nausea, diarrhea
Famciclovir Guanine nucleoside analog Famciclovir is a prodrug metabolized to
Headache Acute herpes zoster
Penciclovir Inhibits viral DNA synthesis active penciclovir
Tumors, testicular toxicity
Herpes / Varicella / CMV
HSV
Tri flurting w/Kera's
Trifluridine Pyrimidine analog Cornea inflammation
tits & HSV
(Keratoconjunctivitis)
(Epithelial keratitis)
Iritis, vitritis, ↑ intraocular pressure Don't give to patients who have taken CMV (retinitis)
Fomivirsen Antisense oligonucleotide
Vision changes cidofovir in past month (in HIV patients unresp)
Dexamethasone Croup
IFNα & IFNβ bind cellular receptors → activate JAK- Flu-like symptoms, bone marrow HPV
Interferons STAT → ↑ 2,5-oligoadenylate synthetase & kinase IM or SC injection suppression, fatigue, infections, anorexia, Hepatits B & C
→ ↓ protein syn diarrhea, depr, anxiety Kaposi's sarcoma, MS
Peripheral neuropathy
Stavudine Lactic acidosis, hepatic steatosis,
Zitty Zal went nuclear
HIV
lipoatropy, central fat, ↑lipids
& did stab a baby
Inhibits viral reverse transcriptase → terminates Resistance to AZT develops more slowly lamb he tends.
Lamivudine DNA chain elongation
Pancreatitis (pediatric patients)
if you add lamivudine
HIV
Hepatitis B
Emtricitabine Hyperpigmentation
Nightmares, hallucinations
Rifampin → ↓ efav
↑ [rifampin, rigabutin, ergot, triazolam,
Binds next to RT activation site → change Given w/AZT & didanosine Never ever tell a nun
Delavirdine Rash midazolam, cisapride] HIV
conformation → inhibit RT activity Least potent a lie.
Efavirenz Rx & SJW → ↓ dela
↓ [rifampin, ketoconazole, ethinyl
Nevirapine Given w/didanosine & stavudine Rash, fever, nausea, hepatotoxicity estradiol (BC)]
SJW → ↓ nevir
Indinavir
Diarrhea, nausea, vomiting, lipodystrophy,
hyperglycemia
Saquinavir SJW lowers concentration
Fosamprenavir
(Intermediate τ)
↓ automaticity, prolonged QT, widened Can cause paradoxical ↑ in heart rate in
Na+ blocker
Quinidine & K+ channels rate w/A flutter, cinchonism, lupus-like Chronic SVT
Class 1A Blocks α-adren. & vagus
QRS, ↑ SA & AV node conduction velocity
syndrome
atrial flutter
Blocks V-G Na+ channels ↓ automaticity GI, hypotension, torsades, Converted to active metabolite NAPA →
Ventricular tachycardia
Procainamide & K+ channels ↑ refractory period heart block, agranulocytosis, lupus-like no Na+ channel activity but blocks K+
SVT
(no ANS effects) ↓ conduction velocity syndrome channels
IV use only (↑ first pass metab) Seizures
Na+ blocker
(Rapid τ)
Metoprolol β1 blocker
Class II - β Blockers
Non-selective β blocker
Carvedilol α blocker
Antioxidant properties Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Intrinsic SNS activity, but no membrane Angina
Acebutolol Lupus-like syndrome
stabilizing effects
Blocks K+ channels Prolonged QT, ↓ automaticity, ↓ Corneal deposits (100%), liver dz, hypo &
Miscellaneous Ca2+ channel Class III - K+ channel blockers
Verapamil
blockers
Hypotension → reflex tachy, neg. inotropy, More active L-isomer first pass met.
↓ HR, ↓ CX, ↓ conduction velocity (AV), SVT
Blocks L-type Ca2+ channels heart block (AV conduction dz), bradycardia
prolongs AV refractory period (acute or chronic)
(SA conduction dz), GI Less negative inotropic effects
Diltiazem (less ↓ CX)
Arrhythmias SVT
Direct: Blocks Na+/K+ ATPase ↑ CX (↑ Ca2+) Rx Interax: ↑ [Digoxin]
Digoxin Indirect: vagal stimulation Vagal: ↓ atrial AP & ↑ AV refractory
Nausea
quinidine & verapamil
(acute or chronic)
CNS effects CHF (↑ CO)
Binds adenosine receptors → opens Shortens atrial AP, ↓ automaticity, Transient: asystole, dyspnea, bronchoCX IV use only Atrial tachycardia
Adenosine ACh-sens. K+ channels (in ↑ AV refractory period, Atrial fibrillation Rx Interax: theophylline & caffeine block Atrial fibrillation
SA/AV/atria) ↓ AV conduction velocity Flushing adenosine receptors Produce controlled hypotension
Drug Mechanism Metabolism Toxicity What makes it unique Treats
2 day half-life delirium, anorexia, N/V, abdominal pain, Aglycone portion = for cardiac activity
Prefers E1-P form → stabilize to E2-P
color vision, halos, bradycardia, AV Monosaccharide chain = metab. Heart failure
form >90% plasma protein bound block, ectopic beats, SA arrest, Eubacterium lentum in gut inactivates
Na & Mg favor binding
Digitoxin Hepatic elimination ventricular arrhythmias, EKG changes
K favors release 7 day half-life
Miscellaneous
Hyponatremia, hypokalemia,
Furosemide Diuresis & peripheral vasodilation → Short acting
hypocalcemia, hypomagnesemia, Heart failure
Bumetamide ↓ cardiac workload Very potent
hypophosphatemia
Diuretics
Cyanide → thiocyanate
Hypotension, coronary steal, angina, Heart failure
Sodium nitroprusside cyanide toxicity, thiocyanate toxicity
(eliminated kidneys)
Angina
Metabolized to NO → venous & arterial No tolerance (different NOS from NG)
Isosorbide dinitrate vasodilation → ↓ preload & afterload CHF (acute & chronic)
Vasodilators
Secreted into lumen via OA trx Metabolic acidosis, renal CaPO4 stones, CHF edema, Glaucoma
Inhibits CA in the PCT →
Acetazolamide Inhibits 85% of PCT HCO3 reabs hypokalemia, CNS, allergy Urine alkalinization
Anhydrase
Inhibitors ↓ Na & HCO3- reabsorption
Carbonic
Inhibits 45% of total HCO3 reabs Contraind: cirrhosis (encephalopathy) Mountain sickness
Chlorothiazide
Thiazide Diuretics
Competitive aldosterone receptor in DCT & ↓ Na+ reabsorption & ↓ K+ secretion Also inhibits DHT receptor → Cirrhosis (ascites)
Potassium-Sparing Diuretics
Must be given IV
Filtered & excreted exerting osmotic pull in Headache, nausea, vomiting, Intracranial pressure
Mannitol PCT & loop of henle
↑ flow → ↑ urea excretion →
hypernatremia/dehydration, pulmonary edema
Initial rapid expansion of plamsa volume
Renal excretion of toxins
↓ ability to concentrate urine
(~SIADH)
Contains melatonin
May inhibit PLA2 → arachadonic Contraind: anti-coagulants Dizziness, nausea, indigestion, Migraines
Feverfew acid (may inhibit platelet aggregation) heartburn, oral ulcer, rash
Does work, but not better than
Arthritis
traditional treatment
Lowers blood pressure
GI distress, allergy, dermatitis,
Garlic Lowers cholesterol
bleeding, odor
Culture media for C. botulinum Hypertension
(small & brief)
Herbal medications & Nutrient supplements
Gi discomfort, nausea,
Stimulate cartilage cells → GAG & Osteoarthritis
Glucosamine proteoglycans
photosensitivity, systolic HTN,
Wound healing
proteinuria
DHEA →androstenedione & Rash, dyspnea, N/V, diarrhea,
Creatine Athletic performance
testosterone & androsterone nervousness, fatigue, migraine,
Androstenedione Weight loss
Creatine → phosphocreatine myopathy, seizures, a-fib, testo
Drug Mechanism Metabolism Toxicity What makes it unique Treats
GHRH Binds GHRH receptor → ↑cAMP → 40-80% of GH deficienct children Hexorelin: ↑cardiac performance Dx pituitary defect
Sermorelin ↑GH synthesis & release respond normally to GHRH (dilated cardiomyopathy) Hypothalamic GH deficiency
Hexa/Capromorelin
Binds SRIF receptor → ↓cAMP → Synthetic SRIF is resistant to Acromegaly
Somatostatin ↓GH release (synthesis intact) enzymes (t1/2: 3min→2hr)
↓GI motility & secretions, ↓bile PVR of hypothalamus = 14 AAs
Carcinoid tumors
Octreotide production, ↓gallbladder CX δ cells of pancreas = 28 AAs
Also inhibits TSH secretion Selective for GH (vs. insulin) VIPomas
PEGylated to ↑t1/2,
GH lysine replaced by glycine → GH ↑hepatic aminotransferase Does not reduce size of GH tumor or
Pegvisomant antagonist
↓immunogenicity…but ↓affinity
(otherwise well-tolerated) lower GH levels
Acromegaly
(8 AA substitutions fix that)
Bromocriptine
Paradoxical inhibitory effect on Headache, N/V, dizziness, postural
Cabergoline somatroph adenomas (↓GH)
Cabergoline > bromocriptine
hypotension, insomnia
Most useful in ↑GH & ↑prolactin Somatroph adenomas
Pergolide
CRH (hypothalamus) → ACTH (ant.
ACTH
HPA Axis
CRH Binds CRH receptor → ↑cAMP → Ovine CRH = ↑t1/2 & potency Flushing, SOB, tachycardia, Blood drawn from inferior petrosal Dx ACTH-secreting tumor
Corticorelin ↑POMC → ↑ACTH (over synthetic) hypotension sinus after CRH stimulation location
TRH Binds TRH receptor → ↑Ca2+ → Admin: IV over 15-30 seconds Transient nausea, hypo/HTN, Dx 2° hypothyroidism
Protirelin ↑TSH & ↑prolactin (TSH → 2-5x basal in 30 min) flushing, palpitations Measure PRL reserves
Male infertility
hCG Used for LH activity (acts at same
Cryptorchidism
Choriogonadotropin-α receptor as LH, but longer t1/2)
Dx Leydig cell failure
Partial estrogen agonist (competitive Ovarian enlargement, vasomotor ↑amplitude (not frequency) of Induce ovulation
Clomiphene inhibitor of ER)
Admin: oral x5 days
flushing, OHSS pulsatile LH & FSH secretion Dx gonadotropin secr'n
Binds V1a receptors → GI/vasoCX Desmopressin challenge: urine Osm Central diabetes insipidus
Post.
Vasopressin VasoCX
Binds V1b receptors → ↑ACTH Nasal spray, subQ should ↑50% w/central DI Dx central/nephro DI
y
Progesterone
↑fat deposition & weight gain
The only role of the progestin
Progestins
Acne
component of combination oral
Admin: IM Menstrual abnormalities Endometriosis
Medroxyprogesterone contraceptives is to protect
>oral activity than progesterone Uterine cramps Dys/amenorrhea
endometrium from estrogen-induced
Hirsutism (androgenic preps)
hyperplasia & cancer
Norethindrone ↑risk of breast cancer
Oral contraceptive
Norgestrel Suppress gonadotropins
Levonorgestrel
Pure estrogen receptor antagonist → Admin: IM (x1/month) ER+ metastatic breast
Estrogen Receptor
Traps thyroid iodide & blocks thyroid Coadmin: β-blockers & Ca2+ channel
Sodium Iodide hormone release blockers & thionamide
Thyrotoxic crisis
Binds PTH receptors → ↑Ca2+ bone Daily intermittent admin ↑osteoblasts Hypoparathyroidism
PTH mobilization & ↑renal Mg & Ca (↓PO4) & bone formation Not used to treat hypocalcemia Dx pseudohyperPTH
Teriparatide acetate
Calcium Homeostasis
Hydrocortisone
Short-acting
Cortisone
Bind glucocorticoid receptors →
Prednisone Short-acting
↑gluconeogenesis Addison's disease
Glucocorticoids
ACTH analog w/complete biological Plasma cortisol measured 30-60 min Replaced therapeutically with steroid
Cosyntropin activity after IM/IV administration hormones
Dx of adrenal insufficiency
Hypernatremia, hypokalemia
Binds mineralocorticoid receptor → Primary adrenocortical
Fludrocortisone ↑Na+ reabs. & ↑K+ secretion
Metabolic alkalosis, hypervolemia
deficiency
Hypertension
Corticosteroid Antagonists
Unknown Coadmin: doxycycline Cinchonism, hypersensitivity (P. vivax & P. ovale) PF malaria
Quinidine Only used in chloroquin-resistant Blackwater fever, ↓glucose, uteroCX No P. falciparum gametocyte kill
GI
Schizonticide PF malaria
Mefloquine Used as prophylaxis
Long half-life (~20 days) Neuropsychiatric
(chloroquine resistant)
Cardiac & blood dyscrasias
GI, methemoglobinemia Only agent active against dormant
Absorbed GI
Primaquine Synthetic 8-aminiquinoline
Half-life: 3-8 hours
Hemolysis in G6PD hypnozoite liver form
Cardiac & blood dyscrasias (P. vivax & P. ovale)
Folate
Inhib.
Halofantrine
GI
Admin: IV Adding pentamidine may increase Early hemolymphatic
GI
Admin: IM or IV Cutaneous & visceral
Stibogluconate Pentavalent antimonial
(daily)
Fever, arthralgias First line therapy
leishmaniasis
T wave changes, QT prolong
(not tissue)
Little GI absorption
Paromomycin Renal excretion
GI Entamebiasis
Effective against tissue E. hystolytica Heart failure Use limited to severe amebiasis
Emetine trophozoites Hypotension when metronidazole unavailable
Admin: IM or IV Cardiovascular
Injectable (trypanosomatid) Trypanosomes
Pentamidine Effective against trypanosoma & P. carinii Half-life: ~6 hr Pancreatic, hepatic, renal, blood
Inhalation (pneumocystis) P. carinii
Accumulates in tissues (12 days) Bronchospasm, dyspnea
Giardiasis
Blocks pyruvate:ferredoxin oxidoreductase Useful in trx metro-resistant protozoa
Nitazoxanide pathway
Converted to active tizoxanide
& tapeworms
Cryptosporidiasis
(+ tapeworms)
Direct GABA agonist
Admin: oral
Piperazine Blocks ACh at NMJ to produce nematode
Excretion: w/in 24 hrs
GI Cure rate of ascariasis (>90%) Ascariasis
flacid paralysis
Ascariasis
Tetrahydropyrimidine derivative Admin: oral GI ACh release & AChE inhibition
Pyrantel pamoate NMJ blocking agent → paralyzes & expels Poorly absorbed from GI (good!) Insomnia Cure rates >90%
Pinworm
Anti-Helminths
Hookworm
Admin: oral Ascariasis
Hypersensitivity reactions
Mebendazole Inhibits microtubule synthesis Poorly absorbed from GI
Alopecia
Wide-spectrum Trichuriasis
(effect ↑w/fatty meal) Pin & Hookworm
Mild GI Admin fasting: luminal parasite Cysticercosis
Admin: oral
Albendazole Active albendazole sulfoxide
Metabolized in liver to active form
Long-term use (hydatid): Admin fatty meal: tissue parasite Hydatid disease
↑liver enzyme & blood dyscrasia Coadmin: corticosteroids (cyst) Round, Pin, Hook
Salicylamide derivative
Niclosamide Inhibits oxidative phosphorylation
Admin: oral Mild GI Tapeworm
Schistosomiasis
Isoquinoline-pyrazine derivative Admin: oral
Mild: headache, dizziness, GI, Hydatid disease
Praziquantel ↑cell membrane permeability to Ca2+ → [↑]: cimetidine or carbs Bitter taste (don't chew)
Anti-Trematodes
GI
Bithionol Admin: oral
Skin rash
Fascioliasis
Amphetamine derivative
Phentermine Inhibits NE reuptake Coadmin: fenfluramine Fenfluramine releases 5-HT &
Noradrenergic Targets
(Pulmonary HTN & valve problems) Drug mouth, insomnia, constipation, inhibits 5-HT reputake
Diethylproprion Interax: MAOI, guaneth, stim, EtOH, ↑BP, ↑HR, abuse Contraind: hyperthyroid, HTN, CVD,
sibutramine, TCA glaucoma, anxiety
Phendimetrazine Inhibit NE reuptake Obesity
Benzphetamine
Withdrawn in 2000 due to Only approved OTC appetite
Phenylpropanolamine NE target
hemorrhagic strokes in women suppressant
Obesity
Cardiac arrest, HTN, arrhythmia,
Ephedra Appetite suppressant & weight loss ↑weight loss w/: caffeine & aspirin
stroke, seizure, MI
Found in the herb Ma Huang Asthma
URI
Target
Orlistat absorption
Interax: cyclosporine
↓absorption of ADEK & β-carotene
Improves H1Ac & sulfonylurea dose
Contraind: malabsorption, cholestitis
Drug Mechanism Metabolism Toxicity What makes it unique Treats
Short-acting
Zinc insulin crystals in a neutral,
Regular insulin unbuffered suspension
Admin: IV or subQ Hypoglycemia
(30-60 min before meal) (Counter-reg. often impaired)
Mild: juice/glucose
Insulin(-) complexed w/protamine(+) Severe: glucagon Insulin requirements ↑ during 2nd
NPH insulin & zinc
Insulin
~ half of pregnancy
Intermediate-acting Allergy ~ Type 1 diabetes
30% semilente insulin + 70% (insulin or protamine) If impaired renal fx: ↓insulin
Lente insulin ultralente insulin crystals in acetate ~ clearance
buffer Insulin resistance (IgG)
~
Excess zinc (produces large Lipohypertrophy
Ultralente insulin crystals) in acetate buffer
Long-acting
Amylin analog → ↓gastric emptying Admin: subQ w/mealtime insulin ↑Insulin-induced severe Type 1 diabetes
Pramlintide
Peptides
& ↑satiety & ↓post-pran glucagon Don't use w/acarbose hypoglycemia Contraind: hypersensitivity, Type 2 diabetes
gastroparesis, hypoglycemia
Glucagon-like peptide agonist → GLP-1 secreted in response to food unawareness
Exenatide ↓gastric emptying & ↓post-pran to potentiate glucose-stim insulin N/V, diarrhea Type 2 diabetes
glucagon & ↑insulin secretion release
First generation:
Tolbutamide Shortest acting
Least potent
First generation: May induce SIADH
Chlorpropamide Longest acting (60 hours) Severe hypoglycemia or alcohol flush reaction
Sulfonylureas
Metabolized by liver
Repaglinide Bind SUR receptors associated w/ Half-life: 1 hour
ATP-sensitive K+ channels (diff. site Hypoglycemia
Used for post-pran hyperglycemia Type 2 diabetes
from sulfonylureas) → ↓K+ current Weight gain
→ ↑insulin secretion Metabolized by liver
Nateglinide Half-life: even shorter & rapider
↓ gluconeogenesis
Biguanides
Low systemic bioavailability Flatulence, nausea, diarrhea Do not cause hypoglycemia, lactic
→ ↓carbohydrate digestion/absorb Type 2 diabetes
α
Miglitol Taken with a meal Contraind: IBS, obstruction, ulcer acidosis, or weight gain
Blunted post-prandial glucose
4 inhib
Dipep
↑ open time of ATP-sensitive K+ Metabolized in liver Nausea/vomiting Does not inhibit the synthesis of
Diazoxide channel → ↓insulin release Half-life: 48 hours Fluid & salt retention insulin, only the release
Insulinoma
s
Binds glucagon receptor → ↑cAMP Admin: subQ, IM, IV Inotropic & chronotropic Severe hypoglycemia
Glucagon → ↑(P) glycogen phosphorylase & Half-life: 3-6 minutes Nausea & vomiting RX of GI smooth muscle Shock & GI RX
synthase Metabolism: 25% first-pass Release catecholamines & CT Dx pheochr-cytoma
Drug Mechanism Metabolism Toxicity What makes it unique Treats
Used w/: HMG CoA reductase inh. Hepatotoxic, glucose intol., gout FC hyperTAG
Gemfibrozil Bind PPAR-α+ RXR → ↓apoC-III & GI disturbances HyperTAG
Half-life: 1.5 hours
Fenofibrate apoB & ↑lipoprotein lipase → ↓VLDL
Highly albumin bound
Rash, myopathy, arrhythmia Dysbetalipoproteinemia
Clofibrate → ↓LDL & ↑apoA Fatigue FC hyperTAG
(+) charged resins that bind bile
Cholestipol HyperTAG Negligible systemic bioavailability Familial HyperTAG
acids → ↓reabsorption of bile acids Taken with meals PO
Cholestyramine GI (constipation) Approved for use in children FC hyperTAG
→ ↓cholesterol & ↑LDL receptors
Inhibit HMG CoA reductase (HMG First pass metabolism Myopathy (↑CK)
↑BMP-2 → ↑osteoblasts → Hypercholesterolemia
Statins CoA → mevalonate) → ↓cholesterol Cytochrome P450 metabolized Renal dysfx (myoglobinuria)
↓fracture risk (& familial)
& ↑LDL receptors Extensively protein bound Rhabdomyolysis (w/gemfribrozil)
↓cholesterol transport at brush Enterohepatic recycling
Cholesterol lowering effect limited
Ezetimibe border in small intestine lumen → Half-life: 22 hours
by ↑liver cholesterol synthesis
Hypercholesterolemia
↓cholesterol & ↓LDL-C & ↑HDL Low systemic bioavailability
↓lipid oxidation Progestins have undesirable effects
Estrogen
Cholesterol
Plant stanol
↓absorption of dietary cholesterol
esters
Ointment
Gram (+) bacteria
Bacitracin Used w/neomycin or polymyxin Allergic contact dermatitis
Anaerobes (cocci)
Absorbed through skin
Bacterial Infections
PEG vehicle can irritate nasal Impetigo
Mupirocin Effective against most gram (+) Intranasal preparation
mucosa (S. aureus & S. pyogenes)
P. aeruginosa
Polymyxin B E. coli, enterobacter
Klebsiella
Effective against most gram (-) Topical
Sensitization
Neomycin
Cross-sensitivity to streptomycin,
Gentamycin kanamycin, gentamycin
Dermatophytes
Use in onychomycosis only effective
Topical Antifungals
Naftifine Allylamines
Dermatophytes
Terbinafine Inhibit ergosterol synthesis
Amphotericin B
Well tolerated Superficial candidiasis
Nystatin
Diarrhea
Effective against growing cells
Antifungals
Gynecomastia
Interax: benzos → ↑sedation Chronic gen. MC candidiasis
Ketoconazole statins → rhabdomyolysis
Hepatitis
Dermatophytes
Ventricular dysfx
Limited MC HSV
Hematotoxicity
Lindane ~Absorbed via skin, ↑in fatty tissue,
Neurotoxicity
Pediculosis pubis
excreted in urine in 5 days Scabies
Produce repigmentation of
Trioxsalen Skin cancer
depigmented macules Vitiligo
Methoxsalen Cataracts
Psoralens intercalate w/DNA
Tretinoin (ATRA) Erythema May appear worse in the first month,
Admin: topical Acne vulgaris (comedones)
Retinoic acid ↓epidermis cohesion
Applied to dry skin only
Dryness as quiescent comedones emerge &
Light-damaged skin
↑cell turnover Sunlight sensitivity rupture
Similar to hypervitaminosis A:
Synthetic retinoid-like drug
Isotretinoin Decreases sebaceous gland function
Admin: oral dryness, itching, IBS Severe cystic acne
IBS, muscle pain, teratogen
Anti-inflammatory
Tazarotene Extreme caution in young women Psoriasis
Antiproliferative
Skin dryness
Calcipotriene Synthetic vitamin D3
Itching
Anaphylactic shock
Salicylic acid Solubilize cell surface protein debris Irritation & inflammation
Salicylism
Keratolytics
Xerosis
↑prekeratin & keratin solubility →
Urea ↑elimination
Hyperkeratosis
(palms & soles)
Pruritis
Potent histamine receptor (H1 & H2) SE's & contraindications similar to Atopic dermatitis
Doxepin antagonist
Admin: oral or topical Allergic contact dermatitis
anticholinergics Lichen simplex chronicus
& urate phagocytosis Deacetylated in liver CNS depression, shock Familial Med. fever
Admin: oral GI
Inhibits proximal tubule reabsorption
Uricosuric
Probenecid Half-life: 6-12 hours Dermatitis Not to be used in acute gout attacks
Agents
of urate
Interax: PCN, ASA, sulfa, allopurinol Nephrotic syndrome
Hyperuricemia control
Inhibits proximal tubule reabsorption
Potentiates insulin & oral
Sulfinpyrazone of urate Very highly plasma protein bound
hypoglycemics
No anti-inflammatory or analgesia
Comp. inhibits xanthine oxidase Metabolized to oxipurinol (active) Maculopapular rash (pruritus)
Inhib.
Urate
Prednisone
Admin: oral
Methylprednisone Systemic corticosteroid effects
Inhibit late-phase reactions of Hoarseness
inflammation Oropharyngeal candidiasis
Methylprednisone
Decrease bronchial reactivity Admin: IV Coughing, wheezing Acute asthma
Hydrocortisone Most potent anti-asthma agents HPA axis suppression
available Long-term therapy (>3weeks) only if
Beclomethasone
refractory to other trx Reformulated as HFA inhaler
Flunisolide Admin: inhalation
systems (+MDI)
Triamcinolone
Troleandomycin
TAO = macrolide antibiotic → inhibit
Gold salts corticosteroid metabolism
Steroid-sparing therapy
Methotrexate
Weak anti-inflammatory & Best if added to ICS therapy Asthma
Montelukast bronchodilator actions (allows lower doses) (maintenance)