Secret Pharmacology Step 1 Study

Guide

“All you need for Step 1 Pharm”

Abciximab

Antiplatelet: monoclonal antibody to fibrin

receptor (glycoprotein IIb/IIIa) on PLTs. Used

to prevent clotting after coronary

angioplasty

Acarbose

Oral hypoglycemic: !-glucosidase inhibitor.

Prevents oligosaccharide hydrolysis leading

to less postprandial hyperglycemia. Tox: GI

disturbances

Acetaminophen

Antipyretic analgesic: CNS-active antipyretic,

analgesic. Less toxic than aspirin but more

dangerous in overdose (causes hepatic

necrosis-antidote: acetylcysteine)

Acetazolamide, dorzolamide

Diuretic: carbonic anhydrase inhibitor. Causes

NaHCO3 diuresis and bicarbonate depletion at

proximal tubule. Used in alkalosis, alkalinizing urine,

glaucoma. Tox: metabolic acidosis. and therefore

has self-limited action. Dorzolamide is a topical for

glaucoma (decreases aqueous humor production)

Acyclovir, valacyclovir penciclovir,

famciclovir

Antiviral: converted to dNTP analogs, inhibit

DNA polymerase in HSV, VZV, EBV. Activated

by viral thymidine kinase. Tox: tremor,

delirium, crystallization in urinary tract

Adenosine

Antiarrhythmic: "Class V". IV only.

Hyperpolarizes AV node, blocking

conduction for 10-15 sec. Used to dx,

abolish nodal reentry arrhythmias.

Albendazole, mebendazoleAntihelminth: inhibit microtubule synthesis.

Used for all roundworm infections.

Allopurinol

Antigout: inhibitor of xanthine oxidase;

prevents attacks during chronic gout and

during chemotherapy for leukemia/

lymphoma

Albuterol, terbutaline"2-agonists for asthma. Acute attacks only.

Tox: tremor, arrhythmia.

Alprazolam, lorazepam

Benzodiazepine: intermediate duration of

action. Used in anxiety states, selectivity for

panic attacks and phobias. Tox: psychologic

and physical dependence, additive e#ects

with other CNS depressants

Amantadine, rimantadine

Antiviral: prevents uncoating of influenza A

inside host cells. Reduces duration of flu

symptoms. Amantadine also causes release

of dopamine for Parkinson’s. Tox: ataxia,

dysphasia.

Amiodarone

Antiarrhythmic: action in all 4 Classes. Used

for life-threatening atrial and ventricular

arrhythmias. Tox: pulmonary fibrosis,

hepatoxicity, thyroid dysfunction

Amitriptyline, nortriptyline, desipramine,

imipramine

TCA: blocks reuptake of NE and 5-HT. Tox: antimuscarinic (atropine-like), anti-! (orthostatic hypotension), sedation, overdose (seizures, coma,

QRS widening). Additive e#ects with other CNS depressants. Use bicarb in toxicity.

Amoxicillin, ampicillin

Penicillin (beta-lactam): better coverage than

PCN. Amoxicillin is oral pills. Can be used

for almost all mild infections. Penicillinase-

susceptible unless given w/ inhibitor. Tox:

penicillin allergy

Amphetamine

Indirect sympathomimetic: releases

catecholamine store. CNS stimulant action.

Used for narcolepsy, obesity, ADHD. Tox:

psychosis, HTN, MI, seizures

Amphotericin B

Antifungal: 1st line for most systemic mycoses. Emulsifies fungal cell membrane by binding

ergosterol. Tox: “shake and bake,” nephrotoxicity. Must be given intrathecally for meningitis. Nystatin

is similar and used topically. Flucytosine is used w/ amphotericin to inhibit DNA/RNA synthesis.

Anistreplase (APSAC)

Thrombolytic: longer acting in body than

other thrombolytics (rt-PA, streptokinase,

urokinase). Tox: bleeding, allergy to

streptococcal protein

Aspirin

NSAID prototype: inhibits cyclooxygenase

(COX) I and II irreversibly. Potent antiplatelet

agent as well as antipyretic analgesic anti-

inflammatory drug. In overdose, alkalinize

urine and dialyze

Atenolol

"1-selective blocker: low lipid solubility, less

CNS e#ect; used for HTN. Mnemonic for "1-

selective blockers: their names start with A

through M. (except labetalol)

Atropine

Antimuscarinic: lipid soluble, CNS e#ects. Tox: “blind as a bat, dry as a bone, hot as a hare, mad

as a hatter, red as a beet," urinary retention, mydriasis. Use physostigmine in toxicity. Blocks

“SLUD”: salivation, lacrimation, urination, defecation

Azathioprine

Immunosuppressant: similar to 6-MP but for

kidney transplant. Tox: myelosuppression,

xanthine oxidase-dependent

Aztreonam

Monocyclic "-lactam. Penicillinase-resistant.

Used only against GN bugs, especially nasty

GNRs. Not a cross-allergen w/ PCN, can be

used in CKD patients (unlike

aminoglycosides)

Baclofen GABA-analog spasmolytic: activates GABAB

receptors in the spinal cord.

Beclomethasone Inhaled corticosteroid for chronic asthma.

BenztropineCentral antimuscarinic for Parkinsonian

tremor/rigidity

Bethanechol

Muscarinic agonist: choline ester with good

resistance to cholinesterase. Used for postop

or neurogenic ileus or urinary retention.

Bismuth, sucralfateAntiulcer: protect ulcer base and hasten

recovery.

Bleomycin

Antineoplastic: causes free radical DNA

damage. Used in testicular ca, lymphomas

(ABVD). Tox: pulmonary fibrosis.

Bromocriptine, pramipexole,ropinirole

Ergot alkaloid: dopamine agonist in CNS;

inhibits prolactin. Used in Parkinson’s

hyperprolactinemia. Tox: CNS, dyskinesias,

hypotension

Bupivacaine, lidocaine, tetracaine, procaine,

cocaine

Local anesthetics: block Na+ channels. 2 I’s in name: amide. 1 I in name: ester. Does not

penetrate infected tissue well. Causes loss of sensation in this order: pain, temperature, touch, pressure. Tox: CNS excitation, severe myocardial

toxicity (bupivicaine), arrhythmia (cocaine).

Bupropion

Heterocyclic antidepressant: MOA unknown.

Also used for smoking cessation. Tox:

stimulant-like, seizure in bulimics.

Buspirone

Anxiolytic: atypical drug that interacts with

5HT1A receptors; slow onset. Minimal

potentiation of CNS depressants including

ethanol; negligible abuse liability

BusulfanAntineoplastic: DNA alkylator. Used in CML.

Tox: pulmonary fibrosis.

Captopril

ACE inhibitor: used in HTN, diabetic renal disease, and CHF. Tox: cough, angioedema (both due to increased bradykinin) proteinuria, teratogen to

fetal kidneys, hyperkalemia. In CKD, the action of A-II may be all that is preserving GFR.

Carbachol, pilocarpine

Nonselective muscarinic and nicotinic

agonist: choline ester with good resistance

to cholinesterase; used for glaucoma (not

1st-line)

Carbamazepine

Anticonvulsant: 1st line for tonic-clonic and trigeminal neuralgia, also used ( phenytoin, valproate) for partial seizures. Same MOA as

phenytoin (Na+ channel blocker). Tox: diplopia, ataxia, agranulocytosis, aplastic anemia, hepatotoxicity, teratogen, induces P450

CaspofunginAntifungal: disrupts fungal cell wall

synthesis.

Cefazolin, cephalexin

1st-gen cephalosporin: bactericidal "-

lactamase-resistant "-lactams. Used for

GPCs, weak activity against GNRs. Tox:

potential allergy

Cefuroxime, cefoxitin, cefotetan2nd-gen cephalosporin. Used for GPCs, H.

flu, Klebsiella, in sinusitis or otitis.

Ceftriaxone, ceftaz, ceftiz

3rd-gen cephalosporin. Used in nasty GN

sepsis and meningitis (also covers

Pneumococcus).

Cefepime4th-gen cephalosporin: developed to treat

Pseudomonas.

Celecoxib, rofecoxib First COX-II-selective NSAIDs. Reduced GI

toxicity, increased thrombosis

Chloramphenicol

Antibiotic: inhibits peptidyl transferase at 50S subunit. Can be used for almost any bugs, but is rarely used due to side e#ects. Tox: reversible

myelosuppression, aplastic anemia, “gray baby” syndrome due to inhibition of UDP-glucuronyl

transferase

Chloroquine, mefloquineprimaquine

Antimalarial: kill blood forms of

Plasmodium. Chloroquine resistance is

widespread. Primaquine is active against

liver forms. Tox: GI distress, rash, G6PD

oxidant e#ect

Cholestyramine, colestipol

Antilipemic: bind bile acids to prevent

reabsorption; body converts more

cholesterol to bile salts to compensate. Tox:

constipation, bloating, terrible taste

Cimetidine

H2 blocker prototype: used in GERD, ulcers.

Tox: inhibits hepatic drug metabolism;

antiandrogen e#ects. Analogs w/ neither

toxicity:: ranitidine, famotidine, etc

Ciprofloxacin, “-floxacins”

Fluoroquinolone: bactericidal inhibitor of

topoisomerase. Used against most GNRs in UTIs,

bacterial diarrhea. Tox: GI distress, cartilage

damage in tendons causing tendonitis, tendon

rupture. Avoid in children and pregnant women.

Cisplatin

Antineoplastic: DNA alkylator. Used for

testicular, bladder ca. Tox: kidney, acoustic

nerve. Carboplatin is similar.

Clindamycin

Antibiotic: bacteriostatic, inhibits formation of initiation complex at the 50S subunit. Used against anaerobic pneumonia and GPCs. Tox:

GI distress, pseudomembranous colitis. Linezolid is similar but used for MRSA, VRE.

Clomiphene

Estrogen partial agonist at pituitary: causes

release of FSH and LH, inducing ovulation.

Used to treat infertility. Tox: hot flashes,

ovary-megaly, twins or triplets.

Clonidine

!2 agonist: acts centrally to reduce SNS

outflow, lowers BP. Tox: rebound HTN,

sedation, dry mouth. Methyldopa is similar

but causes positive Coombs’.

Clozapine, olanzapine, risperidone

Atypical antipsychotic: low a$nity for dopamine D2

receptors, higher for D4 and 5-HT2A receptors.

Used for schizophrenia; olanzapine used for OCD,

anxiety, etc. Tox: less EPS, anticholinergic e#ects

than neuroleptics. Clozapine requires weekly WBC

for r/o agranulocytosis, causes weight gain

Cocaine

Indirect sympathomimetic: blocks catecholamine reuptake. Local anesthetic (ester

type). Used for nasal surgery. Marked CNS stimulation, euphoria; high abuse liability. Tox:

stroke, psychosis, arrhythmias, seizures

Colchicine Microtubule assembly inhibitor: “freezes”

WBCs in gouty joints. Tox: GI, hepatic, renal

CromolynAnti-asthma: mast cell stabilizer. 3rd line

agent for prophylaxis.

CyanideToxin: poisons oxidative phosphorylation

and creates metHb. Use nitrites in toxicity

Cyclophosphamide, ifosfamide

Antineoplastic, immunosuppressive: DNA

alkylating agent. Used in HL, breast ca. Tox:

Hemorrhagic cystitis (prevent w/ mesna),

myelosuppression

Cyclosporine

Immunosuppressant: inhibits calcineurin,

and thereby IL-2. Used in transplant

immunosuppression. Tox: nephrotoxicity

(dose-limiting), infections. Tacrolimus is

nearly identical

CytarabineAntineoplastic: DNA polymerase inhibitor.

Used in AML. Tox: leukopenia.

Cytokines

EPO: renal-failure anemia. G-CSF/GM-CSF:

recover bone marrow. IFN-!: HBV or HCV,

HHV-8. IFN-": MS. IFN-%: CGD.

Dactinomycin

Antineoplastic: intercalates in DNA. Used in

Wilms’, Ewing’s, rhabdomyosarcoma (kids’

tumors)

Dantrolene

Blocker of Ca2+ release from sarcoplasmic

reticulum of skeletal muscle. Used for

malignant hyperthermia, muscle spasm,

malignant neuroleptic syndrome, and

serotonin syndrome.

Daunorubicin Like doxorubicin but only used for AML

Deferoxamine Chelator: chelates Fe very avidly, aluminum

less so

Desmopressin ADH analog: synthetic peptide used for

pituitary diabetes insipidus, vWD.

Dexamethasone Glucocorticoid: very potent, long-acting; no

mineralocorticoid activity

Diazepam

Benzodiazepine: binds to BDZ receptors at the GABAA receptor, increasing frequency of channel

opening. Uses: anxiety, EtOH detox, muscle spasms, status epilepticus. Tox: psychologic and physical dependence, additive e#ects with other

CNS depressants

Digoxin

Cardiac glycoside prototype: positive inotropic drug

for CHF. Used in CHF, a-fib (decreases AV nodal

conduction). Half-life 40h. Renal excretion. Can cause

long PR, short QT, ST scooping, inverted T. Tox: N/V,

diarrhea. Toxicity exacerbated by hypokalemia, renal

failure, quinidine. Anti-dig Fab available.

Dimercaprol Chelator (British AntiLewisite): used for As,

Pb, Hg poisoning. 1st line for Pb

Diphenhydramine, chlorpheniramine

Antihistamine H1 blocker prototype: used in

hayfever, motion sickness, sleep aid. Tox:

antimuscarinic, anti-!, sedative

Dobutamine "1 agonist: pure inotrope for ICU care.

Donepezil, tacrine

Antialzheimer: centrally-active

cholinesterase inhibitor to slow progression

of symptoms

Dopamine

Neurotransmitter and agonist drug at

dopamine receptors: pressor for shock and

to increase renal blood flow

Doxorubicin

Antineoplastic: anthracycline drug (cell cycle-nonspecific); intercalates between base pairs to disrupt DNA functions and forms cytotoxic free radicals. Used in breast, most solid tumors, HL

(ABVD regimen) Tox: cardiotoxicity, myelosuppression

Edetate (EDTA) Chelating agent: 1st line for Pb poisoning.

Tox: renal tubular necrosis

Ephedrine

Indirect sympathomimetic: like amphetamine

but less CNS stimulation. Used for nasal

decongestion, urinary incontinence

Epinephrine

Agonist at all ! and " receptors. Used in

anaphylaxis, asthma, ICU hypotension,

vasoconstriction w/ local anesthesia.

Erythromycin, azithromycin, clarithromycin

Macrolide: bacteriostatic, inhibits translocation at the 50S subunit. Used mostly for atypical

pneumonias and Chlamydia UTI. Tox: cholestatic hepatitis, erythromycin inhibits P450 to increase

warfarin, theophylline, cyclosporine concentrations.

Etanercept Soluble TNF receptor: used in RA, psoriasis.

Ethacrynic acid Loop diuretic: same as furosemide in action

and toxicity w/o gout or allergy.

Ethanol

Sedative-hypnotic: increases flow through GABAA channels. Metabolized by alcohol dehydrogenase to acetaldehyde, then by aldehyde dehydrogenase to

acetate. Disulfiram inhibits aldehyde dehydrogenase, causing accumulation of acetaldehyde. Consumes NAD

+ and produces NADH. Zero-order elimination kinetics, chronically induces its own metabolism.

Ethosuximide

Anticonvulsant: 1st line for absence. Blocks

thalamic T-type Ca2+ channels. Tox: GI

distress, lethargy, Stevens-Johnson

Etidronate, pamidronate, alendronate

Bisphosphonates: reduce resorption of bone

by inserting into hydroxyapatite. Used in

Paget’s disease, osteoporosis, PTH-rP

secretion. Tox: severe esophageal ulceration

Etoposide

Antineoplastic: inhibits topoisomerase only

during G2. Used in small cell carcinomas.

Tox: myelosuppression

Fexofenadine, loratadine, desloratadine2nd generation antihistamine; does not

enter CNS, little or no sedation

Finasteride

Steroid inhibitor of 5!-reductase: inhibits

synthesis of DHT, the active androgen in

prostate. Used in BPH.

Flecainide, encainide,

Class IC antiarrhythmics. Used for severe,

refractory ventricular arrhythmias. Tox:

propafenone arrhythmogenic,

contraindicated post-MI

Fluconazole, itraconazole

Antifungal: inhibits fungal and host P450.

Used for more severe infxns than

ketoconazole: Cryptococcal meningitis,

Candida sepsis. No antiandrogenic e#ects.

Fludrocortisone

Synthetic corticosteroid: high

mineralocorticoid and moderate

glucocorticoid activity; long duration of

action

Flumazenil

Benzodiazepine antagonist: used to reverse

CNS depressant e#ects of benzos in

overdose or in anesthesia

5-Fluorouracil

Antineoplastic: pyrimidine antimetabolite (S

phase) that decreases dTMP. Used mainly for

colon ca or superficial tumors. Tox:

myelosuppression not rescuable w/

leucovorin

Fluoxetine, paroxetine, sertraline, citalopram

SSRI antidepressant. Also used for OCD. Takes e#ect in 2-3 weeks. Tox: less antimuscarinic,

cardiotoxic; more GI distress and sexual dysfunction. Causes serotonin syndrome if used w/ MAOI. Fluoxetine inhibits P450.

Flutamide Androgen receptor antagonist: nonsteroid

that blocks DHT. Used in prostate ca.

Furosemide

Loop diuretic: blocks Na+/K+/2Cl- transporter,

preventing urine concentration. Used for edema

states, hypercalcemia. Can be used in severe

renal disease. Tox: hypokalemia, allergy to sulfa,

ototoxicity, hypovolemia, gout, hypocalcemia.

Gabapentin

Anticonvulsant and analgesic: increases CNS

GABA. Used for general and partial seizures

and peripheral neuropathy. Tox: sedation,

ataxia.

Ganciclovir, foscarnet

Antiviral: GTP analog that requires activation

by thymidine kinase. Used for CMV. Tox:

neutropenia. Foscarnet does not require

activation.

Gemfibrozil, clofibrate

Antilipemics: stimulate lipoprotein lipase to

convert TGs to FAs. Used in

hypertriglyceridemias and mixed

triglyceridemia/hypercholesterolemia. Tox:

liver (increased LFTs), myositis

Gentamicin, tobramycin, streptomycin

Aminoglycoside: bactericidal, inhibits formation of initiation complex at the 30S subunit. Used against all aerobic GNRs as in sepsis, and will

clear out bowels if given chronically or so intended. Tox: nephrotoxicity (major cause of

acute tubular necrosis), ototoxicity, teratogenic.

Glipizide, glyburide

Oral hypoglycemics: 2nd generation. Close K

+ channels on " cells, depolarize cell, cause

fusion of insulin vesicles w/ membrane. Tox:

hypoglycemia

Griseofulvin

Antifungal: interferes w/ microtubules in

keratinized tissues. Used in topical

dermatophytic infxns.

Guanethidine

Postganglionic sympathetic neuron blocker:

depletes monoamine stores. Ee#ect reversed

by TCAs, cocaine. Tox: severe orthostatic

hypotension, sexual dysfunction

Haloperidol, fluphenazine, thioridazine,

chlorpromazine

Antipsychotic: blocks central dopamine D2 receptors.

Used in schizophrenia, psychosis. Tox: EPS e#ects

(acute dystonia, akinesia, akithisia, tardive

dyskinesia), hyperprolactinemia, antimuscarinic, anti-

!. Less ANS adverse e#ects than phenothiazines.

Neuroleptic malignant syndrome. (“neuroleptics”)

Halothane, isoflurane, enflurane,

methoxyflurane

General anesthetic: inhaled halogenated hydrocarbon, MOA unknown. Cause myocardial

depression, respiratory depression, increased ICP. Halothane is hepatotoxic, enflurane is proconvulsant. All can cause malignant

hyperthermia, particularly w/ succinylcholine.

Heparin

Anticoagulant: large polymeric molecule with

antithrombin, and anti-factor X activity.

Rapid onset. Tox: bleeding, HIT, use

protamine as antidote. LMW-heparins target

Xa w/o PTT monitoring.

HexamethoniumSNS-plegic: nAChR antagonist. Used in HTN.

Tox: orthostatic hypotension, blurred vision

Hydralazine

Antihypertensive: increases cGMP to dilate

arterioles, reduce afterload. Used in HTN,

CHF. Tox: tachycardia, volume retention,

SLE-like

Hydrochlorothiazide

Thiazide diuretic prototype: blocks Na+/Cl-

symporter in distal tubule; Ca2+ is

reabsorbed instead. Used in HTN, CHF,

chronic calcium stones. Tox: hypokalemia,

retention of urate, glucose, lipids, calcium

Ibuprofen

NSAID prototype: short duration. Inhibits

cyclooxygenase (both I and II) reversibly.

Used in arthritis, dysmenorrhea, muscle

inflammation. Tox: peptic ulcer, renal

damage

Imipenem, meropenem

Antibiotic: broad-spectrum carbapenem "-

lactam. Penicillinase-resistant. Used for almost

all infections except VRE and MRSA. Imipenem is

given w/ cilastatin to inhibit renal metabolism.

Tox: PCN allergy, seizures in overdose

Indinavir, saquinivir, others

Antiviral: HIV protease inhibitor. Prevents

cleavage of polyprotein to produce

functional viral enzymes. Tox: bu#alo hump

or truncal obesity, hyperlipidemia. Ritonavir

inhibits P450.

Indomethacin

NSAID prototype: highly potent and acute

(gout). Closes PDA. Tox: ulcers, renal

damage

Infliximab Anti-TF Ab: used in Crohn’s, RA.

Ipratropium

Antimuscarinic agent: aerosol for asthma,

COPD. Good bronchodilator in 20-30% of

patients. 2nd line choice.

Isoniazid

Antimycobacterial: inhibits synthesis of mycolic

acid. Used as part of treatment regimen or for

single prophylaxis of contacts or positive PPD. Fast

or slow metabolism by N-acetyltransferase (genetic

variability). Tox: peripheral neuropathy (reversed by

pyridoxine), G6PD hemolysis, SLE-like, hepatitis

Isoproterenol

"1, "2 agonist: bronchodilator, cardiac

stimulant. Always causes tachycardia

because both direct and reflex actions

increase HR. Tox: AV block (rare), angina

Ivermectin

Antihelminth: activates worm’s GABA

receptor. Used in onchocerciasis (river

blindness)

Ketamine

Dissociative anesthetic: acts at NMDA

glutamate receptor. Stimulates myocardium,

excellent analgesic. Tox: hallucination,

disorientation, nightmares.

Ketoconazole, clotrimazole

Antifungal azole: inhibits fungal P450 to decrease ergosterol synthesis. Used for Candida,

dermatophytes and weak systemic mycoses. Used in PCOS to prevent hirsutism (is antiandrogenic).

Tox: hepatic dysfunction, inhibits steroid synthesis and P450. Clotrimazole is topical.

Labetalol !- and "-blocker: used in HTN. Tox: AV

block, hypotension

Lamotrigine

Anticonvulsant: blocks voltage-gated Na+

channels. Used in partial and general

seizures. Tox: Stevens-Johnson.

Leuprolide

GnRH analog: agonist when pulsatile,

antagonist when continuous. Used for

infertility (pulsatile), prostate ca or

leiomyoma (continuous). Tox: antiandrogen,

N/V.

Levodopa/carbidopa

Dopamine precursor. Used in parkinsonism.

Tox: arrhythmia, dyskinesia, resumption of

Parkinson symptoms between doses (“on-

o#” phenomena)

Lidocaine, mexetiline, tocainide

Class IB antiarrhythmics. Medium duration

amide anesthetic (lido). Shorten AP duration.

Used in ventricular arrhythmias (v-fib,

v-tach), as seen post-MI. Tox: CNS

excitation, CV depression

Lithium

Antimanic prototype: drug of choice in mania and bipolar a#ective disorders; blocks phosphatidyl inositol system. Tox: tremor, hypothyroidism,

nephrogenic diabetes insipidus, narrow therapeutic index, seizures (in overdose),

teratogen (Ebstein’s malformations)

LosartanAngiotensin II receptor blocker. Tox:

hyperkalemia, teratogen (fetal kidneys).

Lovastatin, other “-statins”

Antilipemic: inhibit HMG-CoA reductase to

decrease LDL and increase HDL. Tox: liver

damage (elevated LFTs), myositis

Mannitol

Diuretic: osmotic action creates large volume

of urine. Used in ARF, shock, or to decrease

ICP

Maprotiline

Heterocyclic antidepressant: NE reuptake

inhibitor. Tox: sedation, orthostatic

hypotension

Meperidine

Opioid analgesic: synthetic and taken orally.

Strong agonist at mu opioid receptors, is

anti-muscarinic receptors, so it is the drug

of choice for cholecystectomy analgesia b/c

it prevents sphincter of Oddi spasm.

6-Mercaptopurine

Antineoplastic: blocks purine synthesis. Used

in leukemias & NHL. Myelosuppression

increases with allopurinol (metabolized by

xanthine oxidase).

Metformin

Oral biguanide hypoglycemic: MOA

unknown, may inhibit gluconeogenesis. Can

be used in DM1. Tox: lactic acidosis

Methotrexate

Antineoplastic, immunosuppressant: S-phase specific drug, inhibits dihydrofolate reductase,

decreasing dTMP. Tox: Myelosuppression. Leucovorin (folinic acid) rescue used to reduce

toxicity after very high doses

Metoprolol

"1-selective blocker: used in HTN, CHF, and

for prevention of post-MI sudden death,

arrhythmias. Tox: bradycardia, AV block,

impotence

Metronidazole

Antiprotozoal antibiotic: damages bugs by oxidizing DNA. Used in anaerobic bacterial

infections and Giardia, Entamoeba, Trichomonas, Gardnerella. Tox: GI distress, disulfiram-like

reaction to alcohol. Subject to P450 inhibition or induction

Mifepristone (RU 486)

Progesterone and glucocorticoid inhibitor:

abortifacient (implantation requires

progesterone). Tox: bleeding, GI

disturbances

Milrinone, amrinone

Phosphodiesterase inhibitors: increase

contractility by increasing cAMP. Used in

acute heart failure (as in ICU) only.

Mirtazapine

Heterocyclic antidepressant: antagonist of

!2, central 5-HT receptors. Tox: sedation,

weight gain

Misoprostol

PGE1 derivative: increases mucus barrier and

decreases acid in stomach. Prevents ulcers

due to NSAIDs, maintains PDA, induces

labor. Tox: diarrhea, abortion.

Morphine

Opioid analgesic: strong mu receptor agonist. Poor oral bioavailability. E#ects include analgesia,

constipation, emesis, sedation, respiratory depression, miosis, and urinary retention. Tolerance may be

marked; high potential for psychologic and physical dependence. Additive e#ects with other CNS depressants. Codeine is a morphine prodrug.

Nafcillin, “-oxacillins”

Penicillinase-resistant penicillin. Used for

Staph. Tox: allergy, methicillin is no longer

used but caused interstitial nephritis

Naloxone

Opioid mu receptor antagonist: used to

reverse CNS depressant e#ects of opioid

analgesics (overdose or when used in

anesthesia)

Neostigmine, physostigmine

Cholinesterase inhibitors. “-stigmines” are carbamates that inhibit

cholinesterase by pyridostigmine, edrophonium carbamylation.

Neostigmine: used for postop ileus or neuromuscular blockade

reversal, treatment of myasthenia gravis. Physostigmine: used for

glaucoma (crosses BBB) or atropine overdose. Pyridostigmine: long-

acting, used for treatment of myasthenia gravis. Edrophonium:

short-acting, used to dx myasthenia gravis.

Nevirapine

Nonnucleoside HIV-RT inhibitor: allosteric

inhibition. Others: efavirenz, delavirdine.

Tox: Stevens-Johnson, induction of P450,

insomnia/nightmares

Niacin Antilipemic: reduces VLDL secretion from

hepatocytes. Tox: flushing (reduces w/ use)

Nifedipine

Calcium channel blocker prototype:

vasoselective. Used in angina, HTN. Tox:

edema, flushing, (no arrhythmias b/c not

cardioactive)

Nitroglycerin, nitroprusside

Antianginal vasodilator prototype: releases NO in veins >> arteries. Reduces preload. Used for stable, Prinzmetal angina. Tox: tachycardia,

hypotension, headache. Isosorbide nitrate is long-acting version. Nitroprusside has di#erent but

similar mechanism, can lead to cyanide toxicity.

Nitrosoureas (“-mustines)Antineoplastic: DNA alkylator. Cross BBB, so

used in GBM, other brain ca. Tox: CNS.

Norepinephrine

Agonist at all ! and at "1 adrenoceptors.

Used as ICU pressor but sacrifices renal

blood perfusion. Causes reflex bradycardia.

Tox: renal ischemia, HTN

Octreotide

Somatostatin analog. Used in acromegaly,

carcinoid, gastrinoma, glucagonoma, VIP-

oma, varices

Omeprazole

Antiulcer: irreversible blocker of H+/K+

ATPase proton pump in parietal cells of

stomach. Used in ZE, GERD, ulcers. Tox:

none

Ondansetron, granisetron,

Antiemetics. “-setrons” are 5-HT3 receptor

blockers used for cancer chemotherapy and

Metoclopramide for postop N/V.

Metoclopramide is a dopamine antagonist at

the area postrema.

Orlistat

Antiobesity: inhibits pancreatic lipase. Tox:

steatorrhea, bloating, fat-soluble vitamin

deficiency

Oxybutin, glycopyrrolateAntimuscarinic: target GU system to prevent

incontinence in quadriplegics

OxytocinStimulates labor, uterine contractions, milk

letdown.

Paclitaxel (-“axels”)

Antineoplastic: prevents anaphase by

“freezing” spindle. Used in female cancers.

Tox: myelosuppression.

Parathion, malathion, Echothiophate

Organophosphate acetylcholinesterase inhibitor: used as insecticide, are poisons. Other

organophosphates: DFP, soman, tabun, Causes “DUMBBLSS”: diarrhea, urination, miosis, bronchospasm, bradycardia, lacrimation,

sweating, salivation.

Penicillamine

Chelator, immunomodulator: Cu poisoning

and sometimes Pb, Hg, As. Used in Wilson’s

disease and rheumatoid arthritis

Penicillin G

Penicillin. Used against all GP bugs, GNCs.

Penicillinase-susceptible. Tox: penicillin

allergy, Coombs-positive hemolytic anemia.

Phenelzine, trancylcypromine isocarboxazid

MAOI antidepressant: increase levels of all

monoamines. Only used for psychotic

depression due to side e#ects. Tox: hypertensive

crisis with tyramine or meperidine intake,

serotonin syndrome with tryptophan ingestion

Phenobarbital, thiopental

Barbiturate. Used for sedation, most seizures. Increases duration of GABAA channel opening.

Nonteratogenic: 1st line anticonvulsant in pregnancy. Tox: dependence, CNS/respiratory depression

(additive), induces P450, induces ALA synthase (cannot be used in porphyrics). Thiopental used for induction

of general anesthesia

Phenoxybenzamine, phentolamine

!-blocker. Phenoxybenzamine is

irreversible, phentolamine is reversible. Used

in pheochromocytoma. Tox: orthostatic

hypotension

Phenylephrine !1 agonist: pure pressor for ICU shock.

Phenytoin (carbamazepine, valproate)

Anticonvulsant: blocks neuronal Na+ channels, inhibiting glutamate

release from presynaptic excitatory neuron. 1st line for tonic-clonic

tx, status epilepticus prophylaxis. Serum levels variable due to first-

pass metabolism and dose-dependent nonlinear elimination kinetics.

Tox: nystagmus, ataxia, diplopia, sedation, SLE-like, P450 induction

drug-binding interactions. Chronic: gingival hyperplasia in kids,

peripheral neuropathy, hirsutism, B12 depletion. Teratogen.

Pilocarpine

Muscarinic agonist: used as eyedrops for

narrow or wide-angle glaucoma. Tox:

sweating, salivation

Pioglitazone, “-glitazones”

Oral hypoglycemic: increases insulin

sensitivity. Used alone or in combination.

Tox: weight gain.

Piperacillin, ticarcillin, carbenicillin

GN-active penicillin. Penicillinase-

susceptible; given w/ inhibitor. Used for

Pseudomonas or other GNRs. Tox: allergy.

“Takes Care of Pseudomonas”

Pirenzipine, propantheline

Antiulcer: antimuscarinics active on parietal,

ECL cells. Tox: tachycardia, dry mouth,

diplopia.

Piroxicam NSAID with longest duration of action (t1/2

about 40 h)

Pralidoxime Acetylcholinesterase regenerator: binds

phosphorus in organophosphates toxicity

Praziquantel

Antihelminth: causes parasite paralysis by

calcium-influx pathway. Used in all fluke and

tapeworm infections.

Prazosin, terazosin, doxazosin!1-selective blockers: used in HTN. Tox:

first-dose orthostatic hypotension

Prednisone

Glucocorticoid prototype: potent, short-acting; much less mineralocorticoid activity than cortisol but more than dexamethasone or triamcinolone. Common in chemotherapy, immunosuppression.

May cause apoptosis or inhibit division. Tox: Cushing’s

Probenecid

Uricosuric: inhibitor of renal weak acid

secretion and reabsorption in S2 segment of

proximal tubule; prolongs half-life of

penicillin, inhibits reabsorption of uric acid.

Probucol

Antilipemic: MOA unknown. Withdrawn but

may be e#ective in preventing restenosis of

coronaries after angioplasty. Tox:

arrhythmias, decreased HDL

Propranolol

Nonselective "-blocker prototype. All "-

blockers are also Class II antiarrhythmics,

which slow conduction through AV node.

Tox: see metoprolol.

Propylthiouracil, methimazole

Antithyroid: reduces iodination of tyrosine,

MIT/DIT coupling, peripheral T4-to-T3

conversion (T4 is majority but T3 is more

active). Tox: rash, agranulocytosis (rare),

aplastic anemia.

Prostacyclin PGI2: vasodilator, inhibitor of platelet

aggregation.

Quinidine, amiodarone, procainamide,

disopyramide

Class IA antiarrhythmics and local anesthetics. Slow Phase 0 and increase firing threshold,

increasing AP duration, refractory period. Used for a-fib, a-flutter, v-tach. Tox: cinchonism, torsade (quinidine), SLE-like (procainamide).

Amiodarone is primarily Class III.

Quinine, quinidine

Antimalarial: kill blood forms, no e#ect on

liver stages. Tox: cinchonism, positive

Coombs test

Reserpine

Antihypertensive: depletes monoamine

stores. Used in HTN. Tox: sedation,

depression

Ribavirin

Antiviral: inhibits viral RNA polymerase.

Guanosine analog. Used for RSV, influenza,

HCV. Tox: hemolytic anemia, teratogen.

Rifampin

Antimicrobial: inhibits bacterial RNA

polymerase. Used in TB, leprosy, and for

contacts of those with meningococcal or

H.flu infxn. Tox: orange urine, hepatitis,

induces P450.

Salmeterol"2 agonist: inhaled, long-acting for chronic

asthma. Tox: arrhythmia, tremor.

ScopolamineAntimuscarinic: centrally-active drug for

motion sickness

Selegiline, entacapone,

Dopamine breakdown inhibitors. Selegiline is

selective for MAO-B, “-capones” inhibit

tolcapone COMT

SibutramineAntiobesity: inhibitor of NE, 5-HT uptake.

Tox: HTN, tachycardia.

Sildenafil

Boner pill: phosphodiesterase inhibitor,

causes increased cGMP, relaxation of smooth

muscle. Tox: headache, blue/green vision,

hypotensive crisis w/ nitrates

Somatotropin GH analog. Used in GH deficiency, Turner’s

Sotalol, bretylium, ibutilide

Class III antiarrhythmics. Increase AP

duration, refractory period. 2nd line agents

for atrial and ventricular arrhythmias. Tox:

Sotalol—torsades. Ibutilide—Torsades.

Bretylium—arrhythmogenic.

Spironolactone, amiloride, triamterene

Diuretics: non-K+-wasting. Spironolactone antagonizes aldosterone activity in collecting tubule.

Other 2 block ENaC mobilization by another mechanism. Used in K+-wasting diuresis,

hyperaldosteronism, CHF. Spironolactone has antiandrogenic e#ects (gynecomastia) and can be used

in PCOS to prevent hirsutism.

Streptokinase Thrombolytic: accelerates plasminogen-to-

plasmin conversion. Tox: bleeding, allergy

Succimer (DMSA) Chelator: dimercaptosuccinic acid; used to

chelate Pb and As

Succinylcholine

Depolarizing paralytic: nAChR antagonist selective for motor receptor. Short duration (5

min). No antidote for Phase 1 (depolarized) block, use neostigmine to reverse Phase 2 (repolarized)

block. Contraindicated in any hyperkalemic condition.

Sulfasalazine

Immunosuppressant: sulfa drug + ASA

derivative, activated in gut. Used in

ulcerative colitis, Crohn’s.

Sumatriptan,

5-HT1D receptor agonists. Vasocontrict,

short half-life. Used to abort migraine

attacks. other "-triptans" Tox: Prinzmetal-

like vasospasm, contraindicated in coronary

artery dz

Tamoxifen, raloxifen

Estrogen partial agonists ("SERMs"). Used in

breast ca, osteoporosis prevention.

Tamoxifen increases uterine ca risk.

Tetracycline, doxycycline

Antibiotic: blocks amino-acyl tRNA at 30S subunit. Used for zoonoses, Chlamydia UTI,

atypical pneumonia. Doxycycline is excreted in feces; can use in CKD patients. Tox: bone deformity and dental discoloration in kids,

Fanconi’s syndrome, photosensitivity

Thalidomide

Antiinflammatory: decreases TNF production

to improve leprosy skin symptoms. Tox:

teratogen (causes flipper limbs)

Theophylline

Anti-asthma: phosphodiesterase inhibitor

favors bronchodilation. Lower therapeutic

index. 3rd line agent.

Ticlopidine, clopidogrel

Antiplatelet: blocks ADP receptor to prevent

aggregation. Prevents strokes, occlusion

after angioplasty

Tolbutamide, chlorpropamide

Oral hypoglycemics: older sulfonylurea

group. Tox: hypoglycemia, disulfiram-like

e#ect

Topiramate

Anticonvulsant: Blocks Na+ channels,

increases GABA. Used for general and partial

seizures. Tox: sedation, “mental dulling,”

kidney stones, weight loss

t-PA

Thrombolytic: tissue plasminogen activator.

Used in acute MI to recanalize the occluded

coronary. Occasionally used in pulmonary

embolism, stroke. Tox: bleeding. Antidote is

aminocaproic acid

TrastuzumabAntineoplastic: monoclonal Ab against Her2/

neu. Tox: cardiotoxicity.

TrazodoneHeterocyclic antidepressant: 5-HT reuptake

inhibitor. Tox: sedation, nausea, priapism

Trimethoprim-sulfamethoxazole

Antibiotics: cause blockade at dihydrofolate

reductase and dihydropteroate synthase. Used for

PCP prophylaxis/treatment, Salmonella, pneumonia,

chronic UTI. Tox: sulfa reaction including Stevens-

Johnson and hemolytic anemia, kernicterus in

neonates, may require leucovorin rescue

Tropicamide, topical atropine Antimuscarinic: eyedrops for ophthalmologic

mydriasis

Tubocurarine

Nondepolarizing paralytic: competitive

nAChR antagonist. “-curiums” and “-

curoniums” have di#erent structures. Tox:

histamine release, hypotension. Reverse

blockade w/ cholinesterase inhibitor.

Valproate (carbamazepine, phenytoin)

Anticonvulsant: 1st line for tonic-clonic.

Also used for absence, myoclonic seizures.

Blocks Na+ channels, increases GABA. Tox:

GI distress, hepatic necrosis (rare),

teratogenic (spina bifida)

Vancomycin

Antibiotic: bactericidal glycopeptide inhibitor

of cell wall synthesis. Binds D-ala residues.

Used only against GP bugs, especially MRSA

and C. di#. Tox: “red man syndrome” w/ fast

infusion, ototoxicity, nephrotoxicity

VenlafaxineHeterocyclic antidepressant: monoamine

reuptake inhibitor. Also used for anxiety.

Verapamil, diltiazem

Calcium channel (L-type) blocker prototype: has more depressant e#ect on heart than

dihydropyridines (eg, nifedipine). Class IV antiarrhythmics: slow AV nodal conduction for SVT. Tox: AV block, CHF, edema, constipation.

“The cardiac-specialized CCBs”

Vinblastine, vincristine

Antineoplastic: alkaloid that blocks

microtubule polymerization during M phase.

Used in lymphoma, Wilms. Tox:

myelosuppression. Vincristine – peripheral

neuropathy

Warfarin

Oral anticoagulant prototype: prevents %-

carboxylation of vitamin K-dependent factors (2,

7, 9, 10), making them useless. Tox: bleeding,

teratogenic, drug-drug interactions. Antidote:

vitamin K, fresh plasma. Monitor PT or INR.

Zafirlukast, montelukastAnti-asthma: block leukotriene receptors.

3rd line agent.

Zanamivir, oseltamivir

Antiviral: prevents release of influenza A and

B particles from host cells. Used to treat and

prophylax both influenzae.

Zidovudine (AZT), Didanosine (DDI)

Antiviral: nucleoside inhibitor of HIV RT. Inhibit RT and when incorporated cause production of a defective

virion. Tox: megaloblastic anemia (AZT), pancreatitis (DDI), peripheral neurpathy (DDI). Can be used during

pregnancy to reduce transplacental transmission. Others: lamivudine, stavudine, zalcitabine.

ZileutonAnti-asthma: 5-lipoxygenase inhibitor. 3rd

line agent.