Step 1 Drugs

MicroDrug Class Usepenicillin B-lactam GP (not Staph), Syph

nafcillin S. aureus (not MRSA)dicloxacillinmethicillinampicillin aminoPCNamoxicillinticarcillin Pseudomonas (+AG) and GNRpiperacillin Pseudomonas (+AG) and GNRcarbenicillin Pseudomonas (+AG) and GNRclavulanic acidsulbactamtazobactamcefazolin 1G ceph GPC, Proteus, E. coli, K. pneumocephalexin 1G cephcefoxitin 2G cephcefalcor 2G cephcefuroxime 2G cephceftriaxone 3G ceph

ceftazidime 3G ceph Pseudomonascefipime 4G ceph Pseudomonas and GPaztreonam monobactam GNRs ONLY (no anaerobes)

imipenem/cilastatin carbapenemmeropenem carbapenemvancomycin glycopeptide

gentamicin AG GNR, synergistic w/ B-lactamsamikacin AG GNR, synergistic w/ B-lactamstobramycin AG GNR, synergistic w/ B-lactamsneomycin AG bowel surgery

doxycycline tetracyclinedemeclocycline tetracycline +ADH antagonist (diuretic in SIADH)minocycline tetracycline +meningococcal prophylaxis (2nd line)erythromycin macrolideclarithromycin macrolideazithromycin macrolidechloramphenicol meningitis (H. flu, N. meningitides, S. pneumo)

clindamycin lincosamide anaerobes in aspiration pneumonia

PCNase-resistant PCN

certain GPs (Listeria, enterococci) and GNRs (Proteus, H. flu, E. coli, Salmonella)

extended spectrum PCN

B-lactamase inhibitor

GPC, Proteus, E. coli, K. pneumo, H. flu, Enterobacter, Neisseria, Serratia

Neisseria, gonorrhea prophylaxis, H. flu meningitis

GPC, GNR, anaerobes; broad spectrum, B-lactamase resistant

GPs ONLY, esp MDR (MRSA, Enterococci, and C. diff)

tetracycline

tetracycline I intracellulars: Lyme, H. pylori, M. pneumo, Rickettsia, Chlamydia (no CNS penetration)

atypical pneumonia (Legionella, M. pneumo, Chlamydia), URI, STD, cocci (GP and Neisseria)

sulfa- sulfonamide GP, GN, Nocardia, ChlamydiaSMX +UTI

trimethoprim +SMX

ciprofloxacin FQ GNR (esp of UTI/GI infxn), Neisseria, some GPsenoxacin FQmetronidazole

colistimethane polymyxin resistant GNsdapsone M. leprae (oral, long term), PCPclofazimine M. leprae (added to dapsone)rifampin

INH (isoniazid)

pyrazinamide M. TB (quad tx)ethambutol M. TB (quad tx)pentamidine (aerosolized) PCP (second line, after bactrim)linezolid VREquinupristin streptogramin VREdalfopristin streptogramin VREamphotericin B

nystatin Candida (thrush, diaper rash, vaginal)miconazole azole topical (esp tinea)ketoconazole azole

fluconazole azole Cryptococcal meningitis in AIDS, Candidaflucytosine systemic infxn along with Amphotericin Bcaspofungin Invasive Aspergillosisterbinafinegriseofulvin

pyrimethamine antiprotozoan P. falciparum, +sulfadiazine=toxosuramin antiprotozoan Trypanosomes, no CNS penetrationmelacortin antiprotozoan Trypanosomes, CNS penetrationnifurtimox antiprotozoan T. cruziNa stibogluconate antiprotozoan Leishmaniasischloroquine antiprotozoan Plasmodiummefloquine antiprotozoan Plasmodium (resistant to chloroquine)quinine antiprotozoan chloroquine-resistant Plasmodium when used with pyrimethamine and sulfonamide; Babesia

sulfonamide I

UTIs (tx or prophylactic for recurrent), Shigella, Salmonella, PCP (tx/prophylaxis)

GI protozoa (Giardia, Entamoeba), vaginal (Trichomonas, Gardnerella), anaerobes

M. leprae (delays resistance to dapsone), prophylactic for H. flu and N. meningitides; M. TB (quad tx)

M. TB (quad tx and prophylaxis)

serious systemic mycoses: Histoplasma, Blastomyces, Coccidioides, Aspergillus, Candida, Mucor

Candida, Histoplasma, Blastomyces, PCOS (hirsutism), Coccidioides, hypercortisolism

dermatophytes (esp onychomycosis)oral tx of superficial infxn, esp dermatophytes (tinea, ringworm)

mebendazole antihelminthpyrantel pamoate antihelminth Enterobius, Ascaris, hookwormsivermectin antihelminth Onchocerca, Strongyloidesdiethylcarbamazine antihelminth Loa loa, Wuchereria bancrofti, Toxocara canispraziquantel antihelminth tapeworms and flukesamantidinerimantidine

zanamivir influenza A and Boseltamivirribavirin RSV, chronic hep Cacyclovir HSV (tx and prophylaxis), VZV, EBVfamciclovir herpes zostergangciclovir CMV (mostly in immunocompromised)foscarnet

saquiNAVIR protease I HIVindiNAVIR protease I HIVdidanosine (ddI) HIVzalcitabine (ddC) HIVstavudine (d4T) HIVzidovudine (ZDV) HIV (tx, prophylaxis, pregnancy)nevirapine NNRTI HIVefavirenz NNRTI HIVdelaviridine NNRTI HIVenfuvirtide fusion inhibitor

IFN-α recombinant

IFN-β recombinant MSIFN-γ recombinant NADPH oxidase deficiency

ImmuneDrug Class Mechanismcyclosporine

tacrolimus

sirolimus (rapamycin) inhibits mTOR and TC response to IL-2daclizumab MAb w/ high affinity for IL-2R on activated TCazathioprine

aldesleukin recombinant IL-2erythropoietin recombinant epoetin

GI, Echinococcus, neurocysticercosis

Influenza A (tx and prophylaxis), Parkinson's dz

gangciclovir-resistant CMV retinitis, acyclovir-resistant HSV

nucleoside reverse transcriptase inhibitor

HIV (used in pts w/ persistent viral replication despite HAART)

chronic hep B/C, Kaposi's sarcoma, leukemias, malignant melanoma

Binds cyclophilins, inhibits calcineurin preventing IL-2 and IL-2R production

Binds FK-BP, inhibits IL-2 and IL-2R production (and other cytokines)

antimetabolite precursor to 6-MP (interferes w/ nucleic acid synth)

muromonab-CD3 (OKT-3)

MAb that binds CD3 (epsilon chain) on TC, blocks signal transduction

filgrastim recombinant Granulocyte Colony Stimulating Factorsargramostim recombinant GMacrophage-CSFoprelvekin recombinant IL-11thrombopoietin recombinant thrombopoetindigoxin immune Fab therapeutic abetanercept recombinant form of TNF-R (sequesters TNF)infliximab therapeutic ab anti-TNF-α

adalimumab therapeutic ab anti-TNF-αPharm/Cardio

Drug Class Mechanismmetyrosine inhibits tyrosine hydroxylase (makes DOPA)guanethidine inhibits NE release (replaces it in vescicles)carbachol direct ACh agpilocarpine direct ACh ag

bethanechol direct ACh ag ACh ag, resistant to AChEmethacholine direct ACh ag inhaled, causes bronchoconstrictionedrophonium AChEI extremely short actingneostigmine AChEI no CNS penetration

pyridostigmine AChEI no CNS penetration, long actingphysostigmine AChEI CNS penetrationechothiophate AChEI CNS penetrationtropicamide ACh ant in eyeatropine ACh ant

pralidoxime regenerates AChEscopolamine ACh ant CNSipratropium ACh ant competitive block of MACh-Roxybutynin ACh ant GUglycopyrrolate ACh antmethsopolamine ACh antpirenzepine ACh antpropantheline ACh anthexamethonium nicotinic ag ganglionic blockerepinephrine Symp ag

NE Symp ag α>β1isoproterenol Symp ag βDA Symp ag D>β>α, inotropic and chronotropicdobutamine Symp ag β1>β2, inotropicphenylephrine Symp ag α1>α2

ACh ag, resistant to AChE; contract ciliary m and increase outflow of aq humor

GI (block M1R on ECL cells [decrease histamine] and M3R on parietal cells [decrease H secretion])

vasoconstriction decreases aq humor production; low dose: β>α; high: α>β

metaproterenol Symp ag selective β2 ag (β2>>β1)albuterolsalmeterolephedrine release stored catecholaminescocaine

clonidineα-methyldopaphenoxybenzamine irreversible nonselective α-blockerphentolamine reversible nonselective α-blocker(praz)-osin α1-blocker (smooth m relaxation)carvedilol nonselective α- and β-blockerlabetalol nonselective α- and β-blockernadolol nonselective β-blockerpindolol nonselective partial β-agonistacebutolol β1 partial agonist (>β2)betaxolol selective β1-blockerpropranolol nonselective β-blockertimolol nonselective β-blockeresmolol selective β1-blocker, short-actingatenolol selective β1-blockermetoprolol selective β1-blockerhydralazine vasodilator

nifedipine (DHP) (L-type) CCBverapamil (non-DHP)

diltiazem (non-DHP) reduce mm contractility, ventricle<vessels

nitroglycerin venodilatorisosorbide dinitrate venodilatornitroprusside short acting, same as nitroglycerinfenoldopam D1 ag, relaxes renal vascular smooth mdiazoxide K-ch opener hyperpolarizes/relaxes vascular smooth m -statin HMG-CoA RI inhibits chlsl to mevalonateniacin B3

cholestyramine bile acid resincolesevelamezetimibe prevents chlsl reabs at small intestine brushgemfibrozil fibrate upregulate LPL causing increased TG Cl.

catecholamine reuptake inhibitor, inactivates Na channels

central α2 ag, decrease central adrenergic outflow

AND class II anti-arrhythmics

increased cGMP, relaxing smooth m; arterioles>veins, afterload reduction

reduce mm contractility, ventricle=vessels; nitrate-like antianginal (L-type) CCB

+type IV anti-arrhythmic

reduce mm contractility, ventricle>vessels; β-blocker-like antianginal

release NO in smooth m causing increased cGMP, veins>aa, decrease preload

decreases hepatic VLDL secretion into circ, inhibit lipolysis in adipose tissue

prevents intestinal reabs of bile acids, liver uses chlsl to make more

digoxin cardiac glycoside

procainamidedisopyramidequinidinemexiletinelidocainetocainideflecainideencainidepropafenonesotalolibutilidebretyliumdofetilideamiodarone

adenosine antiarrhythmic

K antiarrhythmic depress ectopic pacemakers in hypokalemiaMg antiarrhythmic

EndocrineDrug Class Mechanismbromocriptine DA ag, inhibits PRL secretioncabergoline DA ag, inhibits PRL secretionmethimazolepropylthiouraciloctreotide

desmopressin (ddAVP) ADH analog; releases endothelial vWF storelisproaspartinsulinNPH intermediateglarginedetemirtolbutamide 1G sulfonyl-ureachlorpropamideglyburide 2G sulfonyl-ureaglimepirideglipizide

inhibition of Na/K ATPase causes indirect inhibition of Na/Ca exchanger; increases [Ca]i, positive inotropy, stimulates vagus

class IA anti-arrhythmics

increase AP duration, effective refractory period, and QT; big gap in phase 3 from normal

class IB anti-arrhythmics

decrease AP duration, preferentially target ischemic/depolarized Purkinje and ventricular tissue

class IC anti-arrhythmics

no effect on AP duration, significantly prolongs refractory period in AV node

class III anti-arrhythmics: K-channel blockers

increase AP duration, effective refractory period, and QT; big gap in phase 3 from normal

increase K outside causes hyperpol and decreased Ca current

inhibits peroxidase-coupling of MIT/DIT and thyroid hormone synthesis

somatostatin analog (in stomach, inhibit ECL cell secretion of histamine)

rapid-acting insulin

bind insulin receptor; liver: increased glycogen synthesis; muscle: increased glycogen and protein synthesis, K uptake; fat: aids TG storage

long-acting insulin

close K-channel in β-cell membrane, causes cell depolarization and triggers Ca influx and insulin release

metformin biguanide

pioglitazonerosiglitazoneacarbosemiglitolpramlintide mimetic decrease glucagonexenatide GLP-1 analog increse insulin, decrease glucagonlevothyroxine thyroxine replacementtriiodothyronineGH hormone replacementoxytocin hormone replacementhydrocortisonebeclomethasonedexamethasoneprednisone + triggers apoptosis

GIDrug Class MechanismfamoTIDINEraniTIDINEcimeTIDINEnizaTIDINEomeprazole PPI irreversibly inhibit H/K ATPase in parietal cellslansoprazolebismuthsucrasulfate

misoprostol

Al(OH)3 antacidMg(OH)2CaCO3sulfasalazine

ondansetron 5HT3 ant, powerful central antiemeticmetoclopramide

Heme/OncDrug Class Mechanismheme and glucose inhibits ALA synthase(RLS of heme synth)pyridoxamine (B6)vitamin A (xs)

heparin

decreases gluconeogenesis, increase glycolysis and peripheral glucose uptake

thiazolidine-diones

increase peripheral insulin sensitivity, binds PPAR-γ

α-glucosidase inhibitor

inhibit intestinal brush border enzymes, delays sugar hydrolysis/absorption

synthetic glucocorticoid

inhibits virtually all cytokines by inactivating NF-kappaB (TNF-alpha transcription factor)

reversible block of H2R on gastric parietal cells causes decreased H secretion

bind to ulcer base, provides physical protection, allows HCO3 secretion

PGE1 analog, increased production of gastric mucous, decreased H production

can affect absorption, bioavailability, and excretion of other drugs (alters pH or delaying gastric emptying)

sulfa- antibiotic + 5-aminosalicylate (anti-inflammatory), activated by bacteria

D2R ant causes increased resting tone, LES tone, motility, contractility

for PML: inhibits retinoic acid receptor causing promyelocyte differentiation

activates antithrombin, acts most on Xa and thrombin; very short t1/2; watch PTT

enoxaparin LMW heparin

(bival)-IRUDIN hirudin directly inhibit thrombinwarfarin

tPAurokinasestreptokinase bind w/ plasminogen, activate plasminogenanistreplase streptokinase bound to plasminogenclopidogrelticlopidineabciximab therapeutic ab glycoprotein IIb/IIIa Ab for activated platelets

methotrexate (MTX)

5-FU

6-MP6-thioguanine (6TG)cytarabine (ara-C) pyrimidine analog, inhibits DNA Poldactinomycin antitumor abx intercalates DNA

daunorubicinbleomycin free radical formation, breaks DNA (G2)(eto)-POSIDE (VP-16) inhibits topoisomerase II (S and G2)cyclophosphamide alkylating agentsifosfamide

busulfan alkylates DNAvincristinevinblastinepaclitaxel -TAXOLs(cis/carbo)-PLATIN cross-link DNAhydroxyurea (S-phase) ribonucleotide reductase inhibitortrastuzumab (herceptin) therapeutic ab

imatinib (Gleevec) NOT AN Ab bcr-abl tyrosine kinase inhibitorrituximab therapeutic ab Ab against CD-20 (on most BC neoplasms)

acts more on Xa, better bioavailability, longer t1/2; subQ, fine if unmonitored

inhibit vitamin K activation, inhibit synth of mature II, VII, IX, X, protein C and S

direct thrombolytic

convert plasminogen to plasmin, which degrades fibrinogen and fibrin

indirect thrombolytic

binds ADPR on platelets, inhibits GpIIb/IIIa expression, inhibits fibrinogen binding

anti-metabolite (all work on S-phase)

folic acid analog, inhibits DHFR, decreasing dTMP and DNA/protein synth

pyrimidine analog, activated to 5F-dUMP, covalently binds DHFR, which inhibits thymidylate synthase, decreasing dTMP

purine analog, inhibits de novo purine synth, activated by HGPRT

doxorubicin (adriamycin)

noncovalently intercalate in DNA causing breaks; generate free radicals

covalently cross-link DNA at guanine N7, require activation by liver

nitrosurea (-mustines)

require bioactivation, cross BBB

microtubule inhibitor (M-phase)

bind tubulin, block polymerization, inhibit mitotic spindle formation

hyperstabilize polymerized microtubules, inhibit mitotic spindle degradation

Ab against HER-2 (erb-B2); possibly kills through Ab-dependent cytotoxicity

Musculoskeletalaspirin (ASA) NSAIDs

ibuprofennaproxenketorolacindomethacincelecoxib reversibly inhibit COX-2 acetaminophen

(etid)-RONATE bisphos-phonateszoledronate (IV)colchicine

probenecid

allopurinol

NeuroDrug Class Mechanismbrimonidine α aglatanoprost

morphine opioid, muRcodeine opioidheroin opioidmeperidine opioiddextromethorphan opioidloperamide opioiddiphenoxylate opioidfentanyl opioidmethadone opioidenkephalin opioid, deltaRdynorphin opioid, kappaRtramadol opioid very weak opioid, SNRIbutorphanol opioid

buprenorphine opioid opioid, partial agphenytoin

fosfentoin parenteralcarbamazepine increased Na channel inactivation

lamotrigine blocks voltage-gated Na channels

irreversibly acetylates COX (1 and 2), prevents conversion of AA to TXA2, PGE2, PGI2

reversibly inhibit COX (1 and 2), blocks prostaglandin synthesis; COX-1 maintains gastric mucosa, COX-2 in inflammatory cells and vascular endothelium

reversibly binds COX, mostly in CNS (peripherally inactivated)

inhibits osteoclast activity, reduce resorption + formation of hydroxyapatite

binds and stabilizes tubulin, impairing chemotaxis and degranulation

inhibits reabsorption of uric acid in PCT, inhibits secretion of PCN

inhibits xanthine oxidase, decreased conversion of xanthine to uric acid

PGF2a (increases outflow of aq humor)

decrease synaptic transmission by opening K-ch and closing Ca-ch; inhibits release of ACh, NE, 5HT, glu, substance P

opioid, partial agonist at mu-R, agonist at kappa-R

also IB anti-arrhythmic

increased Na channel inactivation (increased refractory period), inhibits presynaptic excitatory glutamate release

gabapentin

topiramate blocks Na channels, propagates GABA actionphenobarbital barbiturate

thiopental barbiturate (IV)

valproate

ethosuximide blocks thalamic T-type Ca channelstiagabine inhibit GABA reuptakevigabatrin irreversibly inhibit GABA transaminaselevetiracetam unknown

triazolam short-acting BDZ oxazepammidazolamchlordiazepoxide BDZlorazepamdiazepamzolpidem non-BDZ hypnoticzaleploneszopiclonehalothane

enfluranemethoxyfluranearylcyclohexylamine (ketamine) PCP analog, block NDMA-Rpropofol

succinylcholine

tubocurarinepancuroniumdantrolene

bromocriptine DA ag (ergot derivative)pramipexole DA ag (non-ergot derivative, so preferred)ropiniroleamantidine increases DA releaselevodopa/carbidopa

ente-/tol-capone COMTIbenztropine antimuscarinic (atropine)

inhibits HVA Ca channels (designed as GABA analog)

propagates GABAA action by increasing duration Cl channel is open

high potency, highly lipid soluble; decreases cerebral blood flow

increased Na channel inactivation, increase GABA concentration

MgSO4

increase frequency of Cl channel opening causing propagation of GABAA action; decrease REM

act via BZ1 receptor subtype; reversed by flumazenil

unknown; high blood solubility=slower induction and recovery time; high lipid solubility=high potency=lower MAC

potentiates GABAA

motor nACh-R blocker

phase I=prolonged depol (no antidote, potentiated by neostigmine); II=repol but blocked (antidote=neostigmine)

compete for AChRs, reversible w/ cholinesterase inhibitors

prevents release of Ca from sarcoplasmic reticulum of skeletal mm

converted to DA in CNS; carbidopa= peripheral dopa-decarboxylase inhibitor

reserpine

tetrabenazine amine depleting (DA)memantine NMDA-R ant (prevent excitotoxicity)rivastigmine AChEIdonepezilgalantaminesumatriptan

PsychDrug Class Mechanismthioridazine

chlorpromazinetrifluoperazinefluphenazinehaloperidolquetiapine block 5-HT2, DA, α, and H1 receptorsreisperidonearipiprazoleziprasidoneclozapineolanzapinelithium mood stabilizer

buspirone

desipramineamitriptylinenotriptylineimipramineclomipramine(flu)-OXETINE SSRIsertralinecitalopramvenlafaxine SNRI 5-HT>NE reuptake inhibitorduloxetine 5-HT<NE reuptake inhibitoratomoxitene 5-HT and NE reuptake inhibitor, nonstimulantphenelzine MAOI nonselective MAOI, increase NE, 5HT, DAtranylcypromineisocarboxazidselegiline selective MAO-BI (main metabolyzer of DA)bupropion increased NE and DAmirtazapine

inhibits DA, NE, and 5HT into vescicles (amine depleting)

5HT1B, 1D ag causes vasoconstriction, inhibits V activation and VIP release; short t1/2 (<2h)

antipsychotic (typical, neuroleptic)

block D2R, but can also block muscarinic, α, and histamine receptors, all low potency; highly lipid soluble (long t1/2)

block D2R, high potency; highly lipid soluble (long t1/2)

atypical antipsycotics

unknown (maybe inhibits PI3 cascade), ADH antagonist; exclusively excreted by kidneys, most reabsorbed at PCT with Na

5HT1A agonist

tricyclic anti-depressants

SNRI-like mechanism; amitriptyline=3° (most anticholinergic); notriptyline=2° (least anticholinergic)

usually takes 2-4 weeks for antidepressant effects

atypical anti-depressants 5HT2&3 and α2-blocker (increased NE and DA)

maprotiline blocks NE reuptaketrazodone blocks 5HT reuptakemethylphenidate CNS stimulant release stored catecholaminesamphetaminedexedrine amphetamine

AddictionDrug/Type WithdrawalDepressants anxiety, tremor, seizures, insomniaacute EtOHchronic EtOHStimulants crash, depression, lethargy, wt gain, headachecaffeinenicotine irritability, anxiety, cravingHallucinogensPCP

LSDmarijuana irritability, depression, insomnia, N, anorexia; peak in 48h, last up t

Antidotesdrug class antidotesalicylate NaHCO3 (alkalinize urine), dialysisiron (hemochromatosis) deferoxaminelead 1st line: CaEDTA and dimercaprol, 2nd: penicillamine; succimer for kidsmercury dimercaprol (BAL), succimerarsenic dimercaprol (BAL), succimer, penicillaminegoldcopper (Wilson's) penicillaminecyanide nitrite, hydroxocobalamin, thiosulfatemethemoglobin methylene blue, vitamin CCO 100% O2, hyperbaric O2methanol ethanol, fomepizole, dialysisethylene glycolbenzenenitrofurantoinprocarbazine

RenalDrug Class Mechanismmannitol osmotic diureticacetazolamide carbonic anhydrase inhibitor

ethacrynic acid loop diuretic phenoxyacetate derivative, same as Lasixfurosemide

atypical anti-depressants

severe: DT (life threatening, peaks 2-5d after last drink, ANS hyperactivity [tachycardia, seizures], psychosis, confusion)

depression, anxiety, irritability, restlessness, anergia, thought/sleep disturbances

Amanita phalloides (poison mushroom)

inhibit cotransport of NaK2Cl; lose hyper-tonicity of medulla, increase Ca excretion

hydrochlorothiazide thiazide

eplerenone competitive aldoR antspironolactone + mild testosterone R anttriamterine block ENaC in DCTamiloridecaptopril ACEIlisinoprilenalapril

ReproDrug Class Mechanismleuprolide GnRH ag pulsatile=agonist, continuous=antagonistmethyltestosterone T agonist at androgen receptors

finasteride 5α-reductase inhibitor, lower DHTflutamide nonsteroidal competitive T-receptor antethinyl estradiol estrogen Estrogen receptor antagonistmestranoldiethylstilbestrolclomiphene SERM inhibits negative feedback on hypthalamustamoxifen ag: bone, endometrium; antag: breastraloxifene ag: bone; antag: endometrium, breastHRT

exemestane aromatase inhibitoranastrozoleprogestin

mifepristone (RU-486) competitive progesterone inhibitordinoprostone PGE2 analog (dilation, uterine contraction)terbutaline Symp ag β2ritodrinetamsulosin

sildenafil inhibit cGMP PDE5Ivardenafil

RespiratoryDrug Class Mechanismdiphenhydramine 1G H1 blockers reversible inhibitors of H1 histamine Rchlorpheniramineloratadine 2G H1 blockersfexofenadinedesloratadinecertirizinetheophylline methylxanthine PDEI (decreases cAMP hydrolysis)cromolyn stabilizes mast cell granules

inhibit NaCl reabs in distal tubule, low Ca excretion

K-sparing diuretics

inhibit inactivation of bradykinin (vasodilator); causes renin release by loss of feedback inhibition

reduce growth and vascularization of endometrium

α1A,DR ant (on prostate, α1BR on vessels)

zileuton antiLT 5-lipoxygenase inhibitor (AA to LTs)(zafir)-lukast LT receptor antagonistguaifenesinN-acetylcysteine mucolytic, glutathione precursorbosentan endothelin-1 receptor antagonist (lower PVR)

MicroMechanism

Same as PCN, but bulkier R group

"""for serious gram negative infxn

for serious gram negative infxn"

dehydropeptidase I stable, lower risk of seizures; GI distress, skin rash

binds 23S or 50S and inhibits translocation

binds 50S and inhibits translocation

Bind PBP, inhibit transpeptidase cross-linking of cell wall, and activate autolytic enzymes

Same as PCN, wider spectrum, PCNase sensitive (use with clavulanic acid)

Same as PCN, PCNase sensitive (use with clavulanic acid)

B-lactam, but less susceptible to PCN-ases, bactericidal

inhibits cell wall synth (binds PBP3), B-lactamase-resistant, synergistic w/ AGs

cilastatin=renal dehydropeptidase I inhibitor, decreases inactivation of drug; seizures, GI distress, rash

inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of precursors

bind 30S, inhibit initiation complex, cause misreading of mRNA; require O2 for uptake (no anaerobes); modifying transferase enzymes (acetylation) can lead to resistance

binds 30S and prevents attachment of AA-tRNA; resistance by decreased uptake or increased efflux by pumps (plasmid-encoded); do not take w/ milk, antacids, or Fe (divalent cations inhibit abs)

inhibits 50S peptidyltransferase; plasmid-encoded acetyltransferase inactivates drug

bacterial DHFRase I

free radical toxic metabolites that damage DNA

disrupts membranes (basic cations=detergent)

DNA-dep RNA pol inhibitor

same as amphotericin B

converted to 5FU, inhibits DNA synthβ-glucan cell wall synthesis inhibitorsqualine epoxidase I (ergosterol precursor)

inhibits plasmodial DHFRaseinhibits energy metabolism enzymesinhibits sulfhydryl enzymesforms intracellular oxygen radicalsinhibits glycolysis at PFK

chloroquine-resistant Plasmodium when used with pyrimethamine and sulfonamide; Babesia

PABA antimetabolytes inhibit DHpteroate synthetase; resistance=all mechanisms

topoisomerase II inhibitor; resistance=mutated DNA gyrase

decreased synth of mycolic acid, activated by bacterial catalase-peroxidase

binds ergosterol, forms pores in membrane; does not cross BBB (intrathecal for meningitis)

inhibit fungal ergosterol synthesis by inhibiting P450 enzyme (lanosterol 14-α-demethylase); for systemic mycoses; ketoconazole also inhibits human enzyme desmolase (T-synth)

microtubule inhibitor, deposits in keratin-containing tissues

blocks plasmodium heme polymerase (buildup of toxic hemoglobin products)

inhibits glucose uptake and microtubule synthstimulates depolarization-induced paralysis by stimulating nicotinic receptors at NMJamplifies GABA-mediated inhibition leading to immobilization; doesn't cross BBB (no effect on humans)

increases membrane permeability to Ca (contraction, paralysis)

inhibit neuraminidase

inhibit IMPDH (guanine synthesis)

ImmuneUse

kidney transplant w/ cyclosporine and steroids

kidney transplant

RCC, metastatic melanomaanemias (esp renal failure)

blocks viral penetration/uncoating (M2); also causes release of DA from intact nerves; resistance=mutated M2 (90% of flu A resistant)

guanosine analog: monophosphorylated by viral thymidine kinase, triphosphate made in human cells; leads to chain termination

viral DNA pol inhibitor, binds to PP-binding site, no activation required

prevents cleavage of polypeptide products of pol gene, thus inhibiting virion assembly

competitively inhibit nucleotide binding site on RT causing DNA chain termination; must be activated first by viral thymidine kinase

bind to RT at site different from NRTIs, do not require phosphorylation

bind gp41: inhibit conformational change necessary for fusion with CD4 cells

synthesized by viral infected cells to block replication of DNA and RNA viruses

some autoimmune disorders, suppresses organ rejection

suppresses organ rejection (very strong immunosuppressant)

kidney transplant, autoimmune disorders (including GN, hemolytic anemia, UC)

bone marrow recoverybone marrow recoverythrombocytopeniathrombocytopeniaantidote for digoxin intoxicationCrohn's, RA, psoriatic arthritis

Crohn's, RA, psoriatic arthritisPharm/Cardio

Usehtn from pheo (prevents catecholamine synth)htnglaucoma, causes miosis, relieve IOP

postop and neurogenic ileus/urinary retentionchallenge test for dx of asthmadx of myasthenia gravis

myasthenia gravisglaucoma and atropine ODglaucomacauses mydriasis and cyclopegia +tx of cholinesterase poisoning

with atropine, for cholinesterase poisoningmotion sicknessasthma, COPD

peptic ulcers (rarely used)

used in experiments only

hypotension (but decreases renal perfusion)lowers BP (not used), asthmashock (increases renal perfusion), CHFCHF, cardiac stress testingpupillary dilation, vasoconstriction, nasal decongestion

Crohn's, RA, psoriatic arthritis, ankylosing spondylitis

glaucoma emergency; stimulates sweat, tears, saliva, causes miosis

postop and neurogenic ileus/urinary retention, myasthenia gravis, post-op reversal of NMJ blockade

reduce urgency in mild cystitis and reduce bladder spasms

anaphylaxis, open angle glaucoma, asthma, hypotension

acute asthmaacute asthmalong term asthma (attack prophylaxis)nasal decongestant, urinary incontinence, hypotensioncauses vasoconstriction, local anesthesia

pre-op on pheo

htn, urinary retention in BPH

malignant htnmalignant htnmalignant htnlower LDL>>TG, raise HDL a littlelower LDL>TG, raise HDL a bunch

lower LDL, slightly raise HDL and TG

lower LDLlower TG>>>LDL, raise HDL a little

htn, esp. in renal disease (no decrease in renal blood flow), 1st line in preg (+ hydralazine)

htn (decrease CO, decrease renin secretion [β blockade on JGA cells]), angina (decrease afterload, decrease HR and contractility [via calcium channels] causing decreased O2 consumption), MI (decrease mortality), CHF (slows progression), glaucoma (timolol, carve-dilol, betaxolol, decrease secretion of aqueous humor), antiarrhythmics (VT [even during AFib and AFlutter] and SVT; decrease cAMP, Ca currents, and AV conduction velocity, increase PR); headache, essential tremor (propranolol)

htn in pregnancy (1st line, with methyldopa), severe htn, CHF

htn, angina (incl. Prinzmetal's; nifedipine and virapamil), Raynaud's, arrhythmias (nodal arrhythmias [SVT, eg]: slow conduction velocity, increase refractory period and PR, decrease slope of phase 1)

angina, pulmonary edema, aphrodisiac, erection enhancer, esophageal spasm

dx/tx of SVT; very short acting (~15s)

digoxin toxicitytorsades and digoxin toxicity

EndocrineUsePRLoma, neuroleptic malignant szPRLomahyperthyroidism

central DI, von Willebrand's dz

CHF, AFib (depresses SA node, slow AV nodal conduction); 75% bioavailable, 20-40% protein bound, t1/2=40h, urinary excretion

good for atrial and ventricular arrhythmias, especially reentrant and ectopic SVT, and VT

acute ventricular arrhythmias (esp post-MI) and digitalis-induced arrhythmias (lidocaine)

VT (esp that go to VFib), intractible SVT, last resort in refractory tachyarrhythmias, only in pts w/o structural abnormalities

used when other arrhythmics fail; amiodarone has class I, II, III, and IV effects bc it alters the lipid membrane

GHoma, NET, gastrinoma, glucagonoma, acute variceal bleed, VIPoma, carcinoid tumor

DM, gestational DM, life-threatening hyperkalemia, stress-induced hyperglycemia

T2DM (stimulates endogenous release of insulin, need some β-cell function, so useless in T1DM)

T2DM (monotherapy or combo)

T2DM (monotherapy or combo)

T2DMT2DMhypothyroidism, myxedema

GH deficiency, Turner'sstimulates labor, uterine contractions, milk let-down, controls uterine hemorrhage

+ dx of Cushing's dz (suppression test) + CLL, Hodgkins

GIUsePUD, gastritis, mild esophageal reflux

PUD, gastritis, esophageal reflux, Zollinger-Ellison Sz

all cause hypokalemia

UC, Crohn's

decrease vomiting (post-op, chemo)

Heme/OncUseacute intermittent porphyriasideroblastic anemia, prevent neurotoxicity and lupus from INHacne, PML (AML M3)

oral, can be used in pts w/o islet function (T1 or 2DM)

Addison's, inflammation, immune suppression (Crohn's), asthma (1st line for chronic)

improved ulcer healing, traveller's diarrhea, + metronidazole + amoxicillin (or tetracycline) for H. pylori

prevention of NSAID-induced ulcer, induce labor, maintenance of ductus arteriosus

gastroparesis (DM or post-surgery), does not influence colon transport time

immediate anticoagulation: PE, CVA, acute coronary sz, MI, DVT; safe for pregnancy

heparin alternative in HITchronic anticoagulation, oral

early MI, early ischemic stroke

leukemia or lymphoma (not CLL or HL), UCALLAML, ALL, high grade NHL

Hodgkins, myelomas, sarcomas, solid tumors

testicular and HodgkinsSCC of lung/prostate, testicular

brain tumors (including glioblastoma multiforme)

CML, pre-marrow-transplant marrow ablationHodgkins, Wilm's, chorioca

ovarian and breast

testicular, bladder, ovary, lungmelanoma, CML; sickle-cell (increase HbF)HER-2-overexpressing breast cancer

CML (Philadelphia chr., main target), GISTBC non-Hodgkin's lymphoma, RA (+ MTX)

immediate anticoagulation: PE, CVA, acute coronary sz, MI, DVT; safe for pregnancy

acute coronary sz, coronary stenting, decrease risk of thrombotic stroke

prevent cardiac ischemia in unstable angina and in pts txed w/ percutaneous coronary intervention, acute coronary sz

leukemia, lymphoma, chorioca, sarcomas; abortion, ectopic pregnancy, RA, psoriasis

solid tumors, topical for basal cell ca, synergistic w/ MTX

Ewing's sarcoma, rhabdomyosarcoma, childhood tumors (Wilm's)

NHL, breast, ovarian; also good immunosuppressants

Musculoskeletal

+ induces closure of PDA, nephrogenic DIRA, OA, pts w/ gastritis/ulcersantipyretic, analgesic, NO anti-inflammatory

acute gout (with NSAIDs, esp indomethacin)

NeuroUseglaucomaglaucoma

pain, acute pulmonary edema

+ cough suppression + diarrhea + diarrhea(stronger than morphine)(partial ag, long acting) opioid addictionendogenousendogenouschronic painpain

pain, opioid addiction, used w/ naloxone

partial and tonic clonic

low dose (<300mg/day, TXA2): antiplatelet; intermed dose (300-2400mg/day, PGE2): antipyretic and analgesic; high dose (2400-4000mg/day): anti-inflammatory

antipyretic, analgesic, anti-inflammatory, acute gout (w/ colchicine, esp indomethacin), migranes

malignancy-associated hypercalcemia, Paget's dz of bone, postmenopausal osteoporosis

chronic gout, also given w/ PCN to prolong t1/2

chronic gout; lymphoma/leukemia w/ chemo to prevent tumor lysis urate nephropathy

seizures (all but absence), first line for tonic clonic or status prophylaxis, arrhythmias (IB)

partial, tonic clonic (1st line), trigeminal neuralgia (1st line), bipolar

partial and tonic clonic

absence (first line)partial seizurespartial seizurespartial and tonic cloniceclamptic seizures (1st line)

insomnia

dissociative anestheticrapid anesthesia induction

non-depolarizing paralytic

Parkinson , PRLomaParkinson

Parkinson; influenza A, rubellaParkinson

ParkinsonParkinson (tremor and rigidity, not bradykinesia)

partial and tonic clonic, peripheral neuropathy, bipolar

partial + tonic clonic (esp in pregnancy/kids), anxiety, insomnia, Crigler-Najjar Sz type II

induction of anesthesia (decrease cerebral blood flow)

seizures (all but status, first line in tonic clonic), myoclonic seizures, bipolar

anxiety, spasticity, detox (esp EtOH withdrawal and DT), night terrors, sleepwalking, general anesthetic, insomnia, cocaine OD, panic disorder, GAD

+ status epilepticus (first line) or eclamptic seizures (after MgSO4)

inhaled anesthetic (increase cerebral blood flow, depress CV/resp)

depolarizing paralytic (for pts on a mechanical vent or during surgery)

malignant hyperthermia and neuroleptic malignant syndrome

Huntington

HuntingtonAlzheimer'sAlzheimer's

Migrane, cluster headache

PsychUse

+ Huntingtonschizophrenia (positive and negative sx)

+ OCD, anxiety, depression, mania, Tourette's

GAD, anxiety

major depression, fibromyalgia, panic disorder

+ bedwetting + OCD

depression, GADdepression, diabetic peripheral neuropathyADHD

+ Parkinson (use w/ L-dopa)bipolar, depression, smoking cessation

schizophrenia (mostly positive sx), psychosis, mania (acute), Tourette's (esp haloperidol)

bipolar, blocks relapse and acute manic events; SIADH

OCD, bulimia, social phobia, specific phobia, panic disorder, PTSD, GAD, anorexia/bulimia, anxiety, depression (a-/typical)

atypical depression, anxiety, hyperchondriasis

bipolar, depression, insomnia

bipolar, depressioninsomnia, depression (very high doses)narcolepsy, obesity, ADHD

ADHDAddiction

Intoxicationmood elevation, decreased anxiety, sedation, behavioral disinhibition, respiratory depression

mood elevation, psychomotor agitation, insomnia, arrhythmias, tachycardia, anxietyrestlessness, diuresis, muscle twitchingrestlessness

fever, nystagmus, tachycardia, psychomotor agitation, belligerence, impulsiveness, homocidality, delerium

paranoid delusions, slowed time perception, social withdrawal, dry mouth, hallucinationsAntidotes

SFX/othernot for gout (need too high of a dose)

1st line: CaEDTA and dimercaprol, 2nd: penicillamine; succimer for kids

can be from nitroprusside (tx for malignant htn)created by nitrite bc it binds CN strongly

aplastic anemiahemolysis in G6PD deficiencydisulfiram-like rxn w/ EtOHhepatotoxicity/necrosis

RenalUseshock, drug OD, increased ICP/IOPglaucoma, urinary alk, MAlk, altitude sickness

diuresis in sulfa-allergies or gout pts

emotional lability, ataxia, coma, serum GGT (sensitive EtOH use), AST>2*ALT; acute EtOH=P450 down; chronic EtOH=P450 up, gynecomastia

flashbacks, pupillary dilation, marked anxiety/depression, delusions, visual hallucinations

edema (CHF, cirrhosis, nephrotic sz, pulmonary edema), htn, hypercalcemia

htn, CHF, idiopathic hypercalciuria, nephrogenic DI

+ nephrogenic DIhtn, CHF, diabetic renal dz

ReproUseinfertility, prostate ca (+ flutamide), fibroids

BPH, male pattern baldnessprostate cancer (+ leuprolide)

ovulation inductionbreast cancer (ER-positive), prevent osteoporosis

pregnancy termination (+ misoprostol)labor inducerreduce premature uterine contractions

BPH (inhibits only prostatic smooth m)

ED

RespiratoryUseallergy, motion sickness, sleep aid

allergy

asthma, adenosine toxicityonly for asthma/allergy prophylaxis, not tx

hyperaldo, K-depletion, CHF, hirsutism (spironolactone)

hypogonadism, develop 2° sex characteristics, burn pts (promotes anabolism)

hypogonadism, POF, menstrual abnormailities, postmenopausal HRT, androgen-dependent prostate cancer

menopausal sx (hot flashes, vaginal atrophy, osteoporosis [E2 decreases osteoclast activity])

ER-positive breast cancer in postmenopausal women

oral contraceptives, endometrial cancer, abnormal uterine bleeding

asthmaasthma (especially aspirin-induced)expectorantloosen plugs (CF), acetaminophen ODpulmonary htn

MicroSFx/Other

same as PCN

+interstitial nephritispseudomembranous colitis +higher oral availability; rash

dehydropeptidase I stable, lower risk of seizures; GI distress, skin rash

+fecally eliminated (can be used in pts w/ renal failure) +diabetes insipidus

bacteriocidal; G=IV, V=oral; can cause hypersensitivity rxn (all PCNs) or hemolytic anemia, SJS

Hypersensitivity (cross hypersensitivity with PCNs in 5-10%), vitamin K deficiency, disulfiram-like rxn with EtOH (only in some cephalosporins), increase nephrotoxicity of aminoglycosides

no cross-allergenicity w/ PCN or cephalosporins, good in renal insufficiency; occasional GI upset

cilastatin=renal dehydropeptidase I inhibitor, decreases inactivation of drug; seizures, GI distress, rash

rarely SFx: nephrotoxicity + ototoxicity, thrombophlebitis, "red man syndrome" (preventable by slow infusion)

nephrotoxic (especially when used w/ cephalosporins), ototoxic (especially when used w/ loop diuretics), teratogenic (CN VIII agenesis)

GI distress, teratogen (teeth discoloration), bone growth inhibition in kids, hypersensitivity; expired causes Fanconi's

prolonged QT, GI discomfort, acute cholestatic hepatitis (avoid in liver disease), eosinophilia, skin rashes; P450 down (increases efficacy of theophylline and oral anticoagulants)

anemia (dose dependent), aplastic anemia (dose ind), gray baby sz (in preemies, lack of UDP-glucuronyl transferase)

pseudomembranous colitis, fever, diarrhea

neurotoxic, nephrotoxic (acute renal tubular necrosis)

orange body fluids, minor hepatotoxicity, ups P450

topical (too toxic for oral)

+ can cross BBBN/V/D/bone marrow suppression, nonmegaloblastic macrocytic anemiaGI upset, flushing

hypersensitivity, SJS, hemolysis (G6PDD), nephrotoxic (tubulo-interstitial nephritis), teratogen (kernicterus), photosensitive, megaloblastic anemia, P450 down

pancytopenia (leuko-, granulocyto-, megaloblastic anemia; may alleviate w/ supplemental folinic acid [leucovorin rescue])

GI upset, superinfxns, tendonitis/rupture (not for pregnant women/kids), headache, dizziness, rash

metallic taste, disulfiram-like effect w/ EtOH, headache, mutagenesis

hemolysis, methemoglobimemia, agranulocytosis

neurotoxic (seizures), hepatitis, lupus; pyridoxine (B6) can prevent neurotoxicity and lupus; hemolytic in G6PD deficiency, P450 down

fever/chills, hypotension, nephrotoxicity (reduced by hydration), arrhythmias, IV phlebitis, anemia

liver dysfunction (P450 inhibitor), fever, chills + hypocortisolism (blocks hormone synthesis in adrenals), gynecomastia, amenorrhea

teratogen, carcinogen, confusion, headache, increase P450 and warfarin metabolism

primaquine=hemolytic anemia in G6PD deficiencycinchonism (flushing, sweating, tinnitus, blurred vision, confusion, rash, abdominal pain, N/V/D, headache, vertigo)

stimulates depolarization-induced paralysis by stimulating nicotinic receptors at NMJamplifies GABA-mediated inhibition leading to immobilization; doesn't cross BBB (no effect on humans)

increases membrane permeability to Ca (contraction, paralysis)ataxia, dizziness, slurred speech

hemolytic anemia, teratogen (severe)no effect on latent virus; resistance=lack of viral thymidine kinase

thrombocyto-/leuko-/neutro-penia, nephrotoxicnephrotoxic; resistance by mutated DNA pol

+thrombocytopenia

+megaloblastic anemia

hypersensitivity, increased risk of bacterial pneumonia

neutropenia

neutropenianeutropenia

ImmuneSFx/Other

hyperlipidemia, thrombocytopenia, leukopenia

cytokine release syndrome, hypersensitivity rxn

doesn't cross BBB, fewer CNS SFx m

hyperglycemia, N/D, lipodystrophy, P450 inhibition

bone marrow suppression (can be reversed with GCSF and erythropoietin), peripheral neuropathy, lactic acidosis

bone marrow suppression (can be reversed with GCSF and erythropoietin), peripheral neuropathy, rash

nephrotoxic (prevented by mannitol diuretic), higher risk for viral infxn and lymphoma

significant: nephrotoxicity, peripheral neuropathy, htn, pleural effusion, hyperglycemia

bone marrow suppression, worsened w/ allopurinol (6-MP broken down by xanthine oxidase), nonmegaloblastic macrocytic anemia

respiratory infxn (reactivation of latent TB), fever, hypotension

Pharm/CardioSFx/Other

tx OD w/ physostigmine salicylate

+ tachycardia, dry mouth, difficulty focusing eyes

severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction

tachycardia

pupillary dilation, vasoconstriction, nasal decongestion

exacerbation of COPD, asthma, and peptic ulcers; severe/OD on AChEI: DUMBBELS=diarrhea, urination, miosis, bradycardia, bronchospasm, excitation of CNS and skeletal mm, lacrimation, sweating, salivation

constipated, urine retention, mydriasis, cyclopegia, acute angle closure glaucoma, bronchodilation, tachycardia, disorientation, increased temp, and dry eyes, skin (flushed), and mouth

tremor, arrhythmianasal decongestant, urinary incontinence, hypotension

direct Coombs-positive hemolytic anemiaorthostatic hypotension, reflex tachycardia

1st dose orthostatic hypotension, dizziness, headache

CN toxicity

hyperglycemia (reduces insulin release)hepatotoxicity, rhabdomyolysis

rare increase in LFTmyositis, hepatotoxicity (LFT), chlsl gallstones

abnormal fetal, fetal addiction, placental abruption, coronary vasospasm; OD: pupil dilation, hallucinations (esp tactile), paranoid, angina, tx=BDZ; withdrawal: suicidal, hypersomnolent, malaise

impotence, exacerbation of asthma, CV effects (bradycardia, AV block, CHF), CNS effects (sedation, sleep alteration), caution in DM (tx OD w/ glucagon), partial agonists (pindolol and acebutolol) contraindicated in angina; metoprolol can cause dyslipidemia

reflex tachycardia (contraindicated in angina/CAD, commonly given w/ β-blocker), Lupus-like sz

cutaneous flushing, cardiac depression, AV block, peripheral edema, dizziness, constipation

reflex tachycardia, hypotension, flushing, headache (esp when used on Monday after loss of tolerance over weekend; tolerance common)

cutaneous flushing (esp face), hyperglycemia, acanthosis nigricans, hyperuricemia

pts hate it: tastes bad, GI discomfort, decreased abs of fat soluble vitamins, chlsl gallstones

Lupus-like sztoxicity increased w/ hyperkalemia (all class I)

Torsades, excessive β-blocktorsadesnew arrhythmias, especially w/ hypotension

EndocrineSFX/other

+ hepatotoxicitynausea, cramps, steatorrhea

given intranasal for DIhypoglycemia, hypersensitivity (very rare)

hypoglycemia

gynecomastia, cholinergic (N/V/D), blurry yellow vision, ECG (high PR, low QT, scooping, inverted-T, arrhythmia), hyperK; OD worse w hypoK, renal failure, and quinidine (decreased clearance); tx OD w/ digoxin immune Fab, slowly normalize K, lidocaine, cardiac pacer, Mg

Torsades, cinchonism (tinnitus, headache), thrombocytopeniaCNS stimulation/depression, CV depression, toxicity increased w/ hyperkalemia (all class I)

proarrhythmic, esp post MI (contraindication), toxicity increased w/ hyperkalemia (all class I)

pulmonary fibrosis, hepatotoxicity, thyroid dysfunction (40% I by wt), hypersensitivity, corneal deposits, photodermatitis, blue/gray skin deposits, CNS effects, constipation, CV effects (bradycardia, heart block, CHF, NOT TORSADES)

cutaneous flushing, hypotension, chest pain (blocked by theophylline)

skin rash, aplastic anemia, agranulocytosis (rare)

disulfiram-like effect w/ EtOH, hypoglycemia

lactic acidosis (contraindicated in renal failure)

weight gain, edema, hepatotoxicity, CV toxicity

GI disturbances

hypoglycemia, N/DN/V, pancreatitistachycardia, heat intolerance, tremors, arrhythmias

stimulates labor, uterine contractions, milk let-down, controls uterine hemorrhage

GISFX/other

diarrhea, abortifacient

constipation, hypophosphatemia, mm weakness, osteodystrophy, seizurediarrhea, hyporeflexia, hypotn, cardiac arresthyperCa, rebound acid level, chelates other drugs malaise, nausea, sulfa, reversible oligospermia

headache, constipation

Heme/OncSFX/other

sideroblastic anemia, prevent neurotoxicity and lupus from INH

iatrogenic Cushing's (incl. osteoporosis, peptic ulcers, and DM), adrenal insufficiency when drug stopped after chronic use

none (most H2 blockers); cimetidine: P450 down, gynecomastia (antiandrogenic, PRL release, impotence, decreased libido), can cross BBB (confusion, dizziness, headaches); ranitidine and cimetidine: decrease renal excretion of creatinine

Parkinsonian, restlessness, drowsiness, depression, N/D; interacts w/ digoxin and diabetic agents; contraindicated in SI obstruction

teratogen (spontaneous abortion, cleft palate, cardiac abnormalities); when txing PML, can release Auer rods and cause DIC

follow PTT; bleeding, thrombocytopenia (HIT), osteoporosis; antidote= protamine sulfate (positive, binds heparin)

not easily reversible, similar sfx

neutropeniableeding, thrombocytopenia

myelosuppression (thymidine rescue), photosensitivity

marrow depression, can be given w/ allopurinolleukopenia, thrombocytopenia, megaloblastic anemiamyelosuppression

myelosuppression, GI irritation, alopecia

neurotoxic (areflexia, peripheral neuritis), paralytic ileusbone marrow suppressionmyelosuppression, hypersensitivity

nephrotoxic, ototoxicnonmegaloblastic macrocytic anemia, GI upsetcardiotoxic

fluid retention

monitor PT, metabolized by P450, teratogen (crosses placenta); skin/ tissue necrosis; antidote=vitamin K; for more rapid reversal, give FFP; teratogen (bone deformities, fetal hemorrhage, abortion)

bleeding, treat toxicity with aminocaproic acid (plasminogen activation inhibitor)

myelosuppression (leucovorin rescue), macrovescicular fatty liver change, mucositis, teratogenic; tx OD by alkalinizing urine

nonmegaloblastic macrocytic, GI, liver; increased toxicity w/ allopurinol

cardiotoxicity (dilated CM), myelosuppression, alopecia; toxic to tissues with extravasation

pulmonary fibrosis, skin changes, minimal myelosuppression

myelosuppression, hemorrhagic cystitis (lessened by mesna, better control w/ ifosfamide); SIADH for cyclophosphamide; aplastic anemia

CNS toxicity; all alkylating agents: teratogen (missing digits), aplastic anemia

pulmonary fibrosis, hyperpigmentation, aplastic anemia

Musculoskeletal

higher risk of thrombosis, sulfa allergy, lower incidence of GI sfx

corrosive esophagitis, N/D, osteonecrosis of jaw no corrosive esophagitis (IV)

NeuroSFX/otherno pupillary or vision changesdarkens iris

similar to opioids, decreases seizure thresholdless respiratory depression, causes withdrawal if on full ag

SJS

all NSAIDs: inhibit dilation of afferent arteriole, drop GFR (acute renal failure), intersitial nephritis and aplastic anemia; hemolytic anemia in G6PDD, gastric upset/ulceration, UGI bleed, tinnitus (CN VIII); Reye's syndrome in kids (esp w/ viral infxn)

interstitial nephritis, aplastic anemia, fluid retention, GI distress, ulcers; ibuprofen: hemolytic anemia in G6PDD

no Reye's sz, but OD causes hepatic necrosis (metabolyte depletes glutathione and forms toxins in liver), N-acetylcysteine is antidote

GI side effects, agranulocytosis

SJS, increases concentrations of azathioprine and 6-MP (both metabolyzed by xanthine oxidase, give 6-tG instead of 6-MP)

Respiratory depression, miosis (pinpoint pupils), additive CNS depression with other drugs, addiction, constipation, N/V; tolerance does not develop to miosis and constipation; -OD (life-threatening) txed w/ naloxone or naltrexone (opioid ant) -withdrawal: sweating, dilated pupils, piloerection ("cold turkey"), fever, rhinorrhea, N/D/stomach cramps (flu-like); symptomatic tx -heroin: high risk for hepatitis, abscess, OD, hemorrhoids, AIDS, RHF

nystagmus, diplopia, ataxia, sedation, teratogen (fetal hydantoin sz), Lupus-like sz, gingival hyperplasia, hirsutism, peripheral neuropathy, megaloblastic anemia (low folate absorption), P450 induction, SJS

diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenic, P-450 induction, SIADH, SJS

sedation, ataxia

sedation, mental dulling, kidney stones, weight loss

proconvulsantnephrotoxicityCV stimulant, disorientation, hallucinations, bad dreams, increase cerebral BFless post-op nausea than thiopental

can cause hyperCa, hyperK, malignant hyperthermia

reversal: AChEI (neostigmine, edrophonium)

can cause ataxia

sedation, tolerance, dependence, P-450 induction (contraindicated in porphyria), CNS depression (additive w/ EtOH), SJS; OD: respiratory/ cardiac depression (can cause death), supporative tx and HCO3

- (alkalinize urine); withdrawal: delerium, CV collapse (life-threatening)

GI distress, hepatotoxicity/necrosis (can be fatal, measure LFTs), teratogen (neural tube defects), tremor, weight gain

fatigue, GI distress, headache, urticaria, SJS

much larger safety margin than barbiturates, and less respiratory depression; usually long t1/2 and active metabolites (short acting BDZs have higher addictive potential); sedation, tolerance, dependence, CNS depression (additive w/ EtOH); OD: ataxia, minor respiratory depression; tx=flumazenil (competitive antagonist at GABA-R)

short t1/2 (rapidly degraded in liver), so less day-after SFX; ataxia, headaches, confusion; lower dependence risk than BDZ

hepatotoxicity/necrosis, malignant hyperthermia (all but N2O)

arrhythmias from peripheral conversion to DA; long term can cause dyskinesia following dose, akinesia between doses

Parkinson-like sz

dizziness, confusion, hallucinationsN/V, dizziness, insomnia

PsychSFX/other

far fewer extrapyramidal and anticholinergic SFx than neuroleptics

wt gain

no sedation, addiction, tolerance, EtOH interaction (BDZ/barbiturates)

stimulant effects (htn most common), sedation, nausea

+ may enhance SFX from levodopa

sedation, increased appetite, dry mouth, increased serum cholesterol

coronary vasospasm (don't use in pts with CAD or Prinzmetals angina), mild tingling

dry mouth, constipation, hypotn, sedation; corneal (chlorprom-) or retinal (thiorid-) deposits; both: neuroleptic malignant sz: autonomic instability, myoglobinuria, rigidity, hyperpyrexia, encephalopathy

extrapyramidal (4h=dystonia [mm spasm]; 4d=akinesia [parkinsonian]; 4wk=akathisia [restlessness]; 4mo=tardive dyskinesia [irreversible stereotypic oral-facial movements from long-term use]), hyperPRL

wt gain, agranulocytosis (requires weekly WBC monitor)

teratogen (atrialized RV [Ebstein's anomaly, malformation of great vessels]), hypothyroid, nephrogenic DI, sedation, edema, heart block, tremor; narrow therapeutic window

sedation (least=desipramine), convulsions (most=desipramine), α-blocking and anticholinergic (tachycardia, arrhythmias, urinary retention, confusion, hallucinations; 3°>>>2°), hyperpyrexia; tx OD w/ NaHCO3 (alkalinize urine)

less than TCAs: GI distress, sexual dysfunction, "Seratonin sz" (drug interactions, too much 5-HT causes HyperThermia, HyperTonism, CV collapse, flushing, diarrhea, seizures; tx=cyprohepadine [5HT2 ant])

htnsive crisis (w/ tyramine ingestion and beta-ag), CNS stimulation, contraindicated w/ SSRIs or meperidine (prevent seratonin sz)

stimulant effects (tachycardia, insomnia), headache, seizure in bulimia

sedation, orthostatic hypotensionsedation, nausea, priapism, postural hypotension

AddictionIntoxicationmood elevation, decreased anxiety, sedation, behavioral disinhibition, respiratory depression

mood elevation, psychomotor agitation, insomnia, arrhythmias, tachycardia, anxietyrestlessness, diuresis, muscle twitching

teratogen (preterm labor, placental problems, IUGR, ADHD)

fever, nystagmus, tachycardia, psychomotor agitation, belligerence, impulsiveness, homocidality, delerium

paranoid delusions, slowed time perception, social withdrawal, dry mouth, hallucinationsAntidotes

RenalSFX/otherpulmonary edema, dehydration, contraindicated in anuria and CHF

OD: pupil dilation, prolonged wakefulness, delusions, hallucinations, fever; withdrawal: stomach cramps, hunger, hypersomnolent

emotional lability, ataxia, coma, serum GGT (sensitive EtOH use), AST>2*ALT; acute EtOH=P450 down; chronic EtOH=P450 up,

, pupillary dilation, marked anxiety/depression, delusions, visual hallucinations

hyperchloremic MAc, neuropathy, NH3 toxicity, sulfa

ototoxicity, hypokalemia, dehydration, interstitial nephritis + sulfa allergy and gout

hyperkalemia, MAc endocrine SFx (antiandrogen, gynecomastia, amenorrhea)hyperkalemia, MAc

ReproSFX/otherantiandrogen, N/V

gynecomastia

teratogen (vaginal clear cell adenoC)

heavy bleeding, N/V, anorexia, abdominal pain

RespiratorySFX/othersedation, antimuscarinic, anti-alpha-adrenergic

less entry to CNS than 1G, so far less sedation

narrow TI (OD=beta-blocker), cardio-/neuro-toxic, metabolized by P450

hypokalemic MAlk, hyponatremia (low big 3), hyperglycemia, hyperlipidemia, hyperuricemia (gout), hypercalcemia, sulfa allergy

cough (not ARBs), teratogen (renal damage), angioedema, proteinuria, taste change, hypotn, rash, hyperkalemia; avoid in bilateral renal artery stenosis (decrease GFR by preventing constriction of efferents)

masculinization in females, reduces intratesticular testosterone in males (inhibits LH) causing gonadal atrophy, premature closure of epiphyseal plates, raise LDL, lower HDL

endometrial cancer, postmenopausal bleeding, VTE; contraindications: ER-positive breast cancer, hx of DVTs

hot flashes, ovarian enlargement, multiple pregnancies, visual disturbancesendometrial carcinoma, hot flashes

unopposed estrogen RT increases the risk of endometrial cancer (P added), possible increased CV risk

headache, flushing, dyspepsia, impaired blue-green color vision, life-threatening hypotn in pts taking nitrates

does not suppress cough reflex

P450 interactions endingup down -afilbarbiturates sulfonamides -anephenytoin erythromycin -azepamcarbamazepine cimetidine -zolamgriseofulvin ketoconazole -azinerifampin isoniazid -azolechronic EtOH use acute EtOH use -barbitalSt. John's Wort grapefruit juice -cainequinidine HIV protease inhibitors -cycline

-etine -ipramine -navir -operidol -oxin -phylline -terol

slow AV nodal conduction II, IV, dig -tidine -triptan -triptyline

function exampleerectile dysfunction sildenafilinhalational general anesthetic halothaneBDZ diazepamBDZ alprazolamphenothiazine (neuroleptic, antiemetic) chlorpromazineantifungal ketoconazolebarbiturate phenobarbitallocal anesthetic lidocaineprotein synth inhibiting abx tetracyclineSSRI fluoxetineTCA imipramineprotease inhibitor saquinavirbutyrophenone (neuroleptic) haloperidolglycoside (inotrope) digoxinmethylxnthine theophyllineβ2 ag albuterolH2 ant cimetidine5HT1B/1D ag (migrane) sumatriptanTCA amitriptyline

nonselective α- and β-blocker carvedilol, labetalolnonselective β-blocker nad, propran, timnonselective partial β-agonist pindselective β1-blocker betax, esm, aten, metoprβ1 partial agonist (>β2) acebut

Cardiodisease txessential htn diuretics, ACEI, ARBs, CCBhtn in CHF diuretics, ACEI, ARBs, CCB, β blockershtn in DM ACEI, ARBs, CCB, diuretics, β-blocker, α-blockermalignant htn nitroprusside, fenoldopam, diazoxideangina nitrates and β-blockersAFib digoxin, β-blockers, anticoag, non-DHPAFlutter ablation, anticoag, non-DHPSVT class IA/C, class II, class IV, adenosineVT class I, class II

Neurodisease txtonic clonic seizure first line: phenytoin, carbamazepine, valproateabsence seizure first line: ethosuximide; otherwise, valproatestatus seizure acute: BDZ; prophylaxis: phenytoin

Cardioother

no β blockers in decompensated CHF, esp K-sparing diureticsACEI protective against diabetic nephropathy

Neuro

first line in pregnancy and children: phenobarbital

NeuroName SxHuntington

Parkinson

Alzheimer dementia, can get intracranial hemorrhage

Pick's Dz (FTD)

LBD Parkinsonism w/ dementia and hallucinationsCJD rapidly progressive dementia with myoclonusNPH urinary incontinence, ataxia, dementia

MS

pellagra diarrhea, dementia, dermatitis (glossitis)Renal

Immune depositsSub-epithelialMembranous GNPostinfectious GNLupus nephritis V

Immunofluorescence PatternGranularMembranous nephropathyPostinfectious GNMembranoproliferative GN

Other Characteristics

Diffuse Glomerular ProliferationPostinfections GNMembranoproliferative GNSLE

agression, depression, dementia, chorea, athetosis (writhing fingers)

pill-rolling tremor (at rest), cogwheel rigidity, akinesia, postural instability

dementia, aphasia, Parkinsonian, change in personality

internuclear ophthalmoplegia (nystagmus, dyplopia), scanning speech, intention tremor, incontinence, optic neuritis (loss of vision), hemisensory sx; relapsing/remitting

NeuroPathophys

α-synuclein defectprions cause α-helix to β-sheet transformation

B3 def (can be from Hartnup's, carcinoid sz, low B6)Renal

Immune depositsSub-endothelialCryoglobulinemiaMembranoproliferative GNLupus nephritis III-V

Immunofluorescence PatternLinearGoodpasture's

Other CharacteristicsLow ComplementPostinfectious GNMembranoproliferative GNCryoglobulinemiaSLE

NMDA excitotoxicity causes atrophy of striatal nuclei (loss of ACh and GABA) cause loss of motion inhibitors

loss of DAergic neurons in substantia nigra pars compacta cause increased inhibitory input on thalamus

APP degradation by β-/γ-secretase yields N-APP (DR6L) or Aβ40/42 (cell death signal or aggregate into plaques)

frontotemporal atrophy (spares parietal lobe and posterior 2/3 of central gyrus)

expanding ventricles cause corona radiata distortion (no increase in subarachnoid space volume)

autoimmune inflammation and demyelination of CNS; commonly hits MLF, optic nerve, spinal cord

NeuroOther

Lewy bodies (α-synuclein intracellular inclusions)

Pick bodies (hyperphosphorylated intracellular tau)

spongiform cortex

Renal

Immune depositsMesangialBerger's Dz (IgA nephropathy)

Lupus nephritis II-V

Immunofluorescence PatternLight and Dark AreasBerger's Dz (IgA nephropathy)

Other Characteristics

chromosome 4, AD (CAG)n expansion, anticipation

cortical atrophy, decreased ACh, intracellular neurofibrillary tangles (hyperphosphorylated tau); early onset=APP, presenilin-1/-2; late=ApoE4; ApoE2=protective (degrades plaques)

CSF: increased protein (IgG, oligoclonal bands are dxtic); periventricular plaques (oligodendrocyte loss, reactive gliosis), preservation of axons; tx: beta-IFN, immunosuppression, sxatic tx for neurogenic bladder, spasticity, pain