Micro Drug penicillin nafcillin dicloxacillin methicillin ampicillin amoxicillin ticarcillin piperacillin carbenicillin clavulanic acid sulbactam tazobactam

cefazolin cephalexin cefoxitin cefalcor cefuroxime ceftriaxone ceftazidime cefipime aztreonam imipenem/cilastatin meropenem vancomycin gentamicin amikacin tobramycin neomycin tetracycline doxycycline demeclocycline minocycline erythromycin clarithromycin azithromycin chloramphenicol clindamycin sulfaClass B-lactam Use GP (not Staph), Syph

PCNase-resistant S. aureus (not MRSA) PCN aminoPCN extended spectrum PCN B-lactamase inhibitor 1G ceph 1G ceph 2G ceph 2G ceph 2G ceph 3G ceph 3G ceph 4G ceph monobactam carbapenem carbapenem glycopeptide AG AG AG AG tetracycline tetracycline tetracycline tetracycline macrolide macrolide macrolide GPC, Proteus, E. coli, K. pneumo GPC, Proteus, E. coli, K. pneumo, H. flu, Enterobacter, Neisseria, Serratia Neisseria, gonorrhea prophylaxis, H. flu meningitis Pseudomonas Pseudomonas and GP GNRs ONLY (no anaerobes) GPC, GNR, anaerobes; broad spectrum, Blactamase resistant GPs ONLY, esp MDR (MRSA, Enterococci, and C. diff) GNR, synergistic w/ B-lactams GNR, synergistic w/ B-lactams GNR, synergistic w/ B-lactams bowel surgery I intracellulars: Lyme, H. pylori, M. pneumo, Rickettsia, Chlamydia (no CNS penetration) +ADH antagonist (diuretic in SIADH) +meningococcal prophylaxis (2nd line) atypical pneumonia (Legionella, M. pneumo, Chlamydia), URI, STD, cocci (GP and Neisseria) meningitis (H. flu, N. meningitides, S. pneumo) lincosamide sulfonamide anaerobes in aspiration pneumonia GP, GN, Nocardia, Chlamydia certain GPs (Listeria, enterococci) and GNRs (Proteus, H. flu, E. coli, Salmonella) Pseudomonas (+AG) and GNR Pseudomonas (+AG) and GNR Pseudomonas (+AG) and GNR

SMX trimethoprim ciprofloxacin enoxacin metronidazole colistimethane dapsone clofazimine rifampin

sulfonamide I +SMX FQ FQ

+UTI UTIs (tx or prophylactic for recurrent), Shigella, Salmonella, PCP (tx/prophylaxis) GNR (esp of UTI/GI infxn), Neisseria, some GPs GI protozoa (Giardia, Entamoeba), vaginal (Trichomonas, Gardnerella), anaerobes resistant GNs M. leprae (oral, long term), PCP M. leprae (added to dapsone) M. leprae (delays resistance to dapsone), prophylactic for H. flu and N. meningitides; M. TB (quad tx) M. TB (quad tx and prophylaxis)

polymyxin

INH (isoniazid) pyrazinamide ethambutol pentamidine (aerosolized) linezolid quinupristin streptogramin dalfopristin streptogramin amphotericin B

nystatin miconazole ketoconazole fluconazole flucytosine caspofungin terbinafine griseofulvin pyrimethamine suramin melacortin nifurtimox Na stibogluconate chloroquine mefloquine quinine mebendazole pyrantel pamoate ivermectin

azole azole azole

antiprotozoan antiprotozoan antiprotozoan antiprotozoan antiprotozoan antiprotozoan antiprotozoan antiprotozoan antihelminth antihelminth antihelminth

M. TB (quad tx) M. TB (quad tx) PCP (second line, after bactrim) VRE VRE VRE serious systemic mycoses: Histoplasma, Blastomyces, Coccidioides, Aspergillus, Candida, Mucor Candida (thrush, diaper rash, vaginal) topical (esp tinea) Candida, Histoplasma, Blastomyces, PCOS (hirsutism), Coccidioides, hypercortisolism Cryptococcal meningitis in AIDS, Candida systemic infxn along with Amphotericin B Invasive Aspergillosis dermatophytes (esp onychomycosis) oral tx of superficial infxn, esp dermatophytes (tinea, ringworm) P. falciparum, +sulfadiazine=toxo Trypanosomes, no CNS penetration Trypanosomes, CNS penetration T. cruzi Leishmaniasis Plasmodium Plasmodium (resistant to chloroquine) chloroquine-resistant Plasmodium when used with pyrimethamine and sulfonam GI, Echinococcus, neurocysticercosis Enterobius, Ascaris, hookworms Onchocerca, Strongyloides

diethylcarbamazine praziquantel amantidine rimantidine zanamivir oseltamivir ribavirin acyclovir famciclovir gangciclovir foscarnet saquiNAVIR indiNAVIR didanosine (ddI) zalcitabine (ddC) stavudine (d4T) zidovudine (ZDV) nevirapine efavirenz delaviridine enfuvirtide IFN- IFN- IFN- Drug cyclosporine tacrolimus sirolimus (rapamycin) daclizumab azathioprine muromonab-CD3 (OKT3) aldesleukin erythropoietin filgrastim sargramostim oprelvekin thrombopoietin digoxin immune Fab

antihelminth antihelminth

Loa loa, Wuchereria bancrofti, Toxocara canis tapeworms and flukes Influenza A (tx and prophylaxis), Parkinson's dz

influenza A and B RSV, chronic hep C HSV (tx and prophylaxis), VZV, EBV herpes zoster CMV (mostly in immunocompromised) gangciclovir-resistant CMV retinitis, acyclovirresistant HSV HIV HIV HIV HIV HIV HIV (tx, prophylaxis, pregnancy) HIV HIV HIV HIV (used in pts w/ persistent viral replication despite HAART) chronic hep B/C, Kaposi's sarcoma, leukemias, malignant melanoma MS NADPH oxidase deficiency Immune Class Mechanism Binds cyclophilins, inhibits calcineurin preventing IL-2 and IL-2R production Binds FK-BP, inhibits IL-2 and IL-2R production (and other cytokines) inhibits mTOR and TC response to IL-2 MAb w/ high affinity for IL-2R on activated TC antimetabolite precursor to 6-MP (interferes w/ nucleic acid synth) MAb that binds CD3 (epsilon chain) on TC, blocks signal transduction IL-2 epoetin Granulocyte Colony Stimulating Factor GMacrophage-CSF IL-11 thrombopoetin

protease I protease I nucleoside reverse transcriptase inhibitor NNRTI NNRTI NNRTI fusion inhibitor recombinant recombinant recombinant

recombinant recombinant recombinant recombinant recombinant recombinant therapeutic ab

etanercept infliximab adalimumab Drug metyrosine guanethidine carbachol pilocarpine bethanechol methacholine edrophonium neostigmine

recombinant therapeutic ab therapeutic ab Class

form of TNF-R (sequesters TNF) anti-TNF- anti-TNF- Pharm/Cardio Mechanism inhibits tyrosine hydroxylase (makes DOPA) inhibits NE release (replaces it in vescicles) ACh ag, resistant to AChE; contract ciliary m and increase outflow of aq humor ACh ag, resistant to AChE inhaled, causes bronchoconstriction extremely short acting no CNS penetration

direct ACh ag direct ACh ag direct ACh ag direct ACh ag AChEI AChEI

pyridostigmine physostigmine echothiophate tropicamide atropine

AChEI AChEI AChEI ACh ant ACh ant

no CNS penetration, long acting CNS penetration CNS penetration in eye

pralidoxime scopolamine ipratropium oxybutynin glycopyrrolate methsopolamine pirenzepine propantheline hexamethonium epinephrine NE isoproterenol DA dobutamine phenylephrine metaproterenol albuterol salmeterol ephedrine cocaine

ACh ant ACh ant ACh ant ACh ant ACh ant ACh ant ACh ant nicotinic ag Symp ag Symp ag Symp ag Symp ag Symp ag Symp ag Symp ag

regenerates AChE CNS competitive block of MACh-R GU GI (block M1R on ECL cells [decrease histamine] and M3R on parietal cells [decrease H secretion]) ganglionic blocker vasoconstriction decreases aq humor production; low dose: >; high: > >1 D>>, inotropic and chronotropic 1>2, inotropic 1>2 selective 2 ag (2>>1)

release stored catecholamines catecholamine reuptake inhibitor, inactivates Na channels

clonidine -methyldopa phenoxybenzamine phentolamine (praz)-osin carvedilol labetalol nadolol pindolol acebutolol betaxolol propranolol timolol esmolol atenolol metoprolol hydralazine nifedipine (DHP) verapamil (non-DHP) diltiazem (non-DHP) nitroglycerin isosorbide dinitrate nitroprusside fenoldopam diazoxide -statin niacin cholestyramine colesevelam ezetimibe gemfibrozil digoxin

central 2 ag, decrease central adrenergic outflow irreversible nonselective -blocker reversible nonselective -blocker 1-blocker (smooth m relaxation) nonselective - and -blocker nonselective - and -blocker nonselective -blocker nonselective partial -agonist 1 partial agonist (>2) selective 1-blocker AND class II anti- nonselective -blocker arrhythmics nonselective -blocker selective 1-blocker, short-acting selective 1-blocker selective 1-blocker vasodilator increased cGMP, relaxing smooth m; arterioles>veins, afterload reduction (L-type) CCB reduce mm contractility, ventricle=vessels; (L-type) CCB reduce mm contractility, ventricle>vessels; +type IV antiblocker-like antianginal arrhythmic reduce mm contractility, ventricle<vessels venodilator venodilator release NO in smooth m causing increased cGMP, veins>aa, decrease preload short acting, same as nitroglycerin D1 ag, relaxes renal vascular smooth m K-ch opener hyperpolarizes/relaxes vascular smooth m HMG-CoA RI inhibits chlsl to mevalonate B3 decreases hepatic VLDL secretion into circ, inhibit lipolysis in adipose tissue bile acid resin prevents intestinal reabs of bile acids, liver uses chlsl to make more prevents chlsl reabs at small intestine brush fibrate upregulate LPL causing increased TG Cl. cardiac glycoside inhibition of Na/K ATPase causes indirect inhibition of Na/Ca exchanger; increases [Ca]i, positive inotropy, stimulates vagus class IA antiarrhythmics class IB antiarrhythmics class IC antiarrhythmics increase AP duration, effective refractory period, and QT; big gap in phase 3 from normal decrease AP duration, preferentially target ischemic/depolarized Purkinje and ventricular tissue no effect on AP duration, significantly prolongs refractory period in AV node

procainamide disopyramide quinidine mexiletine lidocaine tocainide flecainide encainide

class IC antiarrhythmics propafenone sotalol ibutilide bretylium dofetilide amiodarone

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

class III antiincrease AP duration, effective refractory period, arrhythmics: K- and QT; big gap in phase 3 from normal channel blockers

adenosine K Mg Drug bromocriptine cabergoline methimazole propylthiouracil octreotide desmopressin (ddAVP) lispro aspart insulin NPH glargine detemir tolbutamide chlorpropamide glyburide glimepiride glipizide metformin pioglitazone rosiglitazone acarbose miglitol pramlintide exenatide levothyroxine triiodothyronine GH oxytocin hydrocortisone beclomethasone

antiarrhythmic antiarrhythmic antiarrhythmic Class

increase K outside causes hyperpol and decreased Ca current depress ectopic pacemakers in hypokalemia Endocrine Mechanism DA ag, inhibits PRL secretion DA ag, inhibits PRL secretion inhibits peroxidase-coupling of MIT/DIT and thyroid hormone synthesis somatostatin analog (in stomach, inhibit ECL cell secretion of histamine) ADH analog; releases endothelial vWF store bind insulin receptor; liver: increased glycogen synthesis; muscle: increased glycogen and protein synthesis, K uptake; fat: aids TG storage

rapid-acting insulin

intermediate long-acting insulin 1G sulfonyl-urea close K-channel in -cell membrane, causes cell depolarization and triggers Ca influx and insulin 2G sulfonyl-urea release

biguanide thiazolidinediones -glucosidase inhibitor mimetic GLP-1 analog

decreases gluconeogenesis, increase glycolysis and peripheral glucose uptake increase peripheral insulin sensitivity, binds PPAR inhibit intestinal brush border enzymes, delays sugar hydrolysis/absorption decrease glucagon increse insulin, decrease glucagon thyroxine replacement hormone replacement hormone replacement inhibits virtually all cytokines by inactivating NFkappaB (TNF-alpha transcription factor)

synthetic glucocorticoid

synthetic glucocorticoid dexamethasone prednisone Drug famoTIDINE raniTIDINE cimeTIDINE nizaTIDINE omeprazole lansoprazole bismuth sucrasulfate misoprostol Al(OH)3 Mg(OH)2 CaCO3 sulfasalazine ondansetron metoclopramide antacid Class

inhibits virtually all cytokines by inactivating NFkappaB (TNF-alpha transcription factor) + triggers apoptosis GI Mechanism reversible block of H2R on gastric parietal cells causes decreased H secretion

PPI

irreversibly inhibit H/K ATPase in parietal cells 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 (antiinflammatory), activated by bacteria 5HT3 ant, powerful central antiemetic D2R ant causes increased resting tone, LES tone, motility, contractility Heme/Onc Mechanism inhibits ALA synthase(RLS of heme synth) for PML: inhibits retinoic acid receptor causing promyelocyte differentiation activates antithrombin, acts most on Xa and thrombin; very short t1/2; watch PTT

Drug heme and glucose pyridoxamine (B6) vitamin A (xs) heparin enoxaparin (bival)-IRUDIN warfarin

Class

LMW heparin hirudin

acts more on Xa, better bioavailability, longer t1/2; subQ, fine if unmonitored directly inhibit thrombin inhibit vitamin K activation, inhibit synth of mature II, VII, IX, X, protein C and S convert plasminogen to plasmin, which degrades fibrinogen and fibrin bind w/ plasminogen, activate plasminogen streptokinase bound to plasminogen binds ADPR on platelets, inhibits GpIIb/IIIa expression, inhibits fibrinogen binding glycoprotein IIb/IIIa Ab for activated platelets

tPA urokinase streptokinase anistreplase clopidogrel ticlopidine abciximab

direct thrombolytic indirect thrombolytic

therapeutic ab

methotrexate (MTX) 5-FU

6-MP 6-thioguanine (6TG) cytarabine (ara-C) dactinomycin

anti-metabolite folic acid analog, inhibits DHFR, decreasing dTMP (all work on S- and DNA/protein synth phase) 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 pyrimidine analog, inhibits DNA Pol antitumor abx intercalates DNA noncovalently intercalate in DNA causing breaks; generate free radicals free radical formation, breaks DNA (G2) inhibits topoisomerase II (S and G2) covalently cross-link DNA at guanine N7, require activation by liver require bioactivation, cross BBB alkylates DNA bind tubulin, block polymerization, inhibit mitotic spindle formation hyperstabilize polymerized microtubules, inhibit mitotic spindle degradation cross-link DNA ribonucleotide reductase inhibitor Ab against HER-2 (erb-B2); possibly kills through Ab-dependent cytotoxicity bcr-abl tyrosine kinase inhibitor Ab against CD-20 (on most BC neoplasms) Musculoskeletal irreversibly acetylates COX (1 and 2), prevents conversion of AA to TXA2, PGE2, PGI2

doxorubicin (adriamycin) daunorubicin bleomycin (eto)-POSIDE (VP-16) cyclophosphamide alkylating agents ifosfamide nitrosurea (mustines) busulfan vincristine microtubule vinblastine inhibitor (Mpaclitaxel phase) -TAXOLs (cis/carbo)-PLATIN hydroxyurea (S-phase) trastuzumab (herceptin) therapeutic ab imatinib (Gleevec) rituximab aspirin (ASA) NOT AN Ab therapeutic ab NSAIDs

ibuprofen naproxen ketorolac indomethacin celecoxib acetaminophen (etid)-RONATE zoledronate (IV) colchicine

reversibly inhibit COX (1 and 2), blocks prostaglandin synthesis; COX-1 maintains gastric mucosa, COX-2 in inflammatory cells and vascular endothelium reversibly inhibit COX-2 reversibly binds COX, mostly in CNS (peripherally inactivated) bisphos-phonates inhibits osteoclast activity, reduce resorption + formation of hydroxyapatite binds and stabilizes tubulin, impairing chemotaxis and degranulation

probenecid allopurinol

inhibits reabsorption of uric acid in PCT, inhibits secretion of PCN inhibits xanthine oxidase, decreased conversion of xanthine to uric acid Neuro Class Mechanism ag 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

Drug brimonidine latanoprost morphine codeine heroin meperidine dextromethorphan loperamide diphenoxylate fentanyl methadone enkephalin dynorphin tramadol butorphanol buprenorphine phenytoin fosfentoin carbamazepine lamotrigine gabapentin topiramate phenobarbital thiopental valproate ethosuximide tiagabine vigabatrin levetiracetam MgSO4 triazolam oxazepam midazolam

opioid, muR opioid opioid opioid opioid opioid opioid opioid opioid opioid, deltaR opioid, kappaR opioid opioid opioid also IB antiarrhythmic parenteral

very weak opioid, SNRI opioid, partial agonist at mu-R, agonist at kappa-R opioid, partial ag increased Na channel inactivation (increased refractory period), inhibits presynaptic excitatory glutamate release increased Na channel inactivation blocks voltage-gated Na channels inhibits HVA Ca channels (designed as GABA analog) blocks Na channels, propagates GABA action 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 blocks thalamic T-type Ca channels inhibit GABA reuptake irreversibly inhibit GABA transaminase unknown

barbiturate barbiturate (IV)

short-acting BDZ increase frequency of Cl channel opening causing propagation of GABAA action; decrease REM

increase frequency of Cl channel opening causing propagation of GABAA action; decrease REM chlordiazepoxide lorazepam diazepam zolpidem zaleplon eszopiclone halothane enflurane methoxyflurane arylcyclohexylamine propofol succinylcholine motor nACh-R blocker BDZ

non-BDZ hypnotic

act via BZ1 receptor subtype; reversed by flumazenil unknown; high blood solubility=slower induction and recovery time; high lipid solubility=high potency=lower MAC (ketamine) PCP analog, block NDMA-R potentiates GABAA 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 DA ag (ergot derivative) DA ag (non-ergot derivative, so preferred) increases DA release converted to DA in CNS; carbidopa= peripheral dopa-decarboxylase inhibitor COMTI antimuscarinic (atropine) inhibits DA, NE, and 5HT into vescicles (amine depleting) amine depleting (DA) NMDA-R ant (prevent excitotoxicity) AChEI

tubocurarine pancuronium dantrolene bromocriptine pramipexole ropinirole amantidine levodopa/carbidopa ente-/tol-capone benztropine reserpine tetrabenazine memantine rivastigmine donepezil galantamine sumatriptan

5HT1B, 1D ag causes vasoconstriction, inhibits V activation and VIP release; short t1/2 (<2h) Psych Class antipsychotic (typical, neuroleptic) Mechanism block D2R, but can also block muscarinic, , and histamine receptors, all low potency; highly lipid soluble (long t1/2) block D2R, high potency; highly lipid soluble (long t1/2) atypical antipsycotics block 5-HT2, DA, , and H1 receptors

Drug thioridazine chlorpromazine trifluoperazine fluphenazine haloperidol quetiapine reisperidone aripiprazole

atypical antipsycotics ziprasidone clozapine olanzapine lithium

block 5-HT2, DA, , and H1 receptors

mood stabilizer

buspirone desipramine amitriptyline notriptyline imipramine clomipramine (flu)-OXETINE sertraline citalopram venlafaxine duloxetine atomoxitene phenelzine tranylcypromine isocarboxazid selegiline bupropion mirtazapine maprotiline trazodone methylphenidate amphetamine dexedrine Drug/Type Depressants acute EtOH chronic EtOH Stimulants caffeine nicotine Hallucinogens PCP LSD marijuana tricyclic antidepressants

unknown (maybe inhibits PI3 cascade), ADH antagonist; exclusively excreted by kidneys, most reabsorbed at PCT with Na 5HT1A agonist SNRI-like mechanism; amitriptyline=3 (most anticholinergic); notriptyline=2 (least anticholinergic)

SSRI

usually takes 2-4 weeks for antidepressant effects

SNRI

MAOI

5-HT>NE reuptake inhibitor 5-HT<NE reuptake inhibitor 5-HT and NE reuptake inhibitor, nonstimulant nonselective MAOI, increase NE, 5HT, DA

atypical antidepressants

selective MAO-BI (main metabolyzer of DA) increased NE and DA 5HT2&3 and 2-blocker (increased NE and DA) blocks NE reuptake blocks 5HT reuptake release stored catecholamines

CNS stimulant amphetamine

Addiction Withdrawal anxiety, tremor, seizures, insomnia severe: DT (life threatening, peaks 2-5d after last drink, ANS hyperactivity [tachycardia, seizures], psychosis, confusion) crash, depression, lethargy, wt gain, headache irritability, anxiety, craving depression, anxiety, irritability, restlessness, anergia, thought/sleep disturbances

irritability, depression, insomnia, N, anorexia; peak in 48h, last up to 7days; can be detected in urine Antidotes drug class antidote salicylate NaHCO3 (alkalinize urine), dialysis iron (hemochromatosis) deferoxamine

lead mercury arsenic gold copper (Wilson's) cyanide methemoglobin CO methanol ethylene glycol benzene nitrofurantoin procarbazine Amanita phalloides (poison mushroom) Drug mannitol acetazolamide ethacrynic acid furosemide hydrochlorothiazide eplerenone spironolactone triamterine amiloride captopril lisinopril enalapril Drug leuprolide methyltestosterone finasteride flutamide ethinyl estradiol mestranol diethylstilbestrol clomiphene tamoxifen raloxifene HRT Class

1st line: CaEDTA and dimercaprol, 2nd: penicillamine; succimer for kids dimercaprol (BAL), succimer dimercaprol (BAL), succimer, penicillamine penicillamine nitrite, hydroxocobalamin, thiosulfate methylene blue, vitamin C 100% O2, hyperbaric O2 ethanol, fomepizole, dialysis

Renal Mechanism osmotic diuretic carbonic anhydrase inhibitor phenoxyacetate derivative, same as Lasix inhibit cotransport of NaK2Cl; lose hyper-tonicity of medulla, increase Ca excretion inhibit NaCl reabs in distal tubule, low Ca excretion competitive aldoR ant + mild testosterone R ant block ENaC in DCT inhibit inactivation of bradykinin (vasodilator); causes renin release by loss of feedback inhibition Repro Class GnRH ag Mechanism pulsatile=agonist, continuous=antagonist T agonist at androgen receptors 5-reductase inhibitor, lower DHT nonsteroidal competitive T-receptor ant Estrogen receptor antagonist

loop diuretic

thiazide K-sparing diuretics

ACEI

estrogen

SERM

inhibits negative feedback on hypthalamus ag: bone, endometrium; antag: breast ag: bone; antag: endometrium, breast

exemestane anastrozole progestin mifepristone (RU-486) dinoprostone terbutaline ritodrine tamsulosin sildenafil vardenafil Drug diphenhydramine chlorpheniramine loratadine fexofenadine desloratadine certirizine theophylline cromolyn zileuton (zafir)-lukast guaifenesin N-acetylcysteine bosentan Class 1G H1 blockers 2G H1 blockers

aromatase inhibitor reduce growth and vascularization of endometrium competitive progesterone inhibitor PGE2 analog (dilation, uterine contraction) 2 1A,DR ant (on prostate, 1BR on vessels) inhibit cGMP PDE5I Respiratory Mechanism reversible inhibitors of H1 histamine R

Symp ag

methylxanthine antiLT

PDEI (decreases cAMP hydrolysis) stabilizes mast cell granules 5-lipoxygenase inhibitor (AA to LTs) LT receptor antagonist mucolytic, glutathione precursor endothelin-1 receptor antagonist (lower PVR)

Micro Mechanism Bind PBP, inhibit transpeptidase cross-linking of cell wall, and activate autolytic enzymes Same as PCN, but bulkier R group

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 " " " for serious gram negative infxn for serious gram negative infxn " inhibits cell wall synth (binds PBP3), B-lactamaseresistant, synergistic w/ AGs cilastatin=renal dehydropeptidase I inhibitor, decreases inactivation of drug; seizures, GI distress, rash dehydropeptidase I stable, lower risk of seizures; GI distress, skin 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) binds 23S or 50S and inhibits translocation

inhibits 50S peptidyltransferase; plasmid-encoded acetyltransferase inactivates drug binds 50S and inhibits translocation PABA antimetabolytes inhibit DHpteroate synthetase; resistance=all mechanisms

PABA antimetabolytes inhibit DHpteroate synthetase; resistance=all mechanisms bacterial DHFRase I topoisomerase II inhibitor; resistance=mutated DNA gyrase free radical toxic metabolites that damage DNA disrupts membranes (basic cations=detergent)

DNA-dep RNA pol inhibitor

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

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

same as amphotericin B inhibit fungal ergosterol synthesis by inhibiting P450 enzyme (lanosterol 14--demethylase); for systemic mycoses; ketoconazole also inhibits human enzyme desmolase (T-synth) converted to 5FU, inhibits DNA synth -glucan cell wall synthesis inhibitor squaline epoxidase I (ergosterol precursor) microtubule inhibitor, deposits in keratin-containing tissues inhibits plasmodial DHFRase inhibits energy metabolism enzymes inhibits sulfhydryl enzymes forms intracellular oxygen radicals inhibits glycolysis at PFK blocks plasmodium heme polymerase (buildup of toxic hemoglobin products) en used with pyrimethamine and sulfonamide; Babesia inhibits glucose uptake and microtubule synth stimulates depolarization-induced paralysis by stimulating nicotinic receptors at NMJ amplifies GABA-mediated inhibition leading to immobilization; doesn't cross BBB (no effect on humans)

increases membrane permeability to Ca (contraction, paralysis) blocks viral penetration/uncoating (M2); also causes release of DA from intact nerves; resistance=mutated M2 (90% of flu A resistant) inhibit neuraminidase inhibit IMPDH (guanine synthesis) 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

Immune Use some autoimmune disorders, suppresses organ rejection suppresses organ rejection (very strong immunosuppressant) kidney transplant w/ cyclosporine and steroids kidney transplant, autoimmune disorders (including GN, hemolytic anemia, UC) kidney transplant RCC, metastatic melanoma anemias (esp renal failure) bone marrow recovery bone marrow recovery thrombocytopenia thrombocytopenia antidote for digoxin intoxication

Crohn's, RA, psoriatic arthritis Crohn's, RA, psoriatic arthritis, ankylosing spondylitis Crohn's, RA, psoriatic arthritis Pharm/Cardio Use htn from pheo (prevents catecholamine synth) htn glaucoma, causes miosis, relieve IOP glaucoma emergency; stimulates sweat, tears, saliva, causes miosis postop and neurogenic ileus/urinary retention challenge test for dx of asthma dx of myasthenia gravis postop and neurogenic ileus/urinary retention, myasthenia gravis, post-op reversal of NMJ blockade myasthenia gravis glaucoma and atropine OD glaucoma causes mydriasis and cyclopegia +tx of cholinesterase poisoning

with atropine, for cholinesterase poisoning motion sickness asthma, COPD reduce urgency in mild cystitis and reduce bladder spasms peptic ulcers (rarely used)

used in experiments only anaphylaxis, open angle glaucoma, asthma, hypotension hypotension (but decreases renal perfusion) lowers BP (not used), asthma shock (increases renal perfusion), CHF CHF, cardiac stress testing pupillary dilation, vasoconstriction, nasal decongestion acute asthma acute asthma long term asthma (attack prophylaxis) nasal decongestant, urinary incontinence, hypotension causes vasoconstriction, local anesthesia

htn, esp. in renal disease (no decrease in renal blood flow), 1st line in preg (+ hydralazine) pre-op on pheo htn, urinary retention in BPH htn (decrease CO, decrease renin secretion * 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 malignant htn malignant htn malignant htn lower LDL>>TG, raise HDL a little lower LDL>TG, raise HDL a bunch lower LDL, slightly raise HDL and TG lower LDL lower TG>>>LDL, raise HDL a little 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

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

dx/tx of SVT; very short acting (~15s) digoxin toxicity torsades and digoxin toxicity Endocrine Use PRLoma, neuroleptic malignant sz PRLoma hyperthyroidism GHoma, NET, gastrinoma, glucagonoma, acute variceal bleed, VIPoma, carcinoid tumor central DI, von Willebrand's dz DM, gestational DM, life-threatening hyperkalemia, stress-induced hyperglycemia

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

oral, can be used in pts w/o islet function (T1 or 2DM) T2DM (monotherapy or combo) T2DM (monotherapy or combo) T2DM T2DM hypothyroidism, myxedema GH deficiency, Turner's stimulates labor, uterine contractions, milk let-down, controls uterine hemorrhage Addison's, inflammation, immune suppression (Crohn's), asthma (1st line for chronic)

+ dx of Cushing's dz (suppression test) + CLL, Hodgkins GI Use PUD, gastritis, mild esophageal reflux

PUD, gastritis, esophageal reflux, Zollinger-Ellison Sz improved ulcer healing, traveller's diarrhea, + metronidazole + amoxicillin (or tetracycline) for H. pylori prevention of NSAID-induced ulcer, induce labor, maintenance of ductus arteriosus all cause hypokalemia

UC, Crohn's decrease vomiting (post-op, chemo) gastroparesis (DM or post-surgery), does not influence colon transport time Heme/Onc Use acute intermittent porphyria sideroblastic anemia, prevent neurotoxicity and lupus from INH acne, PML (AML M3) immediate anticoagulation: PE, CVA, acute coronary sz, MI, DVT; safe for pregnancy

heparin alternative in HIT chronic anticoagulation, oral

early MI, early ischemic stroke

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 leukemia or lymphoma (not CLL or HL), UC ALL AML, ALL, high grade NHL Ewing's sarcoma, rhabdomyosarcoma, childhood tumors (Wilm's) Hodgkins, myelomas, sarcomas, solid tumors

testicular and Hodgkins SCC of lung/prostate, testicular NHL, breast, ovarian; also good immunosuppressants brain tumors (including glioblastoma multiforme) CML, pre-marrow-transplant marrow ablation Hodgkins, Wilm's, chorioca ovarian and breast testicular, bladder, ovary, lung melanoma, CML; sickle-cell (increase HbF) HER-2-overexpressing breast cancer CML (Philadelphia chr., main target), GIST BC non-Hodgkin's lymphoma, RA (+ MTX) Musculoskeletal low dose (<300mg/day, TXA2): antiplatelet; intermed dose (300-2400mg/day, PGE2): antipyretic and analgesic; high dose (2400-4000mg/day): antiinflammatory antipyretic, analgesic, anti-inflammatory, acute gout (w/ colchicine, esp indomethacin), migranes + induces closure of PDA, nephrogenic DI RA, OA, pts w/ gastritis/ulcers antipyretic, analgesic, NO anti-inflammatory malignancy-associated hypercalcemia, Paget's dz of bone, postmenopausal osteoporosis acute gout (with NSAIDs, esp indomethacin)

chronic gout, also given w/ PCN to prolong t1/2 chronic gout; lymphoma/leukemia w/ chemo to prevent tumor lysis urate nephropathy Neuro Use glaucoma glaucoma pain, acute pulmonary edema

+ cough suppression + diarrhea + diarrhea (stronger than morphine) (partial ag, long acting) opioid addiction endogenous endogenous chronic pain pain pain, opioid addiction, used w/ naloxone 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 partial and tonic clonic, peripheral neuropathy, bipolar partial and tonic clonic 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 absence (first line) partial seizures partial seizures partial and tonic clonic eclamptic seizures (1st line) anxiety, spasticity, detox (esp EtOH withdrawal and DT), night terrors, sleepwalking, general anesthetic, insomnia, cocaine OD, panic disorder, GAD

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) insomnia

inhaled anesthetic (increase cerebral blood flow, depress CV/resp) dissociative anesthetic rapid anesthesia induction depolarizing paralytic (for pts on a mechanical vent or during surgery) non-depolarizing paralytic malignant hyperthermia and neuroleptic malignant syndrome Parkinson , PRLoma Parkinson Parkinson; influenza A, rubella Parkinson Parkinson Parkinson (tremor and rigidity, not bradykinesia) Huntington Huntington Alzheimer's Alzheimer's

Migrane, cluster headache Psych Use schizophrenia (mostly positive sx), psychosis, mania (acute), Tourette's (esp haloperidol)

+ Huntington schizophrenia (positive and negative sx)

schizophrenia (positive and negative sx)

+ OCD, anxiety, depression, mania, Tourette's bipolar, blocks relapse and acute manic events; SIADH GAD, anxiety major depression, fibromyalgia, panic disorder

+ bedwetting + OCD OCD, bulimia, social phobia, specific phobia, panic disorder, PTSD, GAD, anorexia/bulimia, anxiety, depression (a-/typical) depression, GAD depression, diabetic peripheral neuropathy ADHD atypical depression, anxiety, hyperchondriasis

+ Parkinson (use w/ L-dopa) bipolar, depression, smoking cessation bipolar, depression, insomnia bipolar, depression insomnia, depression (very high doses) narcolepsy, obesity, ADHD ADHD Addiction

Intoxication mood elevation, decreased anxiety, sedation, behavioral disinhibition, respiratory depression emotional lability, ataxia, coma, serum GGT (sensitive EtOH use), AST>2*ALT; acute EtOH=P450 down; chronic EtOH=P450 up gynecomastia mood elevation, psychomotor agitation, insomnia, arrhythmias, tachycardia, anxiety restlessness, diuresis, muscle twitching restlessness fever, nystagmus, tachycardia, psychomotor agitation, belligerence, impulsiveness, homocidality, delerium flashbacks, pupillary dilation, marked anxiety/depression, delusions, visual hallucinations paranoid delusions, slowed time perception, social withdrawal, dry mouth, hallucinations Antidotes SFX/other not for gout (need too high of a dose)

penicillamine; succimer for kids

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

aplastic anemia hemolysis in G6PD deficiency disulfiram-like rxn w/ EtOH hepatotoxicity/necrosis Renal Use shock, drug OD, increased ICP/IOP glaucoma, urinary alk, MAlk, altitude sickness diuresis in sulfa-allergies or gout pts edema (CHF, cirrhosis, nephrotic sz, pulmonary edema), htn, hypercalcemia htn, CHF, idiopathic hypercalciuria, nephrogenic DI hyperaldo, K-depletion, CHF, hirsutism (spironolactone) + nephrogenic DI htn, CHF, diabetic renal dz

Repro Use infertility, prostate ca (+ flutamide), fibroids hypogonadism, develop 2 sex characteristics, burn pts (promotes anabolism) BPH, male pattern baldness prostate cancer (+ leuprolide) hypogonadism, POF, menstrual abnormailities, postmenopausal HRT, androgen-dependent prostate cancer ovulation induction breast cancer (ER-positive), prevent osteoporosis 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 pregnancy termination (+ misoprostol) labor inducer reduce premature uterine contractions BPH (inhibits only prostatic smooth m) ED Respiratory Use allergy, motion sickness, sleep aid allergy

asthma, adenosine toxicity only for asthma/allergy prophylaxis, not tx asthma asthma (especially aspirin-induced) expectorant loosen plugs (CF), acetaminophen OD pulmonary htn

SFx/Other bacteriocidal; G=IV, V=oral; can cause hypersensitivity rxn (all PCNs) or hemolytic anemia, SJS same as PCN +interstitial nephritis pseudomembranous colitis +higher oral availability; rash

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 tor, decreases inactivation of drug; seizures, GI distress, rash eizures; GI distress, skin 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 +fecally eliminated (can be used in pts w/ renal failure) +diabetes insipidus 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 hypersensitivity, SJS, hemolysis (G6PDD), nephrotoxic (tubulo-interstitial nephritis), teratogen (kernicterus), photosensitive, megaloblastic anemia, P450 down

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 neurotoxic, nephrotoxic (acute renal tubular necrosis) hemolysis, methemoglobimemia, agranulocytosis orange body fluids, minor hepatotoxicity, ups P450

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 topical (too toxic for oral) liver dysfunction (P450 inhibitor), fever, chills + hypocortisolism (blocks hormone synthesis in adrenals), gynecomastia, amenorrhea + can cross BBB N/V/D/bone marrow suppression, nonmegaloblastic macrocytic anemia GI upset, flushing teratogen, carcinogen, confusion, headache, increase P450 and warfarin metabolism

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

is by stimulating nicotinic receptors at NMJ ng to immobilization; doesn't cross BBB (no effect on humans)

contraction, paralysis) ataxia, dizziness, slurred speech doesn't cross BBB, fewer CNS SFx m

hemolytic anemia, teratogen (severe) no effect on latent virus; resistance=lack of viral thymidine kinase thrombocyto-/leuko-/neutro-penia, nephrotoxic nephrotoxic; resistance by mutated DNA pol hyperglycemia, N/D, lipodystrophy, P450 inhibition +thrombocytopenia bone marrow suppression (can be reversed with GCSF and erythropoietin), peripheral neuropathy, lactic acidosis +megaloblastic anemia bone marrow suppression (can be reversed with GCSF and erythropoietin), peripheral neuropathy, rash hypersensitivity, increased risk of bacterial pneumonia neutropenia neutropenia neutropenia SFx/Other nephrotoxic (prevented by mannitol diuretic), higher risk for viral infxn and lymphoma significant: nephrotoxicity, peripheral neuropathy, htn, pleural effusion, hyperglycemia hyperlipidemia, thrombocytopenia, leukopenia bone marrow suppression, worsened w/ allopurinol (6-MP broken down by xanthine oxidase), nonmegaloblastic macrocytic anemia cytokine release syndrome, hypersensitivity rxn

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

SFx/Other

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 tx OD w/ physostigmine salicylate

+ tachycardia, dry mouth, difficulty focusing eyes

severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction

tachycardia

decongestion

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

direct Coombs-positive hemolytic anemia orthostatic hypotension, reflex tachycardia 1st dose orthostatic hypotension, dizziness, headache 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/ 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) CN toxicity hyperglycemia (reduces insulin release) hepatotoxicity, rhabdomyolysis cutaneous flushing (esp face), hyperglycemia, acanthosis nigricans, hyperuricemia pts hate it: tastes bad, GI discomfort, decreased abs of fat soluble vitamins, chlsl gallstones rare increase in LFT myositis, hepatotoxicity (LFT), chlsl gallstones 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 Lupus-like sz toxicity increased w/ hyperkalemia (all class I) Torsades, cinchonism (tinnitus, headache), thrombocytopenia CNS stimulation/depression, CV depression, toxicity increased w/ hyperkalemia (all class I) proarrhythmic, esp post MI (contraindication), toxicity increased w/ hyperkalemia (all class I)

proarrhythmic, esp post MI (contraindication), toxicity increased w/ hyperkalemia (all class I) Torsades, excessive -block torsades new arrhythmias, especially w/ hypotension 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)

SFX/other

skin rash, aplastic anemia, agranulocytosis (rare) + hepatotoxicity nausea, cramps, steatorrhea given intranasal for DI hypoglycemia, hypersensitivity (very rare)

disulfiram-like effect w/ EtOH, hypoglycemia hypoglycemia

lactic acidosis (contraindicated in renal failure) weight gain, edema, hepatotoxicity, CV toxicity GI disturbances hypoglycemia, N/D N/V, pancreatitis tachycardia, heat intolerance, tremors, arrhythmias

lk let-down, controls uterine hemorrhage iatrogenic Cushing's (incl. osteoporosis, peptic ulcers, and DM), adrenal insufficiency when drug stopped after chronic use

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

SFX/other 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

diarrhea, abortifacient constipation, hypophosphatemia, mm weakness, osteodystrophy, seizure diarrhea, hyporeflexia, hypotn, cardiac arrest hyperCa, rebound acid level, chelates other drugs malaise, nausea, sulfa, reversible oligospermia headache, constipation Parkinsonian, restlessness, drowsiness, depression, N/D; interacts w/ digoxin and diabetic agents; contraindicated in SI obstruction SFX/other

ty and lupus from INH 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

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)

neutropenia bleeding, thrombocytopenia

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

nonmegaloblastic macrocytic, GI, liver; increased toxicity w/ allopurinol marrow depression, can be given w/ allopurinol leukopenia, thrombocytopenia, megaloblastic anemia myelosuppression cardiotoxicity (dilated CM), myelosuppression, alopecia; toxic to tissues with extravasation pulmonary fibrosis, skin changes, minimal myelosuppression myelosuppression, GI irritation, alopecia 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 neurotoxic (areflexia, peripheral neuritis), paralytic ileus bone marrow suppression myelosuppression, hypersensitivity nephrotoxic, ototoxic nonmegaloblastic macrocytic anemia, GI upset cardiotoxic fluid retention

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

higher risk of thrombosis, sulfa allergy, lower incidence of GI sfx no Reye's sz, but OD causes hepatic necrosis (metabolyte depletes glutathione and forms toxins in liver), N-acetylcysteine is antidote corrosive esophagitis, N/D, osteonecrosis of jaw no corrosive esophagitis (IV) GI side effects, agranulocytosis

SJS, increases concentrations of azathioprine and 6-MP (both metabolyzed by xanthine oxidase, give 6-tG instead of 6-MP) SFX/other no pupillary or vision changes darkens iris 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

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

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 SJS sedation, ataxia sedation, mental dulling, kidney stones, weight loss 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)

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) proconvulsant nephrotoxicity CV stimulant, disorientation, hallucinations, bad dreams, increase cerebral BF less post-op nausea than thiopental can cause hyperCa, hyperK, malignant hyperthermia

reversal: AChEI (neostigmine, edrophonium)

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

Parkinson-like sz

dizziness, confusion, hallucinations N/V, dizziness, insomnia

coronary vasospasm (don't use in pts with CAD or Prinzmetals angina), mild tingling SFX/other 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 far fewer extrapyramidal and anticholinergic SFx than neuroleptics

far fewer extrapyramidal and anticholinergic SFx than neuroleptics

wt gain, agranulocytosis (requires weekly WBC monitor) wt gain teratogen (atrialized RV [Ebstein's anomaly, malformation of great vessels]), hypothyroid, nephrogenic DI, sedation, edema, heart block, tremor; narrow therapeutic window no sedation, addiction, tolerance, EtOH interaction (BDZ/barbiturates) sedation (least=desipramine), convulsions (most=desipramine), -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]) stimulant effects (htn most common), sedation, nausea

htnsive crisis (w/ tyramine ingestion and beta-ag), CNS stimulation, contraindicated w/ SSRIs or meperidine (prevent seratonin sz) + may enhance SFX from levodopa stimulant effects (tachycardia, insomnia), headache, seizure in bulimia sedation, increased appetite, dry mouth, increased serum cholesterol sedation, orthostatic hypotension sedation, nausea, priapism, postural hypotension OD: pupil dilation, prolonged wakefulness, delusions, hallucinations, fever; withdrawal: stomach cramps, hunger, hypersomnolent

ion, behavioral disinhibition, respiratory depression GT (sensitive EtOH use), AST>2*ALT; acute EtOH=P450 down; chronic EtOH=P450 up,

nsomnia, arrhythmias, tachycardia, anxiety teratogen (preterm labor, placental problems, IUGR, ADHD)

tor agitation, belligerence, impulsiveness, homocidality, delerium

iety/depression, delusions, visual hallucinations on, social withdrawal, dry mouth, hallucinations

SFX/other pulmonary edema, dehydration, contraindicated in anuria and CHF hyperchloremic MAc, neuropathy, NH3 toxicity, sulfa ototoxicity, hypokalemia, dehydration, interstitial nephritis + sulfa allergy and gout hypokalemic MAlk, hyponatremia (low big 3), hyperglycemia, hyperlipidemia, hyperuricemia (gout), hypercalcemia, sulfa allergy hyperkalemia, MAc endocrine SFx (antiandrogen, gynecomastia, amenorrhea) hyperkalemia, MAc 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) SFX/other antiandrogen, N/V masculinization in females, reduces intratesticular testosterone in males (inhibits LH) causing gonadal atrophy, premature closure of epiphyseal plates, raise LDL, lower HDL gynecomastia endometrial cancer, postmenopausal bleeding, VTE; contraindications: ERpositive breast cancer, hx of DVTs teratogen (vaginal clear cell adenoC) hot flashes, ovarian enlargement, multiple pregnancies, visual disturbances endometrial carcinoma, hot flashes unopposed estrogen RT increases the risk of endometrial cancer (P added), possible increased CV risk

heavy bleeding, N/V, anorexia, abdominal pain

headache, flushing, dyspepsia, impaired blue-green color vision, lifethreatening hypotn in pts taking nitrates SFX/other sedation, 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

does not suppress cough reflex

P450 interactions up barbiturates phenytoin carbamazepine griseofulvin rifampin chronic EtOH use St. John's Wort quinidine

down sulfonamides erythromycin cimetidine ketoconazole isoniazid acute EtOH use grapefruit juice HIV protease inhibitors

slow AV nodal conduction

II, IV, dig

ending -afil -ane -azepam -zolam -azine -azole -barbital -caine -cycline -etine -ipramine -navir -operidol -oxin -phylline -terol -tidine -triptan -triptyline

function erectile dysfunction inhalational general anesthetic BDZ BDZ phenothiazine (neuroleptic, antiemetic) antifungal barbiturate local anesthetic protein synth inhibiting abx SSRI TCA protease inhibitor butyrophenone (neuroleptic) glycoside (inotrope) methylxnthine 2 ag H2 ant 5HT1B/1D ag (migrane) TCA nonselective - and -blocker nonselective -blocker nonselective partial -agonist selective 1-blocker 1 partial agonist (>2)

example sildenafil halothane diazepam alprazolam chlorpromazine ketoconazole phenobarbital lidocaine tetracycline fluoxetine imipramine saquinavir haloperidol digoxin theophylline albuterol cimetidine sumatriptan amitriptyline carvedilol, labetalol nad, propran, tim pind betax, esm, aten, metopr acebut

Cardio disease essential htn htn in CHF htn in DM malignant htn angina AFib AFlutter SVT VT tx diuretics, ACEI, ARBs, CCB diuretics, ACEI, ARBs, CCB, blockers ACEI, ARBs, CCB, diuretics, -blocker, -blocker nitroprusside, fenoldopam, diazoxide nitrates and -blockers digoxin, -blockers, anticoag, non-DHP ablation, anticoag, non-DHP class IA/C, class II, class IV, adenosine class I, class II Neuro disease tonic clonic seizure absence seizure status seizure tx first line: phenytoin, carbamazepine, valproate first line: ethosuximide; otherwise, valproate acute: BDZ; prophylaxis: phenytoin

Cardio other no blockers in decompensated CHF, esp K-sparing diuretics ACEI protective against diabetic nephropathy

Neuro first line in pregnancy and children: phenobarbital

Neuro Name Huntington Parkinson Alzheimer Sx agression, depression, dementia, chorea, athetosis (writhing fingers) pill-rolling tremor (at rest), cogwheel rigidity, akinesia, postural instability dementia, can get intracranial hemorrhage

Pick's Dz (FTD) LBD CJD NPH MS

dementia, aphasia, Parkinsonian, change in personality Parkinsonism w/ dementia and hallucinations rapidly progressive dementia with myoclonus urinary incontinence, ataxia, dementia internuclear ophthalmoplegia (nystagmus, dyplopia), scanning speech, intention tremor, incontinence, optic neuritis (loss of vision), hemisensory sx; relapsing/remitting diarrhea, dementia, dermatitis (glossitis) Renal Immune deposits Sub-epithelial Membranous GN Postinfectious GN Lupus nephritis V

pellagra

Immunofluorescence Patt Granular Membranous nephropathy Postinfectious GN Membranoproliferative GN Other Characteristics Diffuse Glomerular Proliferation Postinfections GN Membranoproliferative GN SLE

Neuro Pathophys 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 -/-secretase yields N-APP (DR6L) or A40/42 (cell death signal or aggregate into plaques) frontotemporal atrophy (spares parietal lobe and posterior 2/3 of central gyrus) -synuclein defect prions cause -helix to -sheet transformation 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

B3 def (can be from Hartnup's, carcinoid sz, low B6) Renal Immune deposits Sub-endothelial Cryoglobulinemia Membranoproliferative GN Lupus nephritis III-V Immunofluorescence Pattern Linear Goodpasture's

Other Characteristics Low Complement Postinfectious GN Membranoproliferative GN Cryoglobulinemia SLE

Other chromosome 4, AD (CAG)n expansion, anticipation Lewy bodies (-synuclein intracellular inclusions) cortical atrophy, decreased ACh, intracellular neurofibrillary tangles (hyperphosphorylated tau); early onset=APP, presenilin-1/-2; late=ApoE4; ApoE2=protective (degrades plaques) Pick bodies (hyperphosphorylated intracellular tau)

spongiform cortex

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

Mesangial Berger's Dz (IgA nephropathy) Lupus nephritis II-V

ttern Light and Dark Areas Berger's Dz (IgA nephropathy)