Step 1 Drugs
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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