Usmle Pharm 2

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atypical antipsychotic

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chronic EPS for tardive dyshyemia

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antipyschotic AE

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EPS, dysphoria(decreases compliance), endocrine( NMS, increased prolactin, wt gain) , hypotnesion due to alpha blockage

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Typicals

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chlorpromazine, thioridazine, fluphenazile, haloperidol

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atypicals

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clozapine, olanzapine, risperidone, aripiprazole

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thioridiazine

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better antimusacrin, incrased sedation, increased alpha blockate, cardiac toxicity(quinidine like), retinal deposits, allergies , typical antipsych

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haloperidol

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NMS and TD, typical antipsych

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clozapine

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block D2C and 5HT2, AE- agranulocystosis, NO TD, increased salivation(due to serotnin) , seziures(due to antimuscarinic) , atypical antipsychotic

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olanzapie and risperidone

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atypical, blocks 5HT2 improves negative symptoms

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aripiprazole

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partial agonist of D2, blocks 5HT2 receptors

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phenelzine and tranylcypromine

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MAOI , use- atypical depression, AE- HYPERTENSIVE CRISSI, DI with tyramine, TCA, levodopa, alpha 1 agonist, SEROTONIN SYN

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serotonin syn

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sweating, rigidity, myoclonus, hyperthermia, ANS instabiliy, seizures , Drugs- SSRI, TCA, meperidine

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TCA

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amitriptiline, imipramine, clomipramine, non specific block of 5HT and NE, DI- hypertensive crisis with MAOI, seronin syn, AE- 3 Cs(coma, convusion, cardiotoxic)

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clomipramine

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TCA for OCD

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amytriptyline

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TCA for neuropathic pain, can also use carbemazepine

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imipramine

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decreased slow wave sleep, works on phase IV of sleep, night terrors

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fluoxetine, paroxetine, sertraline, citalopram, fluvoxamine

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slective blockade of 5HT reuptake , USE- depression, anxiety, DI- CYP inh(fluvoxamine and fluxetine), benzo

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citalopram

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safe for interactions

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trazodone

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5HT agonist, AE- arrthmias, pirapism

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venlafazine

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nonselective reuptake blocker devoid of ANS effects

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buproprion

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DA reuptake blocker, used in smoking cessation

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Mirtazapine

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alpha 2 antagonist, wt gain and anorexia

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lithium

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DOC for bipolar, decreases PIP2 and camp, AE- life threatining sezures, hypothyroidsimwith goiter(decreased TSH), NDI(decreased ADH)- tx with amiloride, chronic thazide decreases clearance of LI, use K sparing, teratogenic(ebsteins- malformed tricuspid)

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methylphenidate

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amphetatime like, AE- cardio toxicity, use- ADHD

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atomoxetine

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selective NE reuptake inhibitor, USE- ADHD

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amphetamine

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block reuptake of NE and DA, relase amines from mobule pool

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benzo toxcitiy

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tx with flumazenil, cant use for barbituate toxcitiy

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benzo MOA

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potnetiate GABA with GABA A (BZ1 and BZ2)

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barbituate+ alcohol

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lif threatening seziure

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marijuana

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interact of CB 1 and CB2

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PCP

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NMDA antagonist, AE- rhabdomylosysi, convulsions and edeath

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ketamine

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hallucinations, glutamate receptro antagonist

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MDMA

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5HT, excstasy, raves

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inhanats

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solvent abuse, multiple organ damage

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macrolides

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erythromycin, azithromycin clarithromycin, USE- g+, atypicals, C jejuni, MAC, H pylori, CYP inh, AE- stim gut motilin

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clarithromycin

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macroline with less GI symptosm

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azitrhomycin

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macrolide with least CYP inh , H pyroli

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telitrhomycin

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ketoline, macrolide resistn S pneumona

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clindamycin

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not macrolide but same mechanism and resistance, G+, b fragilis and anarobes, use in osteomylitis with g+, AE- C DIFFICLE COLITIS

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linezolid

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MOA- inhibits initation complex in bac translation, prevents formation of tRNA complex, USE- tx for VRSA and VRE, drug resist penumoccoa, 50 S

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quinupristin-Dalfopristin

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50S, like tetracycline, streptogramins, binding to 50S prevent interaction of amino acyl tRNA with acceptor site , USE- VRE, VRSA

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sulfonamides

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inhibit dihydropteroate synthetase , DON’T USE ALONE- resistance

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trimethoprim and pyrimethamine

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inhibit dihdrofolate reductase , Bone marrow suprresion, problemtatic in HIV pts

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sulfasalazine

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ulcertative coilitis and rheumatoid arthritis

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Ag sulfadiazine

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burns

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GI conjugases

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carbamezipine and phenytoin, allows for transport of folate

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cotrimoxazole

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trimethoprim-sulfamethoxazole, DOC for nocardia, listeria, g- infections, g+ infections, PCP, toxoplasm, AE- allergies, take with lots of water( to avoid stones), kernicterus in babeis, phototoxciiy

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chloramphenicol

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bacteriostatic, met by hepatic glucorination, CYP inh, dose dep marrow supreesion, back up for salmonella and ricettksa, AE- GRAY BABY SYN

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Doxycyline

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lipid soluble, proststis(gonorhea+chlamydia, boreilla , hepatic met

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minocycline

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menigicoocal carrier state( rifampin more frequent- organge body fluids)

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Demeclocycline

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SIADH

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tigecycline

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MRSA and VRE skin and complicated infections

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ADH

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increased by carbamazepine, decreased by LI , decreased by demeclocyline

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tetracycline

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chelators, bacteriostatic, borad- atypicas, h pylori, ricketsia, boreilla, brucella, vibrio, treponema(back up) , AE- tooth enamel dysplsia and decreased bone , CI in preggers( liver issues)

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drugs that cause photoxicity

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tetracucline, sulfonamide, quinolones

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gentamicin, tobramycin, amikacin, streptomycin

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aminoglycosides, AE- nephrotoxicity(ATN) , otoxicity, NEUROMUSCLAR BLOCKADE , once daily dosing

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streptomycin

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TB, DOC for bubonic plague and tularemia

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CI in pregancy

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aminoglycosides, fluroquinolones, sulfonamides, tetracycline

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aminoglycosides(30S), linezolid(50S)

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interenes with initiation, misreading of code(aminoglycosdies only- cidal)

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tetracycline (30S)and dalfopristin/quinupristin (50S)

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blocks attachemnt of aminoacyl tRNA to acceptor site(static)

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chloramphenicol (50S)

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inhibit the activity of peptidyl transferase(-static)

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macrolides and clindamycin (50S)

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ihibits translocation of peptidyl tRNA from acceptor to donor site

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otoxoic

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aminoglycosides, loop diuretics(ethycrinic acid more) , vancomycin

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vancomyci

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binds Dala Dala and hinders the transglyclation and invovlved in the elognation of peptidoglycan chains, NO ROLE IN PBPs, USE- MRSA, enterococci C difficiel(not DOC, metronizadle is) , resistance- termanial Dala is replaced by D lactate, orally for colitis, AE- red man syndrome, otoxotic

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aztreonam

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resistant to B lactmases, no cross allogeniencity, ONLY G-

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Imipenem and Meropenem

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Reistant to B lactams, nosocmial epiric for life threathening, give with CILASTATIN to prevent RENAL TOXCITIY , USE- enterobacter and pseudomonas, AE- seizures

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cefazolin, cephalexin

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first gen cephalosporin, surgical prolylacis, g+, NO ENTRY INTO CNS, long half life

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cefotetat, cefaclor, cefuroxime

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second gen cephalospin, cefuroxime enters CNS

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ceftriazone, cefotaxime, cefdinir, cefixime

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g+, g- rods and coci, epiric for menginitis and spesisi

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cefipime

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IV, reistant to beta lactamase, wide spect, enters CNS

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cefoperazone, ceftriazole

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bile eleminated

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cefotetaan, cefoperazone

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disulfiram like

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inhibition of bacterial cell well synthesis

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pencillins, cephalosporin, imipenem/meropenem, aztrenam, vancomycin

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ihibitoion of bacterial protein sysntehsis

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aminoglycosides, chloramphenicol, macrolindes, tetraclylines, strepgtamins, linezolid, clindamycin

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inhibition of nucelic syntehsis

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fluoroquinilone, rifampin

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inhibition of folic acind syntehsis

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sulfonamide, trimethoprim, prymethamine

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pencillin and cephalosporins reistance

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production of B lactamases, which cleave the beta lactam ring structure, change in PBPs, change in porin

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aminoglycosides resistance

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conjugate rxns that transfer acetyl, phosphoryl, adenyl groups

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macrolides resistance

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formation of methyltransferases that alter drug binding sites on 50S, active transport out of cells

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tetracyclines resistance

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increased pumping drug out of cell

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sulfonamides resistance

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change in sensitivty of inhibiton of target enzyme, increased PABA formation, exogenous folic acid

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fluroquinilone resistance

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change in sensivity to ninhbition of target enzymes, increased activity of transport systems that promote drug efflux

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chloramphenicol resistance

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formation of activating acetyl transferase

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pencillin

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interacts with cytoplasmic membrane binding proteins to inhibit transpeptidation reaction invovled in cross linking, AE- hypersensivity, interstitial nephritis with methicillin, JHR rxn with tx of syphulis(flushing joint pain, proof tht drug is working- used to be assessment too in olden days)

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nafcillin, methicillin, oxacimmin

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betalacatase resistant, staph

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benzathine

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long acting , pencillin G

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amoxicillin

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boreilla, H pylori

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ampicllin

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listeria

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ticarcillin, piperacillin, azlocillin

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extended spectrum, antipseudomonal, betalactamase sensitive

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clavunic acid and sulbactam

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irreversible B lactamase inhibitors

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naficillin and oxacillin

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eliminated via bile

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quinilones

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ciprofloxacin, levofloxacin, MOA- bacteriacidal, interfere with DNA syntehsis, inhibit top II, USE- UTI res to cotromixazole, oral tx for gonnia(1 disoe), skin, soft tissue and bone infections, Diarreha resistant to cotrimixazole(salmonella, shigella, e coli, campylobacter, DONT take with meals, CI in pregnancy, AE- tenodinits, tendon rupture

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metroniddazole

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DOC for giardia, trichomonas, entamoeba, AE- metallic taste, disulfiram like effect

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isoniazid

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anti TB, inhibits mycolic acid syn(only in TB), resistance- del in katG, AE- hepatitis, peripheral neuricts(due to B6 def), SLE

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rifampin

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anti TB, inhibits DNA dep RNA pol, red orange metabolites, 450 induction

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ethambutol

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inhbits syn of arabinaglactan(cell wall comp), decreases red green visual acuity, anti TB

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streptomycin

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anti TB, AE- deafness, nepthroxic

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ampoteracin B

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interactis with ergosterol and forms pores in membres, disrupt membraine permeabiltiy, DOC for systemic infections fungal , IV, poor BBB penetration so need to use it intrathecally, slow clearlance, AE- nefphrotoxic(looks like CRF)

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nyastatin

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topically for local infeciotn, swish and swallow for candiasi, too toxicy for systemic

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azoles

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inhibits 14 alpha demytylase which converts lanestrol to ergosteron, preferred to amph when possible due to less toxicity, AE- gynecomastia, LFTs , CYP inhibitors

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ketoconazole

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DOC for histo para and balsto(preferrered to ampho due to less txocitiy) , decreased absoprtion by antacids

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fluconazole

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DOC for esophageal and invasive candiasis, crypotcoall meningits prohpylactic , CAN CROSS BBB

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Itraconazole and voriconazole

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DOC for blastomyces, sporotrichoses, aspergilloses , itra- increased absoprtion by food

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flucytosine

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cytosine deaminase to 5-FU, 5 FU forms 5Fd UMP which inhibits thymidylate synthase which decreases thymine

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griseofulvin

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acts only against dermatophytes, AE- disufliram rxn

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terbinafine

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only dermatphytes, inhibits squalene epoxidase

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amantidine, enfuvirtide, maraviroc

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block viral penetration/ uncoating

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acyclovir, foscarnet, ganciclovir

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inhibit viral DNA polymerases

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foscarnet, ribavirin

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inhibit viral RNA polymerases

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zidovudine, didanosine, zalcitabine, lamivudine, stavudine, nerviapine, efavirenz

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inhibit viral reverse transcriptase

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idinavir, ritonavir, saquinivir, nelfinavir

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inhibits viral asparate protease

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zanamivir, oseltamivir

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inhibits viral neuraminidase

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acylovir

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viral thymidine kinase, HSV, VZV, AE- NOT HEMATOXIC, neurotxic and crystalluria , chain termination because lacks OH group , res due to change in kianse

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ganciclovir

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viral specific thymidine kihase, phophotransferase(UL97) in CMV, causes chain termination, USE- mostly for CMV prophylacis for retinitis in AIDS and transplant pts , AE- DOSE LIMITING HEMATOXICITY , SEIZURES

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Foscarnet

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inhibits viral DNA and RNA pol, dose limiting nephrotxicity, avoid pentamidine IV(increases nephrotoxicity and hypocalcemia- used for PCP) , USE- acyclovir res strains of HSV

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NNRTs

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do not reuqire metabolic activation- nevirapine and efavirenz, inibits RT at another site different from NRTI bidning

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Zidovudine , AZT

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phosphyrlated nonspecifically to triphospate that can inihibit RT, chain termination , AE- hematoxic, don’t use with stavudine

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Didanosine , DDI

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NRTI, AE- pnaacreatitis, don’t use with zalcitabine

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zalcitabine , DDC

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peripheral neurophaty , don’t use with diadanosine

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stavudine, D4T

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meylosuppresion and periphjeral nuerppathy , don’t use with zidovudine

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lamivudine, 3TC

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least toxic, active in Hep B

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indinavir

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protease inhibitor, cleaves precursor polypetides in HIV so mature portines cant form, resistance due to pt mutation in pol gene, AE- crystalluria

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ritonavir

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protease inhibhitor, induces and inhbits CYP, can lead to type II diabetes and cardiovasvual dsiease

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raltegravir

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integrase inhibitor , prevents integration of viral genome in host cell

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enfuviritide

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binds to gp41 and inhbits fusion of HIV1 and CD4

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maraviroc

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blocks CCR5 protein on macrophages to prevent viral entry

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amantidine

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blocks attachment, penetration and unconatinng of infleunza A, AE- livedo reticualris

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zanamivir, oseltamivir

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inhibits nueromainase A and B, propylaictic fro infleuncza

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Ribivarin

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inhibits viral RNA pol, RNA viruses(RSV, lasssa), AE- hematotxic

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Antitumor interforms

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kaposi(intf gamma)

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Cyclophosphamide

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antiCA, alkylating agent attacks guanine N 7, USE- NHL, breast ca, neurobasltoma, AE- hemoraggic cystitis(tx with mesna)

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mesna

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tx hemoragic cystitc causes by cyclophosphamide

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cisplatin

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anticCA, alkymates DNA, USE- testicular, ovarian, bladder, lung CA, AE- nephrotoxic and neurotoxic(use amifostine for kindesy)

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amifostine

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tx nephrotoxicity with cisplatin

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procarbizine

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antiCA, hodgkins

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Doxirubucin

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atti CA, MOA- antitumor antovdy, AE- cardiotoxcity, free radical gen, USE- HL, breast, lung, endomet, dilated cardiomyopathy

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Methotrexate

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DHF reducatase inh(S phase), USE- lymphoma and lukemia, RA and psoriasis, rescue with leucoverin

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5-Flyroyracin

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pyrimidine antimetabolite( S sphase) to inhibit thymidylate synthetase, colorectal CA

Front 138

6-Mercaptopurine

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purine antimetabolite, USE- ALL, increaed gout with allopurinol

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Bleomycin

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complexes with Fe and O2, G2 phase, USE- HL, testicular, head, neck, skin CA, pneumonitis, pul fibrosis

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viblastin and vincristine

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decrease microtubular polym( Mphase) , vinblastin- BMS, vincristine- neurotoxic, USE- vinblastic( HL, testicular, kaposi), Vincritine(HL, testicular, wilms)

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ATRA

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differentiating agent, t(15;17) differntiation syndrome(resp distress, plerual, pericardial effucsion)

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Renal toxcitiy

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cisplatin, methotrexate

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pulmonary toxicity

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bleomycin, busulfan, procarbizine

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cardiac toxcitiy

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doxarubicin, danurubicin

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neurologic toxicitiy

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vincristine, cisplatin

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immunosuppressive

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cyclophosphamide, methotrexate

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Filgrastim

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increased granulocytes

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Sargromostin

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increased granulocytes and macrophages , AE- CAPILLARY LEAKAGE SYN

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imatinib

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tyrosine kinase inhibitor, used for CML, inhibits bcr abl t(9,22)

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ANTICA with no BMS

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cisplatin, bleomycin, vincritine, asperginase