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35 Cards in this Set
- Front
- Back
isoniazid
MOA MOR SE |
MOA - inhibit mycolic acid synthesis
MOR - chromosomal: katG, inhA, ndh SE - hepatotoxicity (fast acetylators), peripheral neuritis (slow acetylators), hemolysis (G6PD) |
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rifampin
MOA MOR SE |
MOA - inhibit DNA dep. RNA polymerase
MOR - chromosomal: rpoB SE - orange metabolites, decrease effectiveness of OCPs |
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ethambutol
MOA MOR SE |
MOA - inhibit synth of arabinogalactan (cell wall)
MOR - chromosomal: embCAB SE - optic neuritis, ↓ visual acuity |
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pyrazinamide
MOA MOR SE |
MOA - inhibits trans-translation
MOR - chromosomal: pncA SE - hyperuricemia, hepatic dysfunction, porphyria |
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treatment principles of TB & leprosy
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TB: for latent, give either INH or rifampin
active, give all 4 (RIPE) to prevent resistance leprosy: ALWAYS give multiple drugs multibacillary = dapsone + rifampin + clofazimine paucibacillary = dapsone + rifampin |
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tx of TB in HIV+
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need to substitute RIFABUTIN for rifampin
rifampin will induce P450 and interact w/ protease inhibitors |
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macrolides
MOA MOR |
50S, inhibit translocation
methyltransferases alter binding site |
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chloramphenicol
MOA MOR |
50S, inhibit transpeptidation
inactivating acetyltransferases |
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aminoglycosides
MOA MOR |
30S, blocks initiation, elicits premature termination, incorporate incorrect AA
acetyl, phosphoryl, or adenylyl conjugation |
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tetracyclines
MOA MOR |
30S, prevent binding the incoming charged tRNA
"pump out" |
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fluroquinolones
MOA MOR |
inhibiting topoisomerase
∆ in sensitivity of TE "pump out" |
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rifampin
MOA MOR |
inhibits DNA dependent RNA polymerase
∆ in enzyme |
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sulfas
MOA MOR |
inhibition of folic acid synthesis
↓ sensitivity of target enzymes ↑ formation of PABA use of exogenous folate |
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beta lactams
MOA MOR |
inhibition of bacterial cell wall synthesis (inhibit transpeptidation)
penicillinase, modification of PBPs (transpeptidase), ∆ of porins |
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vancomycin
MOA MOR |
inhibition of peptidoglycan chain elongation
∆ in pentapeptide, D-ala-D-lactate (DNA mutation) |
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tendon rupture
other SEs of this class? |
FQs
also prolong QT interval & hepatotoxic |
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3 shortcomings of cipro?
|
• not very effective against anaerobes
• not effective against pneumococci • not great CNS penetration ***moxi– & gemifloxacin have improved on these 3 weaknesses |
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4 major drug classes for anaerobic infections?
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• chloramphenicol
• carbapenems • combo of extended spectrum penicillin w/ penicillinase inhibitor • metronidazole |
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3 agents that are used only for UTIs? why?
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nitrofurantoin
methenamine mandelate nalidixic acid don't reach high enough [plasma] but they get concentrated in the urine, making them effective for UTIs |
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major route of elimination for cephalosporins? drug interaction?
which 2 cephs are eliminated by a different route? |
• most by kidney
• acid, so probenecid will compete & ↓ excretion, prolonging t1/2 • cefoperazone = 100% liver • ceftriaxone = 50% liver (these are both 3rd gen) |
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3 drugs that are beta-lactamase inhibitors, used in combo w/ penicillins
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• clavulanic acid
• sulbactam • tazobactam |
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staph aureus treatment:
beta-lactamase negative beta-lactamase + methicillin resistant |
• if doesn't produce beta-lactamase, penicillin is DOC
• staph can acquire beta-lactamase via PLASMID. in this case, penicillinase resistant pen is DOC • MRSA is due to modification of PBPs via CHROMOSOMAL mutation. vancomycin is DOC |
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2nd line drugs for treatment of MRSA?
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TMP-SMX, minocycline, linezolid, daptomycin, tigecycline
|
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side effect of imipenem
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seizures
|
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ICWS that is very resistant to penicillinase and is effective against only gram –
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aztreonam
(class is monobactams) also important to know that it has NO cross hypersensitivity w/ penicillin or cephalosporins |
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inhibitor of protein synthesis that is bactericidal
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aminoglycosides
includes gentamicin, tobramycin, amikacin, streptomycin, neomycin |
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triple antibiotic combo for post-op wound healing
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neomycin + bacitracin + polymixin
|
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which macrolide can be used during pregnancy?
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azithromycin
|
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streptogramins
drug name? MOA? use? SE? |
• dalfopristin, quinupristin
• 50S binding; synergistic action • developed for VRSA & VRE; only gr+ & only parenteral • inhibits P450 (watch out for warfarin/phenytoin) |
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oxazolindinones
drug name? MOA? use? SE? |
• linezolid
• inhibit protein synthesis • only gr+; very high tissue penetration into CNS • reversible MAO inhibition, so lots of drug interactions, esp. tyramine containing foods |
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drug most famous for pseudomembranous colitis?
treatment for PMC? |
• clindamycin (they can all cause PMC, but this is the classic drug)
• tx w/ metronidazole (DOC) or oral vancomycin |
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treatment for osteomyelitis
what makes this drug an effective choice? |
• clindamycin
• it accumulates in the bones and is excellent for staph aureus (mcc of osteomyelitis) |
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macrolides
diarrhea & P450 spectrum? |
• erythromycin: worst for diarrhea & inhibits P450
• clarithromycin: causes the least diarrhea, but still inhibits P450 • azithromycin: causes moderate diarrhea level, but does NOT inhibit P450 |
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drug to treat ENL (erythemo nodosum leprosum)
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thalidomide
|
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sulfa drug used topically
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silver sulfadiazine
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