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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)
rifampin
MOA
MOR
SE
MOA - inhibit DNA dep. RNA polymerase
MOR - chromosomal: rpoB
SE - orange metabolites, decrease effectiveness of OCPs
ethambutol
MOA
MOR
SE
MOA - inhibit synth of arabinogalactan (cell wall)
MOR - chromosomal: embCAB
SE - optic neuritis, ↓ visual acuity
pyrazinamide
MOA
MOR
SE
MOA - inhibits trans-translation
MOR - chromosomal: pncA
SE - hyperuricemia, hepatic dysfunction, porphyria
treatment principles of TB & leprosy
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
tx of TB in HIV+
need to substitute RIFABUTIN for rifampin

rifampin will induce P450 and interact w/ protease inhibitors
macrolides
MOA
MOR
50S, inhibit translocation

methyltransferases alter binding site
chloramphenicol
MOA
MOR
50S, inhibit transpeptidation

inactivating acetyltransferases
aminoglycosides
MOA
MOR
30S, blocks initiation, elicits premature termination, incorporate incorrect AA

acetyl, phosphoryl, or adenylyl conjugation
tetracyclines
MOA
MOR
30S, prevent binding the incoming charged tRNA

"pump out"
fluroquinolones
MOA
MOR
inhibiting topoisomerase

∆ in sensitivity of TE
"pump out"
rifampin
MOA
MOR
inhibits DNA dependent RNA polymerase

∆ in enzyme
sulfas
MOA
MOR
inhibition of folic acid synthesis

↓ sensitivity of target enzymes
↑ formation of PABA
use of exogenous folate
beta lactams
MOA
MOR
inhibition of bacterial cell wall synthesis (inhibit transpeptidation)

penicillinase, modification of PBPs (transpeptidase), ∆ of porins
vancomycin
MOA
MOR
inhibition of peptidoglycan chain elongation

∆ in pentapeptide, D-ala-D-lactate (DNA mutation)
tendon rupture

other SEs of this class?
FQs

also prolong QT interval & hepatotoxic
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
4 major drug classes for anaerobic infections?
• chloramphenicol
• carbapenems
• combo of extended spectrum penicillin w/ penicillinase inhibitor
• metronidazole
3 agents that are used only for UTIs? why?
nitrofurantoin
methenamine mandelate
nalidixic acid

don't reach high enough [plasma] but they get concentrated in the urine, making them effective for UTIs
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)
3 drugs that are beta-lactamase inhibitors, used in combo w/ penicillins
• clavulanic acid
• sulbactam
• tazobactam
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
2nd line drugs for treatment of MRSA?
TMP-SMX, minocycline, linezolid, daptomycin, tigecycline
side effect of imipenem
seizures
ICWS that is very resistant to penicillinase and is effective against only gram –
aztreonam
(class is monobactams)

also important to know that it has NO cross hypersensitivity w/ penicillin or cephalosporins
inhibitor of protein synthesis that is bactericidal
aminoglycosides

includes gentamicin, tobramycin, amikacin, streptomycin, neomycin
triple antibiotic combo for post-op wound healing
neomycin + bacitracin + polymixin
which macrolide can be used during pregnancy?
azithromycin
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)
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
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
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)
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
drug to treat ENL (erythemo nodosum leprosum)
thalidomide
sulfa drug used topically
silver sulfadiazine