Antimicrobial drugs
Terms
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- Penicillins
- M: Bind PBPs to inhibit peptidoglycan cross-linking; U: gram-positive, Neisseria; SE: allergies; R: altered PBP, B-lactamase
- Ampicillin, Amoxicillin
- M: same as penicillin U: Gram + and HELPS (H influ, E coli, listeria, Proteus, Salmonella, enterococci); can use with clavulanic acid (B-lactamase inhibitor)
- Methicillin, Nafcillin, Oxacillin
- M: same as penicillins; use to treat S. aureus
- Carbenicillin, piperacillin, ticarcillin
- Use vs. Pseudomonas
- 1st gen cephalosporins
- B-lactam drugs but less susceptible to B-lactamases; U: gram-positive + PEcK
- 2nd gen cephalosporins
- gram-positive + HEN PEcKS
- 3rd gen cephalosporins
- good gram negative coverage; treat meningitis, and gonorrhea (ceftriaxone)
- 4th gen cephalopsporin (cefepime)
- Pseudomonas coverage
- Monobactam (Aztreonam)
- Binds PBP3, no cross-reactivity with penicillins, gram - ONLY,
- Imipenem/cilastatin
- Cilastatin is an inhibitor of renal dehydropeptidase I to preserve imipenem from cleavage; hits + and -; SE: seizures
- Vancomycin
- Binds D-ala-D-ala linkage of peptidoglycan backbone to prevent ligase access for peptidoglycan polymerization; GRAM + only (MRSA, C. dificle); SE: ototoxicity, nephrotoxicity, Red-man syndrome; R: changes D-ala-D-ala to D-ala-D-lac
- Aminoglycosides (gentamicin, other "mycins")
- M: Block initiation complex; U: gram negative rods; synergistic w/ B-lactams; SE: nephrotoxicity, ototoxicity, pregnancy contraindicated; R: altered 30S subunit
- Tetracyclines ("cyclines")
- M: prevent tRNA binding; U: Broad-spectrum (VACUUM BedRoom Tonight); SE: Ca2+ chelator for discolor teeth, stunt bone growth; phototoxicity
- Chloramphenicol
- M: Blocks peptide bond formation; U: meningitis (H flu, Neisseria, Strep pneumo) but limited b/c of toxicity; SE: aplastic anemia, gray baby; R: enzymatic inactivation
- Macrolides (erythromycin)
- M: Block translocation; U: URIs, pneumonias (CAP), gram + cocci; SE: inhibit P450; R: ribosomal RNA (rRNA) methylation
- Clindamycin
- M: Blocks ribosome function; U: ANAEROBES above diaphragm except C. dificile; SE: risk for pseudomembranous colitis by C. dificile; R: rRNA methylation
- Linezolid
- Against MRSA and PRSP; block initiation at 50S
- Sulfonamides
- M: Block dihydropteroate synthase as PABA analog; U: ulcerative colitis, UTI, burns; SE: kernicterus, hemolysis, allergies; R: increased DHFR
- Trimethroprim
- M: Inhibits DHFR; U: as TMP-SMX for PCP, gram +/-, traveler's diarrhea; SE: megaloblastic anemia (for TMP), reversible thrombocytopenia by giving leucovorin
- Fluoroquinolones
- M: Inhibit DNA gyrase/topo IV, concentration-dep killing; U: Pseudomonas in CF pts, UTI/STDs; SE: cartilage damage, tendinitis
- Isoniazid
- M: Inhibits mycolic acid synthesis; U: First-line TB drug, use as prophylaxis; SE: Neuropathy, hepatotoxicity; R: metabolized by N-acetyltransferase at diff rates, so can use pyroxidine
- Ethambutol
- M: Inhibit arabinosyltransferases needed to make cell wall; penetrates CNS for TB meningitis SE: retrobulbar neuritis (eye)
- Rifampin
- RNA polymerase inhibitor; revs up P450; red/orange body fluids; rapid resistance if used alone
- Pyrazinamide
- polyarthralgia, hepatitis