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25 Cards in this Set
- Front
- Back
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Erythromycin MOA? Bacteri-? What is the group called along with other members?
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Binds to 50S ribosome -> inhibits protein synthesis. Bacteriostatic (but may be bactericidal at [higher]. Macrolides also include clarithromycin, azithromycin, and ketolides.
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Erythromycin spectrum?
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Gram pos like penicillin + [Chlamydia, legionella, mycoplasma]. Gram neg like Neisseria and rickettsia.
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Erythromycin resistance (4)?
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drug efflux, reduced uptake, methylase ribosomal protection, esterases that destroy drug
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Erythromycin absorption?
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Erratic absorption orally. Acid labile. Give on empty stomach. 4 preparations: acid insoluble salt (stearate). Acid insoluble ester (estolate). Enteric coated tables. Plymer Coated
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Erythromycin elimination and drug interaction reason?
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in liver (bile). Metabolized by P450s but metabolites inhibit CYP3A4…
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Erythromycin toxicity (3)?
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GI irritation (#1 problem). 2) liver toxicity -> cholestatic jaundice (estolate). 3) Ototoxicity
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Erythromycin drug interactions (6)?
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Digitoxin, Theophylline, Warfarin, Cyclosporine, Methylprednisolone, lovastatin
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Erythromycin DOC for what 2 things? Also useful for?
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DOC in corynebacterial (diphtheria or corynebacterial sepsis). DOC for Pneumonia b/c pneumococcus, mycoplasma, legionella. Also good for Chlamydia.
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Clarithromycin has 2 advantages over erythromycin? 3 additional bugs mentioned for clarithromycin?
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acid stable and less GI disturbances. H. influenzae, N. gonorrhea, M. avium
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Azithromycin structural difference? 3 advantages? This along with clarithromycin can be used for what prophylaxis?
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lactone ring from adding methylated nitrogen. 1) long t1/2 = daily dosing. 2) much higher [tissue] than [serum]. 3) DOES NOT INACTIVATE P450! (…). Both can be used for BE
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Ketolide (telithromycin) structure difference? Mechanism? Changes in resistance?
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replaced a sugar with 3-keto group. Same as other macrolides. Higher affinity to ribosome and weaker as a substrate to efflux pump.
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Ketolide (telithromycin) Advantage? Administration? Adverse effects?
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macrolide-resistant bacteria. Oral. Same as erythromycin -> inhibits CYP3A4
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Clindamycin structure? MOA?
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Distinct from and smaller than erythromycin. Binds to 50S ribosome at same site too so they are ANTAGONISTIC
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Clindamycin spectrum (3)?
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gram pos (except S. faecalis). Effective against Bacteroides (B. fragilis) and other anaerobes (G +/-)
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Clindamycin resistance, both mechanisms and organisms.
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Mutation of ribosomal proteins, activate methylase. C. diff always resistant. Some pneumococci, S. pyogenes, enterococci are resistant. Some MRSA resistant to erythromycin also resistant
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Clindamycin administration/distribution/excretion
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orally or parenterally. 2) good in soft or hard tissue (bone). 3) liver -> bile
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Clindamycin reactions (3)
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1) Antibiotic-Associated Colitis = pseudomembranous colitis (by overgrowth of C. diff: Tx Metronidazole or Vancomycin). 2) Hypersensitivity. 3) Hematopoetic stuff
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Clindamycin clinical use (4)
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1) ANAEROBIC: Bacteroides, Fusobacterium, Actinomyces, C. perfringens… 2) Combined with Aminoglycosides or cephalosporin for wounds in the abdomen or gut. 3) infections allergic to penicillin. 4) BE prophylaxis
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Vancomycin MOA? Bacteri-? Spectrum?
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Binds to D-Ala-D-Ala of polyglycan cell wall. 2) bactericidal. 3) gram-positive only. Effective against staph/strep/Clostridia/Actinomyces/oral anaerobes -> E. faecalis
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Vancomycin Tx (4)? DOC for?
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1) resistant staph/strep in tissue/bone (osteomyelitis). 2) allergies to penicillin. 3) In combination with Aminoglycosides for endocardities from S. faecalis. 4) AAC. DOC for MRSA
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Vancomycin absorption, clearance?
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Poor GI -> oral use only for AAC but everything else IV. 90% renal.
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Vancomycin adverse reactions (4)
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1) Ototoxicity. 2) Nephrotoxicity (additive with aminoglycosides). 3) Phlebitis at injection. 4) Hypersensitivity both delayed (skin rashes), immediate (uticaria), and anaphylactic-type (red-neck syndrome).
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Linezolid MOA? Bacteri-?
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Bind to 50S large subunit and affect 70S formation. Bacteriostatic (except bactericidal for streptococci).
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Linezolid spectrum? Resistance?
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gram positive, and moderately for TB. 2) decrease drug binding to 23S rRNA
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Linezolid Tx? Absorb/distrib/excretion?
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1) reserved for MRSA, VRSA, and VRE. 2) Completely absorbed orally, widely distributed, both renal and non-renal excretion.
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