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RavLect17: Macrolide


Macrolides Erythromycin Clarithromycin Azithromycin Fidaxomicin
Macrolide MoA Mainly static: reversible binding to 50S ribosomal subunit; inhibit protein synthesis
Mech of Resistance to Macrolides 1) induction of active efflux pumps 2) induction of methylase enzyme: decreased drug binding 3) production of an esterase enzyme or phosphorylase enzyme 4) chromosomal mutation of 50s ribosome
Macrolide PK Low conc in urine (goes to bowel instead) -> not for UTI Tx. Ok for STDs though.
Macrolide available forms IV & PO: Erythromycin, Azithromycin Oral only: Clarithromycin
Erythromycin SoA G+ cocci and bacilli: Staph., Strept., Corynebacterium diphtheriae, Clostridium perfringens Also C. trachomatis, E. histolytica, L. monocytogenes, B. burgdorferi, M. pneumoniae, T. pallidum, U. urealyticum
Erythromycin clinical use PCN allergic patients Chlamydia acne (as topical ointment, solution or gel) ophthalmic surgical prophylaxis with neomycin promote GI motility for post-op atonic colon
Pediazole (erythromycin and sulfisoxazole) Not given if under 2 years because of sulfonamide issues in pediatrics
Clarithromycin SoA (Synthetic modification of erythromycin) Spectrum same as erythro, but more against G+, H. flu, M. catarrhalis, CAP atypicals, and MAC. Also Tx M. leprae, toxoplasmosis and cryptosporidium plasmodium
Clarithromycin use CAP, COPD exacerbation, Bronchitis, Tonsilitis, OM (good ear conc), STD’s, MAC (only as combo with ethambutol +/- rifabutin), H. Pylori
Erythromcin ADRs GI problems (NVD) Jaundice & hepatotoxcitiy rash nephritis dose-related ototoxicity prolonged QT interval
Clarithromycin ADRs Fewer GI issues than erythromycin & augmentin rarely: rash, hepatic dysfxn, CNS problems, QT prolongation, nephritis
Azithromycin (Z-Pak, Tri-Pak, Zmax) PK Synthetic modification of erythromycin: less acid degredation Long half-life! Good for Kids & Adults
Azithromycin ADRs Less GI issues (NVD) Rare: Hepatitis & LFT increases Rare: otoxicity (hearing problems) QT prolongation
Azithromycin usage CAP, bronchitis, Sinusitis, STDs Also for pneumonia & otitis media in kids
Fidaxomicin (Dificid) Oral, nonsystemic macrolide. Like Vanco, Fidaxomicin shouldn't be used for systemic infection! Main target: C. diff Must be 100% compliant or else resistance!
Created by: cheeoh