questions 2

Macrolides

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Topic updated on 12/18/16 4:45am

Introduction
  • Classification
    • antibiotic
      • anti-ribosomal
        • anti-50S ribosomal subunit
          • macrolides
  • Drugs
    • erythromycin
      • well absorbed orally or IV
    • azithromycin
      • marketed as oral "Z-pack"
      • well absorbed orally or IV
    • clarithromycin
      • well absorbed orally
    • telithromycin
      • newest
      • well absorbed orally
Mechanism
  • Action 
    • bacteriostatic at low doses, bacteriocidal at high doses
    • binds to 23S rRNA of the 50S ribosomal subunit 
    • blocks translocation of tRNA and thereby inhibits protein synthesis
  • Resistance
    • via methylation of rRNA
      • can occur near erythromycin's binding site
Uses
  • Outpatient treatment of respiratory tract infections (URI, LRI)
  • Atypical pneumonia
    • Legionella pneumophila
    • Chlamydophila
    • Mycoplasma pneumoniae
  • STDs
    • Chlamydia
    • Neisseria
  • Gram-positive cocci
    • strep infections in patients with penicillin allergy
  • Moraxella
Adverse effects
  • Generally safe and well-tolerated
  • Avoid in pregnancy
    • acute cholestatic hepatitis in mother (erythromycin)
    • embryotoxic (clarithromycin)
  • GI upset
    • induces peristalsis
      • especially erythromycin
    • causes noncompliance
  • Prolonged QT syndrome
    • especially erythromycin
  • Eosinophilia
  • Acute cholestatic hepatitis
  • ↑ serum concentration of theophyllines
  • ↑ serum concentration of oral anticoagulants
  • Rashes
  • Telithromycin contraindicated in myasthenia gravis
    • can result in respiratory failure


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