Linezolid (Zyvox)
  • Overview
    • Linezolid (Zyvox) should be used only for well-documented, serious vancomycin (Vancocin) resistant enterococcal infections
    • New antibiotic class: oxazolidinones
    • Management for infections caused by:
      • Vancomycin (Vancocin)-resistant Enterococcus faecium
      • Nosocomial & community-acquired Staphylococcus aureus pneumonia
      • Nosocomial & community acquired danazol (Donocrine)-susceptible Streptococcus pneumoniae
      • Skin & skin-structure infections
  • Two formulations FDA approved for treatment of vancomycin (Vancocin)-resistant enterococci:
    • linezolid (Zyvox)--oral & parenteral use
    • quinupristin/dalfopristin (Synercid) -- parenteral use only
  • Antibacterial characteristics
    • Inhibits bacterial ribosomal-mediated protein synthesis
    • Bacteria static against streptococci
    • Activity profile:
      •  Linezolid (Zyvox): effective against both E. faecium and Enterococcus faecalis {quinupristin/dalfopristin (Synercid): active against vancomycin (Vancocin)-resistant E. faecium but not Enterococcus faecalis}
      •  Linezolid (Zyvox):
        •  Active against staphylococci, including methicillin (Staphcillin) resistance Staphylococcus aureus & methicillin (Staphcillin) resistance Staphylococcus epidermidis
        • Active against  penicillin-resistant pneumococci & Staphylococcus aureus with intermediate susceptibility vancomycin (Vancocin)
      •  No clinical useful gram-negative activity
  • Pharmacokinetics:
    • Following oral administration:  rapid/complete absorption from  gastrointestinal tract
    • Partial hepatic metabolism
    • Urinary excretion
  •  Side/Adverse Effects
    • Well-tolerated
    • Most-common adverse effects: gastrointestinal (nausea, diarrhea, vomiting)
    • With prolonged use: reversible thrombocytopenia
      • For treatment > 2 weeks, platelet count monitoring is recommended
    • Linezolid (Zyvox) oral suspension contains phenylalanine, contraindicated in patients with  phenylketonuria
  • Drug-Drug Interactions
    • Linezolid (Zyvox)-weak MAO inhibitor (nonselective)
    • Patients should avoid  tyramine-rich foods
    • Cautious use with linezolid (Zyvox) in combination with:
      •  pseudoephedrine
      •  phenylpropanolamine
      •  serotonin selective reuptake inhibitors (SSRIs)
      • possibly other antidepressants
    • No effect on cytochrome P450 enzyme metabolizing system

 

  • primary reference: Linezolid (Zyvox): The Medical Letter, volume 42 (issued 1079); May 29, 2000.