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Related Experiment Videos

Linezolid: an oxazolidinone antimicrobial agent.

H B Fung1, H L Kirschenbaum, B O Ojofeitimi

  • 1Critical Care Center, Veterans Affairs Medical Center, Bronx, New York 10468, USA. horatio.fung@med.va.gov

Clinical Therapeutics
|April 25, 2001
PubMed
Summary

Linezolid is an effective oxazolidinone antibiotic for serious gram-positive infections, including vancomycin-resistant Enterococcus faecium. Reserve linezolid for resistant infections due to potential bacterial resistance.

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Area of Science:

  • Pharmacology and Infectious Diseases
  • Antimicrobial Resistance Mechanisms
  • Drug Development and Clinical Trials

Background:

  • Linezolid is the first marketed oxazolidinone antibiotic in the U.S.
  • Indicated for nosocomial pneumonia, complicated skin infections, and vancomycin-resistant Enterococcus faecium infections.
  • Also treats uncomplicated skin infections and community-acquired pneumonia caused by susceptible bacteria.

Purpose of the Study:

  • To review the pharmacologic properties of linezolid.
  • To assess the clinical usefulness of linezolid in treating various infections.
  • To evaluate its efficacy and safety profile.

Main Methods:

  • Literature search of multiple databases (MEDLINE, HealthSTAR, etc.) from 1966 to September 2000.

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  • Included terms: linezolid, PNU-100766, and oxazolidinone.
  • Reviewed meeting abstracts from relevant infectious disease conferences.

    • Main Results:

    • Linezolid targets protein synthesis early, with unlikely cross-resistance.
    • Effective against gram-positive bacteria, with resistance reported in enterococci.
    • Pharmacokinetics are not significantly affected by age, sex, or organ function; metabolism is CYP450-independent.
    • Clinical trials show efficacy in various infections, including those with resistant organisms.
    • Adverse effects include thrombocytopenia, diarrhea, headache, and nausea.
    • Preliminary data suggest shorter hospital stays for linezolid recipients.

    Conclusions:

    • Linezolid demonstrates efficacy with an acceptable tolerability profile.
    • Due to resistance risk, linezolid should be reserved for documented serious vancomycin-resistant enterococcal infections.