Linezolid: an oxazolidinone antimicrobial agent

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.
• 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.