Focus on... Linezolid: a synthetic oxazolidinone antimicrobial for treatment of serious gram-positive infections.

Linezolid is the first in a new class of antimicrobials called oxazolidinones. It is the first agent since vancomycin to be approved with a specific indication for methicillin-resistant Staphylococcus aureus (MRSA) infections. Linezolid possesses a unique mechanism of action that accounts for its effectiveness in multidrug-resistant gram-positive infections. It disrupts protein synthesis of gram-positive bacteria by binding to the 50S ribosomal subunit and inhibiting formation of the 70S initiation complex. Phase III trials have shown linezolid to be effective in the treatment of infections caused by vancomycin-resistant Enterococcus faecium and hospital-acquired pneumonia, including cases caused by MRSA. Linezolid is well tolerated, with headache, nausea, and diarrhea being the most common adverse effects. The drug's 5-hour elimination half-life and short postantibiotic effect allow twice-daily dosing. Availability of both intravenous and oral formulations allows for 'IV to PO' switching without the need for dosage or antimicrobial changes. [ABSTRACT FROM AUTHOR]

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