Therapeutic Uses

Linezolid is FDA-approved for treatment of infections caused by vancomycin-resistant E. faecium; nosocomial pneumonia caused by methicillin-susceptible and-resistant strains of S. aureus; community-acquired pneumonia caused by penicillin-susceptible strains of S. pneumoniae; complicated skin and skin-structure infections caused by streptococci and methicillin-susceptible and -resistant strains of S. aureus; and uncomplicated skin and skin-structure infections. Linezolid (600 mg twice daily) has had clinical and microbiological cure rates in the range of85—90% in treatment of a variety of infections caused by vancomycin-resistant E. faecium. A 400-mg, twice-daily dosage regimen is recommended only for treatment of uncomplicated skin and skin-structure infections.

Cure rates with linezolid (~60%) were similar to those with vancomycin for nosocomial pneumonia caused by methicillin-resistant or -susceptible S. aureus. Linezolid efficacy also was similar to that of either oxacillin or vancomycin for skin and skin-structure infections, the majority of cases due to by S. aureus. Linezolid appears comparable in efficacy to vancomycin for methicillin-resistant strains. Linezolid may be effective for patients with methicillin-resistant S. aureus infections who are failing vancomycin therapy or whose isolates have reduced susceptibility to vancomycin. Linezolid is bacteriostatic for staphylococci and enterococci and probably should not be used to treat suspected endocarditis.

Linezolid should be reserved as an alternative agent for infections caused by multiple-drug-resistant strains. It should not be used when other agents are likely to be effective. Indiscriminant use and overuse will hasten selection of resistant strains and the eventual loss of this valuable new agent.

untoward effects The drug generally has minor side effects (e.g., GI complaints, headache, rash). Myelosuppression, including anemia, leukopenia, pancytopenia, and thrombocy-topenia, has been reported. Platelet counts should be monitored in patients with risk of bleeding, preexisting thrombocytopenia, or disorders of platelet function and in patients receiving therapy for >2 weeks. Linezolid is a weak, nonspecific inhibitor of MAO. Patients receiving concomitant therapy with adrenergic or serotonergic agents or consuming more than 100 mg of tyramine daily may have palpitations, headache, or hypertensive crisis. Peripheral and optic neuropathy after prolonged use reverse upon drug discontinuation.

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