Rx Update: August 2000

Linezolid

Mary Ross, R.Ph., M.B.A.
Peer Review Status: Internally Reviewed


Linezolid (Zyvox®- Pharmacia & Upjohn) is an oxazolidone antimicrobial agent that is unrelated to other commercially available agents. Linezolid use is reserved for the treatment of resistant infections due to vancomycin-resistant Enterococcus faecium and methicillin-resistant Staphylococcus aureus (MRSA).

The most common adverse effects associated with the use of linezolid are diarrhea, headache, nausea, vomiting, insomnia, constipation, rash, dizziness, fever, thrombocytopenia, pseudomembranous collitis, and tongue discoloration or coating. Thrombocytopenia has occurred in 2.4% of linezolid-treated patients. Platelet counts should be monitored in patients at increased risk of bleeding, with pre-existing thrombocytopenia, receiving concomitant medications that may decrease platelet count or function, or requiring more than 2 weeks of therapy.

Linezolid is a competitive, reversible inhibitor of monoamine oxidase and it has the potential to interact with adrenergic and serotonergic agents. Patients taking linezolid should avoid large quantities of tyramine-containing foods or beverages (>100 mg per meal). Linezolid may also cause a reversible pressor response to indirect acting sympathomimetics, vasopressor, or dopaminergic agents (e.g., pseudoephedrine, phenylpropanolamine). Concurrent therapy with linezolid and serotonergic agents (e.g., fluoxetine, paroxetine) should be administered cautiously and the patients should be monitored for signs and symptoms of serotonin syndrome (i.e., hyperpyrexia, cognitive dysfunction).

The recommended dose of linezolid is 600 mg intravenously or orally every 12 hours. No dosage adjustment is necessary when switching form intravenous to oral administration. Linezolid should be administered by intravenous infusion over 30 to 120 minutes. Linezolid should not be infused concomitantly with other medications. If the same intravenous line is used for the infusion of several drugs, the line should be flushed before and after infusion of linezolid with a compatible solution (e.g., NS, D5W, LR). Oral linezolid can be taken without regard to meals. Linezolid is available as 600 mg tablets, a 100 mg per 5 ml oral suspension, and a 600 mg per 300 ml isotonic intravenous solution.


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