Clinical Information

Flucytosine is a broad-spectrum antifungal agent generally used in combined therapy (often with amphotericin B) for treatment of fungal infections such as cryptococcal meningitis. Concerns with toxicity (bone marrow suppression, hepatic dysfunction) and development of fungal resistance limit use of flucytosine, particularly as a monotherapy. The drug is well-absorbed orally, but can also be administered intravenously (available outside of the United States).

There is good correlation between serum concentrations of flucytosine with both efficacy and risk for toxicity. Because of the drug’s short half-life (3-6 hours), therapeutic monitoring is typically performed at peak levels, 1 to 2 hours after an oral dose or 30 minutes after intravenous administration.

Flucytosine is eliminated primarily as unmetabolized drug in urine. Patients with renal dysfunction may require dose adjustments or more frequent monitoring to ensure that serum concentrations do not accumulate to excessive levels. Nephrotoxicity associated with use of amphotericin B can affect elimination of flucytosine when the drugs are coadministered.