[Pharmacokinetic evaluation of fluconazole in healthy volunteers]

Abstract

Fluconazole, a novel triazole antifungal agent, was studied for its safety and pharmacokinetics following single oral or intravenous dose to 8 healthy male volunteers. Dosages employed were 25 mg, 50 mg and 100 mg orally and 25 mg and 50 mg intravenously. With oral doses, peak plasma levels were achieved in 2 hours in all subjects, with maximum plasma levels of 0.53 microgram/ml at a dose of 25 mg, 0.92 microgram/ml at 50 mg and 1.88 micrograms/ml at 100 mg showing a clear dose-response. Plasma-half lives of the drug were about 31 hours in both oral and intravenous administrations. Its urinary recoveries were about 70% as given orally as well as intravenously. There was no difference between areas under plasma concentration-time curves (AUC) obtained with the 2 administration methods. No side effects nor abnormal clinical test values were reported with any subjects studied.