[Pharmacokinetic evaluation of fluconazole in healthy volunteers].
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.
Shiba
K
K
Second Department of Internal Medicine, Jikei University School of Medicine.
Saito
A
A
Miyahara
T
T
D000284:Administration, Oral; D000328:Adult; D000935:Antifungal Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001774:Blood Chemical Analysis; D004361:Drug Tolerance; D015725:Fluconazole; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D012016:Reference Values; D014230:Triazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D000935:Antifungal Agents; D014230:Triazoles; D015725:Fluconazole