title: Influence of fluconazole on antipyrine kinetics in rats.
abstract: The present study was undertaken to examine the effect of fluconazole on in vivo drug metabolism in rats, using the model substrate antipyrine. Oral doses of fluconazole, 20 mg/kg, were administered once (acutely) or twice daily for 4 days (chronically). Control animals received oral drug vehicle. Antipyrine kinetics were determined following an intravenous dose of 20 mg/kg given either 1 or 12 h after the single or last dose of fluconazole respectively. Acute fluconazole treatment significantly increased antipyrine half-life by 250% and reduced its clearance by 50%, without affecting its volume of distribution. Chronic treatment with fluconazole failed to affect antipyrine pharmacokinetics. This study demonstrates that acute fluconazole inhibits the metabolism of antipyrine in rats.
authors.affiliation: Department of Pharmacy, University of Sydney, Australia.
authors.forename: I
authors.initials: I
authors.lastname: Ramzan
authors.forename: M
authors.initials: M
authors.lastname: Chan
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000983:Antipyrine / Q000097:blood / Q000493:pharmacokinetics*; D004334:Drug Administration Schedule; D004347:Drug Interactions; D015725:Fluconazole / Q000008:administration & dosage / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D015725:Fluconazole; D000983:Antipyrine