Increased Gastric pH and the Bioavailability of Fluconazole and Ketoconazole

Excerpt Two orally active antifungal agents are currently available, ketoconazole and fluconazole. However, the absorption of ketoconazole depends on gastric pH for tablet disintegration and dissolution (1, 2). Reduced serum concentrations of ketoconazole have been reported in patients with achlorhydria and in patients receiving concomitant treatment with antacids or cimetidine (1-3). Our study was done to determine the effects of cimetidine-induced increases in gastric pH on the relative bioavailability of fluconazole and ketoconazole. Methods Twenty-four healthy male volunteers, 19 to 43 years of age, gave written informed consent to participate in the study. The study protocol was approved by the...