Induction of Fluconazole Metabolism by Rifampin: In Vivo Study in Humans

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Abstract
The effects of rifampin on the pharmacokinetics of fluconazole were analyzed in an open‐label, placebo‐controlled, parallel study. Sixteen healthy male volunteers, randomized into two groups, received 200 mg of oral fluconazole on days 1 and 22. On days 8 through 27, group I received oral rifampin, 600 mg/d, and group II received placebo. Fluconazole in serum was analyzed by HPLC. On days 1 and 22, respectively, the AUC (μg · hr/mL) (mean ± SD) was 160.5 ± 19.5 and 124 ± 22.2 in group I, 152 ± 25 and 152.8 ± 33.9 in group II; the Kel (hr−1) was .0211 ± .0030 and .0264 ± .0040 in group I, .0219 ± .0036 and .0216 ± .0053 in group II. Cmax and Tmax did not change significantly in either group. Urinary 6β‐hydroxycortisol/cortisol increased from 3.47 ± 1.04 to 15.2 ± 5.07 in group I, but was unchanged (3.54 ± 1.33–4.26 ± 2.36) in group II on days 1 and 22, respectively. The findings in this study indicate that rifampin induces the metabolism of fluconazole.

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