European journal of clinical pharmacology
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Eur. J. Clin. Pharmacol. · Nov 2000
Randomized Controlled Trial Clinical TrialEffects of metronidazole on midazolam metabolism in vitro and in vivo.
Case reports have described elevated concentrations of CYP3A4 substrates (e.g. cyclosporin) during metronidazole treatment. Therefore, we wanted to study whether metronidazole affects CYP3A4 activity, using midazolam as a model substrate in vitro and in vivo. ⋯ Metronidazole had no effects on the 1'-hydroxylation of midazolam in vitro or on the pharmacokinetics and pharmacodynamics of midazolam in vivo. These findings indicate that metronidazole is not an inhibitor of CYP3A4.