Abstract
This case discusses the pharmacokinetic interaction between midazolam and itraconazole, resulting in increased sedation. Midazolam is a cytochrome P450 3A4 substrate and itraconazole is a 3A4 inhibitor.
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Quinney SK, Galinsky RE, Jiyamapa-Serna VA, et al. Hydroxyitraconazole, formed during intestinal first-pass metabolism of itraconazole, controls the time course of hepatic CYP3A inhibition and the bioavailability of itraconazole in rats. Drug Metab Dispos. 2008;36:1097–101.
Isoherranen N, Kunze KL, Allen KE, et al. Role of itraconazole metabolites in CYP3A4 inhibition. Drug Metab Dispos. 2004;32:1121–31.
Olkkola KT, Backman JT, Neuvonen PJ. Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole. Clin Pharmacol Ther. 1994;55:481–5.
Ahonen J, Olkkola KT, Neuvonen PJ. Effect of itraconazole and terbinafine on the pharmacokinetics and pharmacodynamics of midazolam in healthy volunteers. Br J Clin Pharmacol. 1995;40:270–2.
Olkkola KT, Ahonen J, Neuvonen PJ. The effects of the systemic antimycotics, itraconazole and fluconazole, on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Anesth Analg. 1996;82:511–6.
Krishna G, Moton A, Ma L, et al. Effects of oral posaconazole on the pharmacokinetic properties of oral and intravenous midazolam: a phase I, randomized, open-label, crossover study in healthy volunteers. Clin Ther. 2009;31:286–98.
Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Effects of the antifungal agents on oxidative drug metabolism: clinical relevance. Clin Pharmacokinet. 2000;38:111–80.
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Wittwer, E.D., Sprung, J., Nicholson, W.T. (2015). When Enough Is Now Too Much. In: Marcucci, C., et al. A Case Approach to Perioperative Drug-Drug Interactions. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-7495-1_81
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