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Induction of the metabolism of etizolam by carbamazepine in humans

  • Pharmacokinetics and Disposition
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Abstract

Objective

To examine the effect of carbamazepine on the single oral dose pharmacokinetics of etizolam.

Methods

Eleven healthy male volunteers received carbamazepine 200 mg/day or placebo for 6 days in a double-blind, randomized, crossover manner, and on the sixth day they received a single oral 1-mg dose of etizolam. Blood samplings and evaluation of psychomotor function by the Digit Symbol Substitution Test and Stanford Sleepiness Scale were conducted up to 24 h after etizolam dosing. Plasma concentration of etizolam was measured using high-performance liquid chromatography.

Results

Carbamazepine treatment significantly decreased the peak plasma concentration (17.5±4.1 ng/ml versus 13.9±4.1 ng/ml; P<0.05), total area under the plasma concentration–time curve (194.8±88.9 ng h/ml versus 105.9±33.0 ng h/ml; P<0.001), and elimination half-life (11.1±4.6 h versus 6.8±2.8 h; P<0.01) of etizolam. No significant change was induced by carbamazepine in the two pharmacodynamic parameters.

Conclusions

The present study suggests that carbamazepine induces the metabolism of etizolam.

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Correspondence to T. Fukasawa.

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Kondo, S., Fukasawa, T., Yasui-Furukori, N. et al. Induction of the metabolism of etizolam by carbamazepine in humans. Eur J Clin Pharmacol 61, 185–188 (2005). https://doi.org/10.1007/s00228-005-0904-y

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  • DOI: https://doi.org/10.1007/s00228-005-0904-y

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