Pharmacokinetics and pharmacodynamics of etizolam are influenced by polymorphic CYP2C19 activity.

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Fukasawa T, Yasui-Furukori N, Suzuki A, Inoue Y, Tateishi T, Otani K

Pharmacokinetics and pharmacodynamics of etizolam are influenced by polymorphic CYP2C19 activity.

Eur J Clin Pharmacol. 2005 Dec;61(11):791-5. Epub 2005 Nov 1.

PubMed ID

16261363 [ View in PubMed

]

Abstract

OBJECTIVE: To examine the effect of cytochrome P450 (CYP) 2C19 activity on the single-dose pharmacokinetics and pharmacodynamics of etizolam. METHODS: The subjects were 21 healthy Japanese volunteers. The two mutated alleles (CYP2C19*2 and CYP2C19*3) causing absent CYP2C19 activity were identified by a polymerase chain reaction method. Twelve subjects were extensive metabolizers (EMs) with no or one mutated allele, and nine subjects were poor metabolizers (PMs) with two mutated alleles. The subjects received a single oral 1-mg dose of etizolam, and blood samplings and evaluation of psychomotor function were conducted up to 24 h after dosing. RESULTS: The PMs had significantly larger total area under the plasma concentration-time curve (287+/-74 vs 178+/-122 ng.h/ml, p<0.05) and longer elimination half-life (14.8+/-4.2 vs 10.5+/-3.9 h, p<0.05) of etizolam than the EMs. The area under the score-time curve from 0 to 8 h of the Stanford Sleepiness Scale was significantly larger in the PMs than in EMs (28.9+/-5.2 vs 22.9+/-6.9 score.h, p<0.05). CONCLUSION: The present study suggests that the single-dose pharmacokinetics and pharmacodynamics of etizolam are influenced by polymorphic CYP2C19 activity.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Etizolam	Cytochrome P450 2C19	Protein	Humans	Unknown	Substrate	Details

Drug Interactions

Drugs	Interaction
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