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Randomized Controlled Trial
. 2007 Oct;64(4):445-9.
doi: 10.1111/j.1365-2125.2007.02912.x. Epub 2007 Jul 4.

Atomoxetine pharmacokinetics in healthy Chinese subjects and effect of the CYP2D6*10 allele

Yi M Cui  1 , Choo H Teng, Alan X Pan, Eunice Yuen, Kwee P Yeo, Ying Zhou, Xia Zhao, Amanda J Long, Mark E Bangs, Stephen D Wise
Affiliations
Randomized Controlled Trial

Atomoxetine pharmacokinetics in healthy Chinese subjects and effect of the CYP2D6*10 allele

Yi M Cui et al. Br J Clin Pharmacol. 2007 Oct.

Abstract

Aims: To characterize atomoxetine pharmacokinetics, explore the effect of the homozygous CYP2D6*10 genotype on atomoxetine pharmacokinetics and evaluate the tolerability of atomoxetine, in healthy Chinese subjects.

Methods: Twenty-four subjects, all CYP2D6 extensive metabolizers (EM), were randomized to receive atomoxetine (40 mg qd for 3 days, then 80 mg qd for 7 days) or matching placebo (2 : 1 ratio) in a double-blind fashion. Atomoxetine serum concentrations were measured following single (40 mg) and multiple (80 mg) doses. Adverse events, clinical safety laboratory data and vital signs were assessed during the study.

Results: Atomoxetine was rapidly absorbed with median time to maximum serum concentrations of approximately 1.5 h after single and multiple doses. Atomoxetine concentrations appeared to decrease monoexponentially with a mean apparent terminal half-life (t(1/2)) of approximately 4 h. The apparent clearance, apparent volume of distribution and t(1/2) following single and multiple doses were similar, suggesting linear pharmacokinetics with respect to time. Homozygous CYP2D6*10 subjects had 50% lower clearances compared with other EM subjects, resulting in twofold higher mean exposures. No clinically significant changes or abnormalities were noted in laboratory data and vital signs.

Conclusions: The pharmacokinetics of atomoxetine in healthy Chinese subjects appears comparable to other ethnic populations. Multiple dosing of 80 mg qd atomoxetine was well tolerated in this study.

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Figures

Figure 1
Figure 1
Arithmetic mean (+SD) serum concentration–time profiles of atomoxetine on day 1 following a single dose of 40 mg (N = 16) (formula image) and on day 10 following multiple doses of 80 mg qd (N = 16) (○)
See this image and copyright information in PMC

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