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Br J Pharmacol. 2011 Sep;164(2b):433-43. doi: 10.1111/j.1476-5381.2011.01385.x.

Influence of ABCB1 genetic polymorphisms on the pharmacokinetics of risperidone in healthy subjects with CYP2D6*10/*10.

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1
College of Pharmacy and Institute of Bioequivalence and Bridging Study, Chonnam National University, Gwangju, Korea.

Abstract

BACKGROUND AND PURPOSE:

The objective of this study was to investigate the combined influence of genetic polymorphisms in ABCB1 and CYP2D6 genes on risperidone pharmacokinetics.

EXPERIMENTAL APPROACH:

Seventy-two healthy Korean volunteers receiving a single oral dose of 2 mg risperidone were included in this study.

KEY RESULTS:

Significant differences were observed between the ABCB1 3435C>T genotypes for the pharmacokinetic parameters (peak serum concentration) of risperidone and the active moiety (risperidone and its main metabolite, 9-hydroxyrisperidone). There were no significant differences in the area under the serum concentration-time curves of risperidone and the active moiety among the ABCB1 2677G>T/A and 3435C>T genotypes. However, the peak serum concentration and area under the serum concentration-time curves were significantly different among the ABCB1 3435C>T genotypes in CYP2D6*10/*10.

CONCLUSIONS AND IMPLICATIONS:

These findings indicate that polymorphisms of ABCB1 3435C>T in individuals with CYP2D6*10/*10, which has low metabolic activity, could play an important role in the potential adverse effects or toxicity of risperidone.

PMID:
21449914
PMCID:
PMC3188890
DOI:
10.1111/j.1476-5381.2011.01385.x
[Indexed for MEDLINE]
Free PMC Article
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