Correlation of genetic polymorphism of transporter with resperidone metabolism
- Author:
Qian XIANG
1
Author Information
1. Peking University First Hospital
- Publication Type:Journal Article
- Keywords:
BCRP;
Genetic polymorphisms;
MDR1;
Risperidone
- From:
Chinese Pharmaceutical Journal
2012;47(6):454-457
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE: To study the relationship between the genetic polymorphisms of the main transporter of risperidone and its pharmacokinetics in Chinese healthy volunteers. METHODS: 2 mg of risperidone was orally administered to 23 healthy Chinese subjects, and blood samples were taken after dosing. The polymorphic alleles of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) were determined in each subject. The whole blood concentrations of risperidone and 9-hydroxyrisperidone were measured by high performance liquid chromatography/tandem mass spectrometry(HPLC-MS/MS). RESULTS: The AUC0-∞ and ρmax of 9-hydroxyrisperidone in subjects carrying BCRP 421CA/34GA genotype were 66.6% and 51.1% (P =0.011, P =0.017) of other subjects, respectively. The tmax of risperidone was significantly influenced by BCRP C421A and MDR1 G2677T/A (P < 0.05). CONCLUSION: The disposition of 9-hydroxyrisperidone was affected by BCRP genetic polymorphisms. P-gp and BGRP genotype may also play a role in risperidone absorption. Copyright 2012 by the Chinese Pharmaceutical Association.
