Influence of CYP2D610B genotype on pharmacokinetics of propafenone enantiomers in Chinese subjects

作     者：CHEN Bing CAI Wei-Min Department of Clinical Pharmacology, Jinling Hospital, Nanjing 210002, China 

出 版 物：《Acta Pharmacologica Sinica》 (中国药理学报(英文版))

年 卷 期：2003年第12期

页      面：103-106页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学] 

主　　题：propafenone pharmacokinetics CYP2D6~* 10B genotype phenotype enantiomers 

摘      要：AIM: To study the relationship between genotype of CYP2D6* 10B and pharmacokinetics of propafenone enantiomers. METHODS: Genotype of 17 healthy Chinese HAN subjects was determined by an allele specific amplification method. The blood samples (0-15 h) of the subjects were taken after oral administration of a single dose (400 mg) of propafenone hydrochloride. Concentrations of propafenone enantiomers in plasma were measured by a reverse-phase HPLC with precolumn derivatization. RESULTS: Seventeen subjects characterized for CYP2D6* 10B genotype included (*1/*1) (n=4), (*1/*10) (n=5) and (*10/*10) (n=8). The metabolic ratios (lg MR) of the three genotypes were-2.68±0.23, -2.2±0.7, and -1.1±0.5, respectively. The AUC of the three groups were (1534±334), (1891±793), (3171±1075) μg·h·L-1for S-enantiomer and (1136±345), (1467±817), (2277±745) μg·h·L-1for R-enantiomer, respectively. The AUC of propafenone enantiomers in *10/*10 is about 1.5-2 times of that of *1/*10 group or *1/*1 group, a