CYP2D6^＊10B基因型对中国人普罗帕酮对映体药动学的影响  

作　　者：陈冰 蔡卫民 

机构地区：[1]DepartmentofClinicalPharmacology,JinlingHospital,Nanjing210002,China

出　　处：《Acta Pharmacologica Sinica》2003年第12期1277-1280,共4页中国药理学报（英文版）

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 (400mg) 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^-1 for S-enantiomer and (1136±345), (1467±817), (2277±745)μg·h·L^-1 for 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, and the CL of both enantiomers in ^*10/^*10 is only half of that of ^*1/^*10 group or ^*1/^*1 group (P<0.05). CONCLUSION: CYP2D6^* 10B alleles induce the declined activity of CYP2D6 and impair the metabolism of propafenone.

关 键 词：CYP2D6^＊10B基因型 中国人 普罗帕酮 对映体 药物代谢动力学 

分 类 号：R969.1[医药卫生—药理学]