CYP2D6*10B基因型对中国人普罗帕酮对映体药动学的影响

• 作者: 蔡卫民 陈冰
• 来源期刊: 中国药理学报（英文版）
• 学科: 医学
• 关键词: propafenone pharmacokinetics CYP2D6* 10B genotype phenotype enantiomers
• 年，卷（期）: 2003,（12）
• 所属期刊栏目: 研究原著
• 页码范围: 1277-1280
• 页数: 4页
• 分类号: R97
• 语种: 英文

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 mea sured by a reverse-phase HPLC with precolumn derivatization. RESULTS: Seventeen subjects characterized for CYP2D6* 1 0B 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 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.