Bartoli A, Xiaodong S, Gatti G, Cipolla G, Marchiselli R, Perucca E
Clinical Pharmacology Unit, University of Pavia, Italy.
Ther Drug Monit. 1996 Oct;18(5):586-91. doi: 10.1097/00007691-199610000-00011.
To assess potential ethnic and gender-related differences in the expression of cytochrome CYP1A2-mediated activity, the pharmacokinetics of phenacetin (a CYP1A2 substrate) and its metabolite paracetamol were compared in 20 Caucasian and 20 Chinese subjects after administration of a single oral 900 mg phenacetin dose. Peak plasma concentrations and apparent oral clearance values for phenacetin did not differ between the two groups (geometric means: 3.4 micrograms/ml and 1.56 ml h-1 kg-1, respectively, for Caucasians vs. 4.7 micrograms/ml and 1.25 ml h-1 kg-1, respectively, for Chinese, after excluding one Caucasian with aberrantly low plasma phenacetin values). Pharmacokinetic parameters for metabolically derived paracetamol were also similar in the two groups. When subjects were divided into subgroups according to gender, phenacetin apparent oral clearance values were found to be lower in Chinese women compared with both Chinese men and Caucasian subjects of either sex. It is concluded that there are no major interethnic differences in the expression of CYP1A2-related activity between Caucasians and Chinese, although Chinese women as a subgroup may exhibit comparatively lower enzyme activity.
为评估细胞色素CYP1A2介导活性表达中潜在的种族和性别差异，在20名白种人和20名中国受试者单次口服900毫克非那西丁后，比较了非那西丁（一种CYP1A2底物）及其代谢产物对乙酰氨基酚的药代动力学。排除一名血浆非那西丁值异常低的白种人后，两组中非那西丁的血浆峰浓度和表观口服清除率值无差异（几何均值：白种人分别为3.4微克/毫升和1.56毫升·小时⁻¹·千克⁻¹，中国人分别为4.7微克/毫升和1.25毫升·小时⁻¹·千克⁻¹）。代谢产生的对乙酰氨基酚的药代动力学参数在两组中也相似。当根据性别将受试者分为亚组时，发现中国女性的非那西丁表观口服清除率值低于中国男性和白种人男女两性。结论是，白种人和中国人之间在CYP1A2相关活性表达上没有主要的种族间差异，尽管中国女性作为一个亚组可能表现出相对较低的酶活性。
