药物转运体介导的小肠吸收、肾脏排泄与药物相互作用的-药学学报.PDF

药学学报 Acta Pharmaceutica Sinica 2010, 45 (9) : 1089 1094 ·1089 · 药物转运体介导的小肠吸收、肾脏排泄与 物相互作用的关系 健, 刘克辛* (大连医科大学 学院临床药理教研室, 辽宁 大连 116044) 摘要: 药物相互作用 (drug-drug interaction, DDI) 是指几种 物同时或前后序贯应用时药物原有的理化性 质及 代动力学或 效动力学发生改变。随着 物种类的逐年增加, 新的耐 性不断出现, 使联合用 的几率日 益增加, 加大了 物相互作用特别是不良相互作用发生的频率。体内 物相互作用发生的机制与很多因素有关, 包括许多代谢酶及细胞膜转运蛋白的作用, 其中膜转运蛋白介导某些药物的吸收、分布和消除等过程, 具有重要 的药理学和临床意义。为了避免由转运体导致的不良相互作用, 促进临床合理联合用 , 本文综述了 物转运体 介导的小肠吸收、肾脏排泄与药物相互作用的作用机制。 关键词: 药物相互作用; 膜转运蛋白类; 药代动力学 中图分类号: R969 文献标识码:A 文章编号: 05 13-4870 (2010) 09-1089-06 Intestinal absorption and renal excretion mediated by transporters and the relationship with drug-drug interaction * ZHANG Jian, LIU Ke-xin (Depa rtment of Clinical Pharmacology, College of Pharmacy, Dalian Medical University, Dalian 116044, China) Abstract: Drug-drug interaction (DDI) is referred as the changes of physical and chemical properties, as well as the pharmacokinetics or pharmacodynamics of drugs administered simultaneously or consecutively. The clinical results for drug-drug interaction could be divided into good clinical efficacy and adverse interaction. With the kinds of drugs increasing every year, new drug resistances spring up frequently. This phenomenon makes drug combination increased so that the drug interaction, especially the adverse interaction emerged. The mechanisms of in vivo drug-drug interaction are relevant to a number of factors, including drug-metabolizing enzyme systems and membrane transporters. R