药物转运体介导的小肠吸收、肾脏排泄与药物相互作用的关系

Intestinal absorption and renal excretion mediated by transporters and the relationship with drug-drug interaction

药物相互作用(drug-drug interaction,DDI)是指几种药物同时或前后序贯应用时药物原有的理化性质及药代动力学或药效动力学发生改变。随着药物种类的逐年增加,新的耐药性不断出现,使联合用药的几率日益增加,加大了药物相互作用特别是不良相互作用发生的频率。体内药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药,本文综述了药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。

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. Recent studies have revealed the important role played by transporters in drug absorption, distribution, metabolism and elimination. In order to avoid severe side effects mediated by transporters and to promote rational combination in clinics, the mechanisms of intestinal absorption and renal excretion mediated by transporters are reviewed.