摘要
高原具有的低氧、低气压等环境特点,会使机体产生一系列生理性变化,并影响药物的体内代谢过程。影响这个过程的因素有很多,包括胃排空、血液流变学、心肺功能、肝肾功能、药物代谢酶和药物转运体。其中,药物转运体是介导大部分药物透过细胞膜进入体内发挥药效的关键因素,研究缺氧对药物转运体的影响,对于明确药物的体内代谢过程具有重要的意义。因此,该文将从药物转运体的分类、介导的药物底物、缺氧对药物转运体表达的影响及缺氧条件下药物转运体的调控机制等方面进行综述,为深入研究高原缺氧对药物转运体的影响和药物代谢动力学参数变化提供理论依据。
Abstract Plateau environment has the characteristic of low ox-ygen and low pressure,which leads to a series of physiological changes and Xfects the process of drug metabolism in the body.Many factors Xfect the pharmacokinetic parameters, including gastric emptying, blood rheology,cardiopulmonary function, hepatorenal function,cytochrome P450 enzyme and so on. The present study focuses on drug metabolic enzymes, since drug transporter is the key factor that mediates drugs in their entrance to the body through the cell membrane, producing the curative effect. In order to provide the reference to further research on the effect of plateau hypoxia on pharmacokinetics and guide the rational use of drugs, we review in this paper the classification of the transporter, mediated drug substrates, the influence of hy-poxia on expression levels of drug transporter substrates and the regulatory mechanism of drug transporter under the condition of hypoxia.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2018年第3期316-321,共6页
Chinese Pharmacological Bulletin
基金
国家科技部重大项目军队特需药保密专项(No2008ZXJ09014-010)
国家自然科学基金资助项目(No81401552
81403004
81673508)
全军后勤科研"十二五"重大项目(No AWS14L0005)
全军医学科研"十二五"重点项目(No BWS12J012)
甘肃省自然科学基金资助项目(No 145RJZA111
1606RJZA176)
关键词
缺氧
药物转运体
组织分布
药物底物
药物代谢
调控机制
plateau hypoxia
drug transporter
organization distribution
drug substrate
drug metabolism
regulation mechanism