The special environmental features of high altitude, such as hypobaric hypoxia, low temperature, arid, high solar radiation, variable climate and geochemical anomaly, cause great effects on human physiology and health. It will provide valuable references and new ideas to study drug's metabolism in special environment of high altitude hypoxia, and give the guidance to clinical reasonable medication, avoiding adverse reactions and personalized medicine in plateau areas. This article reviewed the effect of high altitude hypoxia on drug metabolism, elaborated metabolic characteristics of some drugs and the activity and expression of drug metabolism enzymes under hypoxia environment at high altitude, and discussed related mechanism.