Plateau is characterized by low oxygen, low pressure, strong radiation, cold and dryness, among which low oxygen is the main factor that affects the normal life activities of human body. Altitude hypoxia leads to significant changes in the metabolic characteristics of drugs in vivo, which in turn affects the efficacy and adverse actions of drugs. This paper summarizes the present situation of rational drug use in plateau area and pinpoints the existing problems. Meanwhile, we posit the strategies and measures for realizing rational and precise pharmacotherapy of plateau residents. First, we need to acquire a panoramic view of differential and relative pharmacokinetics and pharmacodynamics in between plateau area and plain area by carrying out comparative studies on drug metabolisms and on comprehensive drug efficacies and mechanisms. Second, we must apply the findings from basic research to clinical practice and formulate guidelines and recommendations of drug use for plateau habitants. Finally, we should eventually achieve precise and individualized drug use for plateau habitants based on their characteristic etiology and pathogenesis.