他汀类药物诱导的肌毒性与临床合理用药  

Statin-induced myotoxicity and clinical rational drug use

作　　者：陈焱[1,2] 李清[1] CHEN Yan;LI Qing(Department of Clinical Pharmacology,Xiangya Hospital,Central South University,Changsha 410008,China;Xiangya Medical Laboratory,Central South University,Changsha 410008,China)

机构地区：[1]中南大学湘雅医院临床药理研究所,长沙410008 [2]中南大学湘雅医学检验所,长沙410008

出　　处：《中国临床新医学》2021年第10期964-969,共6页CHINESE JOURNAL OF NEW CLINICAL MEDICINE

基　　金：国家自然科学基金项目(编号:81973401)。

摘　　要：他汀类药物是血脂异常药物治疗的基石,在国内外动脉粥样硬化性心血管疾病(ASCVD)防控中具有重要作用,然而临床常出现他汀类药物诱导的肌毒性现象,表现为轻微的肌痛到罕见的严重的横纹肌溶解,导致患者使用的依从性降低,增加心血管疾病的医疗负担。如何最大化地发挥他汀类药物的降脂作用,同时降低肌毒性不良反应的发生,是临床讨论的热点和重点。他汀类药物诱导肌毒性的机制可能包括他汀类药物在肌细胞中蓄积的药代动力学条件和有利于他汀类药物诱导肌毒性的肌细胞条件两方面。他汀类药物诱导肌毒性的风险因素分为非遗传因素和遗传因素。非遗传因素包括高龄、体重指数较低、多系统疾病等;遗传因素包括影响他汀类药物暴露的SLCO1B1、ABCG2、ABCB1等基因多态性,其中SLCO1B1多态性的影响最显著。因此,将基因检测引入临床,结合其他风险因素,可以更好地规避不良反应,合理使用他汀类药物。Statins are the cornerstone of drug treatment of dyslipidemia and play an important role in the prevention and control of atherosclerotic cardiovascular disease(ASCVD)globally.However,statins often induce muscle toxicity in clinic,ranging from mild myalgia to rare severe rhabdomyolysis,which leads to the reduction of patients′compliance and increases the medical burden of cardiovascular diseases.The hot spot and the focus of the clinical discussion are how to maximize the lipid-lowering effect of statins and reduce the occurrence of myotoxic adverse effects.The mechanisms of myotoxicity induced by statins may include two aspects:the pharmacokinetic conditions resulting in statins accumulation in the myocytes and the myocyte conditions favouring statin-induced myotoxicity.The risk factors of statin-induced myotoxicity can be classified into non-genetic factors and genetic factors.Non-genetic factors include advanced age,low body mass index,multisystem diseases,etc.Genetic factors include SLCO1B1,ABCG2,ABCB1 gene polymorphisms that affect statins exposure,among which SLCO1B1 gene polymorphism has the most significant effect.Therefore,the introduction of gene detection into clinical practice,combined with other risk factors,can better avoid adverse reactions and use statins reasonably.

关 键 词：他汀类药物 肌毒性 遗传因素 合理用药 

分 类 号：R969.3[医药卫生—药理学]