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[他汀类药物:药理学、临床及实验室方面的异同]

[Statins: similarities and differences in the pharmacological, clinical and laboratory aspects].

作者信息

Motti C, Gnasso A, Cortese C

机构信息

Dipartimento di Medicina Interna, Università degli Studi Tor Vergata di Roma.

出版信息

Ann Ital Med Int. 2000 Jan-Mar;15(1):96-102.

Abstract

The inhibitors of 3-hydroxy-3-methylglutaryl-CoA reductase (or statins) are the most powerful drugs affecting lipid and lipoprotein levels in plasma. Results obtained from large controlled trials using simvastatin, pravastatin and lovastatin for the primary or secondary prevention of coronary heart disease have demonstrated that treatment with statins is associated with a significant reduction in coronary morbidity and mortality and in total mortality. This is probably due to a more general anti-atherogenic effect of these drugs beyond their lipid-lowering activity. Meta-analysis of data from these large trials indicates that statins have an impact also on the incidence of cerebrovascular events. Currently, six statins have been approved for therapeutic use in different countries. In spite of the similarities in their chemical structure and mechanisms of action, statins may differ in many aspects such as pharmacological properties (hydrophilic vs lipophilic, elimination half-life, cytochrome P450 metabolism, etc.), effects on lipid and other biochemical variables, or pleiotropic effects on different metabolic processes related to atherosclerosis (endothelial function, platelet aggregation, immune function, etc.). In general, the safety and tolerability profile for all statins currently in use is good with a < 2% incidence of undesirable effects.

摘要

3-羟基-3-甲基戊二酰辅酶A还原酶抑制剂(即他汀类药物)是影响血浆脂质和脂蛋白水平的最强效药物。使用辛伐他汀、普伐他汀和洛伐他汀进行冠心病一级或二级预防的大型对照试验结果表明,他汀类药物治疗可显著降低冠心病发病率、死亡率及总死亡率。这可能是由于这些药物除了降脂活性外,还具有更广泛的抗动脉粥样硬化作用。对这些大型试验数据的荟萃分析表明,他汀类药物对脑血管事件的发生率也有影响。目前,已有六种他汀类药物在不同国家获批用于治疗。尽管他汀类药物在化学结构和作用机制上有相似之处,但它们在许多方面可能存在差异,如药理学特性(亲水性与亲脂性、消除半衰期、细胞色素P450代谢等)、对脂质和其他生化变量的影响,或对与动脉粥样硬化相关的不同代谢过程(内皮功能、血小板聚集、免疫功能等)的多效性作用。总体而言,目前使用的所有他汀类药物的安全性和耐受性良好,不良反应发生率<2%。

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