他汀类药物:作用机制和效果。

C Stancu, A Sima
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引用次数: 740

摘要

他汀类药物的有益作用是因为它们能够减少胆固醇生物合成,主要是在肝脏中,它们在肝脏中选择性分布,以及调节脂质代谢,这源于它们对HMG-CoA还原酶的抑制作用。他汀类药物具有抗动脉粥样硬化作用,与低密度脂蛋白胆固醇的降低百分比呈正相关。此外,它们可以独立于降血脂作用发挥抗动脉粥样硬化作用。由于甲羟戊酸代谢产生一系列对不同细胞功能至关重要的类异戊二烯,从胆固醇合成到控制细胞生长和分化,HMG-CoA还原酶抑制具有有益的多效性作用。因此,他汀类药物在一级和二级预防中都能显著降低冠状动脉事件的发生率,是降低冠状动脉患者死亡率的最有效的降血脂化合物。他汀类药物与降血脂特性无关,它们会干扰骨形成事件并阻碍肿瘤细胞生长。
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Statins: mechanism of action and effects.

The beneficial effects of statins are the result of their capacity to reduce cholesterol biosyntesis, mainly in the liver, where they are selectively distributed, as well as to the modulation of lipid metabolism, derived from their effect of inhibition upon HMG-CoA reductase. Statins have antiatherosclerotic effects, that positively correlate with the percent decrease in LDL cholesterol. In addition, they can exert antiatherosclerotic effects independently of their hypolipidemic action. Because the mevalonate metabolism generates a series of isoprenoids vital for different cellular functions, from cholesterol synthesis to the control of cell growth and differentiation, HMG-CoA reductase inhibition has beneficial pleiotropic effects. Consequently, statins reduce significantly the incidence of coronary events, both in primary and secondary prevention, being the most efficient hypolipidemic compounds that have reduced the rate of mortality in coronary patients. Independent of their hypolipidemic properties, statins interfere with events involved in bone formation and impede tumor cell growth.

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