Fonseca Francisco Antonio Helfenstein
Setor de Lípides, Aterosclerose e Biologia Vascular, UNIFESP-EPM.
Arq Bras Cardiol. 2005 Oct;85 Suppl 5:9-14. Epub 2006 Jan 2.
Statins are lipid lowering agents that promote their effects on plasma lipids through the inhibition of HMG-CoA reductase, a crucial enzyme in the cascade of cholesterol synthesis, leading to reduction of tissue cholesterol pool and consequently, to an upregulation of the LDL receptor expression. There are considerable differences among statins regarding some pharmacokinetic properties, such as the coefficient of hydrophilicity, via liver metabolism (especially regarding P450 cytochrome and isoenzymes), plasma half-life and efficacy of serum lipid changes. They may also differ regarding interactions with other drugs that share the same pathway of metabolism. Recently, many pleiotropic effects have been reported with these drugs, such as anti-inflammatory properties, improvement in endothelial function and benefits on hemostasis.
他汀类药物是降血脂药物,它们通过抑制HMG-CoA还原酶(胆固醇合成级联反应中的一种关键酶)来发挥对血浆脂质的作用,从而导致组织胆固醇池减少,进而使低密度脂蛋白受体表达上调。他汀类药物在一些药代动力学特性方面存在显著差异,例如亲水性系数、肝脏代谢(特别是关于细胞色素P450和同工酶)、血浆半衰期以及血清脂质变化的疗效。它们在与共享相同代谢途径的其他药物的相互作用方面也可能有所不同。最近,已报道这些药物具有许多多效性作用,如抗炎特性、内皮功能改善以及对止血的益处。