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Pleiotropic effects of pitavastatin

机译:匹伐他汀的多效性作用

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3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) are established first line treatments for hypercholesterolaemia. In addition to the direct effects of statins in reducing concentrations of atherogenic low density lipoprotein cholesterol (LDL-C), several studies have indicated that the beneficial effects of statins may be due to some of their cholesterol-independent, multiple (pleiotropic) effects which may differ between different members of the class. Pitavastatin is a novel synthetic lipophilic statin that has a number of pharmacodynamic and pharmacokinetic properties distinct from those of other statins, which may underlie its potential pleiotropic benefits in reducing cardiovascular risk factors. This review examines the principal pleiotropic effects of pitavastatin on endothelial function, vascular inflammation, oxidative stress and thrombosis. The article is based on a systematic literature search carried out in December 2010, together with more recent relevant publications where appropriate. The available data from clinical trials and in vitro and animal studies suggest that pitavastatin is not only effective in reducing LDL-C and triglycerides, but also has a range of other effects. These include increasing high density lipoprotein cholesterol, decreasing markers of platelet activation, improving cardiac, renal and endothelial function, and reducing endothelial stress, lipoprotein oxidation and, ultimately, improving the signs and symptoms of atherosclerosis. It is concluded that the diverse pleiotropic actions of pitavastatin may contribute to reducing cardiovascular morbidity and mortality beyond that achieved through LDL-C reduction.
机译:3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶抑制剂(他汀类药物)是高胆固醇血症的一线治疗药物。除了他汀类药物在降低动脉粥样硬化性低密度脂蛋白胆固醇(LDL-C)浓度方面的直接作用外,多项研究表明他汀类药物的有益作用可能是由于它们的某些胆固醇非依赖性,多重(多效性)作用所致。不同班级的成员可能有所不同。匹伐他汀是一种新型的合成亲脂性他汀类药物,具有不同于其他他汀类药物的许多药代动力学和药代动力学特性,这可能是其潜在的多效性益处,可降低心血管危险因素。这篇综述研究了匹伐他汀对血管内皮功能,血管炎症,氧化应激和血栓形成的主要多效性作用。本文基于2010年12月进行的系统文献检索,并在适当的情况下还提供了最新的相关出版物。来自临床试验以及体外和动物研究的可用数据表明匹伐他汀不仅有效降低LDL-C和甘油三酸酯,而且还具有一系列其他作用。这些措施包括增加高密度脂蛋白胆固醇,降低血小板活化标志物,改善心脏,肾脏和内皮功能,减少内皮应力,脂蛋白氧化并最终改善动脉粥样硬化的体征和症状。得出的结论是,匹伐他汀的多种多效性作用可能有助于降低心血管疾病的发病率和死亡率,而降低LDL-C所达到的效果除外。

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