Cardiovascular Diseases Section, "Monsignor Dimiccoli" Hospital, Barletta, Italy.
Cardiovascular Diseases Section, Department of Emergency and Organ Transplantation (DETO), University of Bari, Bari, Italy.
Curr Vasc Pharmacol. 2019;17(3):213-221. doi: 10.2174/1570161116666180706144824.
Cardiovascular diseases secondary to atherosclerosis are the primary causes of early death and disability worldwide and dyslipidaemia represents one of the most important modifiable risk factors. Among lipid abnormalities that define it, low-density lipoprotein cholesterol (LDL-C) is the primary target of therapy, since multiple randomized controlled trials have shown the positive impact of its reduction on atherosclerosis development. For their ability to lower LDL-C levels, statins are the most studied drugs in cardiovascular disease prevention, of proven utility in slowing the progression or even determining regression of atherosclerosis. In addition, they have ancillary proprieties, with positive effects on the mechanisms involved in the development of atherosclerosis and cardiovascular morbidity and mortality, the so-called "pleiotropic mechanisms". Although sharing the same mechanism of action, the different chemical and pharmacological characteristics of each kind of statins affect their absorption, bioavailability, plasma protein binding properties, excretion and solubility. In this overview, we analysed pharmacokinetic and pharmacodynamic mechanisms of this class of drugs, specifying the differences among the molecules, along with the economic aspects. Detailed knowledge of characteristics and differences of each kind of available statin could help the physician in the correct choice, based also on patient's clinical profile, of this essential tool with a demonstrated high cost-effectiveness both in primary than in the secondary prevention of cardiovascular disease.
动脉粥样硬化引起的心血管疾病是全球范围内导致早逝和残疾的主要原因，血脂异常是最重要的可改变的危险因素之一。在定义血脂异常的异常中，低密度脂蛋白胆固醇（LDL-C）是治疗的主要靶点，因为多项随机对照试验表明降低 LDL-C 水平对动脉粥样硬化发展的积极影响。他汀类药物是预防心血管疾病中研究最多的药物，因其降低 LDL-C 水平的能力而具有实用价值，已被证明可减缓动脉粥样硬化的进展，甚至可确定其消退。此外，它们还具有辅助特性，对涉及动脉粥样硬化和心血管发病率和死亡率的发展的机制具有积极影响，即所谓的“多效机制”。虽然他汀类药物具有相同的作用机制，但每种他汀类药物的化学和药理学特性不同，会影响其吸收、生物利用度、血浆蛋白结合特性、排泄和溶解度。在本篇综述中，我们分析了这类药物的药代动力学和药效学机制，具体说明了分子之间的差异，以及与经济方面有关的差异。详细了解每种可用他汀类药物的特点和差异，可以帮助医生根据患者的临床特征，正确选择这种已被证明具有高成本效益的基本工具，无论是在心血管疾病的一级预防还是二级预防中都具有这种效果。
