Korlipara K
Pike View Medical Centre, Bolton, Lancs, UK.
Int J Clin Pract. 2002 Jun;56(5):379-87.
Cardiovascular disease (CVD) remains a major cause of death in industrialised societies, and elevated serum lipids are a significant, highly prevalent and undertreated risk factor for this condition. The 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors (statins) have revolutionised the treatment of hyperlipidaemia, and results from large-scale, long-term clinical trials have shown that the substantial reductions in low-density lipoprotein cholesterol (LDL-C) achieved with these drugs are associated with dramatic decreases in cardiovascular risk. Results from recent comparative clinical trials that have included a new drug in this class, rosuvastatin (Crestor), have demonstrated that it is significantly superior to atorvastatin, pravastatin and simvastatin in reducing total cholesterol, LDL-C and apolipoprotein B (Apo B). It is also significantly more effective than atorvastatin in increasing high-density lipoprotein cholesterol (HDL-C) and apolipoprotein A-I (Apo A-I). Rosuvastatin was also superior to all these agents in helping patients meet European Atherosclerosis Society (EAS) and National Cholesterol Education Programme (NCEP) goals for LDL-C. The results of an increasing number of studies indicate that statins have a wide range of pleiotropic properties that almost certainly contribute to their ability to decrease cardiovascular risk and may also make them valuable for treatment of other diseases. These actions include plaque stabilisation, improvement of endothelial function, inhibition of smooth muscle cell proliferation and migration, reduction of expression of adhesion molecules, prevention of cholesterol esterification and accumulation, reduction of secretion of matrix metalloproteinases by macrophages, reduction of platelet activity, reduction of formation of thrombogenic factors, chemoprotection and induction of bone morphogenic protein-2 (BMP-2). Further exploration of these actions will provide key information about class effects and properties of specific members of this highly useful group of drugs.
心血管疾病（CVD）仍然是工业化社会中的主要死因，而血清脂质升高是导致这种疾病的一个重要、普遍存在且治疗不足的风险因素。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）彻底改变了高脂血症的治疗方式，大规模长期临床试验结果表明，这些药物使低密度脂蛋白胆固醇（LDL-C）大幅降低，与心血管风险的显著降低相关。最近纳入该类新药瑞舒伐他汀（可定）的比较临床试验结果表明，在降低总胆固醇、LDL-C和载脂蛋白B（Apo B）方面，它显著优于阿托伐他汀、普伐他汀和辛伐他汀。在升高高密度脂蛋白胆固醇（HDL-C）和载脂蛋白A-I（Apo A-I）方面，它也比阿托伐他汀显著更有效。在帮助患者达到欧洲动脉粥样硬化学会（EAS）和美国国家胆固醇教育计划（NCEP）的LDL-C目标方面，瑞舒伐他汀也优于所有这些药物。越来越多的研究结果表明，他汀类药物具有广泛的多效性特性，几乎可以肯定这有助于它们降低心血管风险的能力，也可能使它们在治疗其他疾病方面具有价值。这些作用包括斑块稳定、改善内皮功能、抑制平滑肌细胞增殖和迁移、减少黏附分子表达、防止胆固醇酯化和蓄积、减少巨噬细胞分泌基质金属蛋白酶、降低血小板活性、减少血栓形成因子的形成、化学保护以及诱导骨形态发生蛋白-2（BMP-2）。对这些作用的进一步探索将提供有关这一非常有用的药物组的类效应和特定成员特性的关键信息。
