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大量研究结果证实,动脉粥样硬化和冠心病(CHD)与高胆固醇血症有着密切的关系。据估计,欧美有15％成年人因血脂水平升高而处于罹患心血管疾病的风险中。因此,高水平的总胆固醇(TC)和低密度脂蛋白胆固醇(LD-L-C)已成为预防CHD的主攻目标。 人体胆固醇有两个来源,每日从食物中吸收约300～500mg和内源性生物合成700～900mg,可见抑制生物合成是降低血胆固醇水平的重要途径。而胆固醇生物合成的第一个限速酶是羟甲戊二酰辅酶A(HMG-CoA)还原酶。因此,自20a前发现第1种HMG-CoA还原酶抑制剂以来,对高胆固醇血症的药物治疗已取得了长足的进展;事实上,HMG-CoA还原酶抑制剂已经成为降低TC和LDL-C最有效的药物。美国国家胆固醇教育方案(NCEP)已把这类药物定为抗高脂血症的主要药物。此前,已有洛伐他汀(lovastatin),氟伐他汀(fluvastatin),普伐他汀(pravas-
A large number of studies confirm that atherosclerosis and coronary heart disease (CHD) and hypercholesterolemia are closely related. It is estimated that 15% of adults in Europe and the United States are at risk of developing cardiovascular disease due to elevated blood lipid levels. Therefore, high levels of total cholesterol (TC) and low-density lipoprotein cholesterol (LD-L-C) have become the main targets for the prevention of CHD. There are two sources of human cholesterol, daily intake of about 300 ~ 500mg from food and endogenous biosynthesis 700 ~ 900mg, showing that inhibition of biosynthesis is an important way to reduce blood cholesterol levels. The first rate-limiting enzyme in cholesterol biosynthesis is hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase. Therefore, since the first HMG-CoA reductase inhibitor was discovered prior to 20a, great progress has been made in the medical treatment of hypercholesterolemia; in fact, the HMG-CoA reductase inhibitor has become a substance that reduces TC and LDL- C the most effective drug. The National Cholesterol Education Program (NCEP) has identified such drugs as the primary antihyperlipidemic drug. Previously, there have been lovastatin, fluvastatin, pravast-