Kostner K M, Kostner G M
Abteilung für Kardiologie, Innere Medizin II, Universität Wien.
Wien Klin Wochenschr. 1998 Oct 2;110(18):625-30.
Large scale primary and secondary prevention trials in recent years have revealed that the effective lipid reducing therapy with statins can reduce mortality of coronary heart disease by up to 30%. For the first time it has become possible to reduce LDL-cholesterol pharmacologically by more than 50%, a reduction that was only achieved by LDL-apheresis so far. Cost-effectiveness is becoming an important issue since this varies widely between patients according to the coronary risk. Treating the patients with the highest coronary risk is most cost effective. Currently, there are six statins on the market. Reduction of LDL-cholesterol is mainly mediated by the induction of LDL-receptor activity in the liver. In addition, some statins at high doses also reduce LDL-cholesterol synthesis. Due to variations in the molecular structure of the active compounds these 6 statins have important pharmacological differences, such as their capacity to reduce plasma triglycerides, their interaction with other drugs. The daily recommended doses of the statins range from 0.1 mg (cerivastatin) to 80 mg (atorvastatin). In this review the differences in the pharmacological and clinical actions of the statins are analyzed.
近年来的大规模一级和二级预防试验表明,他汀类药物进行有效的降脂治疗可使冠心病死亡率降低达30%。首次在药理学上使低密度脂蛋白胆固醇(LDL - cholesterol)降低超过50%,而到目前为止,只有通过低密度脂蛋白分离术才能实现这一降幅。成本效益正成为一个重要问题,因为根据冠心病风险不同,患者之间的成本效益差异很大。治疗冠心病风险最高的患者最具成本效益。目前市场上有六种他汀类药物。LDL - cholesterol的降低主要是通过诱导肝脏中LDL受体活性来介导的。此外,一些高剂量的他汀类药物还可减少LDL - cholesterol的合成。由于活性化合物分子结构的差异,这六种他汀类药物具有重要的药理学差异,例如它们降低血浆甘油三酯的能力、与其他药物的相互作用。他汀类药物的每日推荐剂量范围从0.1毫克(西立伐他汀)到80毫克(阿托伐他汀)。在本综述中,分析了他汀类药物在药理学和临床作用方面的差异。