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瑞舒伐他汀:一种用于预防和管理冠状动脉疾病的高效他汀类药物。

Rosuvastatin: a highly potent statin for the prevention and management of coronary artery disease.

作者信息

Kapur Navin K

机构信息

Johns Hopkins University School of Medicine, 600 North Wolfe Street, Carnegie Bldg, Room #568, Baltimore, MD 21287, USA.

出版信息

Expert Rev Cardiovasc Ther. 2007 Mar;5(2):161-75. doi: 10.1586/14779072.5.2.161.

Abstract

Since the identification of a fungal metabolite that inhibits HMG-CoA reductase in 1976, statins have emerged rapidly as the global leader in pharmacotherapeutics designed to lower low-density lipoprotein cholesterol (LDL-C). In conjunction, practice guidelines have recommended increasingly aggressive measures to improve coronary heart disease (CHD) outcomes by lowering LDL-C. By virtue of unique chemical characteristics, enhanced binding thermodynamics and limited cytochrome P450 3A4 metabolism, rosuvastatin calcium has a safety profile in line with currently marketed statins, but a different efficacy profile. Mirroring this chemical profile, the GALAXY program represents a comprehensive evaluation of the efficacy, safety and cost-effectiveness of rosuvastatin in individuals representing various clinical diagnoses, pathophysiological states and ethnicities. Also results from the Justification for the Use of statins in Primary prevention: an Intervention Trial Evaluating Rosuvastatin (JUPITER) study could provide further evidence for the use of rosuvastatin in individuals with traditional and emerging CHD risk factors, such as an elevated high sensitivity C-reactive protein level. This review will provide a comprehensive evaluation of the chemistry, clinical efficacy, safety and tolerability of rosuvastatin, and discuss the future role in the management of CHD and atherosclerosis.

摘要

自1976年发现一种抑制HMG-CoA还原酶的真菌代谢产物以来,他汀类药物迅速成为旨在降低低密度脂蛋白胆固醇(LDL-C)的药物治疗领域的全球领导者。与此同时,实践指南推荐采取越来越积极的措施,通过降低LDL-C来改善冠心病(CHD)的预后。由于具有独特的化学特性、增强的结合热力学以及有限的细胞色素P450 3A4代谢,瑞舒伐他汀钙的安全性与目前上市的他汀类药物相当,但疗效有所不同。与这种化学特性相对应,GALAXY项目代表了对瑞舒伐他汀在各种临床诊断、病理生理状态和种族人群中的疗效、安全性和成本效益的全面评估。此外,他汀类药物在一级预防中的应用:评估瑞舒伐他汀的干预试验(JUPITER)研究结果,可能为瑞舒伐他汀在具有传统和新出现的CHD危险因素(如高敏C反应蛋白水平升高)的个体中的应用提供进一步证据。本综述将对瑞舒伐他汀的化学性质、临床疗效、安全性和耐受性进行全面评估,并讨论其在CHD和动脉粥样硬化管理中的未来作用。

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