The University of Hong Kong, Division of Cardiology, Department of Medicine, Hong Kong, China.
Expert Opin Investig Drugs. 2010 Mar;19(3):437-49. doi: 10.1517/13543781003623223.
Despite effective lowering of low-density lipoprotein cholesterol (LDL-C) with statin for prevention of cardiovascular adverse events, residual risk remains high due to low high-density lipoprotein cholesterol (HDL-C) levels in patients with mixed dyslipidemia. As a result, alternative treatment options to raise HDL-C are being investigated intensively. Currently, niacin is the most potent lipid lowering agent for raising HDL-C levels together with lowering of triglyceride and LDL-C. Previous clinical studies have demonstrated that niacin therapy significantly reduces the risk of cardiovascular events in high risk subjects. However, the clinical use of niacin is limited by its major adverse effect, cutaneous flushing. Although the use of extended-release (ER) formulation can reduce flushing, the tolerability and compliance of niacin remains suboptimal. A selective antagonist of prostaglandin D Type 1 receptor, laropiprant, has been investigated in a number of clinical studies and shown to be effective in reducing niacin-induced flushing. Despite the potential of laropiprant in reducing niacin-induced flushing, the long-term clinical efficacy and potential off-target side effects are not well studied. AREAS COVERED IN THIS REVIEWS: In this article, the pharmacological properties, clinical efficacy and future perspective of this combination therapy of simvastatin/ER niacin/laropiprant are reviewed.
Readers will understand both the mechanism and clinical effects of the combination therapy of simvastatin/ER niacin/laropiprant.
The triple combination therapy of simvastatin/ER niacin/laropiprant may reduce flushing side effects and facilitate a more comprehensive treatment for patients with mixed dyslipidemia.
尽管通过他汀类药物有效降低了低密度脂蛋白胆固醇（LDL-C），以预防心血管不良事件，但由于混合性血脂异常患者的高密度脂蛋白胆固醇（HDL-C）水平较低，残留风险仍然很高。因此，正在积极研究提高 HDL-C 的替代治疗方案。目前，烟酸是提高 HDL-C 水平的最有效的降脂药物，同时还能降低甘油三酯和 LDL-C。以前的临床研究表明，烟酸治疗可显著降低高危患者心血管事件的风险。然而，烟酸的临床应用受到其主要不良反应——皮肤潮红的限制。尽管使用缓释（ER）制剂可以减少潮红，但烟酸的耐受性和顺应性仍不理想。前列腺素 D 型 1 受体选择性拮抗剂拉罗匹仑已在多项临床研究中进行了研究，证明可有效减少烟酸引起的潮红。尽管拉罗匹仑在减少烟酸引起的潮红方面具有潜力，但它的长期临床疗效和潜在的脱靶副作用尚未得到充分研究。本篇综述涵盖的领域：本文回顾了辛伐他汀/ER 烟酸/拉罗匹仑联合治疗的药理学特性、临床疗效和未来前景。
读者将了解辛伐他汀/ER 烟酸/拉罗匹仑联合治疗的作用机制和临床效果。
辛伐他汀/ER 烟酸/拉罗匹仑三联疗法可能减少潮红副作用，并为治疗混合性血脂异常患者提供更全面的治疗方案。
