Department of Medicine and Health, Linköping University, SE-58183 Linköping, Sweden.
Expert Opin Pharmacother. 2010 Jul;11(10):1715-26. doi: 10.1517/14656566.2010.489894.
Prevention of cardiovascular disease has been only partially successful with the use of cholesterol-lowering drugs like statins. There is a residual risk remaining, which may be addressed by increasing protective high-density lipoprotein (HDL) cholesterol and apolipoprotein A1. The best drug available for that purpose is niacin. In addition to increasing HDL cholesterol and apolipoprotein A1, niacin decreases triglycerides, low-density lipoprotein (LDL)-cholesterol and lipoprotein(a) and has been named the broad-spectrum lipid drug.
This review summarizes to what extent a new formulation of niacin may meet this request. The effects of niacin on lipoproteins, atherosclerosis and cardiovascular disease are described, from its first publication in 1955, and also its mechanism of action on lipoproteins and on flushing. The flushing inhibitor laropiprant is described as well as the antiflushing effect of this compound when added to extended-release niacin.
The reader will gain knowledge of the development of niacin as an antiatherosclerosis treatment and of the added value that laropiprant may offer this treatment principle; and also the present place of niacin/laropiprant in the armamentarium of cardiovascular preventive drugs.
Niacin/laropiprant is a welcome means to address the residual risk in high-risk patients on statin therapy. However, the drug combination cannot completely eliminate niacin-induced side effects. Prescribing this treatment, therefore, will require careful provision of information and instruction to the patient.
尽管使用了降低胆固醇的药物（如他汀类药物），但心血管疾病的预防仅取得部分成功。仍然存在残余风险，通过增加保护性高密度脂蛋白（HDL）胆固醇和载脂蛋白 A1 可以解决这个问题。为此目的，可用的最佳药物是烟酸。烟酸除了增加 HDL 胆固醇和载脂蛋白 A1 外，还降低甘油三酯、低密度脂蛋白（LDL）-胆固醇和脂蛋白（a），并被命名为广谱脂质药物。
本综述总结了烟酸的新配方在多大程度上满足了这一需求。描述了烟酸对脂蛋白、动脉粥样硬化和心血管疾病的影响，从 1955 年首次发表以来，以及其对脂蛋白和潮红的作用机制。还描述了潮红抑制剂拉罗匹仑以及将其添加到烟酸缓释制剂中时对潮红的抑制作用。
读者将了解烟酸作为抗动脉粥样硬化治疗的发展，以及拉罗匹仑可能为这种治疗原则带来的附加值；以及烟酸/拉罗匹仑在心血管预防药物武器库中的当前地位。
烟酸/拉罗匹仑是解决他汀类药物治疗高危患者残余风险的一种受欢迎的方法。然而，该药物组合并不能完全消除烟酸引起的副作用。因此，开具这种治疗方案需要向患者提供仔细的信息和指导。
