Center for Endocrinology, Diabetes and Preventive Medicine, University of Cologne, Kerpener St. 62, 50937 Cologne, Germany.
Curr Pharm Des. 2013;19(17):3094-106. doi: 10.2174/1381612811319170017.
The clinically most relevant medications for lipid management are the statins, which constitute in the majority of the cases the basis of any lipid-modulating therapy. However, other agents are often needed to either reduce low-density cholesterol to target levels and/or to treat residual serum lipoprotein abnormalities. Niacin is currently the most potent available agent to increase high-density lipoprotein and reduce lipoprotein(a), both independent risk factors for cardiovascular disease. Niacin also has been found to reduce inflammatory markers like C-reactive protein (CRP) and lipoprotein-associated phospholipase-A2 (Lp-PLA2) and to decrease small-dense LDL and increase large-particle LDL, all potentially anti-atherosclerotic properties. Through its action on the GPR109A receptor niacin seems to also exert various pleiotropic effects such as improvement of endothelial function and reduction of inflammation and oxidative stress. However, niacin is often underused in the clinical setting, mainly due to either potentially preventable or disproportionally feared side effects such as flushing, hyperglycemia, and hyperuricemia, respectively. Even though the results of the AIM-HIGH trial were negative, the results of the larger end point trial HPS2-THRIVE are still pending. Based on the totality of existing evidence, niacin should in the mean time remain high in the list of lipid-modulating agents to be used in clinical practice, second after statins.
用于血脂管理的临床相关药物中，他汀类药物最为重要，它们构成了大多数降脂治疗的基础。然而，为了将低密度胆固醇降低到目标水平和/或治疗残留的血清脂蛋白异常，通常还需要其他药物。烟酸是目前增加高密度脂蛋白和降低脂蛋白（a）最有效的药物，而高密度脂蛋白和脂蛋白（a）都是心血管疾病的独立危险因素。烟酸还被发现可以降低炎症标志物，如 C 反应蛋白（CRP）和脂蛋白相关磷脂酶 A2（Lp-PLA2），减少小而密 LDL 并增加大颗粒 LDL，所有这些都具有潜在的抗动脉粥样硬化作用。烟酸通过作用于 GPR109A 受体，似乎还具有多种多效性作用，如改善内皮功能、减少炎症和氧化应激。然而，烟酸在临床实践中常常未被充分利用，主要是由于其潜在的可预防或不成比例的不良反应，如潮红、高血糖和高尿酸血症。尽管 AIM-HIGH 试验的结果为阴性，但更大终点试验 HPS2-THRIVE 的结果仍在等待中。基于现有证据的总体情况，烟酸在降脂药物的使用清单中仍应处于较高位置，仅次于他汀类药物。
