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Nicotinic acid: pharmacological effects and mechanisms of action.
Annual Review of Pharmacology and Toxicology ( IF 11.2 ) Pub Date : 2007-08-21 , DOI: 10.1146/annurev.pharmtox.48.113006.094746
Andreas Gille 1 , Erik T Bodor , Kashan Ahmed , Stefan Offermanns
Affiliation  

Pharmacological doses of nicotinic acid induce a profound change in the plasma levels of various lipids and lipoproteins. The ability of nicotinic acid to strongly increase the plasma concentration of high-density lipoprotein (HDL) cholesterol has in recent years led to an increased interest in the pharmacological potential of nicotinic acid. There is increasing evidence that nicotinic acid alone or in addition to LDL cholesterol-lowering drugs can reduce the progression of atherosclerosis and reduce the risk of cardiovascular events. The clinical use of nicotinic acid is, however, hindered by harmless but unpleasant side effects, especially by a strong cutaneous vasodilation called flushing. The recent discovery of the G protein-coupled receptor GPR109A (HM74A or PUMA-G) as a receptor for nicotinic acid has allowed for better understanding of the mechanisms underlying the metabolic and vascular effects of nicotinic acid. On the basis of recent progress in understanding the pharmacological effects of nicotinic acid, new strategies are in development to better exploit the pharmacological potential of nicotinic acid. New drugs acting via the nicotinic acid receptor or related receptors, as well as new co-medications that suppress unwanted effects of nicotinic acid, will most likely be introduced as new therapeutic options in the treatment of dyslipidemia and the prevention of cardiovascular diseases.

中文翻译:

烟酸:药理作用和作用机理。

烟酸的药理剂量可引起各种脂质和脂蛋白的血浆水平发生深刻变化。近年来,烟酸强烈增加高密度脂蛋白(HDL)胆固醇的血浆浓度的能力导致人们对烟酸的药理潜力的兴趣增加。越来越多的证据表明,烟酸单独使用或与LDL降低胆固醇的药物一起使用都可以减少动脉粥样硬化的进展并降低发生心血管事件的风险。然而,烟酸的临床使用受到无害但令人不愉快的副作用的阻碍,尤其是由于强烈的皮肤血管舒张作用(称为潮红)。G蛋白偶联受体GPR109A(HM74A或PUMA-G)作为烟酸受体的最新发现使人们可以更好地了解烟酸的代谢和血管作用的潜在机制。在了解烟酸的药理作用的最新进展的基础上,正在开发新的策略以更好地利用烟酸的药理潜力。通过烟酸受体或相关受体起作用的新药物,以及抑制烟酸的有害作用的新联合用药,很可能将被引入血脂异常和预防心血管疾病的新治疗选择。在了解烟酸的药理作用的最新进展的基础上,正在开发新的策略以更好地利用烟酸的药理潜力。通过烟酸受体或相关受体起作用的新药物,以及抑制烟酸的有害作用的新联合用药,很可能将被引入血脂异常和预防心血管疾病的新治疗选择。在了解烟酸的药理作用的最新进展的基础上,正在开发新的策略以更好地利用烟酸的药理潜力。通过烟酸受体或相关受体起作用的新药物,以及抑制烟酸的有害作用的新联合用药,很可能将被引入血脂异常和预防心血管疾病的新治疗选择。
更新日期:2019-11-01
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