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缓释烟酸:其在血脂异常治疗中的应用综述

Prolonged-release nicotinic acid: a review of its use in the treatment of dyslipidaemia.

作者信息

McCormack Paul L, Keating Gillian M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 2005;65(18):2719-40. doi: 10.2165/00003495-200565180-00014.

Abstract

Prolonged-release (PR) nicotinic acid (niacin) [Niaspan] is an oral, once-daily formulation of the lipid-modifying drug designed to produce less vasodilatory flushing than crystalline immediate-release (IR) nicotinic acid and less hepatotoxicity than previous sustained-release formulations of nicotinic acid.PR nicotinic acid appears to retain the same level of efficacy as crystalline IR nicotinic acid and be better tolerated than older nicotinic acid formulations. Nicotinic acid has beneficial effects on all traditional blood lipid and lipoprotein fractions and is the most effective agent for increasing high-density lipoprotein (HDL)-cholesterol (HDL-C) and reducing lipoprotein(a). The effects of PR nicotinic acid are often additive when used in combination with HMG-CoA reductase inhibitors (statins), making it a useful addition when lipid goals are not achieved with the usual statin monotherapy or when additional correction of a specific lipid abnormality is required. PR nicotinic acid also slows atherosclerotic progression and even appears to produce regression of atherosclerosis in patients on stable statin therapy. PR nicotinic acid is a logical drug choice for treating atherogenic dyslipidaemia commonly associated with type 2 diabetes mellitus and the metabolic syndrome, and has been shown to be effective in patients with diabetes without adversely affecting glycaemic control in the majority of patients. The incidence of vasodilatory flushing with PR nicotinic acid is lower than with IR nicotinic acid and it decreases substantially over time as tolerance develops. To date, there has been no clinically significant hepatotoxicity observed with PR nicotinic acid. Therefore, once-daily PR nicotinic acid appears to maximise the potential benefits of nicotinic acid, while minimising any historical tolerability or safety concerns.

摘要

缓释型(PR)烟酸[Niaspan]是一种口服的每日一次的调脂药物制剂,旨在产生比结晶速释型(IR)烟酸更少的血管舒张性潮红,且比先前的烟酸缓释制剂肝毒性更小。PR烟酸似乎保留了与结晶IR烟酸相同水平的疗效,并且比旧的烟酸制剂耐受性更好。烟酸对所有传统血脂和脂蛋白组分均有有益作用,是升高高密度脂蛋白(HDL)胆固醇(HDL-C)和降低脂蛋白(a)最有效的药物。PR烟酸与HMG-CoA还原酶抑制剂(他汀类药物)联合使用时,其效果通常具有相加性,当常规他汀类单药治疗未达到血脂目标或需要额外纠正特定脂质异常时,它是一种有用的添加药物。PR烟酸还可减缓动脉粥样硬化进展,甚至在接受稳定他汀治疗的患者中似乎能使动脉粥样硬化发生逆转。PR烟酸是治疗通常与2型糖尿病和代谢综合征相关的致动脉粥样硬化性血脂异常的合理药物选择,并且已证明对糖尿病患者有效,在大多数患者中不会对血糖控制产生不利影响。PR烟酸引起血管舒张性潮红的发生率低于IR烟酸,并且随着耐受性的形成,其发生率会随着时间的推移而大幅下降。迄今为止,未观察到PR烟酸有临床上显著的肝毒性。因此,每日一次的PR烟酸似乎在最大限度地发挥烟酸潜在益处的同时,将任何历史上的耐受性或安全性问题降至最低。

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