Hotz W
Adv Lipid Res. 1983;20:195-217.
Nicotinic acid is used widely in the treatment of hyperlipoproteinemias and reduces both the cholesterol and the triglyceride concentrations in the plasma. However, very high doses are needed to achieve these therapeutic effects, which is why side effects are common and are particularly known to hinder the compliance of patients. Nicotinic acid derivatives have been developed to overcome this problem. As a result of chemical and galenic retardation, these derivatives lessen the side effects and the necessary doses are considerably reduced in comparison with pure nicotinic acid. However, most of these derivatives are not pure prodrugs, and exert their own synergistic pharmacokinetic and pharmacodynamic effects. In general, when nicotinic acid and its derivatives are used in therapy a desirable modification of the composition of the plasma lipids in the sense of an antiatherosclerotic activity can be expected (reductions of VLDL and LDL and an increase of HDL). Good possibilities for using nicotinic acid in the prevention and remission of atherosclerotic processes arise in connection with the activation of fibrinolysis and the reduction of the tendency toward platelet aggregation. In the light of recent studies on the mechanisms of action of nicotinic acid, an influence on the prostaglandin system has been found, as a result of which an interconnection between its various effects and side effects appears to be possible.
烟酸广泛用于治疗高脂蛋白血症，可降低血浆中的胆固醇和甘油三酯浓度。然而，需要非常高的剂量才能达到这些治疗效果，这就是副作用常见且尤其会妨碍患者依从性的原因。已开发出烟酸衍生物来克服这一问题。由于化学和药剂学缓释作用，这些衍生物减轻了副作用，与纯烟酸相比所需剂量大幅降低。然而，这些衍生物大多并非纯前药，它们自身会产生协同的药代动力学和药效学效应。一般来说，当使用烟酸及其衍生物进行治疗时，可以预期在抗动脉粥样硬化活性方面对血浆脂质组成进行理想的改变（降低极低密度脂蛋白和低密度脂蛋白，增加高密度脂蛋白）。与纤维蛋白溶解的激活以及血小板聚集倾向的降低相关，使用烟酸预防和缓解动脉粥样硬化过程具有良好的可能性。鉴于最近对烟酸作用机制的研究，发现其对前列腺素系统有影响，因此其各种效应和副作用之间似乎有可能存在关联。
