Pleiotropic effects of niacin: Current possibilities for its clinical use

Acta Pharm. 2016 Dec 1;66(4):449-469. doi: 10.1515/acph-2016-0043.

Abstract

Niacin was the first hypolipidemic drug to significantly reduce both major cardiovascular events and mortality in patients with cardiovascular disease. Niacin favorably influences all lipoprotein classes, including lipoprotein[a],and belongs to the most potent hypolipidemic drugs for increasing HDL-C. Moreover, niacin causes favorable changes to the qualitative composition of lipoprotein HDL. In addition to its pronounced hypolipidemic action, niacin exerts many other, non-hypolipidemic effects (e.g., antioxidative, anti-inflammatory, antithrombotic), which favorably influence the development and progression of atherosclerosis. These effects are dependent on activation of the specific receptor HCA2. Recent results published by the two large clinical studies, AIM-HIGH and HPS2-THRIVE, have led to the impugnation of niacin's role in future clinical practice. However, due to several methodological flaws in the AIM-HIGH and HPS2-THRIVE studies, the pleiotropic effects of niacin now deserve thorough evaluation. This review summarizes the present and possible future use of niacin in clinical practice in light of its newly recognized pleiotropic effects.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
  • Antioxidants / adverse effects
  • Antioxidants / therapeutic use
  • Atherosclerosis / chemically induced
  • Atherosclerosis / etiology
  • Atherosclerosis / metabolism
  • Atherosclerosis / prevention & control
  • Disease Progression
  • Drug Therapy, Combination / adverse effects
  • Fibrinolytic Agents / adverse effects
  • Fibrinolytic Agents / pharmacology
  • Fibrinolytic Agents / therapeutic use
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use
  • Hyperlipidemias / drug therapy*
  • Hyperlipidemias / metabolism
  • Hyperlipidemias / physiopathology
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / pharmacology
  • Hypolipidemic Agents / therapeutic use*
  • Models, Biological*
  • Niacin / adverse effects
  • Niacin / pharmacology
  • Niacin / therapeutic use*
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, Nicotinic / metabolism
  • Vasodilator Agents / adverse effects
  • Vasodilator Agents / pharmacology
  • Vasodilator Agents / therapeutic use*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Antioxidants
  • Fibrinolytic Agents
  • HCAR2 protein, human
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Hypolipidemic Agents
  • Receptors, G-Protein-Coupled
  • Receptors, Nicotinic
  • Vasodilator Agents
  • Niacin