Nicotinic acid (niacin): new lipid-independent mechanisms of action and therapeutic potentials

Trends Pharmacol Sci. 2011 Dec;32(12):700-7. doi: 10.1016/j.tips.2011.08.002. Epub 2011 Sep 22.

Abstract

Nicotinic acid (niacin) has been used for decades to prevent and treat atherosclerosis. The well-documented antiatherogenic activity is believed to result from its antidyslipidemic effects, which are accompanied by unwanted effects, especially a flush. There has been renewed interest in nicotinic acid owing to the need for improved prevention of atherosclerosis in patients already taking statins. In addition, the identification of a nicotinic acid receptor expressed in adipocytes and immune cells has helped to elucidate the mechanisms underlying the antiatherosclerotic as well as the unwanted effects of this drug. Nicotinic acid exerts its antiatherosclerotic effects at least in part independently of its antidyslipidemic effects through mechanisms involving its receptor on immune cells as well as through direct and indirect effects on the vascular endothelium. Here, we review recent data on the pharmacological effects of nicotinic acid and discuss how they might be harnessed to treat other inflammatory diseases such as multiple sclerosis or psoriasis.

Publication types

  • Review

MeSH terms

  • Animals
  • Atherosclerosis / drug therapy
  • Atherosclerosis / immunology
  • Atherosclerosis / metabolism
  • Atherosclerosis / prevention & control*
  • Flushing / chemically induced
  • Flushing / metabolism
  • Humans
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / pharmacology
  • Hypolipidemic Agents / therapeutic use*
  • Immunosuppressive Agents / adverse effects
  • Immunosuppressive Agents / pharmacology
  • Immunosuppressive Agents / therapeutic use*
  • Langerhans Cells / drug effects
  • Langerhans Cells / metabolism
  • Macrophages / drug effects
  • Macrophages / immunology
  • Macrophages / metabolism
  • Neutrophils / drug effects
  • Neutrophils / immunology
  • Neutrophils / metabolism
  • Niacin / adverse effects
  • Niacin / pharmacology
  • Niacin / therapeutic use*
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, Nicotinic / metabolism
  • Signal Transduction / drug effects
  • Vasodilator Agents / adverse effects
  • Vasodilator Agents / pharmacology
  • Vasodilator Agents / therapeutic use

Substances

  • HCAR2 protein, human
  • Hypolipidemic Agents
  • Immunosuppressive Agents
  • Receptors, G-Protein-Coupled
  • Receptors, Nicotinic
  • Vasodilator Agents
  • Niacin