Niacin: chemical forms, bioavailability, and health effects

Nutr Rev. 2012 Jun;70(6):357-66. doi: 10.1111/j.1753-4887.2012.00479.x.

Abstract

Elevated low-density lipoprotein cholesterol (LDL-C) has been the main target of lipid-altering therapy to reduce cardiovascular risk associated with dyslipidemia. Residual cardiovascular risk remains, however, after achievement of goal LDL-C levels and is associated in part with other risk markers of cardiovascular disease, including low high-density lipoprotein cholesterol (HDL-C), high lipoprotein a, and hypertriglyceridemia. Niacin is considered a valuable agent for therapy to modify high LDL-C as well as low HDL-C, high lipoprotein a, and hypertriglyceridemia. The forms of niacin available in the marketplace include unbound niacin, or free nicotinic acid (NA); extended-release NA, a form of NA that is released gradually over a period of time; inositol hexanicotinate, six molecules of NA covalently bonded to one molecule of inositol; and nicotinamide, or niacinamide, the amide form of NA, which is readily bioavailable. This review is designed to assist healthcare professionals in evaluating the form(s) of niacin best suited for a particular therapeutic goal. Further, it provides a literature-based evaluation of risk for NA, extended-release NA, inositol hexanicotinate, and nicotinamide.

Publication types

  • Review

MeSH terms

  • Biological Availability
  • Cardiovascular Diseases / blood*
  • Cardiovascular Diseases / prevention & control*
  • Cholesterol, HDL / blood
  • Cholesterol, LDL / blood
  • Dose-Response Relationship, Drug
  • Dyslipidemias / drug therapy
  • Humans
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / chemistry
  • Hypolipidemic Agents / pharmacokinetics
  • Hypolipidemic Agents / therapeutic use
  • Niacin / adverse effects
  • Niacin / chemistry*
  • Niacin / pharmacokinetics*
  • Niacin / therapeutic use

Substances

  • Cholesterol, HDL
  • Cholesterol, LDL
  • Hypolipidemic Agents
  • Niacin