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The resurgence of niacin: from nicotinic acid to niaspan/laropiprant.

Abstract
Hypercholesterolemia is one of the main factors in the development of atherosclerotic cardiovascular disease. The advent of statins led to huge progress in the treatment of hypercholesterolemia, yet the proportion of patients with prohibitive lipid values and the high incidence of cardiovascular events despite treatment are still very high. Niacin, one of the older drugs used to treat hyperlipidemia, was shown to reduce low-density lipoprotein-cholesterol (LDL-C) and triglycerides and to markedly increase high-density lipoprotein-cholesterol (HDL-C) levels. This drug came into disuse owing to frequent side effects, mainly flushing, but in recent years a reemergence of its application has occurred, and multiple clinical trials have shown its effectiveness in the treatment of hyperlipidemia and in the reduction of cardiovascular events. New formulations such as extended-release niacin (ERN) have been developed with the purpose of reducing side effects. Lately, a new compound, laropiprant, which selectively antagonizes the prostaglandin 2 (PGD2) receptor responsible for flushing, has been developed. Laropiprant, when combined with ERN, significantly reduces the incidence of flushing. New and ongoing trials will definitively prove in the long term whether this drug combination significantly reduces the severity of flushing and the incidence of cardiovascular events.
AuthorsArie Markel
JournalThe Israel Medical Association journal : IMAJ (Isr Med Assoc J) Vol. 13 Issue 6 Pg. 368-74 (Jun 2011) ISSN: 1565-1088 [Print] Israel
PMID21809737 (Publication Type: Journal Article, Review)
Chemical References
  • Hypolipidemic Agents
  • Indoles
  • MK-0524
  • Nicotinic Acids
  • Vitamin B Complex
  • Niacin
  • Cholesterol
Topics
  • Cholesterol (blood)
  • Dose-Response Relationship, Drug
  • Humans
  • Hypercholesterolemia (blood, drug therapy)
  • Hypolipidemic Agents (administration & dosage)
  • Indoles (administration & dosage)
  • Niacin (administration & dosage)
  • Nicotinic Acids (administration & dosage)
  • Treatment Outcome
  • Vitamin B Complex (administration & dosage)

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