Author:

Keywords:

Antilipemic Agents, Drug Combinations, Drug Interactions, Dyslipidemias, Flushing, Humans, Indoles, Niacin, Science & Technology, Life Sciences & Biomedicine, Medicine, General & Internal, General & Internal Medicine, dyslipidaemia, niacin, niaspan, flushing, laropiprant, EXTENDED-RELEASE NIACIN, NICOTINIC-ACID, SECONDARY PREVENTION, INDUCED VASODILATION, COMBINATION TABLET, HEART-DISEASE, EFFICACY, SAFETY, SIMVASTATIN, NIACIN/LAROPIPRANT, Hypolipidemic Agents, 1101 Medical Biochemistry and Metabolomics, 3202 Clinical sciences

Abstract:

Niacin has been used for decades to treat dyslipidaemic disorders. Niacin is the most effective agent currently available for increasing levels of high-density lipoprotein. Moreover, significant improvements in cardiovascular outcomes in niacin treated patients have been demonstrated. However, tolerability concerns, particularly flushing, have limited its use in the past. Therefore, ER niacin, a prolonged-release formulation of niacin, has been developed with similar efficacy but a superior tolerability profile compared to the immediate-release formulations. Recent insights on niacin mechanisms of action have led to the development of a new agent called laropiprant. Laropiprant selectively blocks the binding of prostaglandin D2 to its receptor (DP1) in dermal capillaries, which mediates niacin-induced vasodilation. When co-administered with ER niacin, a marked reduction in ER niacin induced flushing is seen.The clinical use of niacin and the novel flush-reducing co-medication, will be discussed.