Niacin, an old drug with new perspectives for the management of dyslipidaemia.
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.
Benhalima
K
K
Dienst Endocrinologie, Universitair Ziekenhuis Gasthuisberg, Herestraat 49, 3000 Leuven, België.
Muls
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E
D004338:Drug Combinations; D004347:Drug Interactions; D050171:Dyslipidemias / Q000188:drug therapy*; D005483:Flushing / Q000139:chemically induced / Q000517:prevention & control; D006801:Humans; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D007211:Indoles / Q000627:therapeutic use; D009525:Niacin / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*
D004338:Drug Combinations; D000960:Hypolipidemic Agents; D007211:Indoles; C518174:MK-0524; D009525:Niacin