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Laropiprant (INN) was a drug used in combination with niacin to reduce blood cholesterol (LDL and VLDL) that is no longer sold, due to increases in side-effects with no cardiovascular benefit. Laropiprant itself has no cholesterol lowering effect, but it reduces facial flushes induced by niacin. Merck & Co. planned to market this combination under the trade names Cordaptive in the US and Tredaptive in Europe. Both brands contained 1000 mg of niacin and 20 mg of laropiprant in each tablet. ==Mechanism of action== Niacin in cholesterol lowering doses (500–2000 mg per day) causes facial flushes by stimulating biosynthesis of prostaglandin D2 (PGD2), especially in the skin. PGD2 dilates the blood vessels via activation of prostaglandin D2 receptors (DP1), increasing blood flow and thus leading to flushes.〔 Laropiprant acts as a selective DP1 antagonist, reducing the vasodilation.〔 Taking 325 mg of aspirin 20–30 minutes prior to taking niacin has also been proven to prevent flushing in 90% of patients, presumably by suppressing prostaglandin synthesis,〔 〕 but this medication also increases the risk of gastrointestinal bleeding,〔 〕 though the increased risk is less than 1 percent. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Laropiprant」の詳細全文を読む スポンサード リンク
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