Acipimox

DescriptionAcipimox is a nicotinic acid derivate that structurally related to nicotinic acid. Like nicotinic acid, lowers lipids effectively, but unlike nicotinic acid, acipimox is longer acting and therefore much less prone to produce free fatty acid rebounding. It is usually employed in man in the therapy of hypertriglyceridemia. In addition to its lipid lowering activity, it produces a beneficial elevation of the anti-atherogenic high density lipoprotein subfraction, HDL2. Acipimox is recommended as a lipid-lowering agent to treat hyperlipidemia in patients with noninsulin dependent diabetes mellitus.

UsesAcipimox is a long-acting antilipemic agent and used for the treatment of hyperlipoproteinemias, in particular hypertriglyceridemias, and as adjunctive therapy for affecting cholesterol metabolism.

PreparationSynthesis of acipimox: Under cooling and stirring, 78 g of maleic anhydride was dissolved in a solution of 60 ml of chloroform, and 40 ml of 30% hydrogen peroxide was added. After 2 h, 4.8 g of 5-Methyl-2-pyrazinecarboxylic acid was added, and the temperature was kept at 0-5 °C for 2 d. The maleic acid was filtered off. Concentrate to a small volume, add ethyl acetate, and filter to obtain 1.1 g of acipimox, the melting point of which is 178-180 °C.