Summary
The effects of Acipimox (5-methylpyracine-2-carboxylic acid-4-oxide, 3 × 250 mg/day) on plasma lipids, lipoproteins, and biliary lipids were studied in 14 healthy male volunteers using a double blind cross-over design.
There was a significant (P < 0.05) rise of HDL-cholesterol by 9.8%, while effects on other lipids and lipoproteins were small and insignificant (total cholesterol minus 6.5%, LDL-cholesterol minus 11.8%, free cholesterol minus 4.2%, total triglycerides plus 13.5% and phospholipids plus 3.9%). There was a significant rise of the HDL-cholesterol/LDL-cholesterol ratio by 23.6% (P < 0.02) and of the HDL-cholesterol/total cholesterol ratio by 16% (P < 0.05). Apolipoproteins AI, AII, and B were not significantly affected. The ratio of HDL-cholesterol/Apo AI increased significantly (P < 0.05), and the ratio of HDL-cholesterol/Apo AII rose from 1.22 to 1.32 (P < 0.05), while the ratio LDL-cholesterol/Apo B fell from 1.96 to 1.73. The composition of HDL and LDL, therefore, must have been altered by Acipimox.
The relative cholesterol concentration in bile was significantly (P < 0.05) increased by treatment with Acipimox, while bile acids and phospholipids were not significantly affected.
The lithogenic index rose significantly by 15.1% (P < 0.02) as calculated according to Admirand and Small [1], while calculations according to Hegard and Dam yielded a slight insignificant rise (P < 0.1).
The findings suggest that treatment with Acipimox might be associated with an increased risk of cholelithiasis. However, only long-term epidemiologic studies can ultimately demonstrate whether or not Acipimox increases the risk of gallstone formation.
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Jung, W., Kohlmeier, M., Nikolaus, T. et al. Effects of acipimox on plasma lipids and biliary lipids in healthy subjects. Res. Exp. Med. 185, 457–468 (1985). https://doi.org/10.1007/BF01851852
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DOI: https://doi.org/10.1007/BF01851852