Reduced triglyceridemia and increased high density lipoprotein cholesterol levels after treatment with acipimox, a new inhibitor of lipolysis.

Acipimox (5-methylpyrazine carboxylic acid 4-oxide) is a new inhibitor of lipolysis with long-lasting activity, whose plasma lipid lowering potential was demonstrated in early clinical trials. The hypolipidemic effect of acipimox was investigated in two double-blind cross-over trials versus placebo. The first trial, carried out in 12 type IV patients, showed a significant triglyceride lowering effect (-35%) following 4 weeks of drug administration at a 250 tid dose. The same regimen, maintained for 9 weeks in 18 type IIA patients, failed to induce a significant reduction of total cholesterolemia. However, in 10 subjects, in whom lipoprotein cholesterol fractionation was carried out, a significant reduction of low density and highly significant increase in high density lipoprotein cholesterol levels (respectively -11% and +20%) were observed.