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Inhibition of lipolysis by nicotinic acid and by acipimox
Author(s) -
Fuccella Luciano M,
Goldaniga Giancarlo,
Lovisolo Pierpaolo,
Maggi Elso,
Musatti Lisa,
Mandelli Virginio,
Sirtori Cesare R
Publication year - 1980
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1980.236
Subject(s) - lipolysis , chemistry , endocrinology , medicine , pharmacology , biochemistry , adipose tissue
Acipimox (5‐methylpyrazinecarboxylic acid 4‐oxide) is a new lipolysis inhibitor that has a distant chemical relationship with nicotinic acid (NA). The tritiated compound (100 mg) is rapidly absorbed, peak plasma radioactivity being reached after 2 hr, with an almost total elimination unchanged in urine. A comparison of the antilipolytic activity of three doses of acipimox and three doses of NA showed acipimox to be 20 times as potent as NA. There was a correlation between intensity and duration of effect for acipimox, but not for NA. Plasma acipimox levels correlated with inhibition of lipolysis. In consideration of the very good subjective tolerability of acipimox at all doses tested, this drug may be suitable for control of lipolysis in hyperlipidemias. Clinical Pharmacology and Therapeutics (1980) 28 , 790–795; doi: 10.1038/clpt.1980.236