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Disposition of etofibrate, clofibric and nicotinic acid esters, and their products in dogs

✍ Scribed by Edward R. Garrett; Paul Altmayer

Book ID
102916927
Publisher
John Wiley and Sons
Year
1985
Tongue
English
Weight
586 KB
Volume
74
Category
Article
ISSN
0022-3549

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✦ Synopsis

Etofibrate, the ethylene glycol diester of clofibric and nicotinic acids, on intravenous infusion into dogs, has a terminal half-life of 2 min. The intermediate half-esters, the nicotinate and the clofibrate, have respective terminal half-lives of 4.6 and 1.7 rnin and appear fleetingly when etofibrate is administered. In contrast to the 42-h terminal half-life of clofibric acid, the other final transformation product, nicotinic acid, shows saturable or dose-dependent pharmacokinetics in dogs that conform to the Michaelis-Menten equation with a terminal half-life of 4.4 rnin at low concentrations (~6.9 pM/kg). Three distinct metabolites of nicotinic acid can be identified and assayed chromatographically in the urine. The partition properties were similar to nicotinic acid. Nicotinic acid is

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Disposition kinetics of nicotine and cot
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The disposition kinetics of nicotine and cotinine enantiomers was determined in rabbits. The clearance of (R)-nicotine was similar to that of (S)-nicotine, but clearance of (R)-cotinine was twice that of (S)-cotinine. Fractional conversions of both enantiomers of nicotine to cotinine were approximat