Solid-state decomposition of para-substituted salicylic acids

✍ Scribed by Pakdee Pothisiri; J. T. Carstensen

• Publisher: John Wiley and Sons
• Year: 1975
• Tongue: English
• Weight: 445 KB
• Volume: 64
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600641204

✦ Synopsis

suggested that product inhibition (including cross-product inhibition) of drug biotransformation processes may be due to an interaction of the inhibitory agents with cytochrome P-450 (8,14). Specifically, a competition between the hydroxylated metabolite and the drug for binding sites on cytochrome P-450 was suggested ( 14).

The observation of product inhibition in the elimination of antipyrine is of particular interest because this drug differs from the others studied so far in that it is very hydrophilic and negligibly bound to plasma proteins. The metabolite 4-hydroxyantipyrine may be a potentially useful inhibitor of drug elimination in human drug therapy (analogous to the use of probenecid as an inhibitor of renal excretion of drugs). However, since its biological half-life in humans is very short', it may be most useful as a n inhibitor of "first-pass'' metabolism. This possibility remains to be explored.