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Xenobiotica
the fate of foreign compounds in biological systems
Volume 14, 1984 - Issue 9
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Original Article

Inhibition of antipyrine metabolite formation in rats in vivo

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Pages 677-686 | Received 21 Jul 1983, Published online: 30 Sep 2009
 

Abstract

1. The effect of four inhibitors of cytochrome P-450-mediated drug oxidations (SKF 52SA, cimetidine, metyrapone and α-naphthoflavone) on the urinary metabolite pattern and 14CO2 exhalation rate (CER)-time profile following [N-methyl-14C]antipyrine administration has been investigated.

2. The CER-time profiles indicated that inhibition of antipyrine metabolism was in the rank order SKF 525A >cimetidine > metyrapone >ANF.

3. The urinary metabolite patterns showed selectivity in action towards particular pathways, 3-hydroxylation being primarily decreased by SKF 525A and cimetidine, and N-demethylation by ANF. The results provide further evidence for involvement of multiple forms of cytochrome P-450 in antipyrine metabolism.

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