Effect of pregnenolone carbonitrile, promethazine and antipyrine pretreatment on antipyrine metabolite formation in rats

Shaw, P.N., Hall, S.T. and Houston, J.B. (1986) Effect of pregnenolone carbonitrile, promethazine and antipyrine pretreatment on antipyrine metabolite formation in rats. Xenobiotica, 16 12: 1109-1116.


Author Shaw, P.N.
Hall, S.T.
Houston, J.B.
Title Effect of pregnenolone carbonitrile, promethazine and antipyrine pretreatment on antipyrine metabolite formation in rats
Journal name Xenobiotica   Check publisher's open access policy
ISSN 0049-8254
1366-5928
Publication date 1986-12
Sub-type Article (original research)
Volume 16
Issue 12
Start page 1109
End page 1116
Total pages 8
Place of publication London, United Kingdom
Publisher Informa Healthcare
Language eng
Formatted abstract
1. The effect of three inducers of cytochrome P-450-mediated drug oxidations (Pregnenolone carbonitrile, promethazine and antipyrine) on antipyrine metabolite kinetics has been investigated using the urinary metabolite pattern and 14CO2 exhalation rate (CER)-time profile following [N-methyl-14C]antipyrine administration.

2. The CER-time profiles showed the characteristic changes associated with induction, namely, increased maximum CER and decreased half-life, previously observed in phenobarbitone and β-naphthaflavone-induced rats.

3. Calculation of formation rate constants based on urinary recovery of 3-hydroxymethyl-, 4-hydroxy- and nor-antipyrine indicated no clear selectivity of induction by any pretreatment. However, the percentage increase of the latter two metabolites was two- to four-fold greater than for the former metabolite. The use of the metabolite ratio (3-hydroxymethylantipyrine/norantipyrine) is proposed to assess the qualitative nature of induction of antipyrine metabolism.
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Pharmacy Publications
 
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Created: Mon, 20 Dec 2010, 14:10:05 EST