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Formation of reactive metabolites of phenacetin in humans and rats


Veronese, ME and McLean, S and D'souza, C and Davies, NW, Formation of reactive metabolites of phenacetin in humans and rats, Xenobiotica, 15, (11) pp. 929-940. ISSN 0049-8254 (1985) [Refereed Article]

Copyright Statement

Copyright 1985 Taylor & Francis

DOI: doi:10.3109/00498258509045046


1. The metabolism of phenacetin to reactive intermediates in humans was estimated from the excretion of thio adducts in urine. N-Hydroxyphenacetin, a precursor of reactive metabolites, was also quantified.

2. Following an oral dose of phenacetin (10 mg/kg) to humans, these metabolites in 24 h urine were: paracetamol-3-cysteine, 44% dose; paracetamol-3-mercapturate, 39%; 3-thiomethylparacetamol, 04%; N-hydroxyphenacetin, 0·5%

3. Rats showed a considerable increase in N-hydroxyphenacetin excretion after chronic dosing with phenacetin at high dosage (500 mg/kg) for one month. Chronic dosing with a low dose (50 mg/kg) did not increase N-hydroxyphenacetin excretion, but a marked increase occurred on concomitant administration of aspirin and caffeine.

Item Details

Item Type:Refereed Article
Research Division:Biomedical and Clinical Sciences
Research Group:Medical biochemistry and metabolomics
Research Field:Metabolic medicine
Objective Division:Expanding Knowledge
Objective Group:Expanding knowledge
Objective Field:Expanding knowledge in the health sciences
UTAS Author:Veronese, ME (Mr Maurice Veronese)
UTAS Author:McLean, S (Professor Stuart McLean)
UTAS Author:D'souza, C (Mr Conrad D'Souza)
UTAS Author:Davies, NW (Associate Professor Noel Davies)
ID Code:102181
Year Published:1985
Web of Science® Times Cited:24
Deposited By:Central Science Laboratory
Deposited On:2015-08-03
Last Modified:2015-09-22

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