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Xenobiotica
the fate of foreign compounds in biological systems
Volume 15, 1985 - Issue 11
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Original Article

Formation of reactive metabolites of phenacetin in humans and rats

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Pages 929-940 | Received 14 Sep 1984, Published online: 30 Sep 2009
 

Abstract

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, 4·4% dose; paracetamol-3-mercapturate, 3·9%; 3-thiomethylparacetamol, 0·4%; 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.

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