THE METABOLIC FATE OF PHENYLBUTAZONE (BUTAZOLIDIN) IN MAN

Two metabolic products of phenylbutazone have been isolated from the urine of subjects receiving the drug. One of them (Metabolite I), has been identified as a derivative of phenylbutazone in which one of the benzene rings is hydroxylated in the para position; the other (Metabolite II) as a derivati...

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Published inThe Journal of pharmacology and experimental therapeutics Vol. 113; no. 4; pp. 481 - 489
Main Authors BURNS, J J, ROSE, R K, GOODWIN, S, REICHENTHAL, J, HORNING, E C, BRODIE, B B
Format Journal Article
LanguageEnglish
Published United States American Society for Pharmacology and Experimental Therapeutics 01.04.1955
Subjects
Analgesics - metabolism
Body Fluids
Old Medline
Phenylbutazone
Urine
ANALGESICS/metabolism
URINE
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Summary:Two metabolic products of phenylbutazone have been isolated from the urine of subjects receiving the drug. One of them (Metabolite I), has been identified as a derivative of phenylbutazone in which one of the benzene rings is hydroxylated in the para position; the other (Metabolite II) as a derivative in which a hydroxyl group has been introduced in the 3 position of the butyl sidechain. Metabolite I is unusually stable in man having a biologic half-life of about two days, while Metabolite II has a half-life of about ten hours. After phenylbutazone administration Metabolite I apparently accumulates in the body in considerable amounts. The possible role of the metabolites of phenylbutazone in the overall antirheumatic or side-effects of the parent compound is discussed.
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ISSN:0022-3565
1521-0103