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Journal of Pharmacology And Experimental Therapeutics, Vol. 113, Issue 4, 481-489, 1955
Copyright © 1955 by American Society for Pharmacology and Experimental Therapeutics

THE METABOLIC FATE OF PHENYLBUTAZONE (BUTAZOLIDIN) IN MAN

J. J. BURNS 1, ROSE K. ROSE 1, SIDNEY GOODWIN 1, JULES REICHENTHAL 1, EVAN C. HORNING 1, and BERNARD B. BRODIE 1

1 Research Service, Third (New York University) Medical Division, Goldwater Memorial Hospital, New York, New York; The Laboratory of Chemical Pharmacology and the Laboratory of Natural Products, National Heart Institute, National Institutes of Health, Public Health Service, Department of Health, Education and Welfare, Bethesda 14, Md.

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.

Submitted on December 31, 1954






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Copyright © 1955 by the American Society for Pharmacology and Experimental Therapeutics.