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Journal of Pharmacology And Experimental Therapeutics, Vol. 98, Issue 1, 97-104, 1950
Copyright © 1950 by American Society for Pharmacology and Experimental Therapeutics

THE FATE OF ANTIPYRINE IN MAN

Bernard B. Brodie 1 and Julius Axelrod 2

1 Research Service, Third (New York University) Medical Division, Goldwater Memorial Hospital, Department of Biochemistry, New York University College of Medicine, New York, New York
2 Laboratory of Industrial Hygiene, New York, New York

Factors concerned with the physiological disposition and metabolic fate of antipyrine in man have been studied.

The drug is absorbed completely from the gastrointestinal tract and is then evenly distributed throughout the body water. Only about 5 per cent of the drug is excreted in the urine, the remainder being transformed in the body. The transformation of antipyrine is slow, so that plasma levels after a single therapeutic dose decline only 1 to 12 per cent an hour, resulting in sustained plasma levels for fifteen hours or more. This is considerably longer than with acetanilide, phenacetin or N-acetyl p-aminophenol.

One route of metabolism of antipyrine in man was shown to be as follows: 30 to 40 per cent of the drug is oxidized to 4-hydroxyantipyrine, which is quickly conjugated with glucuronic and possibly sulfuric acid and excreted as such; the remainder of the antipyrine is metabolized through an unknown route.

Submitted on October 10, 1949




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Copyright © 1950 by the American Society for Pharmacology and Experimental Therapeutics.