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Journal of Pharmacology And Experimental Therapeutics, Vol. 97, Issue 1, 58-67, 1949
Copyright © 1949 by American Society for Pharmacology and Experimental Therapeutics

THE FATE OF ACETOPHENETIDIN (PHENACETIN) IN MAN AND METHODS FOR THE ESTIMATION OF ACETOPHENETIDIN AND ITS METABOLITES IN BIOLOGICAL MATERIAL

Bernard B. Brodie 1 and Julius Axelrod 1

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

1. Methods are described for the determination of acetophenetidin and p-phenetidin in biological fluids and tissues.

2. The route of metabolism of acetophenetidin in man is as follows: the major fraction of the drug is rapidly deethylated to N-acetyl p-aminophenol; this compound is excreted in a conjugated form; a minor fraction deacetylates to form p-phenetidin; this compound was shown to be the precursor of the substance which oxidizes hemoglobin to methemoglobin. The analgesic and antipyretic action of acetophenetidin is exerted mainly through N-acetyl p-aminophenol which is an active analgesic and antipyretic.

Submitted on June 1, 1949




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