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Journal of Pharmacology And Experimental Therapeutics, Vol. 90, Issue 1, 68-75, 1947
Copyright © 1947 by American Society for Pharmacology and Experimental Therapeutics

THE METABOLIC FATE OF ACETANILID AND OTHER ANILINE DERIVATIVES

II. MAJOR METABOLITES OF ACETANILID APPEARING IN THE BLOOD

DAVID LESTER 1, LEON A. GREENBERG 1, and Richard P. Carroll 1

1 From the Laboratory of Applied Physiology, Yale University

1. In man, the major metabolites of acetanilid appearing in the blood and plasma are N-acetyl p-aminophenol and its hydroxy conjugates.

2. The renal clearance of acetanilid is insignificant; that of N-acetyl p-aminophenol in two subjects ranged from 8 to 24 cc. per minute; and that of the hydroxy conjugates from 93 to 366 cc. per minute, averaging 174 cc. per minute in one subject and 273 cc. per minute in the other.

3. The major metabolism of acetanilid is its oxidation first to N-acetyl p-aminophenol with slow urinary elimination of this substance and the conversion to hydroxy conjugates with rapid elimination.

4. Free aniline and free p-aminophenol were not found as major metabolites.

5. Acetanilid and N-acetyl p-aminophenol penetrate the erythrocytes and tend somewhat to concentrate within them. The hydroxy conjugates do not penetrate the erythrocytes.

6. The methemoglobinemia occurring after acetanilid does not appear to be due to acetanilid or its major metabolites present in the blood.

Submitted on February 17, 1947




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Copyright © 1947 by the American Society for Pharmacology and Experimental Therapeutics.