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Journal of Pharmacology And Experimental Therapeutics, Vol. 161, Issue 2, 373-381, 1968
Copyright © 1968 by American Society for Pharmacology and Experimental Therapeutics

THE ISOLATION AND IDENTIFICATION OF THE URINARY OXIDATIVE METABOLITES OF METRONIDAZOLE IN MAN

J. E. Stambaugh 1, L. G. Feo 1, and R. W. Manthei 1

1 Departments of Pharmacology and Urology, Jefferson Medical College, Philadelphia, Pennsylvania

The oxidative metabolites of 1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole (metronidazole) found in the urine of human subjects receiving this drug orally for the treatment of trichomonas vaginitis were isolated and identified. Unchanged metronidazole and five nitro-containing metabolites were excreted in the majority of the urines studied. These metabolites resulted from side chain oxidation or conjugation of the parent compound. The metabolism of metronidazole was also examined in mice and was similar to that in man. The metabolism of 1-(2-hydroxyethyl)-2-hydroxymethyl-5-nitroimidazole, a major metabolic product of metronidazole, was also studied in mice, and only compounds corresponding to metabolites of metronidazole were found to be excreted in the urine. A second metabolite of metronidazole, 1-acetic acid-2-methyl-5-nitroimidazole, was similarly studied and was found to be excreted in the urine predominantly as the unchanged drug.

Submitted on November 27, 1967
Accepted on February 15, 1968




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