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Journal of Pharmacology And Experimental Therapeutics, Vol. 104, Issue 4, 377-386, 1952
Copyright © 1952 by American Society for Pharmacology and Experimental Therapeutics

THE METABOLISM OF N-C14H3 LABELED MEPERIDINE

Nikolas P. Plotnikoff 1, Henry W. Elliott 1, and E. Leong Way 1

1 Division of Pharmacology, School of Medicine, and The College of Pharmacy, University of California, San Francisco

1. Following the administration of N-C14H3 labeled meperidine, significant amounts of radioactivity are found in the liver, stomach, small and large intestines, and feces of the rat.

2. Evidence for demethylation of meperidine was established by the presence of C14O2 in the expired air (rat) and by identifying nor-meperidine in the urine of the rat and man by countercurrent distribution.

3. Unchanged meperidine excreted in the urine accounts for only a small part of the injected dose in the rat and man.

4. Meperidine is also hydrolyzed in vivo and is excreted in the urine as 1-methyl-4-phenylisonipecotic acid.

5. The sum total of all identified metabolites does not account for all of the radioactivity in the rat urine.

Submitted on November 13, 1951




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