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Journal of Pharmacology And Experimental Therapeutics, Vol. 143, Issue 2, 215-220, 1964
Copyright © 1964 by American Society for Pharmacology and Experimental Therapeutics


THE METABOLITES OF INDOMETHACIN, A NEW ANTI-INFLAMMATORY DRUG

Robert E. Harman 1, M. A. P. Meisinger 1, George E. Davis 1, and Frederick A. Kuehl JR. 1

1 Merck Sharp & Dohme Research Laboratories, Merck & Company, Inc., Rahway, New Jersey

The urinary metabolites of indomethacin in several animal species and in man have been investigated with the use of C14-labeled drug. Most of the drug is accounted for as unchanged indomethacin and its O-desmethyl and N-deschlorobenzoyl derivatives and the corresponding acyl glucuronides. Conjugation and renal excretion of indomethacin occur with lowest efficiency in the dog and the rat. The rabbit, guinea pig and monkey show an increasing degree of glucuronide conjugation and a more rapid and complete renal excretion pattern. Man rapidly excretes indomethacin in the urine entirely as the glucuronide.

Submitted on July 26, 1963
Accepted on October 2, 1963




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