Clometacin--1. Metabolism and bioavailability of clometacin and its metabolites in the rat

Van Cantfort, J.; De Graeve, J.; Hercelin, B.; Gielen, J.E.

Journal de Pharmacie de Belgique 37(6): 401-409

1982


ISSN/ISBN: 0047-2166
PMID: 7161699
Document Number: 190213
The metabolism and bioavailability of 14C clometacin was studied in the rat. The drug is rapidly excreted in the urine and in the feces. It is not detected in any tissues of the treated animals 48 hours after administration. The metabolism of clometacin is very limited under the experimental conditions used in our study. More than 85% of the drug is excreted in an unchanged from. One metabolite, representing 4 to 10% of the excreted radioactivity, was found in the urine and identified as 1-(2-methyl-3-p-chloro phenylcarbinol-6-hydroxy) indol acetic acid. This metabolite was not detected in the feces, nor in the different tissues 4 or 48 hours after i.v. or oral administration of the drug.

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