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Journal of Pharmacology And Experimental Therapeutics, Vol. 160, Issue 1, 201-211, 1968
Copyright © 1968 by American Society for Pharmacology and Experimental Therapeutics

DISPOSITION OF THALIDOMIDE IN RABBITS AND RATS

Herbert Schumacher 1, David A. Blake 1, and James R. Gillette 1

1 Laboratory of Chemical Pharmacology, National Heart Institute, National Institutes of Health, Bethesda, Maryland

The rates of absorption, metabolism and excretion of thalidomide were compared in rabbits and rats. The half-life of the drug was virtually the same (2-3 hr) in rats, rabbits and pH 7.4 buffer. The absorption of orally administered thalidomide was more rapid in rabbits than in rats and the time-course for the elimination of metabolites was different in the two species. Although thalidomide is metabolized mainly by spontaneous hydrolysis in various tissues, the rate of breakdown is considerably greater in rabbit liver. Evidence is presented indicating that thalidomide in both species becomes bound to tissue components, possibly by covalent bonds.

Submitted on June 21, 1967
Accepted on October 25, 1967




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Copyright © 1968 by the American Society for Pharmacology and Experimental Therapeutics.