DISPOSITION OF THALIDOMIDE IN RABBITS AND RATS

  1. Herbert Schumacher,
  2. David A. Blake and
  3. James R. Gillette
  1. Laboratory of Chemical Pharmacology, National Heart Institute, National Institutes of Health, Bethesda, Maryland

    Abstract

    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.

    Footnotes

      • Received June 21, 1967.
      • Accepted October 25, 1967.
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    1. JPET March 1968 vol. 160 no. 1 201-211
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