METABOLISM OF AMINOGLUTETHIMIDE IN THE RAT

  • 1 January 1982
    • journal article
    • research article
    • Vol. 10  (4) , 405-412
Abstract
The metabolism of aminoglutethimide was studied in the rat by use of the 14C-labeled compound. Following oral doses of 5 and 50 mg/kg, the drug was almost completely eliminated within 48 h into urine and feces, mostly in the form of metabolites. In bile duct-cannulated rats, biliary excretion of radioactivity amounted to .apprx. 52% within 24 h of an orally administered 50-mg/kg dose, with the remainder of the dose being eliminated into urine. The major urinary metabolites resulted from acetylation of the aniline moiety, hydroxylation of the glutarimide ring at positions 3 and 4 and oxidative elimination of the ethyl sidechain. The polar metabolites are accounted for by aromatic hydroxylation with subsequent sulfate conjugation and by a glutarimide ring-opened compound. A .gamma.-butyrolactone derivative was also identified.