RT Journal Article
SR Electronic
T1 Metabolism of aminoglutethimide in the rat.
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 405
OP 412
VO 10
IS 4
A1 H Egger
A1 F Bartlett
A1 W Itterly
A1 R Rodebaugh
A1 C Shimanskas
YR 1982
UL http://dmd.aspetjournals.org/content/10/4/405.abstract
AB 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 hr into urine and feces, mostly in the form of metabolites. In bile duct-cannulated rats, biliary excretion of radioactivity amounted to about 52% within 24 hr 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. In addition, a gamma-butyrolactone derivative was also identified.