The absorption, distribution and metabolic fate of danazol in rats, monkeys and human volunteers
Davison, C.; Banks, W.; Fritz, A.
Archives Internationales de Pharmacodynamie et de Therapie 221(2): 294-310
1976
ISSN/ISBN: 0003-9780 PMID: 822792 Document Number: 97025
The metabolism of danazol was investigated in the rat, the rhesus monkey and in human volunteers using 14C-isoxazolo-, 14C-ethynyl, 6,7-tritiated and unlabeled compound. The drug was well absorbed and rapidly metabolized; approximately 60 endproducts were seen in monkey urine. Four compounds were unequivocally identified in monkey fecal extracts by physico-chemical methods; several others were tentatively identified by chromatographic means. Very little unchanged danazol was found in monkey urine or feces at physiological dosages; the major identified urinary and fecal end-products were 2-hydroxymethylethisterone, .DELTA.1-2-hydroxymethylethisterone and ethisterone. In the rat the major portion of the radioactivity was excreted in the fecal matter, while in the monkey about equal portions were eliminated in urine and feces. Tissue distribution studies in monkeys and rats showed concentrations greater than the plasma levels only in the liver, adrenal glands and kidneys.