The absorption, distribution and metabolic fate of danazol in rats, monkeys and human volunteers.
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Danazol was well absorbed and rapidly metabolized in rats, monkeys, and humans, with major metabolites identified in monkey excreta and higher tissue concentrations found in the liver, adrenal glands, and kidneys.
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Abstract
The metabolism of danazol has been investigated in the rat, the monkey and in human volunteers using 14C-isoxazolo-, 14C-ethynyl, 6,7-tritiated and unlabelled compound. The drug was well absorbed, and rapidly metabolized; approximately 60 endproducts were seen in monkey urine. Four compounds have been unequivocally identified in monkey fecal extracts by physico-chemical methods; several others have been 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, delta1-2-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.
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- Effect of liquid volume and food intake on the absolute bioavailability of danazol, a poorly soluble drug 2005
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- GC–MS characterization of urinary metabolites and changes of ethisterone and testosterone profile after oral administration of danazol in equine 2001
- Prolonged inhibition of normal ovarian cycles in the rat and cynomolgus monkeys following a single s.c. injection of danazol 1997
- Characterization and bioavailability of danazol-hydroxypropyl β-cyclodextrin coprecipitates 1996
- Angiotensin-Converting Enzyme Inhibitor and Danazol Increase Sensitivity of Cough Reflex in Female Guinea Pigs 1996
- [<sup>3</sup>H]Dexamethasone Binding Activity in Liver Microsomes is Modulated Differently by 17 α‐Alkylated Androgens and Testosterone<i>in vivo</i> 1995
- A randomized, placebo-controlled, crossover trial of danazol for the treatment of premenstrual syndrome 1995
- Danazol: Prolonged suppression of gonadotropins after subcutaneous administration in the castrate male rat 1994
- Progesterone receptor induction by danazol in cultured cancer cells and the rat uterus 1992
- The Detection of Danazol and Its Significance in Doping Analysis 1992
- The use of danazol as a treatment of endometriosis 1991
- Effects of danazol, gonadotropin-releasing hormone agonist, and a combination of danazol and gonadotropin-releasing hormone agonist on experimental endometriosis 1990
- Comparison of the pharmacology of nafarelin and danazol 1990
- Inhibitory effects of danazol and medroxyprogesterone acetate on [3H]thymidine incorporation in human endometrial cancer cells 1988
- Growth inhibition by danazol in a human endometrial cancer cell line with estrogen-independent progesterone receptors 1987
- Inhibition of gonadotropin-releasing hormone receptors in rat anterior pituitary monolayer cell cultures by danazol 1986
- A COMPARISON OF THE EFFECTS OF DANAZOL AND GESTRINONE ON TESTOSTERONE BINDING TO SEX HORMONE BINDING GLOBULIN <i>IN VITRO</i> AND <i>IN VIVO</i> 1986
- Danazol inhibits steroidogenesis by the human ovary in vivo 1986
- Direct biphasic effects of danazol on gonadotropin-dependent differentiation of cultured rat granulosa cells 1986
- Danazol binds to progesterone receptors and inhibits the growth of human endometrial cancer cells in vitro 1986
- Serum estradiol and danazol. I. Endometriosis response, side effects, administration interval, concurrent spironolactone and dexamethasone 1985
- Danazol—Introductory remarks 1984
- Serum estradiol and danazol. I. Endometriosis response, side effects, administration interval, concurrent spironolactone and dexamethasone 1984
- Endometriosis and infertility 1984
- Pharmacology and clinical effects of danazol 1982
- Hormonal and Surgical Management of Pelvic Endometriosis 1982
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- Actions of danazol in vivo on cytochrome P-450 and steroidogenic enzymes in rat testis and liver microsomal preparations 1981
- Transient Adrenogenital Syndrome due to Exposure to Danazol in Utero 1981
- Pharmacology and Pharmacokinetics of Danazol 1980
- Inhibition of Adrenal Steroidogenesis by Danazol in Vivo 1980
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