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Danazol (Danocrine®)

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by Bill Roberts - Danazol is the drug of choice for long term prophylaxis of hereditary angioedema. It is among the front line drugs for treatment of endometriosis. Plausible mechanisms for which there is evidence for activity in this area include suppression of the midcycle surge of LH/FSH at the hypothalamic level, inhibition of the transcription of the gene for the estrogen receptor in monocytes, inhibition of estrone sulfatase (required to convert estrone sulfate to estradiol), and stimulation of B cells. Danazol therapy is also anti-osteoporotic, whereas many other drugs for endometriosis cause loss of bone mass.

A disadvantage of danazol therapy is that approximately 10% of patients experience hepatocellular damage, and virilizing side effects are frequent at therapeutic doses for treatment of endometriosis. However, application via a vaginal suppository has proven an effective way to target the drug for treatment of endometriosis, which should reduce side effects.

Danazol has also been useful for treatment of fibrocystic myopathy of the breast, mastalgia, idiopathic thrombocytopenic purpurea, mixed tissue disease with protein S deficiency, autoimmune hemolytic anemia, menorrhagia, and "severe PMS."

Danazol binds to low affinity glucocorticoid binding sites (LAGS) in the liver.

Plasma fibrinogen and lipoprotein (a) levels decrease with danazol treatment, and plasminogen levels rise, thus inhibiting the process of thrombosis.

Substance name

Danazol (USAN:INN)
Chemical name

17a-ethynyl-17ß-hydroxyandrost-4-eno[2,3-d]isoxazole

Systematic name  
Index name Pregna-2,4-dien-20-yno(2,3-d)isoxazol-17-ol, (17alpha)-
CAS number 17230-88-5
Merck Index Number  
Molecular formula C22-H27-N-O2
Molecular weight 337.455
Pregnancy category X
Legal status Prescription only (US); DEA Schedule III (US)
Routes of administration Oral
Year introduced 1975

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