|
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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