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Anatrol

Anatrol - General Information

A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Anatrol has been used in the treatment of endometriosis and some benign breast disorders.

 

Pharmacology of Anatrol

Anatrol is a derivative of the synthetic steroid ethisterone, a modified testosterone. It was approved by the U.S. Food and Drug Administration (FDA) as the first drug to specifically treat endometriosis, but its role as a treatment for endometriosis has been largely replaced by the gonadotropin-releasing hormone (GnRH) agonists. Anatrol has antigonadotropic and anti-estrogenic activities. Anatrol acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties.

 

Additional information about Anatrol

Anatrol Indication: For the treatment of endometriosis and some benign breast disorders.
Mechanism Of Action: As a gonadotropin inhibitor, danazol suppresses the pituitary-ovarian axis possibly by inhibiting the output of pituitary gonadotropins. Anatrol also depresses the preovulatory surge in output of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) and therefore reduces ovarian estrogen production. Anatrol also may directly inhibit ovarian steroidogenesis, bind to androgen, progesterone, and glucocorticoid receptors, bind to sex-hormone-binding globulin and corticosteroid-binding globulin, and increase the metabolic clearance rate of progesterone. Endometriosis - As a consequence of suppression of ovarian function, both normal and ectopic endometrial tissues become inactive and atrophic. As a result, anovulation and associated amenorrhea occur. Fibrocystic breast disease - The exact mechanism of action is unknown, but may be related to suppressed estrogenic stimulation as a result of decreased ovarian production of estrogen. A direct effect on steroid receptor sites in breast tissue also is possible. Disappearance of nodularity, relief of pain and tenderness, and possibly changes in the menstrual pattern result. Hereditary angioedema - Anatrol corrects the underlying biochemical deficiency by increasing serum concentrations of the deficient C1 esterase inhibitor, resulting in increased serum concentrations of the C4 component of the complement system. (Source: PharmGKB)
Drug Interactions: Anisindione The androgen increases the anticoagulant effect
Cyclosporine The androgen increases the anticoagulant effect
Carbamazepine Increases the effect of carbamazepine
Dicumarol The androgen increases the anticoagulant effect
Acenocoumarol The androgen increases the anticoagulant effect
Warfarin The androgen increases the anticoagulant effect
Lovastatin Risk of severe myopathy/rhabdomyolysis with this combination
Tacrolimus Increases the effect and toxicity of tacrolimus
Food Interactions: Take without regard to meals.
Generic Name: Danazol
Synonyms: Not Available
Drug Category: Estrogen Antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Danazol: Anatrol; Chronogyn; Cyclomen; Danocrine;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Hepatic, to principal metabolites, ethisterone and 17-hydroxymethylethisterone.
Half Life: Approximately 24 hours.
Dosage Forms of Anatrol: Capsule Oral
Capsule Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C22H27NO2
Danazol on Wikipedia: http://en.wikipedia.org/wiki/Danazol
Organisms Affected: Humans and other mammals