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Classification:

Synthetic androgen (gonadotropin inhibitor)

Action/Kinetics:

Inhibits the release of gonadotropins (FSH and LH) by the anterior pituitary; thus, inhibits synthesis of sex steroids and competitively inhibits binding of steroids to their cytoplasmic receptors in target tissues. In women this action arrests ovarian function, induces amenorrhea, and causes atrophy of normal and ectopic endometrial tissue. Has weak androgenic effects. Onset, fibrocystic disease: 4 weeks. Time to peak effect, amenorrhea and anovulation: 6-8 weeks; fibrocystic disease: 2-3 months to eliminate breast pain and tenderness and 4-6 months for elimination of nodules. t 1/2: 4.5 hr. Duration: Ovulation and cyclic bleeding usually resume 60-90 days after cessation of therapy.

Uses:

Endometriosis amenable to hormonal management in clients who cannot tolerate or who have not responded to other drug therapy. Fibrocystic breast disease. Hereditary angioedema in males and females. Investigational: Gynecomastia, menorrhagia, precocious puberty, idiopathic immune thrombocytopenia, lupus-associated thrombocytopenia, and autoimmune hemolytic anemia.

Contraindications:

Undiagnosed genital bleeding; markedly impaired hepatic, renal, and cardiac function; pregnancy and lactation.

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