Pharmacological Effects
Antigonadotropnoe agent is a synthetic androgen derived from etisterona. Suppresses the production of pituitary gonadotropins LH and FSH in men and women. Women inhibits ovarian activity, inhibits ovulation, causes atrophy of the endometrium. Reversible effect, deprived of estrogens or progestogens action in high doses has a weak androgenic activity with concomitant anabolic effect. When endometriosis affects both normal and ektopirovannuyu endometrial tissue, leading to its inactivation, and atrophy. Reduces the pain that accompanies endometriosis causes regressive changes of endometriotic lesions. Exerts immunosuppressive effects and inhibit lymphocyte proliferation in vitro. Significantly reduces the level of Ig and the production of autoantibodies in patients with endometriosis. With fibrocystic mastopathy promotes partial or complete disappearance of nodular seals and complete relief of pain. Clinical efficacy in hereditary angioedema, possibly due to the increasing content of C1 esterase inhibitor (congenital deficiency of which is characteristic of the disease) and, as a result, increased plasma levels of C4 complement component.
Indications
Endometriosis (with associated infertility), benign tumors of the breast (fibrocystic breast disease), primary menorrhagia, premenstrual syndrome, primary premature puberty, gynecomastia, a hereditary angioedema.
Contraindications
Hypersensitivity, pregnancy, lactation, porphyria (increased activity of liver transaminases), liver and / or renal failure, CHF, thromboembolism, androgen-dependent tumors, vaginal bleeding (unexplained). C care. Diabetes, epilepsy, migraine, disorders of plasma mechanisms of hemostasis.
Side effects
"Vulgar" acne, hypersecretion of the sebaceous glands, fluid retention, hirsutism, "tides" of blood to the skin of the face, profuse sweating, reducing the size of mammary glands, coarsening rates, weight gain, vaginitis, impaired spermatogenesis, virilny syndrome, nausea, dizziness , emotional lability, spasms of skeletal muscles, headache, increased intracranial pressure, lumbodynia, paresthesia, sleep disturbances, visual disturbances, or thrombocytopenia, thrombocytosis, polycythemia, leukocytosis, bleeding in patients with hemophilia, skin rash, dysmenorrhea, cholestatic jaundice, hepatitis, alopecia , increased activity of liver transaminaz.Peredozirovka.
Symptoms: headache, dizziness, tremors, convulsions, nausea, and vomiting. Treatment: gastric lavage, symptomatic therapy.
Dosage and administration
Inside. Treatment starts on the first day of the menstrual cycle. Adults - 200-800 mg / day in 2-4 reception. Endometriosis initial daily dose - 400 mg, further to 800 mg treatment - 6 months, as preoperative preparation - 300-400 mg / day for 1-2 months before surgery. In benign breast disease - 100-300 mg daily for 3-6 months, with primary menorrhagia and premenstrual syndrome - to 100-400 mg / day course of treatment - 3 months, with gynecomastia in men - to 200-600 mg / day. To prevent angioedema initial dose - 200 mg, with subsequent reduction (in the absence of relapse) within 1-3 months. Children: in premature puberty - daily 100-400 mg depending on age and condition of the patient.
Special instructions
Recommended periodic monitoring of liver enzymes. The drug is not used as a contraceptive drug. When assigning patients with diabetes require insulin dose adjustment.
Interaction
Enhances the effect of anticoagulants and coumarin derivatives indandiona (risk of bleeding). Reduces the effect of insulin and oral hypoglycemic drugs (affecting carbohydrate metabolism, increases the concentration of glucose in the blood). Inhibits the metabolism of carbamazepine and increase its concentration in the blood. Increases blood concentrations of cyclosporine and tacrolimus (risk of nephrotoxicity). Increases the concentration of glucagon in plasma.
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