Hormone replacement therapy (HRT) to treat the symptoms of estrogen deficiency associated with natural menopause or induced surgical intervention in perimenopausal and postmenopausal women. Prevention of osteoporosis in post-menopausal women at high risk of future fractures who are intolerant or contraindicated in the use of other drugs approved for the prevention of osteoporosis. There is limited experience in the treatment of women over 65 years of age.
Composition:
1 tabl white contains 2 mg estradiol valerate; 1 tabl blue contains 2 mg estradiol valerate and 10 mg medroxyprogesterone acetate. The drug contains lactose.
Action:
Preparation used in hormone replacement therapy. The active form of estradiol valerate, synthetic 17β-estradiol is identical to human endogenous estradiol. Supplements estrogen deficiency in postmenopausal women and relieves symptoms of menopause. Estrogens counteract the loss of bone density as a result of natural menopause or ovariectomy. The content of progestagens in the preparation reduces the estrogen-induced risk of endometrial hyperplasia in women with a preserved uterus. Following oral administration, estradiol valerate is absorbed from the gastrointestinal tract and hydrolysed to release free estradiol. Cmax in the blood occurs 3.8 -9.4 h after administration. Estradiol binds to SHBG and albumin. It is biotransformed to estrone. It is undergoing enterohepatic circulation. It is excreted mainly in the urine in the form of metabolites (sulphates, glucuronides). Medroxyprogesterone acetate is poorly absorbed after oral administration, Cmax in the blood appears after about 1.1-4,7 h. In over 90% it is associated with albumin. Metabolism occurs in the liver. Metabolites are excreted in urine and bile, mainly with faeces.
Contraindications:
Hypersensitivity to the components of the preparation. Breast cancer in an interview, recognized or suspected. Malignant estrogen dependent tumors, or suspected (eg, endometrial cancer). Undiagnosed bleeding from the genital tract. Untreated endometrial hyperplasia. Idiopathic venous thromboembolism or current (deep vein thrombosis, pulmonary embolism). Active or recent history of arterial thromboembolism (eg angina, myocardial infarction). acute liver disease or a history of liver disease, as long as the results of functional liver tests have not returned to normal. Porphyria. Pregnancy and lactation.
Precautions:
Particularly cautiously use in patients with: myoma or endometriosis, history or risk factors for thromboembolism (eg positive personal or family history, significant obesity - BMI> 30 kg / m2, systemic lupus erythematosus, prolonged immobilization, extensive trauma or surgery; patients using anticoagulants require careful risk-benefit assessment before using HRT), risk factors for estrogen-dependent tumors (eg breast cancer in first-degree relatives), hypertension, liver disease (eg liver adenoma), diabetes with or without vascular complications , gallstones, migraine or severe headaches, systemic lupus erythematosus, endometrial hyperplasia, epilepsy, bronchial asthma, otosclerosis, impaired cardiac or renal function (in patients with terminal renal insufficiency the concentration of active substances may be increased), hypertriglyceridemia. Treatment should be discontinued immediately if: jaundice or abnormal liver function, significant increase in blood pressure, migraine headache, venous thromboembolism or if the patient becomes pregnant. The preparation should be discontinued 4-6 weeks before planned long-term immobilisation after surgery, especially operations in the abdominal cavity or orthopedic surgery on the lower limbs. Do not resume treatment before the patient is completely started.The product contains lactose and should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The use of the drug during pregnancy and lactation is contraindicated.
Side effects:
Adverse reactions (usually mild and receding during use) occur most often during the first months of treatment. Common: headaches, soreness of the breasts, irregular bleeding, body mass, swelling and fatigue. Uncommon: changes in anticoagulants, mood changes, libido disorders, visual disturbances, changes in liver enzymes. Rare: venous thromboembolism. During estrogen therapy, the risk of estrogen-dependent cancers increases: endometrium and breast.
Dosage:
In the perimenopausal period: the first tabl. On the 5th day of menstrual bleeding; in patients after menopause, not menstruating, or menstruating very irregularly, after removal of the reproductive organs: the beginning of treatment is determined arbitrarily. One table is accepted per day, at the same time, for the Next 21 days, according to the numbering. After finishing the packaging (21 dra.), The drug is discontinued for 7 days, in this period the withdrawal bleeding usually occurs in those treated with the preserved reproductive system. In women undergoing cyclic or continuous sequential HRT treatment, treatment should be started the day after the end of the previous treatment cycle (28 days). If you do not take one tablet, you should skip it. If starting or continuing treatment of postmenopausal symptoms, the lowest effective dose should be used for the shortest possible time.
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