Included in the formulation
АТХ:G.03.F.B.05 Norethisterone and estrogen
Pharmacodynamics:The pharmacological action is estrogen-progestational.
It replenishes the deficiency of endogenous hormones. Regulates the exchange of proteins, fats and carbohydrates, water-electrolyte balance, reduces the level of LDL and cholesterol in the blood; maintains the normal structure of bone tissue, improves mood, increases libido.
Pharmacokinetics:Estradiol. After oral administration, it is absorbed from the digestive tract. It is affected by the effect of the first passage through the liver. Metabolized to less active metabolites - estriol and estrone. Metabolites are excreted by the kidneys, a small part through the intestine.
After oral administration of norethisterone acetate is rapidly absorbed and converted into norethisterone. The time to reach the maximum concentration is 0.5-1.5 h, which is 3.9 ng / ml (1.4-6.8 ng / ml). Linkage with proteins: with albumin - 61%, globulins - 36%. The half-life is 8-11 hours.
Metabolised in the liver with the formation of 5-alpha-dihydro-norethisterone and tetrahydro-norethisterone, which are mainly excreted in the urine in the form of sulfate and glucuronide conjugates.
Indications:Estrogenic deficiency in the climacteric period, relief of menopausal symptoms, prevention of osteoporosis in menopause.
IV.E20-E35.E28.3 Primary ovarian failure
IV.E20-E35.E28 Dysfunction of the ovaries
XIII.M80-M85.M81.0 Postmenopausal osteoporosis
XIV.N80-N98.N95.1 Menopause and menopause in women
Contraindications:Hormone-dependent tumors (carcinoma of the breast or endometrium), acute or chronic liver disease (including history), deep vein thrombosis, thromboembolism, cerebral circulation disorders (including history), uterine bleeding of unclear etiology, hemoglobinopathy, porphyria.
Carefully:Assign with caution in hypertension, epilepsy, migraine, diabetes mellitus, bronchial asthma, heart failure (patients should be under the supervision of a doctor). The experience of treating women over the age of 65 is limited.
Pregnancy and lactation:Contraindicated in pregnancy and lactation.
Dosing and Administration:Tablets are intended for continuous combined hormone replacement therapy in women with an unrefined uterus. The drug is taken orally 1 tablet per day without interruption, preferably at the same time of day.
When treating the symptoms of postmenopause, the drug should be started and resumed at the lowest effective dose for short-term therapy.
If there is an insufficient response to therapy after three months, the transition to a higher-dose drug should be discussed.
Patients with amenorrhea who do not receive hormone replacement therapy or who take another combination drug in continuous mode can start taking the pills on any convenient day. When transferring patients from a cyclic regimen of hormone replacement therapy, treatment should be started immediately after the end of menstrual bleeding caused by withdrawal of the drug.
If you miss a regular tablet, the missed tablet should be taken as soon as possible within the next 12 hours. If the drug is delayed for more than 12 hours, the missed tablet should be discarded.Skipping the next dose can cause breakthrough uterine bleeding or the appearance of spotting spotting. Unused medication should be disposed of in accordance with local regulations.
Side effects:In the first months of treatment: soreness of the mammary glands, sporadically arising menstrual bleeding. Rarely - nausea, puffiness, headache. With the continuation of treatment, these phenomena pass independently and do not require cancellation.
Overdose:Overdose may cause nausea and vomiting.
Treatment: symptomatic.
Interaction:With the simultaneous use with inductors of microsomal enzymes, especially cytochrome P450 enzymes, such as anticonvulsants (for example, phenobarbital, phenytoin, carbamazepine) and anti-infective drugs (for example, rifampicin, rifabutin, nevirapine, efavirenz), it is possible to accelerate the metabolism of estrogens and progesterones. On the contrary, ritonavir and nelfinavir, although they are strong inhibitors, with simultaneous use with steroid hormones show inducing properties.
Phytopreparations, which include St. John's wort (Hypericum perforatum), can stimulate the metabolism of estrogens and progestogens.
Elevated metabolism of estrogens and progestogens can clinically be manifested by a decrease in the effect of the drug and a change in the character of uterine bleeding.
Medicinal products that inhibit the activity of microsomal liver enzymes, including ketoconazole, can increase the concentration of circulating components of the drug.
Special instructions:Apply only to women who have had the last menstrual cycle at least 1 year ago.
With long-term treatment, it is recommended to conduct preventive examinations at least once a year.
Estrogens better to appoint a course duration of not more than 1 year, if there is no regular gynecological examination and examination of the mammary glands. Before the beginning of treatment it is necessary to collect a family medical history and to conduct a thorough examination (gynecological, condition of mammary glands, blood pressure).
Admission should be stopped with deep vein thrombosis, thromboembolic disorders, with jaundice, increased migraine pain, sudden visual impairment, a significant increase in blood pressure, and also 4-6 weeks before the scheduled surgical operation.
The drug is not a contraceptive and does not protect against pregnancy.