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Active ingredients
Estriol
Release form
Pills
Composition
Estriol 2 mg; Excipients: silica, colloidal anhydrous dioxide, potato starch, magnesium stearate, povidone, lactose monohydrate.
Pharmacological effect
Estrogenic drug. Estriol is a natural estrogen. In the period preceding menopause and in postmenopausal (natural or surgical), estriol is used to treat symptoms caused by estrogen deficiency. Estriol has a selective effect mainly on the cervix, vagina, vulva and is particularly effective for the treatment of urogenital symptoms caused by estrogen deficiency. In cases of atrophy of the mucous membrane of the vagina, estriol causes increased proliferation of the epithelium of the vagina and cervix, stimulates its blood supply, contributes to the restoration of the epithelium, normal microflora and physiological vaginal environment, affects the quality and amount of cervical mucus. As a result, the resistance of epithelial cells to infection and inflammation is increased .; Unlike other estrogens, estriol has a short-term effect, since it lingers in the nuclei of the endometrium for a short time, and if the recommended dosing regimen is observed, the proliferation of the endometrium should not be expected. In this regard, the cyclic use of progestogens is not necessary, postmenopausal withdrawal bleeding does not occur.
Pharmacokinetics
Absorption; When using the drug inside, as well as topically estriol is quickly and almost completely absorbed .; C max estriol in plasma is achieved within 1 h after ingestion and 1-2 h after intravaginal application. Values of C max estriol in plasma after intravaginal use is higher than after taking the drug inside. Distribution; Plasma albumin binding is 90%; The removal of estriol (in bound form) is carried out mainly by the kidneys; about 2% is excreted unchanged through the intestines. Excretion of metabolites with urine begins within a few hours after the use of the drug and lasts 18 hours.
Indications
- Atrophy of the mucous membrane of the lower urogenital tract, caused by estrogen deficiency, in particular, for the treatment of symptoms such as dyspareunia,vaginal dryness and itching to prevent recurrent infections of the vagina and lower urinary tract; for the treatment of urinary disorders (eg, increased frequency, dysuria) and moderate urinary incontinence; - pre- and postoperative treatment of women in the postmenopausal period; - menopausal disorders (hot flashes and night sweats); - infertility caused by cervical factors.
Contraindications
- identified or suspected estrogen-dependent tumors (breast cancer, endometrial cancer); - vaginal bleeding of unknown etiology; - confirmed venous thromboembolism (deep vein thrombosis, pulmonary thromboembolism) in the last 2 years; - history of venous thromboembolism or thrombosis, if anticoagulant therapy is not performed; - diabetes mellitus with angiopathy; - sickle cell anemia; - Dubin-Johnson syndrome; - Rotor syndrome; - violation of cerebral circulation; - pregnancy; - lactation period (breastfeeding); - hypersensitivity to the active and / or auxiliary substances of the drug .; Precautions should be prescribed the drug in the following conditions: - Familial hyperlipoproteinemia; - increased risk of thromboembolic complications; - Systemic lupus erythematosus; - long immobilization, serious surgical interventions; - severe liver disease; - a history of gallbladder disease (especially cholelithiasis); - hepatic porphyria; - severe itching or cholestatic jaundice (including in history during previous pregnancy); - pancreatitis; - endometriosis; - leiomyoma; - bronchial asthma; - arterial hypertension; - hypercalcemia due to bone metastasis of breast cancer; - herpes pregnant; - epilepsy; - otosclerosis.
Use during pregnancy and lactation
Ovestin is contraindicated for use during pregnancy and lactation (breastfeeding).
Dosage and administration
The drug is used inside. The daily dose should not exceed 8 mg. For atrophy of the lower urogenital tract due to estrogen deficiency, 4-8 mg / day is prescribed for the first 4 weeks, followed by a gradual decrease in dose in accordance with the symptoms until a maintenance dose of 1-2 mg / day is reached; With pre- and postoperative treatment during operations on the vagina in the post-menopausal period - 4-8 mg / day for 2 weeks before surgery, 1-2 mg / day for 2 weeks after surgery .; In the treatment of menopausal disorders (hot flashes,night sweats) - 4-8 mg for a week with a gradual decrease in dose. A minimum effective dose should be used for maintenance therapy. For infertility due to cervical factor, as a rule, 1-2 mg / day are prescribed from the 6th to the 15th day of the menstrual cycle. However, in different patients, the daily dose may vary from 1 mg to 8 mg. The dose should be increased each month to achieve the optimal effect on the mucous membrane of the cervix .; If a woman missed the next dose, and the delay was no more than 12 hours, you must take a pill as soon as possible. If the delay is more than 12 hours, you should skip one dose and then take the drug at the usual time .; Tablets are taken with water, preferably at the same time of day. The daily dose should be taken in 1 reception.
Side effects
On the part of the reproductive system: intermenstrual bloody spotting from the vagina, cervical hypersecretion .; Other: pain and tension of the mammary glands, jaundice, nausea, skin rash, increased blood pressure, headache .; Adverse reactions are usually transient in nature, but may also indicate an overdose of the drug.
Overdose
Symptoms: nausea, vomiting, vaginal bleeding .; Treatment: conduct symptomatic therapy.
Interaction with other drugs
There were no cases of drug interactions with Ovestin other drugs .; There are data on the enhancement of the pharmacological effect of corticosteroids, lipid-lowering agents when used together with estrogen. If necessary, the dose of corticosteroids can be reduced .; Possible weakening of the effects of drugs of male sex hormones, anticoagulants, antidepressants, diuretics, hypotensive and hypoglycemic agents .; Barbiturates, antiepileptic drugs (carbamazepine, phenytoin) increase the metabolism of steroid hormones .; Antibiotics (ampicillin, rifampicin), general anesthesia agents, opioid analgesics, anxiolytics, antiepileptic drugs, some antihypertensive drugs, ethanol reduce the effectiveness of estrogens .; Folic acid and thyroid hormone drugs increase the effect of estriol .; Estriol may alter the effectiveness of oral anticoagulants .; Estriol can increase the pharmacological effect of succiniccholine, theophylline, foleandomycin.
special instructions
Before starting hormone replacement therapy, a full medical examination is necessary .; During treatment, every 6 months, regular examinations should be carried out (including breast examinations, mammography) in accordance with accepted medical practice .; It is necessary to exclude the presence in the history of thromboembolism, repeated spontaneous abortions, which indicates thrombophilia. The risk of thromboembolism increases with prolonged immobilization, severe injuries and surgical interventions. In these cases, it is necessary to temporarily interrupt the hormone replacement therapy (4-6 weeks before the operation); The use of estriol does not lead to an increase in the density of the breast. And perhaps the use of estriol does not increase the risk of developing breast cancer .; Cases of venous thromboembolism (deep vein thrombosis of the lower leg, pelvic vein thrombosis and pulmonary thromboembolism) are more common in women receiving hormone replacement therapy. With regard to the drug Ovestin such data are not available, so it is not known whether its use causes an increase in the incidence of venous thromboembolism. However, it is recommended that you follow the directions given in the "Contraindications" section.