Composition, form of production and packaging
Tablets are white, round, flat, with bevelled edge, labeled "DG" above the figure "8" and the dividing line between them on one side of the tablet and "ORGANON *" - on the other.
1 tab.
Estriol 2 mg
Excipients: silicon dioxide colloidal anhydrous, potato starch, magnesium stearate, povidone, lactose monohydrate.
30 pcs. - blisters (1) - cardboard boxes.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
An estrogen preparation. 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 especially effective for the treatment of urogenital symptoms caused by estrogen deficiency. In cases of atrophy of the vaginal mucosa, estriol causes an increase in the proliferation of the vaginal and cervical epithelium, stimulates its blood supply, promotes the recovery of the epithelium, normal microflora and physiological vaginal environment, influences the quality and quantity of cervical mucus. As a result, the resistance of epithelial cells to infection and inflammation increases.
Unlike other estrogens, estriol has a short-term effect, as it is briefly retained in the nuclei of endometrial cells, and when the recommended dosage regimen is followed, proliferation of the endometrium should not be expected. In this regard, cyclic use of progestogens is not necessary, postmenopausal bleeding cancellations do not occur.
PHARMACOKINETICS
Suction
When the drug is administered orally, as well as topically, estriol is rapidly and almost completely absorbed.
C max estriol in plasma is achieved 1 h after ingestion and 1-2 h after intravaginal application. The C max values ​​of estriol in plasma after intravaginal application are higher than after oral administration of the drug.
Distribution
The binding with albumin plasma is 90%.
Excretion
The excretion of estriol (in a bound form) is carried out mainly by the kidneys; about 2% is excreted through the intestine in an unchanged form. Excretion of metabolites with urine begins within a few hours after application of the drug and lasts 18 hours.
INDICATIONS
- atrophy of the mucous membrane of the lower sections of the urinary tract, caused by estrogen deficiency, in particular, for the treatment of symptoms such as dyspareunia, dryness and itching of the vagina, to prevent recurrent infections of the vagina and lower urinary tract; for the treatment of urinary disorders (eg, frequency, dysuria) and moderate incontinence;
- pre- and post-operative treatment of women in the postmenopausal period;
- climacteric disorders (hot flashes and night sweats);
- infertility caused by a cervical factor.
DOSING MODE
The drug is administered orally. The daily dose should not exceed 8 mg.
When atrophy of the lower urinary tract due to estrogen deficiency is prescribed 4-8 mg / day 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.
At pre-and post-operative treatment for operations on the vagina in the postmenopausal period - 4-8 mg / day for 2 weeks before the operation, 1-2 mg / day - for 2 weeks after the operation.
In the treatment of climacteric disorders (hot flashes, night sweats) - 4-8 mg during the week with a gradual decrease in dose. For maintenance therapy, the minimum effective dose should be used.
Infertility due to the cervical factor, usually prescribed 1-2 mg / day from the 6th to the 15th day of the menstrual cycle. However, in different patients, the daily dose can vary from 1 mg to 8 mg. The dose should be increased every month until the optimal effect is achieved on the mucous membrane of the cervix.
If the woman missed taking the next dose, and the delay was no more than 12 hours, it is necessary to take the pill as soon as possible. If the delay was more than 12 hours, you should skip one dose and continue taking 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 dose.
SIDE EFFECT
On the part of the reproductive system: intermenstrual bloody spotting discharge from the vagina, cervical hypersecretion.
Other: soreness and tension of mammary glands, jaundice, nausea, skin rash, increased blood pressure, headache.
Adverse reactions are usually transient, but may also indicate an overdose of the drug.
CONTRAINDICATIONS
- identified or suspected estrogen-dependent tumors (breast cancer, endometrial cancer);
vaginal bleeding of unclear etiology;
- confirmed venous thromboembolism (deep vein thrombosis, pulmonary thromboembolism) during the last 2 years;
- venous thromboembolism in history or thrombosis if anticoagulant therapy is not administered;
- Diabetes mellitus with angiopathy;
sickle cell anemia;
- Dubin-Johnson syndrome;
- Rotor syndrome;
- impaired cerebral circulation;
- Pregnancy;
- the period of lactation (breastfeeding);
- Hypersensitivity to the active and / or excipients of the drug.
Caution should be given to the drug under the following conditions:
- familial hyperlipoproteinemia;
- increased risk of thromboembolic complications;
- systemic lupus erythematosus;
- prolonged immobilization, serious surgical interventions;
- severe liver disease;
- Chronic gallbladder disease (especially cholelithiasis);
- hepatic porphyria;
- severe itching or cholestatic jaundice (including anamnesis during previous pregnancy);
- pancreatitis;
- endometriosis;
- Leiomyoma;
- bronchial asthma;
- arterial hypertension;
- hypercalcemia caused by bone metastases of breast cancer;
- Herpes pregnant women;
- epilepsy;
otosclerosis.
PREGNANCY AND LACTATION
Ovestin is contraindicated for use in pregnancy and lactation (breastfeeding).
SPECIAL INSTRUCTIONS
Before starting hormone replacement therapy, a full medical examination is necessary.
During treatment every 6 months, regular examinations (including breast examination, mammography) should be performed according to accepted medical practice.
It is necessary to exclude the presence in the anamnesis 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 hormone replacement therapy (4-6 weeks before surgery)
The use of estriol does not lead to an increase in the density of the breast. And perhaps the use of estriol does not lead to an increased risk of developing breast cancer.
Cases of venous thromboembolism (deep vein thrombosis of the lower leg, thrombosis of pelvic veins 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 unknown whether its use causes an increase in the incidence of venous thromboembolism. However, it is recommended that you follow the directions in the "Contraindications" section.
OVERDOSE
Symptoms: nausea, vomiting, vaginal bleeding.
Treatment: conduct symptomatic therapy.
DRUG INTERACTION
No cases of interaction of Ovestin with other drugs were noted.
There are known data on the enhancement of the pharmacological effect of GCS, hypolipidemic agents when combined with estrogens. If necessary, the dose of GCS can be reduced.
Possible weakening effects of drugs male sex hormones, anticoagulants, antidepressants, diuretic, hypotensive and hypoglycemic agents.
Barbiturates, antiepileptic drugs (carbamazepine, phenytoin) increase the metabolism of steroid hormones.
Antibiotics (ampicillin, rifampicin), means for general anesthesia, opioid analgesics, anxiolytics, antiepileptics, some antihypertensives, ethanol reduce the effectiveness of estrogens.
Folic acid and preparations of thyroid hormones increase the effect of estriol.
Estriol can alter the effectiveness of oral anticoagulants.
Estriol can increase the pharmacological effect of succinicholine, theophylline, and foleandomicin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a place protected from light and moisture and inaccessible to children at a temperature of 2 В° from 30 В° C. Shelf life - 5 years.
