Ovestin - instructions for use, dose, side effects, contraindications

Excipients: silicon dioxide colloid 0.75 mg, potato starch 10.0 mg, magnesium stearate 0.50 mg, povidone 1.0 mg, lactose monohydrate up to 100.0 mg (about 87.75 mg), distilled water q.s.*

* - Removed during production.

Description:White round flat tablets with bevel, engraved DG over 8, between which there is a risk on one side and ORGANON* - on the other side.

Pharmacotherapeutic group:Estrogen

ATX: & nbsp

G.03.C.A Natural and semi-synthetic estrogens

G.03.C.A.04 Estriol

Pharmacodynamics:

Ovestin® contains a natural female sex hormone estriol. In the period preceding menopause and in postmenopause (natural or surgical), estriol are 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 epithelium of the vagina and cervix, stimulates its blood supply, helps restore the epithelium, normal microflora and physiological pH of the vaginal environment, affects 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, since it is briefly retained in the nuclei of endometrial cells and, following the recommended dosage regimen, proliferation of the endometrium should not be expected. In this regard, the cyclic use of progestogens is not necessary, postmenopausal bleeding cancellations do not occur.

Pharmacokinetics:

After oral administration estriol quickly and almost completely absorbed in the gastrointestinal tract. The maximum concentration of unconjugated estriol in plasma is reached within 1 hourafter administration. About 90% of estriol binds to plasma albumin and, unlike other estrogens estriol almost does not bind to sex hormone binding globulin (SHGG).

Metabolism of estriol consists mainly of conjugation and deconjugation during intestinal hepatic circulation.

Estriol, the end product of metabolism, is excreted mainly with urine in a conjugated form. Only a small part (± 2%) is excreted with feces, mainly in the form of unconjugated estriol.

Indications:

- Atrophy of the lower urinary tract mucosa due to estrogen deficiency, in particular, for the treatment of symptoms such as dyspareunia, dryness and itching of the vagina; to prevent recurrent vaginal and lower genital tract infections; for the treatment of urinary disorders (eg, frequency, dysuria) and moderate incontinence;

- Pre and postoperative treatment for vaginal operations in the postmenopausal period;

- Menopausal disorders, such as "hot flashes" and night sweats;

- As a diagnostic aid in obtaining an atrophic pattern of a cervical smear;

Infertility due to the cervical factor.

Contraindications:

- Pregnancy, lactation;

- Hypersensitivity to the active and / or excipients of the drug;

- Detected 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 two years;

- Venous thromboembolism in history or thrombosis if anticoagulant therapy is not performed;

- Diabetes mellitus with angiopathy;

- Sickle-cell anemia;

- Syndrome Dubin-Johnson;

- Violation of cerebral circulation;

- Rotor Syndrome.

Carefully:

- Family hyperlipoproteinemia;

- Increased risk of thromboembolic complications;

- Systemic lupus erythematosus;

- Long-term immobilization, serious surgical interventions;

- Severe liver disease;

- Diseases of the gallbladder in history (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.

Dosing and Administration:

The drug is administered orally. The daily dose for oral intake should not exceed 8 mg.

With atrophy of the lower sections of the genito-urinary tract caused by estrogen deficiency 4-8 mg per 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 per day.

Pre and postoperative treatment for vaginal operations in the postmenopausal period: 4-8 mg per day for 2 weeks before the operation, 1-2 mg per day for 2 weeks after the operation.

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.

With infertility due to the cervical factor: as a rule, appoint 1-2 mg per day from 6 to 15 days of the menstrual cycle. However, in different patients, the daily dose can vary from 1 to 8 mg.The dose should be increased every month until the optimal effect is achieved on the cervical mucosa.

If a woman missed taking the next dose, and the delay was no more than 12 hours, you must accept it as soon as possible. If the delay was more than 12 hours, you should skip one appointment 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 one step.

Side effects:

Tenderness and tension of the mammary glands, jaundice, nausea, skin rash, increased blood pressure, headache, intermenstrual bleeding spotting from the vagina, cervical hypersecretion.

Adverse reactions are usually transient, but may also indicate an overdose of the drug.

Overdose:

Overdose causes nausea, vomiting, and vaginal bleeding.

Treatment symptomatic.

Interaction:

There were no reported cases of interaction of Ovestin ® with other drugs. At the same time, there are data on the enhancement of the pharmacological effect of glucocorticosteroids,lipid-lowering drugs when combined with estrogens. If necessary, the dose of glucocorticosteroids can be reduced.

Possible weakening effects of drugs male sex hormones, anticoagulants, antidepressants, diuretic, hypotensive and hypoglycemic drugs.

Barbiturates, antiepileptic medicines (carbamazepine, phenytoin) increase the metabolism of steroid hormones.

Antibiotics (ampicillin, rifampicin), medicines for general anesthesia, narcotic analgesics, anxiolytics, antiepileptic medicines, certain antihypertensive drugs, ethanol reduce the effectiveness of estrogens.

Folic acid and preparations of thyroid hormones increase the effect of estriol.

Estriol can change the effectiveness of oral anticoagulants, increase the pharmacological effect of succinicholine, theophylline, and foleandomicin.

Special instructions:

Before starting hormone replacement therapy, a full medical examination is necessary. During treatment every 6 months, regular examinations (including mammary examinations, 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 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 in the "Contraindications" section.

Form release / dosage:

Tablets, 2 mg.

Packaging:

30 tablets per blister of PVC / Al.

For 1 blister is placed in a pack of cardboard along with instructions for use.

Storage conditions:

At a temperature of 2 to 30 ° C in a dry, dark place.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N013327 / 03

Date of registration:02.04.2010 / 04.12.2014

Expiration Date:Unlimited

The owner of the registration certificate:Aspen Pharma Trading LimitedAspen Pharma Trading Limited

Manufacturer: & nbsp

ORGANON, N.V. Netherlands

Representation: & nbspAspen Hells Ltd.Aspen Hells Ltd.

Information update date: & nbsp21.05.2017

Illustrated instructions

Instructions

Ovestin® (Ovestin®)