Gynestril, pills 50mg 30pcs

Composition

Active ingredients:

mifepristone 50 mg

Excipients: microcrystalline cellulose, sodium carboxymethyl starch, talc, calcium stearate.

Pharmacological action

Pharmaco-therapeutic group: Antigestagen

Pharmacological action

Gynestril® is a synthetic steroid anti-gestational drug (blocks the action of progesterone at the receptor level), has no progestogenic activity. Antagonism with glucocorticoids was noted (due to competition at the level of communication with receptors).

Sex hormones, especially progesterone, play a key role in the pathogenesis of uterine leiomyoma. The use of mifepristone as a progesterone receptor blocker can help both inhibit tumor growth and reduce the size of myomatous nodes and uterus.

Pharmacokinetics

Suction. After use, Cmax is reached in 1.3 hours. Bioavailability is 69%.

Distribution and metabolism. The binding of mifepristone to plasma proteins, albumin and acid alpha-1-glycoprotein, is 98%. It is metabolized with the participation of the CYP3A4 isoenzyme by demethylation and hydroxylation to form three active metabolites.

Output. After the distribution phase, excretion is first slow, the concentration decreases by a factor of 2 between 12-72 hours, then more rapidly with T1/2 18 hours. Terminal T1 / 2 (including for all active metabolites) reaches 90 hours. It is mainly excreted through the intestines (about 90%).

Indications

Treatment of uterine leiomyoma (up to 12 weeks of gestation).

Use during pregnancy and lactation

The drug Gynestril® is contraindicated for use during pregnancy and lactation.

Contraindications

* hypersensitivity to the components of the drug;• pregnancy;• breast-feeding period;• adrenal insufficiency• * long-term therapy with corticosteroids• * acute or chronic renal failure;• acute or chronic liver failure; * porphyria• * hemostatic disorders (including previous treatment with anticoagulants)• * inflammatory diseases of the female genital organs;• severe extragenital pathology• * submucous location of myomatous nodes;• uterine leiomyoma exceeding 12 weeks of gestation;• ovarian tumors;• endometrial hyperplasia.

With caution: Chronic obstructive pulmonary diseases (including bronchial asthma), severe arterial hypertension, cardiac arrhythmias, and chronic heart failure.

Side effects

According to the WHO grading of the frequency of adverse reactions “frequency unknown” – according to the available data, it is not possible to determine the frequency of occurrence of an adverse reaction.

From the reproductive system: frequency unknown – menstrual disorders, amenorrhea, oligomenorrhea, discomfort and pain in the lower abdomen, simple endometrial hyperplasia (reversible after discontinuation of the drug).

From the digestive system: frequency unknown-nausea, vomiting, diarrhea.

Allergic reactions: frequency unknown-pruritus, urticaria.

Other: frequency unknown-headache, dizziness, hyperthermia, weakness.

Interaction

Given that the CYP3A4 isoenzyme participates in the metabolism of mifepristone, it is possible that when used simultaneously, inhibitors of this isoenzyme (ketoconazole, itraconazole, erythromycin, grapefruit juice) may increase, and inducers (rifampicin, dexamethasone, St. John’s wort preparations, phenytoin, phenobarbital, carbamazepine) may decrease the concentration of mifepristone in blood plasma. Caution should be exercised when using mifepristone concomitantly with drugs that are substrates of CYP3A4 and have a narrow therapeutic range (including drugs for general anesthesia), in view of the possible increase in the concentration of these drugs in blood plasma.

Concomitant use of mifepristone and NSAIDs may increase the concentration of the latter in blood plasma; if necessary, simultaneous use should be used NSAIDs in the lowest recommended dose.

Mifepristone may reduce the effectiveness of long-term corticosteroids, including inhaled corticosteroids in patients with asthma, which may require dose adjustment.

How to take, course of use and dosage

Inside at a dose of 50 mg 1 time/day. The course of treatment is 3 months.

Overdose

Symptoms: taking mifepristone in doses up to 2 g does not cause adverse reactions. In cases of overdose of the drug, adrenal insufficiency may occur.

Treatment: symptomatic. If acute adrenal insufficiency is suspected, dexamethasone is recommended (1 mg of dexamethasone is counteracted by 400 mg of mifepristone).

Description

Tablets from light yellow to light yellow with a greenish tinge, flat-cylindrical, with a chamfer.

Special instructions

Patients with artificial heart valves or infectious endocarditis should be treated with prophylactic antibiotics when using Gynestril®.

Influence on the ability to drive vehicles and mechanisms

There is no evidence that the drug may affect the ability to drive a car or other mechanisms. However, when using mifepristone, dizziness may develop. If this side effect develops, you should refrain from driving vehicles and mechanisms.

It is contraindicated in acute or chronic liver failure.

It is contraindicated in acute or chronic renal failure.

Storage conditions

The drug should be stored out of the reach of children, dry, protected from light at a temperature not exceeding 30°C.

Expiration date

Shelf life – 5 years.

Active ingredient

Mifepristone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For women