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Active ingredients
Mifepristone
Release form
Pills
Composition
Mifepristone 50 mg; Auxiliary substances: microcrystalline cellulose - 66.1 mg, sodium carboxymethyl starch - 13.5 mg, talc - 4.05 mg, calcium stearate - 1.35 mg.
Pharmacological effect
Synthetic steroid anti-progestogen (blocking the action of progesterone at the receptor level), does not possess progestogen activity. Antagonism with glucocorticoids has been 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 contribute to both the inhibition of tumor growth and the reduction of the size of myomatous nodes and uterus.
Pharmacokinetics
Absorption; After taking Cmax achieved after 1.3 hours. Absolute bioavailability is 69%. Distribution and elimination; Binding of mifepristone to plasma proteins, albumin and acidic alpha 1-glycoprotein is 98%. T1 / 2 is 18 h. After the distribution phase, elimination at first it happens slowly, the concentration decreases by 2 times between 12-72 h, then more quickly.
Indications
- treatment of uterine leiomyoma (up to 12 weeks gestation).
Contraindications
- pregnancy; - lactation period; - adrenal insufficiency and long-term therapy of corticosteroids; - acute or chronic renal failure; - acute or chronic liver failure; - porphyria; - anemia; - violations of hemostasis (including previous treatment with anticoagulants); - inflammatory diseases of the female genital organs; - the presence of severe extragenital pathology; - submucous arrangement of myomatous nodes; - the value of uterine leiomyoma, exceeding in size 12 weeks of pregnancy; - ovarian tumors and / or endometrial hyperplasia; - hypersensitivity to the components of the drug.; With caution: in chronic obstructive pulmonary diseases (including bronchial asthma), severe hypertension, cardiac arrhythmias and heart failure.
Use during pregnancy and lactation
The drug is contraindicated during pregnancy and lactation (breastfeeding).
Dosage and administration
Assign orally at a dose of 50 mg 1 time / day.The course of treatment is 3 months.
Side effects
On the part of the reproductive system: menstrual disorders, amenorrhea, discomfort and pain in the lower abdomen. On the part of the digestive system: nausea, vomiting, diarrhea.; Other: headache, dizziness, hyperthermia, weakness, urticaria.
Overdose
Reception of Ginestril in doses up to 2 g does not cause undesirable reactions.; Symptoms: adrenal insufficiency is possible.; Treatment: conducting symptomatic therapy.
Interaction with other drugs
should be avoided the simultaneous use of NSAIDs.; When taken simultaneously with the GCS, the dose of the latter should be increased.
special instructions
Patients with artificial heart valves or infective endocarditis with the use of Ginestril should be given prophylactic antibiotics.