Included in the formulation
АТХ:G.03.X.B.01 Mifepristone
Pharmacodynamics:The drug is a steroidal anti-gestagenic drug that blocks the effects of progesterone at the level of gestagen receptors. Antagonism with glucocorticosteroids is noted (due to competition at the level of communication with receptors). Increases the contractile activity of the myometrium (depending on the phase of the menstrual cycle), stimulating the release of interleukin-8 in choroid decidium cells, increasing the sensitivity of the myometrium to prostaglandins (to enhance the effect used in conjunction with the synthetic analogue of prostaglandin);resulting in desquamation of the decidua and excretion of the fetal egg. Promotes inhibition of ovulation.
Pharmacokinetics:Bioavailability is 69%. The drug binds to plasma proteins by 98%, advantageously with α1acid glycoprotein. It is metabolized in the liver by the cytochrome CYP3A4 isoenzyme. The half-life (terminal phase) is 18 hours, is eliminated by the gastrointestinal tract by 83%, by the kidneys by 9%.
Indications:- emergency postcoital contraception;
- interruption of uterine pregnancy in the early stages;
- Lymomyoma of the uterus.
II.D10-D36.D25 Leiomyoma of the uterus
XV.O00-O08.O04 Medical abortion
XV.O60-O75.O62.2 Other types of weakness in labor
XXI.Z30-Z39.Z30.0 General advice and advice on contraception
Contraindications:- severe gestosis;
- premature or premature pregnancy;
- ovarian tumors;
- inflammatory diseases of female genital organs;
- large sizes of leiomyoma (more than 12 weeks of pregnancy);
- lactation;
- pregnancy (in the treatment of leiomyoma);
- submucous location of myoma nodes;
- eclampsia;
- endometrial hyperplasia.
Carefully:Smoking in women over 35 years of age, anemia, hemostasis disorders, chronic kidney / liver diseases, insulin-dependent diabetes mellitus, hypocoagulation.
Chronic obstructive pulmonary diseases, bronchial asthma, arterial hypertension, arrhythmias, chronic heart failure, heart rhythm disturbances.
Pregnancy and lactation:Category FDA - X. Applied for the purpose of interrupting uterine pregnancy. There are no other indications for mifepristone during pregnancy. If it is necessary to administer mifepristone, breastfeeding should be stopped for 14 days.
The use of mifepristone to prepare the cervix for delivery does not affect subsequent lactation.
Dosing and Administration:For abortion: once 600 mg. Then the patient should be under medical supervision for 2 weeks.
For the purpose of contraception: 10 mg orally for 72 hours after unprotected intercourse, regardless of the phase of the menstrual cycle.
For the preparation and induction of labor: once 200 mg, re-reception after 24 hours.
For the treatment of uterine leiomyoma: once 50 mg. Treatment for 3 months.
Side effects:From the digestive system: nausea, vomiting, diarrhea.
From the side of the central nervous system: dizziness, headache.
On the part of the reproductive system: bleeding from the genital tract, menstrual disorders, amenorrhea, acute inflammation of the uterus and appendages, lohiometra, uterine subinvoljutcija.
Allergic reactions: hives.
Other: a feeling of discomfort and pain in the lower abdomen, weakness, hyperthermia.
Overdose:Acute adrenal insufficiency. Treatment is symptomatic. There is no specific antidote.
Interaction:Do not combine with non-steroidal anti-inflammatory drugs.
Anticoagulants - possibly excessive bleeding.
Glucocorticoids (long-term), inducers of cytochrome P450 (carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampicin, Drugs Hypericum perforatum) - despite the absence of these observations, it is possible induction of metabolism of mifepristone with a decrease in its plasma concentrations.
Inhibitors of cytochrome P450 (erythromycin, grapefruit juice, itraconazole, ketoconazole) - despite the absence of the described observations, it is possible to suppress the metabolism of mifepristone with an increase in its concentration in the blood plasma.
Special instructions:If a patient has an infective endocarditis or an artificial heart valve, antibiotic prophylaxis should be given.
When using the drug as an emergency postcoital contraception, the methods of barrier contraception should be used until the end of the current menstrual cycle.
It is not recommended for regular use as a planned continuous contraceptive.