Genale, 10 mg tablets

Genale is an anti-gestagenic, contraceptive.

Pharmacodynamics

Mifepristone is a synthetic steroidal anti-gestagenic agent (blocks the effect of progesterone at the receptor level), it has no gestagenic activity. Antagonism with GCS has been noted (due to competition at the level of receptor binding).

Depending on a phase of a menstrual cycle it causes increase of contractility of myometrium, stimulating release of interleukin-8 in choriodeecidual cells, increasing sensitivity of myometrium to PG. The drug results in desquamation of the decidual membrane and expulsion of the fetal egg. Causes inhibition of ovulation, changes in the endometrium and prevents implantation of the fertilized egg.

Pharmacokinetics

After a single oral administration, C_max is reached after 1.3 h. Absolute bioavailability is 69%. In blood plasma mifepristone is 98% bound to proteins: albumin and acidic α₁-glycoprotein.

After the distribution phase, excretion is slow at first, with concentrations decreasing by a factor of 2 between 12-72 h, then more rapidly. T_1/2 is 18 h.

Indications

Contraception

Emergency (post-coital) contraception within 72 hours of intercourse without previous use of contraceptives or methods, as well as when they have failed (including errors in using the calendar method, failed termination of sexual intercourse, condom breakage or slippage).

Active ingredient

Mifepristone

Composition

Active ingredient:

Mifepristone10 mg;

Ancillary substances:

Lactose monohydrate – 123.4 mg;

Potato starch – 22 mg;

povidone K25 – 6 mg;

sodium carboxymethyl starch (primogel) – 5 mg;

magnesium stearate – 1.6 mg

How to take, the dosage

Intentionally. 1 tablet 2 hours before or 2 hours after a meal (within 72 hours after unprotected intercourse), regardless of the phase of the menstrual cycle.

Interaction

The use of NSAIDs should be avoided for 8-12 days after taking the drug.

Special Instructions

The product does not protect against sexually transmitted diseases and AIDS; it is not recommended to use the product as routine, ongoing contraception after every sexual intercourse or monthly.

After use as postcoital contraception and until the end of the current menstrual cycle, subsequent sexual intercourse without the use of contraceptives is not recommended. For further sexual intercourse a barrier method of contraception should be used.

The dose of 10 mg is insufficient to cause an abortion, so a high-sensitivity pregnancy test should be performed before further use to ensure that the drug is used only if there is no pregnancy. If a pregnancy occurs despite the use of the drug, medical or surgical termination is recommended. If a patient chooses to remain pregnant, the risk to the health of the unborn child cannot be completely ruled out.

The effect on the ability to drive a car or perform work requiring increased speed of physical and mental reactions. No effect of the drug on the ability to drive and operate machinery has been noted.

Contraindications

• having a history of hypersensitivity to mifepristone and/or its adjuvant components;
• adrenal insufficiency;
• acute or chronic renal and/or hepatic insufficiency;
• prolonged therapy with glucocorticosteroids;
• porphyria;
• anemia;
• haemostasis disorders (including prior anticonvulsant treatment.
• past treatment with anticoagulants;
• present severe extragenital pathology;
• pregnancy;
• lactation period.

Side effects

bloody discharge from the genital tract, discomfort and pain in the lower abdomen; exacerbation of inflammatory diseases of the uterus and appendages; weakness, headache, nausea, vomiting, diarrhea, dizziness, hyperthermia, urticaria.

Overdose

Symptoms: adrenal insufficiency may occur in cases of drug overdose.