Expiration date: 07/2025
Clinico-pharmacological group
(Postcoital contraceptive. Gestagen)
(Antigestagens drug)
Release form, composition and packing
Tablets are light yellow with greenish hue color, round, biconcave.
Excipients: lactose monohydrate - 123.4 mg Potato starch - 22 mg, povidone K25 - 6 mg Sodium carboxymethyl starch - 5 mg magnesium stearate - 1.6 mg.
Pharmachologic effect
Antiprogestagenny synthetic steroid drug. Blocks deystvieprogesterona at the receptor level, progestin activity is not. Marked antagonism with corticosteroids due to competition on the level of communication with the receptors.
Depending on the phase of the menstrual cycle causes an increase in contractility of the myometrium stimulating the release of IL-8 in horiodetsidualnyh cells, increasing the sensitivity of the myometrium to prostaglandins. As a result of the drug takes place decidua desquamation and removal of the ovum. It causes ovulation inhibition of endometrial change and prevents implantation of a fertilized egg.
Pharmacokinetics
Absorption and distribution
After a single oral Cmax achieved after 1.3 hours. The absolute bioavailability is 69%. In plasma mifepristone is 98% bound to proteins: albumin and ?1-acid glycoprotein.
breeding
After removing first phase distribution is slow, decreases the concentration of 2-fold between 12-72 hours, and then more quickly. T1 / 2 is 18 h.
Dosage
It should take 1 tablet. inside for 2 hours before or 2 hours after meals (within the next 72 hours after the unprotected coitus contraception), regardless of the phases of the menstrual cycle.
Overdose
In cases of overdose adrenal insufficiency may occur.
Drug interactions
NSAIDs should be avoided for 8-12 days after ingestion.
Pregnancy and lactation
The drug should not be used during pregnancy. Breastfeeding should be discontinued for 14 days after dosing.
Side effects
From the reproductive system: bleeding from the genital tract, discomfort and abdominal pain, exacerbation of inflammatory diseases of the uterus and appendages.
From the digestive system: nausea, vomiting, diarrhea.
CNS: headache, dizziness.
Other: fatigue, pyrexia, rash.
Terms and Conditions of storage
The drug should be stored in a dry, dark, place inaccessible to children at temperature not above 25 ° C. Shelf life - 3 years.
Testimony
- Emergency (postcoital) contraception within 72 hours after sexual intercourse without the prior use of contraceptives or methods, as well as the failure of the application (including an error in applying the calendar method, the unsuccessful coitus interruptus, the condom breaking or slipping).
Contraindications
- Acute or chronic renal and / or hepatic insufficiency,
- Chronic treatment with glucocorticosteroid agents
- Porphyria
- Anemia,
- Hemostasis disorders (including previous treatment with anticoagulants)
- Presence of severe extragenital pathology,
- Adrenal insufficiency,
- Pregnancy,
- Lactation,
- A history of hypersensitivity to mifepristone and / or auxiliary components.
Special instructions
The drug does not protect against sexually transmitted diseases and AIDS through.
It is not recommended to use the drug as planned, permanent contraception after each sexual intercourse, as well as monthly.
After use as a post-coital contraception and the end of the menstrual cycle is not recommended for subsequent sexual intercourse without the use of contraceptives. In further sexual acts should use a barrier method of contraception.
Dose of 10 mg is insufficient to cause an abortion, so to further its application should be held highly sensitive pregnancy test, ensuring that the drug is used only in the absence of pregnancy. In the case of pregnancy, despite the use of the drug, it is recommended to interrupt medication or surgically. If the patient decides to continue the pregnancy, it is impossible to completely eliminate the risk to the health of the unborn child.
Effects on ability to drive vehicles and management mechanisms
Effect on ability to drive and operate with mechanisms were observed.
