Gynepristone, 10 mg tablets

Gynepristone is a synthetic steroidal anti-gestagenic drug, (blocks the effect of progesterone at the receptor level), it has no gestagenic activity.

There is antagonism with glucocorticoids (due to competition at the level of receptor binding).

It increases the contractility of the myometrium by stimulating the release of interleukin-8 in the choriodeecidual cells and increasing the sensitivity of the myometrium to prostaglandins.

Depending on the phase of the menstrual cycle, it causes inhibition of ovulation, changes in the endometrium and prevents implantation of the fertilized egg.

Pharmacokinetics

Intake

After a single oral dose of 600 mg, Cmax is reached after 1.3 h and is 1.98 mg/L. Absolute bioavailability is 69%.

Distribution

The binding to plasma proteins (with albumin and acidic α1-glycoprotein) is 98%.

T1/2 – 18 h. Excretion occurs in two phases: first, slow excretion of the drug (mifepristone plasma concentration decreases 2-fold between 12-72 hours), followed by a fast excretion phase.

Indications

Emergency post-coital contraception (after unprotected intercourse or if the method used cannot be considered reliable).

Active ingredient

Composition

One tablet contains:

The active ingredient:

Mifepristone – 0.01 g;

Ancillary substances:

Microcrystalline cellulose – 0.0746 g,

Carboxymethyl starch

Sodium – 0.0045 g,

Calcium stearate – 0.0009 g.

How to take, the dosage

The drug is taken orally in a single dose of 10 mg (1 tablet) for 72 hours after unprotected intercourse.

In order to maintain the contraceptive effect, it is necessary to refrain from eating 2 hours before and 2 hours after taking the drug.

Gynepristone can be used during any phase of the menstrual cycle.

Interaction

The use of non-steroidal anti-inflammatory drugs should be avoided.

Special Instructions

Synopsis

Features

Contraindications

Side effects

Digestive system disorders: nausea, vomiting.

CNS disorders: dizziness, headache.

In the sexual system: bloody discharge from the reproductive tract, menstrual irregularities.

Allergic reactions: urticaria.

Others: feeling of discomfort in the abdomen, weakness, hyperthermia.

Overdose

Symptoms: possible adrenal insufficiency.

Treatment: symptomatic therapy.

Similarities