MIFREDNOR®10

Composition: Each tablet contains:
Mifepristone . . . . . . . . . . . . . . . . . . . . . . 10 mg
Presentation:
Box of 1 blister x 1 tablet.
Indications:
Mifrednor 10 is an emergency contraceptive pill, which is used within 120 hours after unprotected sexual intercourse.

Additional information

Dosage and administration

Oral administration.
One tablet MIFREDNOR 10 should be taken within 120 hours after unprotected sexual intercourse. However, the sooner the pill is taken, the more likely it is to be effective.

Contraindications

Adrenal failure.
Concurrent corticosteroid therapy.
A history of allergy to mifepristone.
Pregnant women or woman suspecting to be pregnant.
Breastfeeding.

Warnings and precautions for use

MIFREDNOR 10 cannot replace regular contraceptive methods.
Unprotected intercourse after treatment will increase the risk of unintended pregnancy.

Recommendation for pregnancy and breastfeeding

Pregnancy: Mifrednor 10 should not be used in pregnant women. Women who use this method to induce abortion should be warned in advance that if this method fails, in other words, pregnancy is still present, there is a risk of having a baby with fetal malformations. Therefore, if this method fails, it is necessary to seek medical advice to terminate the pregnancy.
Lactation: To date, no data are available to prove or rebut the opinion that mifepristone is excreted in breastmilk. However, for breastfed infant’s safety, it is recommended that the mothers discontinue breastfeeding for 3 to 4 days after mifepristone administration.

Effects on ability to drive and use machines

No studies on the effect of mifepristone on the ability to drive and use machines have been performed.

Interactions, incompatibilities of medicine

Ketoconazole, itraconazole, erythromycin, and grapefruit juice may inhibit mifepristone metabolism (increasing serum levels of mifepristone).
Rifampicin, dexamethasone, St. John’s Wort and certain anticonvulsants (phenytoin, phenobarbital, carbamazepine) may increase mifepristone metabolism (lowering serum levels of mifepristone).
A decrease of the efficacy of the method can occur due to the antiprostaglandin properties of non-steroidal anti-inflammatory drugs (NSAIDs) including aspirin (acetyl salicylic acid) if they are used concomitantly with mifepristone.

Undesirable effects (ADRs)

Besides late period, side effects are mild and rarely occur. Common side effects include hemorrhage (19%), nausea (14%), vomiting (1%), diarrhea (5%), lower abdominal pain (14%), fatigue (15%), headache (10%), dizziness (9%), breast tenderness (8%).
More than 50% and 9% of women had delayed period for about 2 days and 7 days, respectively, compared with expected.
Inform your doctor if any of the side effects occur when using the drug.

Overdose and management

Clinical trials have shown that no side effects occur with a single dose of up to 2 g of mifepristone. If acute poisoning occurs, patients should be hospitalized for monitoring and special treatment.

Pharmacodynamic properties

Properties:
– Mifepristone is an antiprogestin.
– Contraception is an action happening before a fertilized ovum nests. The mode of action of emergency contraception with mifepristone includes two mechanisms: Inhibition of ovulation and prevention of endometrial maturation. The most important effect is to delay ovulation by disrupting the follicular development and the endocrine function of granulosa cells, inhibiting mid-cycle surge of LH. It also works on the endometrium if used after ovulation and could affect the nesting. Additionally, degradation of corpus luteum occurs in 50% of women, which makes endometrium easily to be shed. Mechanism of action:
Mifepristone acts as a progesterone antagonist by competing with endogenous progesterone for binding to their respective receptors. Mifepristone has high affinity for the progesterone receptor (2-10 times higher than that of progesterone).
Mifepristone inhibits the effects of progesterone on the endometrium and peritoneum. This leads to degeneration and shedding of endometrial layers, thus prevents or disrupts the embryo's attachment to the uterus.

Pharmacokinetic properties

The bioavailability of mifepristone is about 70% after oral administration. Peak plasma concentrations occur within 1 to 2 hours after a single dose. Half time is about 20 to 30 hours. The unbound mifepristone is rapidly metabolized in the liver by demethylation and the metabolites are found in plasma about 1 hour after ingestion. Mifepristone and its metabolites are mainly excreted in feces through the biliary tract and small amount by the kidneys.

Storage conditions, shelf-life, quality specification of the medicine

Storage conditions: Protect from humidity and light, below 30 degrees C.
Shelf – life: 36 months from the manufacture date.
Quality specification: In house specification.