Mifestad 10

Mifestad 10

mifepristone

Nhà sản xuất:

Stellapharm J.V.

Nhà phân phối:

Khuong Duy
Thông tin kê toa chi tiết tiếng Anh
Contents
Mifepristone.
Description
Active ingredient: Mifepristone 10 mg.
Excipients/Inactive Ingredients:
Lactose monohydrate, maize starch, povidone K30, quinoline, magnesium stearate, croscarmellose sodium.
Action
Pharmacotherapeutic group: Other sex hormone and modulator of the reproductive function/antiprogestogen. ATC code: G03XB01.
Pharmacology: Pharmacodynamics: Mifepristone is a synthetic steroid, that acts as a progesterone antagonist by competing with endogenous progesterone for receptor binding. It binds with very high affinity (2 to 10 times that of progesterone) to these receptors. The mechanism of action for emergency contraception of mifepristone includes: It disrupts the follicular maturation as well as the endocrine function of the granulosa cells, so actually the patients are far less likely to ovulate if it is taken prior to ovulation.
It disrupts the mid-cycle LH surge, again prohibiting ovulation.
If taken later in the cycle, it interrupts hormonal support to the endometrium, makes the endometrial cavity desynchronous, this leads to degeneration and shedding of the endometrial lining, thereby preventing or disrupting implantation of the conceptus. At doses ranging from 3 to 10 mg/kg orally, it inhibits the action of endogenous or exogenous progesterone in different animal species (rat, mouse, rabbit and monkey). This action is manifested in the form of pregnancy termination in rodents.
Pharmacokinetics: Absorption: After oral doses, peak plasma concentrations of mifepristone occur after about 1 to 2 hours; bioavailability is about 70%.
Distribution: Mifepristone is about 98% bound to plasma proteins, mainly α1-acid glycoprotein.
Biotransformation and elimination: Elimination is biphasic; a slow phase is followed by a more rapid terminal phase, with an elimination half-life of about 18 hours. Mifepristone undergoes hepatic oxidative metabolism, mainly by the cytochrome P450 isoenzyme CYP3A4, and metabolites are excreted in the bile and eliminated in the faeces. Only a small fraction is detected in the urine.
Indications/Uses
Mifestad 10 is indicated for emergency contraception within 120 hours after unprotected sexual intercourse.
Dosage/Direction for Use
1 tablet of Mifestad 10 can be used up to 120 hours after intercourse. However, the earlier it is used, the more effective the treatment is.
Administration: Mifestad 10 is taken orally.
Overdosage
No case of overdose has been reported. In the event of accidental massive ingestion, signs of adrenal failure might occur. Signs of acute intoxication may require specialist treatment including the administration of dexamethasone.
Contraindications
Known hypersensitivity to mifepristone or any excipient of the drug.
Pregnancy.
Chronic adrenal failure.
Severe uncontrolled asthma.
Renal or hepatic impairment.
Inherited porphyrias.
Special Precautions
In the absence of specific studies, mifepristone is not recommended in patients with: Renal failure, hepatic failure and malnutrition.
Bleeding: The patient must be informed of the occurrence of prolonged vaginal bleeding (an average of about 12 days or more after Mifestad intake) which may be heavy. Bleeding occurs in almost all cases and is not in any way a proof of complete expulsion.
Infection: Very rare cases of fatal or serious toxic shock caused by pathogens like Clostridium sordellii endometritis, Escherichia coli, presenting with or without fever or other obvious symptoms of infection, have been reported after medical abortion with the use of mifepristone.
Emergency contraception should be used temporarily, only in case of emergency; and should not replace regular contraception. Women who present for repeated courses of emergency contraception should be advised to consider a long-term method of contraception.
Emergency contraception could not have the desired effect in all cases. If the unprotected sexual intercourse time was not determined or the woman has had an unprotected sexual intercourse over 120 hours in one period, pregnancy may occur. So, treatment with mifepristone 10 mg after the second sexual intercourse may be ineffective. If the period is later than 5 days, unusual haemorrhage on the day of the period is expected, or pregnancy is suspected due to any other causes, patients have to determine that pregnancy does not occur.
Unprotected intercourse after treatment can increase the risk of an unwanted pregnancy.
Should not repeat treatment in one period because of the risk of menstruation disorder.
Should be used with care in patients with less severe asthma or with chronic obstructive airways diseases, haemorrhagic or cardiovascular disease or associated risk factors, or anaemia.
Should be used with care in patients receiving long-term corticosteroid treatment; a corticosteroid may need to be given if acute adrenal suppression is suspected.
Care is also required in patients receiving anticoagulants because of the increased risk of severe bleeding.
Mifestad 10 contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.
Effects on ability to drive and use machines: Adverse drug reactions such as headache, dizziness and hypotension may occur. If affected, patients should not drive or operate machines.
Use In Pregnancy & Lactation
Pregnancy: Mifepristone should not be used during pregnancy, and the drug cannot cause an abortion.
The dose of 10 mg is too low to cause an abortion but it cannot be excluded that in a few cases a bleeding could be induced if the woman is pregnant.
Lactation: Mifepristone may theoretically be excreted in the mother's breast milk. However, no data is available. Consequently, mifepristone use should be avoided during breast-feeding.
Adverse Reactions
Common: 1/100 ≤ADR <1/10, uncommon: 1/1000 ≤ADR <1/100, rare: 1/10,000 ≤ADR <1000, very rare: ADR <1/10,000.
Nervous system: Rare: Headache.
Gastrointestinal: Very common: Nausea, vomiting, diarrhoea (these gastrointestinal effects related to prostaglandin use are frequently reported).
Common: Cramping, light or moderate.
Skin and subcutaneous tissue: Uncommon: Hypersensitivity: Skin rashes uncommon (0.2%).
Rare: Single cases of urticaria, erythroderma, erythema nodosum, toxic epidermal necrolysis have also been reported.
Very rare: Angioedema.
Infections and infestations: Common: Infection following abortion. Suspected or confirmed infections (endometritis, pelvic inflammatory disease) have been reported in less than 5% of women.
Very rare: Cases of serious or fatal toxic shock caused by pathogens like Clostridium sordellii endometritis or Escherichia coli, presenting with or without fever or other obvious symptoms of infection, have been reported after medical abortion with the use of mifepristone.
Vascular: Uncommon: Hypotension (0.25%).
Reproductive system and breast: Very common: Uterine contractions or cramping (10 to 45%) in the hours following prostaglandin intake.
Common: Heavy bleeding occurs in about 5% of the cases.
General: Rare: Malaise, vagal symptoms (hot flushes, dizziness, chills), fever.
Drug Interactions
Aspirin and NSAIDs should be avoided to be used concomitantly with mifepristone because of a theoretical risk that prostaglandin synthetase inhibitors may alter the efficacy of mifepristone.
Storage
Store in a well-closed container, in a dry place. Do not store above 30°C.
Shelf-Life: 48 months from the date of manufacturing.
MIMS Class
ATC Classification
G03XB01 - mifepristone ; Belongs to the class of antiprogestogens.
Presentation/Packing
Tab (yellow, round-shaped, engraved with "10" on one side, plain on the other side) 10 mg x 1 x 1's, 1 x 10's.
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