Mifepristone Pharmacology

Mifepristone

About Mifepristone
A synthetic steroid, Antiprogestin, Abortifacient,Antineoplastic Agent(Hormone Antagonist).
Mechanism of Action of Mifepristone
Mifepristone is a competitive progesterone receptor antagonist in the presence of Progestins. In the early stage of pregnancy Mifepristone blocks the uterine progesterone receptors and cause decidual breakdown. This leads to detachment of the blastocyst and decreases hCG production. This in turn decreases progesterone secretions from the corpus luteum and further augments decidual breakdown. These all results in increased uterine prostaglandin levels and sensitizes myometrium to contract. It also causes cervical softening and facilitates expulsion of the detached blastocyst
Mifepristone delay ovulation by its action on hypothalamus and pituitary rather than ovary and the mechanism is not known
Pharmacokinets of Mifepristone
Absorption: It is well absorbed after oral administration and its bioavailability is about 69%.
Distribution: It is widely distributed in protein bound from (94%) and also crosses the placenta.
Metabolism: It undergoes hepatic metabolism and forms 3 active compounds
Excretion: Mifepristone and its metabolites are excreted mainly through faeces and small amount in urine.
Onset of Action for Mifepristone
N/A
Duration of Action for Mifepristone
N/A
Half Life of Mifepristone
18 hours
Side Effects of Mifepristone
1.Dizziness
2.Headache
3.Diarrhea
4.Nausea
5.Vomiting
6.Back pain
7.Feeling tired
8.Hot flashes
9.Abdominal pain
10.Anorexia
11.Vginal bleeding
12.Bad-smelling vaginal discharge
13.Fainting
14.Irregular heartbeat
15.Palpitations
16.Chest pain
17.Fever
18.Redness, blistering, peeling or loosening of the skin, including inside the mouth
19.Skin rash
20.Uterine infections
Contra-indications of Mifepristone
1.Hypersensitivity to Mifepristone
2.Ectopic pregnancy
3.Adrenal failure
4.Patient on long term corticosteroid therapy
5.Haemorrhagic disorder
6.Concurrent anticoagulant therapy
7.Inherited porphyria
8.Hepatic impairment
9.Renal impairment
Special Precautions while taking Mifepristone
1.Asthma
2.Chronic obstructive pulmonary diseases
3.Cardiovascular diseases
4.Smoking
5.Alcoholism
6.Should be taken prior to and during surgical abortion to prevent rhesus immunisation.
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Contraindicated
Breast Feeding Related Information
Contraindicated.
Children Related Information
Contraindicated
Indications for Mifepristone
1.Cervical ripening
2.Contraceptive pill
3.Termination of pregnancy
4.Induction of labour
Interactions for Mifepristone
Ketoconazole, itraconazole, erythromycin, and grape fruit may inhibit mifepristone metabolism.
Rifampicin, dexamethasone, phenytoin, phenobarbital, carbamazepine induce mifepristone`s metabolism.
Typical Dosage for Mifepristone
Adult:
1.Cervical ripening: 50 - 600mg to be taken 24 - 30 hour before surgery.
2.Postcoital contraception: 600mg as single dose within 3 days after intercourse.
3.Once a month contraceptive pill: 200mg as single dose on the second day after mid cycle.
4.Termination of pregnancy up to 49 days: 600 mg as single dose and after 2 days takes Misoprostol 400mcg as single dose.
5.Termination of pregnancy up to 63days: 600 mg as single dose and after 36 - 48 hours take Gemeprost vaginally.
6.Termination of pregnancy between 13 - 24 weeks of gestation: 600mg as single dose to be taken 36 - 48 hours before prostaglandin therapy
7.Induction of labour following intrauterine fetal death: 600mg / day for 2 days.
8.Softening and dilatation of cervix before surgical termination of pregnancy: 600 mg as single dose is given 36 - 48 hours before surgery.
Schedule of Mifepristone
N/A
Storage Requirements for Mifepristone
Store at 15 - 30 degree C. Protect from heat and light. Keep out of the reach of children
Effects of Missed Dosage of Mifepristone
For pregnancy termination: Does not apply
For other uses: Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Mifepristone
Give supportive measures and symptomatic treatment.

Home Delivery for Mifepristone in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including mifepristone.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for mifepristone and other medicines and health products. Home delivery services for mifepristone may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take mifepristone only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for mifepristone before they complete the sale. You can get this information while placing the order for mifepristone with the pharmacy.

Mifepristone is a generic medicine name and there are several brands available for it. Some of the brands for mifepristone might be better known than mifepristone itself. If the pharmacy that's willing to deliver medicines to your home doesn't have mifepristone in stock, you can ask for one of the branded alternatives for mifepristone.