Mifepristone

Indications
 Oral
Termination of pregnancy (49 days or less duration)
Adult: 600 mg as a single dose followed 2 days later by 400 mcg of misoprostol as single dose.
Oral
Postcoital contraception
Adult: 600 mg single dose within 72 hr of unprotected intercourse.
Oral
Termination of pregnancy up to 63 days
Adult: 600 mg as a single dose followed by 1 mg gemeprost vaginally after 36-48 hr.
Oral
Induction of labour following intrauterine fetal death
Adult: 600 mg daily for 2 consecutive days.
Oral
Termination of pregnancy between 13-24 wk of gestation
Adult: 600 mg as a single dose given 36-48 hr prior to prostaglandin therapy.
Oral
Softening and dilatation of cervix prior to surgical termination of pregnancy
Adult: 600 mg as a single dose given 36-48 hr prior to the procedure.
Contraindications
 Confirmed or suspected ectopic pregnancy, chronic adrenal failure, concurrent long-term corticosteroid therapy, history of allergy to mifepristone, misoprostol or other prostaglandin, haemorrhagic disorders or concurrent anticoagulant therapy, porphyria, hepatic or renal impairment; pregnancy and lactation; IUD in place; undiagnosed adnexal mass.
Warnings / Precautions
 Asthma, COPD; women smokers >35 yr; CV disease or risk factors; smoking; alcoholism; prosthetic heart valve; history of infective endocarditis.
Adverse Reactions
 Excessive vaginal bleeding; UTI; uterine haemorrhage; uterine infections; unusual tiredness or weakness; back pain; diarrhoea, nausea, vomiting; fever; dizziness; headache; anxiety; GI cramps.
Drug Interactions
 Decreased efficacy with aspirin and NSAIDs. Efficacy of corticosteroids (including inhaled) decreased, monitor patients during co-admin and for several days afterwards.
See Below for More mifepristone Drug Interactions
Mechanism of Actions
 Mifepristone is a progesterone antagonist with antiglucocorticoid activity. It binds to the intracellular progesterone receptor where it competitively inhibits progesterone attachment. It is also a partial progesterone agonist.
Absorption: Peak plasma concentrations after 1.3 hr.
Distribution: Protein-binding: 98%.
Metabolism: Hepatic: Undergoes first-pass metabolism.
Excretion: Faeces (as metabolites); urine (small amounts); 18 hr (ellimination half-life).
Administration
 May be taken with or without food. (Avoid grapefruit juice.)
ATC Classification
 G03XB01 - mifepristone ; Belongs to the class of antiprogestogens.
Available As
  • Mifepristone 100 mg
  • Mifepristone 200 mg

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