Mifepristone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. 1993

R N Brogden, and K L Goa, and D Faulds
Adis International Limited, Auckland, New Zealand.

Mifepristone is a potent oral antiprogestogen which acts at the level of the receptor, having a high affinity for the progesterone receptor. Most of the clinical trials have studied its efficacy in the termination of early pregnancy when used in conjunction with a low dosage of a prostaglandin analogue. In these studies, mifepristone 100 to 600mg administered as a single dose or over 3 or 4 days, 36 to 48 hours before a prostaglandin analogue given vaginally, intramuscularly or orally, induced complete abortion in about 95% of women. Used alone, mifepristone is an effective cervical priming agent prior to termination of first trimester pregnancy by vacuum aspiration, and facilitates termination of second trimester pregnancy by prostaglandin by reducing the interval between the start of prostaglandin treatment and termination, the cumulative prostaglandin dosage, and the adverse effects associated with these drugs. Mifepristone can also be used to induce labour in cases of intrauterine fetal death. Mifepristone has been shown to be an effective postcoital contraceptive with a likely emergency role, since its repeated use modifies the menstrual cycle. Pilot studies have been performed in unresectable meningioma and metastatic breast cancer, and in Cushing's syndrome. Mifepristone is generally well tolerated, and thus is an effective, appropriate, medical alternative to surgical termination of early pregnancy. It has as yet unexplored potential as a postcoital contraceptive and in oncology.

UI MeSH Term Description Entries
D011247 Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH. Gestation,Pregnancies
D003281 Contraceptives, Postcoital Contraceptive substances to be used after COITUS. These agents include high doses of estrogenic drugs; progesterone-receptor blockers; ANTIMETABOLITES; ALKALOIDS, and PROSTAGLANDINS. Emergency Contraceptive,Morning-After Pill,Postcoital Contraceptive,Postcoital Contraceptives,Contraceptive Agents, Post-Coital,Contraceptive Agents, Postcoital,Contraceptives, Post-Coital,Emergency Contraceptives,Contraceptive Agents, Post Coital,Contraceptive, Emergency,Contraceptive, Postcoital,Contraceptives, Emergency,Contraceptives, Post Coital,Morning After Pill,Post-Coital Contraceptive Agents,Post-Coital Contraceptives,Postcoital Contraceptive Agents
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D015735 Mifepristone A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. Mifegyne,Mifeprex,Mifégyne,R-38486,R38486,RU-38486,RU-486,ZK-98296,ZK98296,R 38486,RU 38486,RU 486,RU38486,RU486,ZK 98296

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