Antiprogesterone RU 486--a drug for non-surgical abortion.
RU 486 is the first steroidal antiprogesterone in clinical use. It acts by binding to progesterone receptor, thus blocking the effects of progesterone at the uterine level, and provoking endometrial necrosis and shedding. RU 486 can, therefore, be used to interrupt early human pregnancy. In pregnancies of up to 7-8 weeks duration, the rate of complete abortions with RU 486 has ranged from 50% to 90%. The success rate can, however, be augmented up to 95%-100% by combining RU 486 with a low dose prostaglandin. RU 486 induced abortion has been well tolerated by women and highly acceptable to them. The bleeding starts 2-3 days after RU 486 administration lasting for 12-14 days. Possible clinical uses of RU 486 include induction of menstruation, late post-coital contraception, induction of labour after intrauterine fetal death, preoperative cervical ripening and treatment of progesterone receptor positive mammary tumours. When administered in the follicular phase of the cycle, RU 486 inhibits follicular development. In addition, the antiglucocorticoid properties of RU 486 have been used in symptomatic treatment of hypercortisolemia of Cushings disease. The pharmacokinetics of RU 486 are characterised by high micromolar serum concentrations, long half-life of 26-48 hours and substantial metabolism after oral administration. Although effective and well tolerated, RU 486 has aroused great moral controversy, which is currently hampering further testing and distribution of the drug. So far RU 486 has been accepted for termination of pregnancy in France and in the Peoples Republic of China, to be used with prostaglandins and under strict medical surveillance.
Department of Medical Chemistry, University of Helsinki, Finland.
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O
Heikinheimo
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O
Ylikorkala
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P
Lähteenmäki
D005260:Female; D006801:Humans; D015735:Mifepristone / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D011247:Pregnancy
D015735:Mifepristone