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  • Title: Fertility control with RU 486.
    Author: Ulmann A, Dubois C, Philibert D.
    Journal: Horm Res; 1987; 28(2-4):274-8. PubMed ID: 3331378.
    Abstract:
    RU 486 is a synthetic steroid possessing antiprogestin and antiglucocorticoid activities. This paper summarizes the main pharmacological properties of this molecule. It is now under the phase II-III clinical studies in the world for early pregnancy interruption. By itself, the drug shows a 85% complete efficacy provided it is given at the dose of 600 mg (3 X 200 mg) once in pregnancies below or equal to 41 days of amenorrhea. The clinical tolerance of the drug is extremely satisfactory, but metrorrhagia can in some instances be heavy, thus necessitating an adequate medical monitoring. The antiglucogenic activity of the molecule has no clinical relevance. In the future, soma data suggest that adjunction of a synthetic prostaglandin analog could somehow increase the success rate, but further studies are necessary to evaluate the effectiveness of such a combination. RU-486 is a potent progestin antagonist that acts at the receptor level. Bioassays in rabbits and rats have shown that RU-486 has an antagonistic effect against exogenous progesterone in ovariectomized animals. In pregnant rats RU-486 at 10 mg/kg exerts a total abortive activity from day 3-16. A dose of 25 mg/kg, given orally, induced menstruation within 48 hours in cycling monkeys. A dose of 600 mg was 85% effective in interrupting pregnancy of less than 41 days duration in women. However, in 20% of cases there is abundant, heavy bleeding. 600 mg of RU-486, given at the end of the luteal phase in women at risk of pregnancy, had no greater failure rate and fewer side effects than high-dose estrogen administered for postcoital contraception. When given with prostaglandin analogs, RU-486 successfully terminated pregnancy after 41 days. For fertility control, RU-486 can be used as a contragestive agent up to 15 days after a missed period. At a later stage RU-486 combined with a prostaglandin is a promising abortifacient.
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