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  • Author: C. REVESZ x
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BIOLOGICAL ACTIVITY OF MEDROGESTONE: A NEW ORALLY ACTIVE PROGESTIN

C. REVESZ and C. I. CHAPPEL

Summary.

A new synthetic orally active progestational agent 'Medrogestone' was investigated and its activity compared to progesterone and medroxyprogesterone acetate (map). Medrogestone fulfils the criteria of a pure gestagen, it has a spectrum of biological activity similar to that of progesterone but unlike progesterone, it is orally active. Medrogestone is free of undesirable side effects in experimental animals. It is being investigated clinically as an oral progestin (Carter, Faucher & Greenblatt, 1964).

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AY-11483, A NEW TYPE OF ORALLY ACTIVE OESTROGEN

C. REVESZ, U. K. BANIK and Y. LEFEBVRE

Summary.

The oral oestrogenic activity of AY-11483 has been compared to that of oestriol and mestranol. The compound shows significant activity in the vaginal cornification test in rats and mice; however, it has a relatively weak effect in the uterotrophic assay in rats, mice and rabbits. Furthermore, like oestriol, it exerts a weak effect on the endometrium in rabbits. Based on our findings, AY-11483 should be classified as an impeded oestrogen with possible clinical application.

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ORALLY ACTIVE OESTROGENS AND PROGESTINS IN PREVENTION OF PREGNANCY IN RATS

U. K. BANIK, C. REVESZ and F. HERR

Summary.

Orally active synthetic oestrogens and progestins were studied in tests to prevent pregnancy in rats. By daily administration the contraceptive effect of ethynyloestradiol and a new oestrogen, 17α-[3-furyl]-estra-1,3,5(10),7-tetraene-3,17-diol 3-acetate (AY-11483), was potentiated by three progestins, namely, chlormadinone acetate, 6-chloro-3β,17α-dihydroxypregn-4,6-dien-20-one diacetate (AY-11440) and medrogestone. AY-11483 given alone, or together with AY-11440, was more potent in preventing ovulation and implantation than ethynyloestradiol alone or in combination with other compounds. Chlormadinone acetate or AY-11440 alone were completely inactive in all the assays. The mode of action of oestrogen or oestrogen and progestin in the prevention of ovulation and implantation is discussed. In the rat, implantation seems more vulnerable to oestrogens than does ovulation.