[The antiestrogen effect]

Abstract

The effects of estradiol, which are requisite for the normal occurrence of events related to reproduction, are not restricted to that field. They play a part in the overall trophicity of the female organism. On the other hand, relative or absolute estrogen hyperactivity results in harmful clinical effects and in disastrous cellular consequences, i.e. initiation or promotion of genital carcinomas. After a review of the different steps of the synthesis and action of estradiol, the various compounds that are active on these steps are considered: antigonadotropes (norsteroid progestogens, androgens, danazol, prolactin, corticosteroids, LHRH), inhibitors of estrogen synthesis (aminogluthetimide and testolactone), compounds that increase catabolism (progestogens), and antagonists of the cellular effect of estradiol (tamoxifen, nafoxidin, clomifen, progesterone, progestogens and androgens). The putative or established site of action and the main aspects of therapeutic use are given for each substance.