Post-coital agents and menses inducing drugs.

ABSTRACT

The importance of developing of drugs which could be taken post-coitally or used once-a-month in the case of a delay in the onset of the menses is well recognized. The availability of such technology would limit exposure to fertility regulating agents to such occasions where there is coital exposure or possibility of pregnancy. Methods of post-coital contraception used so far include IUD's inserted post-coitally, estrogens, and combinations of estrogens and gestagens. These are reserved primarily for emergency situations to protect women from unwanted pregnancy resulting from rape or unprotected coitus. Levonorgestrel has shown satisfactory results in terms of contraceptive efficacy and is being further evaluated clinically. A number of problems inherent in the development of post-coital contraception are discussed. Menstrual regulation could be achieved by a number of approaches (a) block progesterone receptors and interfere with the preparation of the endometrium for implantation; (b) luteolysis leading to decreased progesterone levels and interruption of implantation; and (c) termination of early pregnancy by prostaglandins. A number of progesterone antagonists have been evaluated. One of the compounds, RU38486 is being evaluated clinically for termination of very early pregnancy. Deglycosylated derivatives of human chorionic gonadotropin have been shown to antagonize the action of human chorionic gonadotropin and interfere with established pregnancy in rats. Appropriate methods of delivery, immunogenicity and alternate methods for production of human chorionic gonadotropin need to be considered before evaluation of the derivatives for clinical use. In vitro and in vivo models need to be developed for evaluation of the teratogenicity and embryotoxicity of post-coital and menses inducing agents. There are a number of gaps in the knowledge of the processes regulating implantation which should be investigated in rodents and in different non-human primate species.