Extragenital effects of oral contraceptives [antikvár]

The criteria for a combined oral contraceptive formuládon require it to be an effective inhibitor of ovulation and have good cycle control, with minimai metabolic effects at the dosage required to achieve these effects. One of the major reasons for poor compliance and discontinuation of the use of existing formulations is the manifestation of so-called 'minor nuisance effects', which need to be minimized. These objectives shouid be achieved by the introduction of new formulations of existing estrogens and progestogens, or the introduction of new contraceptive steroids. This symposium, dealing with the extragenital effects of a combined formulation of ethinylestradiol at an acceptable dose of 30 (lg, and a new progestogen, is viewed with much interest. This progestogen, dienogest, is a 19-norsteroid which differs from the currently available progestogens. At the 17 position, the 17a-ethinyl group is replaced by a 17a-cyanomethyl group. There is a 13-methyl group in the B-ring of this steroid with an additional double bond between C9 and Ci0. It therefore has properties not unlike the C21 pregnane progestogens, with a marked secretory and somé anti-estrogenic effect on the endometrium and only a moderate anti-gonadotropic action. There is alsó an indication that it acts directly on ovarian fiinction. It does not interfere with the metabolism of ethinylestradiol in the liver (cytochrome P450 complex), and therefore does not affect plasma levels of ethinylestradiol. Nevertheless, in combination with ethinylestradiol, it is an effective inhibitor of ovulation. Unlike other gonane progestogens, it has negligible estrogenic and no androgenic or mineralocorticoid effects and minimai metabolic action. In addition to this highly selective progestational contraceptive effect, it has distinct anti-androgenic properties, thus enhancing its acceptability for that group of women who manifest features of androgenicity in their menstrual cycle or who respond to progestogens with androgenic potential by manifesting such side-effects as acne and seborrhea. In clinicai trials, this formulation has provided reliable contraceptive action with good cycle control and a high level of acceptability, lending