Gestoden, an innovative progestogen.

Abstract

The most widely used estrogen component in oral contraceptive (OC) pills today is ethinylestradiol (EE), synthesized in the laboratories of Schering A.G. since the year 1938. Compared to natural estrogens, it has a much stronger effect on liver metabolism, thereby inducing greater metabolic and hemostatic changes. Some, but not all, epidemiological studies associated rare cardiovascular events to the use of the OC pills, although statistical and diagnostic deficiencies inherent in such studies may have created wrong associations. These events were either of thromboembolic or hypertensive but not of arteriosclerotic origin. If these associations were true, therefore EE-induced adverse changes on the blood coagulation and fibrinolytic systems and its stimulation of the renin-angiotensin-aldosterone mechanism would probably be more important than any changes on the lipid and lipoprotein pattern (e.g., HDL-cholesterol). To counteract adverse EE-induced changes, therefore, synthetic progestogens used in OC pills should have a pronounced anti-estrogenic effect, stronger than natural progesterone, like levenorgestrel, and if possible, an aldosterone-antagonistic effect, resembling natural progesterone. Gestoden is a new synthetic progestogen with a pronounced anti-estrogenic effect and a unique aldosterone-antagonistic effect, unlike other synthetic progestogens available. The high biological progestogenic activity allows very low hormonal content in the pill formulation. Multicentric clinical trials with a combination of only 75 mcg gestoden combined with 30 mcg EE confirm a reliable contraceptive efficacy combined with excellent cycle control and tolerance in 1,095 women over 14,281 treatment cycles. In about 60% of women with elevated blood pressure before treatment, the blood pressure normalized during treatment.(ABSTRACT TRUNCATED AT 250 WORDS)