[Norsteroids: their biological activity and clinical use].

Subsequent to research in the 1940s on the effects of ethinyl derivatives of testosterone an investigation was performed in which norethisterone norethisterone acetate norethynodrel and linestrol were synthesized. Gestagen preparations consist of testosterone and 17-alpha-oxyprogesterone derivatives. Norethisterone norethisterone acetate linestrol and ethinodiol diacetate exhibit androgenic and weak estrogenic effects. 5-alpha-dihydronorethisterone is twice as androgenic as norethisterone. New 19-nonsteroid derived progestagenic steroids are norgestimate gestodene and desogestrel. Gestodene is the strongest gestagen with both androgenic and aldosterone effects. Gestrinone in a dose of 5 mg/day once a week for 10-18 months produced an estrogen concentration in blood plasma similar to the early follicular phase of the menstrual cycle. QRG-2154 (dodecanoat-16-alpha-ethinyl-21-hydroxy-19-norpreg-4-en-3 20-diol) injected in a dose of 200 mg suppresses ovulation for 120-200 days and in a 150 mg dose for 60-120 days. STS-557 (dienogest-17-alpha-cyanomethyl-17-beta-hydroxy-ester-49-dien-3-on) is a highly active progestagen. In rats the suppression of ovulation with levonorgestrel was 28 times higher and norethisterone acetate was twice as effective as dienogestrel. Combination oral contraceptives with less than 50 mg estrogen include the 1-phase preparations Anovlar Ovidon and Nonovlon as well as low-dose 2- and 3-phase preparations. Mini-pills like Femulen and Continuing contain only very low-dose gestagen. Post coital tablets (Postinor) and depo oral contraceptives (Deposition Noristerat) used are less frequently. Gestrinone given to 21 patients with endometriosis in a dose of 5-10 mg/week for 6 months reduced cysts in 2/3 of the patients. Similarly in 57 women a 2 mg/day dose of dienogestrel administered for half a year halted heterotopia in 66.7% and reduced it in 13.7%. 5 mg of gestrinone twice a week for 14 months caused the regression of uterine myomas in most perimenopausal patients as confirmed by sonography.