Dienogest

Abstract

The progestogen dienogest exhibits highly selective binding to the progesterone receptor. It has high progestational and significant antiandrogenic activity, but only moderate antigonadotrophic activity. Dienogest inhibits ovulation, produces secretory transformation of the endometrium and has antiproliferative effects. Oral dienogest 2 mg/day plus ethinylestradiol 30 micrograms/day provides effective contraception (Pearl Index approximately 0.2). Cycle stability is good during long term use of this combination; irregular vaginal bleeding was evident in 6% of women after 12 months' use. Androgenic symptoms (including hirsutism, seborrhoea, alopecia, acne vulgaris and hair and skin greasiness) improved in women treated with dienogest plus ethinylestradiol. The adverse events associated with dienogest are typical of those expected of a progestogen. The drug does not produce androgenic adverse effects and has little clinically significant effect on metabolic, lipid and haemostatic parameters.

Oral contraceptives in the prevention of endometrioma recurrence: does the different progestins used make a difference?

“…For this reason, new progestins are continually tested, in an attempt to find the perfect drug which ensures the desired effects without side effects. Two recent clinical studies in Europe and Japan extensively investigated a new treatment for endometriosis using Dienogest, a 19-nortestosterone derivative that is highly selective for progesterone receptors [25]. The studies demonstrated that at 2 mg daily, this progestin effectively alleviates pain, reduces endometriosis lesions and improves quality of life [26].…”

New developments in oral contraception: clinical utility of estradiol valerate/dienogest (Natazia®) for contraception and for treatment of heavy menstrual bleeding: patient considerations

“…At this dose, DNG exerts only a moderate antigonadotropic activity, but its induction of granulosa cell apoptosis in the follicle also contributes to the effective ovulation inhibition provided by DNG. 35,46 In combination with E 2 V, however, the 3 mg dose was found to be needed for ovulation suppression. 28 At those doses, the anti-estrogenic effect thickens the cervical mucus to block sperm transport into the upper genital tract.…”

“…Clinically, DNG is similar to 19-nortestosterone derivatives in that it has a short plasma half-life, strong progestational effect in the endometrium, and high oral bioavailability. 21,26,34 DNG is similar to progesterone derivatives in that it demonstrates both a relatively low inhibition of gonadotropin secretion 35,36 and anti-androgenic activity 37 (about 40% of cyproterone acetate). 38 DNG has no interaction with specific transport proteins, such as SHBG or cortisol-binding globulin (CBG).…”

Currently available combined oral contraception

“…Dienogest was initially produced in 1979. It is a very potent progestin that also has antiandrogenic activity [30,31]. Chlormadinone acetate is a derivative of 17a-hydroxyprogesterone.…”