Dienogest

Dienogest is an orally active synthetic progesterone (or progestin). It is available for use as an oral contraceptive in combination with ethinylestradiol. It has antiandrogenic activity and as a result can improve androgenic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone.

History
Dienogest was discovered in 1979 in Jena, Germany and first named STS 557. It was found that its potency was 10 times that of levonorgestrel. The first product on the market to contain dienogest as a contraceptive pill Valette in 1995 made by Jenapharm. It has been little used outside of Germany.

Contraception
Dienogest is used primarily as a contraceptive in combination with ethinylestradiol. It is given as a tablet containing 2mg of dienogest and 30μg of ethinylestradiol.

Progestational Activity
Dienogest has moderate affinity for the progesterone receptor in human uterus tissue, in vitro, about 10% that of progesterone.

Inhibition of Ovulation
The minimum effective dose of oral dienogest required to inhibit ovulation is 1 mg/day. The inhibition of ovulation by dienogest occurs mainly via peripheral action as opposed to central action on gonadotrophin secretion. Oral treatment of dienogest 2mg/day in cyclical women reduced serum progesterone levels to anovulatory levels, however serum levels of lutenising hormone and follicle-stimulating hormone are not significantly altered.

Adverse effects
Adverse effects associated with dienogest are the same as those expected of a progestogen. These include weight gain, increased blood pressure, breast tenderness and nausea. It produces no androgenic side effects and has little effect on metabolic and lipid haemostatic parameters.