Dienogest

Dienogest is an oral progestogen (hormone) which is used in combination with the synthetically produced hormone ethinylestradiol for contraception or as a monopreparation for the symptomatic treatment of endometriosis.

The hormone was synthesized and patented in 1977 by the pharmaceutical company Jenapharm.

Pharmacodynamics

Although Dienogest only weakly activates the progesterone receptor, it shows a very strong progestagenic effect in the endometrium, which becomes diluted after prolonged use of the hormone. In addition to relieving endometriosis symptoms, this also contributes to making it more difficult for sperm to implant.

Other contraceptive effects from Dienogest are caused by inhibiting ovulation and blocking the cervix from sperm.

In addition, Dienogest also has antiandrogenic effects, meaning it suppresses male sex hormones and relieves symptoms of acne by regulating sebum production.

Pharmacokinetics

After oral administration, dienogest is rapidly absorbed with a bioavailability of 90%. The maximum concentration in plasma is reached after 1.5 hours and the hormone circulates with 90% bound to albumin.
Dienogest wird vollständig durch das Enzym CYP3A4 verstoffwechselt und wird hauptsächlich mit dem Urin ausgeschieden. Die Halbwertszeit beträgt ca. 9-10 Stunden.

Side effects

Common adverse reactions include weight gain, acne, headache, breast and abdominal pain, menstrual irregularities, mood swings, and gastrointestinal disorders.

Toxicological data

LD50 (mouse, oral): 4 mg/kg