Dienogest

Dienogest
ATC Code G03DB08
Formula C20H25NO2
Molar Mass (g·mol−1) 311,425
Physical State solid
Melting Point (°C) 210-218
CAS Number 65928-58-7
PUB Number 68861
Drugbank ID DB09123
Solubility sparingly soluble in water

Basics

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.

Pharmacology

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.

Toxicity

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

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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