Products
Dienogest is commercially available for endometriosis therapy in tablet form (Visanne, generic).
Structure and properties
Dienogest (C20H25NO2, Mr = 311.4 g/mol) is a derivative of 19-nortestosterone (nandrolone) and carries a cyanomethyl group.
Effects
Dienogest (ATC G03DB08) has progestogenic and antiandrogenic properties. The effects are due to selective binding to progesterone receptors. Dienogest abolishes the trophic effects of estradiol. This results in atrophy of endometrial lesions. Dienogest has a high oral bioavailability of more than 90% and a half-life of 9 to 10 hours, allowing once-daily administration.
Indications
For the treatment of endometriosis.
Dosage
According to the professional information. The tablets are taken once a day regardless of meals. Therapy is continuous without breaks.
Contraindications
For complete precautions, see the drug label.
Interactioen
Dienogest is a substrate of CYP3A4 and corresponding drug interactions with CYP inducers and inhibitors are possible.
Adverse effects
The most common potential adverse effects include headache, breast discomfort, depressed mood, and acne. Dienogest can often cause bleeding problems (eg, spotting, irregular bleeding, absence of bleeding).