Dienogest

Products

Dienogest is commercially available in many countries as a fixed combination with estradiol valerate in tablet form (Qlaira). Furthermore, a monopreparation for endometriosis therapy is available (Visanne, see under Dienogest Endometriosis). The fixed combination with ethinyl estradiol (Valette, generic) was approved in many countries in 2014.

Dienogest + estradiol

Qlaira has been on the market in many countries since 2009. The drug was new in several respects. It was the first birth control pill with dienogest in many countries, it was the first pill to combine a progestin with estradiol instead of ethinyl estradiol, and it is a four-phase contraceptive. Estradiol is naturally produced by women.

Structure and properties

Dienogest (C20H25NO2, Mr = 311.4 g/mol) is a derivative of 19-nortestosterone (nandrolone) and carries a cyanomethyl group. It thus differs from, for example, levonorgestrel, which carries an ethynyl group.

Effects

Dienogest (ATC G03DB08) has progestogenic, contraceptive, and antiandrogenic properties.

Indications

Dienogest is used in combination with with an estrogen for oral contraception. As a monopreparation, it is also administered for therapy of endometriosis (Visanne) see Dienogest Endometriosis.

Contraindications

For complete precautions, see the drug label.

Interactions

Dienogest is a substrate of CYP3A and corresponding drug interactions with CYP inhibitors and inducers are possible.

Adverse effects

The most common possible adverse effects include headache, chest discomfort, depressed mood, and acne.

Cf.

  • Dienogest endometriosis
  • Progestogens, oral contraceptives
  • Antiandrogens