Dienogest
Dienogest is an orally-active semisynthetic, steroidal progestogen (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.Dienogest given in isolation is available for the treatment of endometriosis under the trade name Visanne.
Indications
Contraception
Dienogest is used primarily as a contraceptive in combination with ethinylestradiol. It is given as a tablet containing 2 mg of dienogest and 30 μg of ethinylestradiol.Dienogest is also available in a quadriphasic oral contraceptive pill combined with estradiol valerate, marketed as Natazia in the United States and Qlaira in some European countries and Russia. This formulation is also approved for the treatment of heavy menstrual bleeding.
The minimum dose required to inhibit ovulation has been found to be approximately 1 mg.
Endometriosis
Dienogest is also approved in the European Union for the treatment of endometriosis.It has been shown to be equally effective as leuprorelin,which is a second line medication against endometriosis.
Pharmacodynamics
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 2 mg/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
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