Dienogest

Chemical Name: 17α-Hydroxy-3-oxo-19-norpregna-4,9-diene-21-nitrile
Molecular Formula: C20H25O2
Molecular Weight: 311.43
CAS: 65928-58-7

Dienogest Description and Indication

Dienogest is orally active synthetic progestogen. Dienogest is a 19 norprogestin derived from 19 nortestoster-one. It differs from other 19 norprogestins by possessing a cyanomethyl group instead of an ethinyl group in the 17α-position.Based on its chemical structure, dienogest may be termed a 'hybrid progestogen' with pharmacodynamic properties typical of progesterone derivatives and 19 norprogestins, together with its own specific properties.

Dienogest is an effective, generally well tolerated option for the long-term treatment of endometriosis. Dienogest in combination with Ethinyl Estradiol act as oral contraceptive & with Estradiol Valerate is used in Hormone replacement therapy.

Dienogest Mechanism of Action

Dienogest is a nortestosterone derivative with antiandrogenic activity.Dienogest binds to the progesterone receptor of the human uterus with only 10% of the relative affinity of progesterone. Despite its low affinity to the progesterone receptor, dienogest has a strong progestogenic effect in vivo.

Dienogest causes inhibition of ovulation 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.

Dienogest acts on endometriosis by reducing the endogenous production of oestradiol and thereby suppressing the trophic effects of estradiol on both the eutopic and ectopic endometrium. Dienogest combines the pharmacological properties of 19 progestins and progesterone derivatives, offering a pronounced potent endometrial effect via mechanisms of action that include antiproliferative effects on endometriotic cells, as well as anti-inflammatory and angiogenic actions.Dienogest relieves endometriosis pain with high efficacy, reduces endometriosis lesions.A significant characteristic of dienogest is its lack of androgenic activity, with no affinity for sex hormone binding globulin and, as a consequence, does not alter endogenous testosterone levels.

Dienogest Contraindications

Dienogest should not be used in the presence of any of the conditions:

Dienogest Adverse Drug Effects

The most common undesirable effects include

Dienogest Drug Interactions

Interactions can occur with drugs:

Phenytoin , Barbiturates, Primidone, Carbamazepine, Ketconazole, Itraconazole, Erythromycin & Ritonavir

Dienogest Formulations

Dienogest is available in both fixed dose combination and single entity formulations:

Dienogest Brands

Dienogest alone as single entity

Dienogest in combination with Other Drugs.