VISANNE TABLET 2MG FOR ORAL USE

Product Information

Registration Status: Active

VISANNE TABLET 2MG is approved to be sold in Singapore with effective from 2010-10-29. It is marketed by BAYER (SOUTH EAST ASIA) PTE LTD, with the registration number of SIN13879P.

This product contains Dienogest 2mg in the form of TABLET. It is approved for ORAL use.

This product is manufactured by Bayer Weimar GmbH und Co. KG in GERMANY.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Description

Dienogest is an orally-active semisynthetic progestogen which also possesses the properties of 17α-hydroxyprogesterone. It is a derivative of 19-nortestosterone and has antiandrogenic properties. It is primarily used as a contraceptive in combination with ethinylestradiol, or in other combination form pills approved in United States and Europe however it is not available in the US by itself. In Europe, Australia, Malaysia, Singapore and Japan, dienogest single therapy is an approved treatment for endometriosis to alleviate painful symptoms of endometriosis and reduce endometriotic lesions [A20330]. Dienogest is commonly marketed as Visanne, Natazia and Qlaira.

Indication

Indicated for use as the treatment of endometriosis alone and as a contraceptive in combination with ethinylestradiol.

Mechanism of Action

Dienogest acts as an agonist at the progesterone receptor (PR) with weak affinity that is comparable to that of progesterone but has a very potent progestagenic effect in the endometrium, causing endometrial atrophy after prolonged use [A20331]. It promotes antiproliferative, immunologic and antiangiogenic effects on endometrial tissue. Dienogest reduces the level of endogenous production of oestradiol and thereby suppressing the trophic effects of oestradiol on both the eutopic and ectopic endometrium [L932]. Continous administration of dienogest results in hyperprogestogenic and moderately hypoestrogenic endocrine environment, which causes initial decidualization of endometrial tissue [L931]. It is an antagonist at androgen receptors, improve androgenic symptoms such as acne and hirsutism [A16570].

Pharmacokinetics

Absorption: Dienogest is rapidly absorbed following oral administration, with 91% bioavailability. The peak plasma concentration of 47 ng/mL is reached at about 1.5 hours after single ingestion of 2 mg [L931]. The stable concentrations of the drug are reached after two days of initial treatment [A20331].
Distribution: The apparent volume of distribution (Vd/F) of dienogest is 40 L [L931].
Metabolism: Dienogest undergoes complete metabolism that is mainly mediated by CYP3A4. The metabolites are pharmacologically inactive and rapidly eliminated from the plasma.
Elimination

Clearance

The metabolic clearance rate from serum (Cl/F) is 64 mL/min [L931].

Toxicity

Oral LD50 in mouse is 4 mg/kg [MSDS]. In a long-term carcinogenicity study involving rats and mice, exposure of 10 times the dose of maximum recommended clinical dose of dienogest resulted in increased incidences of pituitary adenomas, fibroepithelial mammary tumours, stromal polyps of the uterus and malignant lymphoma [L932]. These tumors are thought to arise from marked species differences in the optimal oestrogen:progestogen ratio for reproductive function. In rat liver foci assay, dienogest did not induce tumor promotion activity [L932]. Dienogest does not display genotoxic potential.

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.