Information on Dienogest
From Wikipedia, the free encyclopedia
Dienogest is an orally active synthetic progesterone (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.
History
Dienogest was synthesised in 1979 in Jena, Germany under the leadership of Prof. Kurt Ponsold, was initially referred to as STS 557. It was found that its potency was 10 times that of levonorgestrel. The first product on the market to contain dienogest as a contraceptive pill Valette in 1995 made by Jenapharm. It has been little used outside of Germany.
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. The minimum dose required to inhibit ovulation has been found to be approximately 1 mg.
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.
Adverse effects
Adverse effects associated with dienogest are the same as those expected of a progestogen. These include weight gain, increased blood pressure, breast tenderness and nausea. It produces no androgenic side effects and has little effect on metabolic and lipid haemostatic parameters.
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Mochida Launches “Dinagest Tab. 1mg” - A Treatment for Endometriosis
(Tokyo, January 7, 2008) - Mochida Pharmaceutical Co., Ltd. (Head Office: Shinjuku-ku, Tokyo, Japan; President: Naoyuki Mochida) will launch “Dinagest Tab. 1mg” (dienogest), a therapeutic agent for endometriosis on January 21, 2008. “Dinagest Tab. 1mg” was in-licensed from Bayer Schering Pharma AG, and has been developed as a therapeutic agent for endometriosis by Mochida in Japan. This is a novel, oral drug that activates selectively progesterone receptors, and demonstrates its therapeutic effect by inhibiting ovarian function and proliferation of endometrial cells. The results obtained during a long-term clinical trial (for 52 weeks) showed that it did not excessively lower the level of estradiol in the blood, thus preventing the occurrence of low estradiol-induced climacteric symptoms, and no cumulative decrease in bone density and variations in body weight were observed.
Endometriosis is classically defined as the presence of tissues resembling endometrium – the mucosa lining the uterine cavity – outside the uterus, and its lesions may cause hemorrhage and inflammation along with the menstrual cycle, leading to adhesions with surrounding peritoneal tissues. The disease affects a negative impact on quality of life of women by producing symptoms such as dysmenorrhea, pelvic pain, fatigue and infertility. The number of patients with endometriosis is said to be increasing, because the disease is believed to progress with repeated menstruation and women experience shorter periods of amenorrhea due to later marriage and fewer fertilization in recent years.
Mochida Pharmaceutical is committed to improving female health, with a focus on obstetrics and gynaecology as one of its key areas. “Dinagest Tab. 1mg” is expected to improve quality of life of patients by offering a new treatment option for endometriosis.
For Reference Brand Name: Dinagest Tab. 1mg Nonproprietary name: Dienogest Indication: Endometriosis Ingredients and Contents: 1 mg dienogest per tablet
Dosage and Administration Usually, to adults, 2 mg of dienogest is orally administered daily in 2 divided doses, starting from day 2-5 of the menstrual cycle. NHI (National Health Insurance) price: 468.40 Yen per tablet
Package: 100 tablets Date of Approval: October 19, 2007 Date of NHI price listing: December 14, 2007 Date of Launch: January 21, 2008 Manufacturer/Distributor: Mochida Pharmaceutical Co., Ltd.