| 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.
------------------------------------------------------------------
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.
ディナゲスト錠1mg
商標名
DINAGEST Tab. 1mg
有効成分に関する理化学的知見
一般名
ジエノゲスト（dienogest）
化学名
17-hydroxy-3-oxo-19-nor-17α-pregna-4,9-diene-21-nitrile
構造式
分子式
C20H25NO2
分子量
311.42
性状
ジエノゲストは白色～微黄白色の結晶性の粉末である。本品はメタノールにやや溶けにくく、エタノール(99.5)に溶けにくく、水にほとんど溶けない。
融点
210～218℃
包装
PTP：100錠
製造販売元
持田製薬株式会社
部分中文地诺孕素处方资料（仅供参考）
地诺孕素
地诺孕素是德国德国Jenapharm公司开发的避孕新药，由于其强大的排卵抑制作用而应用于口服避孕。
1995年地诺孕素和炔雌醇复方制剂（2mg+0.03mg）作为避孕药在德国上市，2007年在澳大利亚上市，商品名Valette。
2001年地诺孕素与雌二醇戊酸酯的复方制剂（含地诺孕素2mg和雌二醇戊酸酯1或2mg）由先灵公司在德国上市，用于妇女绝经一年以上雌激素缺乏的激素替代疗法。2002年在丹麦、法国、比利时等欧洲国家上市，商品名Climodien。
2007年地诺孕素片剂（1mg）在日本上市，用于治疗子宫内膜异位症。
2008.3.31拜耳医药申请戊酸雌二醇地诺孕素片（五相）进口临床，目前正制定审评计划。
地诺孕素是一种混合孕激素，同时具有天然和合成孕激素的药理学优点。地诺孕素有很高的孕激素活性，其口服半有效剂量为0.11mg/kg。地诺孕素的内分泌药理学特性非常理想，它因仅结合于孕激素受体，故无雌激素、抗雌激素和雄激素活性，抗促性腺激素作用(抑制促卵泡激素和黄体激素的分泌)亦很弱。口服地诺孕素抑制正常行经妇女排卵的最低有效剂量仅1mg/天。地诺孕素抑制排卵的作用主要是通过其外周机理如抑制预排卵和卵巢17β-雌二醇峰等，而非影响促性腺激素分泌的中枢机理来实现的。正常行经妇女在接受口服地诺孕素2mg/天治疗期间，她们的血清黄体酮被降至不排卵水平，但血清促卵泡激素和黄体激素水平却未受到多大影响。
从排卵抑制剂量(mg/天)对于宫内膜转换剂量(mg/月经周期)之比看，醋酸炔诺酮、左炔诺孕酮和孕二烯酮为l，去氧孕烯和诺孕酯为3，醋酸环丙孕酮和醋酸氯地孕酮为5~7，地诺孕素则高达l7。地诺孕素显现出一种明显的以外周作用为主的特性，与天然产生的黄体酮相似，对子宫内膜有益。
地诺孕素还具有一定的抗雄激素活性。 改进的Hershberger法对睾丸素治疗的性腺切除雄鼠进行检测，结果发现地诺孕素的抗雄激素活性大于醋酸氯地孕酮而约为醋酸环丙孕酮的40%。正常行经妇女经口服地诺孕素2mg/天加炔雌醇30μg/天治疗3个月经周期(每月经周期前21天用药，随后停药7天)后，她们的血清雄烷二醇葡萄糖醛酸化物水平可较基线减少38%，血清总睾酮水平减少17~40%，游离睾酮水平减少48~54%，去氢表雄酮硫酸酯水平减少51%。
地诺孕素不与甾体转运蛋白结合，不影响正常行经妇女的血清催乳激素、皮质醇结合球蛋白和性激素结合球蛋白水平。地诺孕素也没有糖皮质激素和盐皮质激素活性，但抗增生作用已为体内、外实验所证实。
口服地诺孕素吸收完全且迅速，绝对生物利用度大于90%，达到最大血清和血浆浓度的时间分别约为2和l~2小时。在血浆中，约10%的地诺孕素以游离形式存在，此生物活性部分的比例较之黄体酮(0.5~4%)相比是相当高的。血浆中另90%的地诺孕素则与血浆白蛋白结合。
地诺孕素主要通过芳香化和11β-羟基化被代谢，代谢物在给药24小时内即自尿中迅速消除。地诺孕素的血浆半衰期较其它孕激素短，仅6.5~l2小时，故每天给药亦无蓄积性，此性质也较左炔诺孕酮更优。
【药品名称】 地诺孕素(Dienogest)
【化学名】 17α-氰甲基-17β-羟基-13β-甲基甾烷-4,9-二烯-3-酮
【适应症】 用于治疗子宫内膜异位症
【剂 型】 片剂
【规 格】 1mg
【用法用量】通常成人每天2mg，分两次服用，从月经周期的第2~5天开始。
【不良反应】本品可能出现的不良反应主要是体重增加、血压上升、乳房疼痛和恶心等
注：本栏药品是在日本本地上市，购买时请以电话咨询为准！
--------------------------------------------------------------
原产地英文商品名:
DINAGEST(ディナゲスト)1mgX 100tablets
原产地英文药品名:
Dienogest
原产地英文化合物名称:
17α-cyanomethyl-17β-hydroxy-estra-4,9-di-ene-3-one
中文参考商品译名:
DINAGEST(ディナゲスト)1毫克X100片/盒
中文参考药品译名:
地诺孕素
中文参考化合物名称:
17α-氰甲基-17β-羟基-13β-甲基甾烷-4,9-二烯-3-酮
生产厂家中文参考译名:
日本持田制药公司
生产厂家英文名:
Mochida | 
