英文药名：DINAGEST Tab（Dienogest） 中文药名：地诺孕素片 生产厂家：持田制药有限公司 DINAGEST(Dienogest 中文药名：地诺孕素片)-为治疗子宫内膜异位症的最先选择新药 ディナゲスト錠1mg 治疗类别名称 子宫内膜异位症的治疗剂 商標名 DINAGEST Tab. 1mg 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 诺孕素是白色结晶粉末，以淡黄白色。此产品微溶于甲醇，乙醇（99.5）微溶，并且几乎不溶于水。 熔点 210〜218℃ 药效药理 1. 作用机序 这种药物对孕酮受体选择性激动剂作用，相信通过卵巢功能抑制和子宫内膜细胞的生长抑制作用，以显示对子宫内膜异位症的有效性。 2. 对类固醇激素受体的影响 (1) 受体激动剂活性 使用与人类固醇激素受体基因转染的细胞在体外研究中，他们表现出对孕酮受体的选择性激动剂活性。 (2) 孕激素作用 使用大鼠和家兔体内研究显示对子宫孕行动。另一方面，雄激素作用，糖皮质激素作用和盐的动作并没有显示。 3. 卵巣机能抑制作用 (1) 健康成年女性 当口服此药每日2mg的21天给予健康的成年女性，崛起在正常月经周期血清看到雌二醇和孕酮浓度的抑制，血清LH和FSH浓度瞬时增加消失它接受。 (2) 子宫内膜异位症患者 当每日1-4mg的16-24周子宫内膜异位症患者口服，血清雌二醇水平呈低值，由于剂量的增加。此外，每天1-4毫克的这种药，血清孕酮浓度低于在所有情况下的卵泡期的参考值时，抑制排卵建议。 核定本剂剂量和给药是一种“口服分为每日两次为2mg。 4. 对子宫内膜的作用 (1) 子宫内膜细胞的增殖抑制效果 在使用人子宫内膜间质细胞在体外研究中，观察到细胞增殖的抑制。 (2) 子宫内假膜蜕膜 在患者子宫内膜异位症，当这种药物1天2毫克为16周口服给药，通过这种药物，观察孕激素作用，子宫内膜的蜕膜虚假临床药理试验。 5. 对子宫内膜异位症的影响 在子宫内膜异位症的大鼠和兔子，体积减小或重量在移植看到内膜件的增加的抑制的试验中，在子宫内膜异位症的治疗效果已建议。 适应症 用于治疗子宫内膜异位症 用法用量 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。 包装规格 1mg PTP：100錠  瓶：56錠 制造厂商 持田制药有限公司 地诺孕素(Dienogest)特点 地诺孕素(Dienogest)是德国Schering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。它具有疗效确切、毒副作用小等特点，正在成为口服避孕的首选药物。地诺孕素(dienogest)是一种混合型孕激素，它具有19- 去甲睾丸酮衍生物和孕酮衍生物的双重性质，并且兼具独特的药效学和药动学性质。地诺孕素(Dienogest)在结构上与传统19-去甲睾丸酮衍生物截然不同的是它具有17α-氰甲基基团的功效。 地诺孕素/炔雌醇 (DNG/EE)2mg/30pg的单相复合片由JnePaharmGmbH&Co.KG于1995年在德国首先上市，商品名Valette，用作口服避孕药，上市前临床的优良结果在上市后监察研究中的广大样本人群得到广泛证实，其避孕作用高且可靠，出血等不良反应低，耐受性亦相当好，所以现已成为德国市场上最畅销的复方口服避孕药。地诺孕素2mg与雌二醇戊酸酷2mg (EZv/DNG) 的复合片由德国ShcernigAG公司以商品Climodine于2002年上市，是第一个连续的用于治疗绝经后妇女的激素替代治疗(HRT)，效果显著。2007年该品种在日本上市，剂型为片剂，规格：1mg，用于治疗子宫内膜异位症。 完整资料附件：http://www.info.pmda.go.jp/go/pack/2499010F1023_1_08/ Dienogest 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. ForReference   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. ---------------------------------------------------------------------- 地诺孕素治疗膀胱子宫内膜异位症效果显著 深部子宫内膜异位症（Deep endometriosis，DE）表现为子宫内膜腺体及基质浸润其他脏器及盆腔腹膜后组织。 根据统计数据，膀胱子宫内膜异位症所占比率小于 4%，其诊断经常被延误，多在合并出现尿路感染、慢性尿道症状、膀胱过度活动症、外阴痛或间质膀胱炎后发现。对于膀胱子宫内膜异位症，外科手术治疗效果显著，但对于部分想要避免术后并发症或者经手术未能成功治愈的患者，还是需要药物治疗方法。 地诺孕素是一种耐受良好的新型孕激素制剂，其对于减轻子宫内膜异位症的疼痛症状效果显著。意大利卡利亚里大学妇产科的 Stefano 等作出的初步研究发现，诺孕素或许能够成为膀胱子宫内膜异位症的保守治疗方法，文章发表在 Gynecological Endocrinology 上。 研究入组的6名研究对象均存在相关症状，超声检查发现膀胱出存在小结节，并行膀胱镜检查术及膀胱组织活检确诊为膀胱子宫内膜异位症。她们在下个月月经来潮第一天开始口服地诺孕素 2mg/d，并其后在第 1、6及12个月作临床评估及疼痛问卷填写，第 3、12 个月时行经阴道超声检查测定膀胱内结节体积大小等。 结果发现，使用地诺孕素治疗后，膀胱子宫内膜异位症症状明显改善，并且膀胱内异症病灶体积显著减小。 对于子宫内膜异位的治疗，腹腔镜下病灶切除术是最有效的治疗手段，但过去多年的临床应用，其局限性也逐渐暴露，如复发率高、并发症多、对生育有不良影响等。本研究结果提示，对于治疗深部子宫内膜异位症，如膀胱子宫内膜异位症等，地诺孕素能够有效地减小病灶并改善症状。