英文药名：Viviant（Bazedoxifene Acetate tablets） 中文药名：醋酸巴多昔芬片 生产厂家：辉瑞制药 ビビアント錠20mg 类别名称 骨质疏松症治疗剂 批准日期：2010年7月23日 商標名 Viviant Tablets 一般名 バゼドキシフェン酢酸塩（Bazedoxifene Acetate） 化学名 1-｛4-［2-（Hexahydro-1H-azepin-1-yl）ethoxy］benzyl｝-2-（4-hydroxyphenyl）-3-methyl-1H-indol-5-ol monoacetate 分子式 C30H34N2O3・C2H4O2 分子量 530.65 構造式 性状 白色〜黄褐色の粉末である。 融点 约176℃ 分配系数（LogD） >3（pH6.56,1-オクタノール/水系） 药效药理 1. 对骨密度和骨强度的影响 在卵巢切除的大鼠模型中，6周口服给药作为巴多昔芬的结果，在为0.1mg/kg/天或更多胫骨密度降低，腰椎骨强度降低被抑制在为0.3mg/kg/天或更多。这些效应也出现在政府为一年。在猴子，巴多昔芬0.2〜18个月给药，结果为25mg/ kg/天，减少腰椎和胫骨由卵巢切除术的骨密度被抑制，骨密度的增加作用和骨强度改进巴多昔芬的积极的效果观察到的相关性。此外，巴多昔芬，抑制骨转换通过骨代谢指标和骨微结构的改变所指示的去卵巢猴子的提高。 2. 骨组织形式的影响 在卵巢切除的大鼠模型中，施用巴多昔芬为1.5mg/kg/天的一年抑制在松质骨小梁骨部体积减小，以形成与正常微结构的骨。此外，即使当巴多昔芬为25mg/ kg /天去势猴18个月，每月给药，观察到对骨微观结构产生不利影响。 3. 对骨折愈合的影响 使用巴多昔芬为1mg/kg/天在卵巢切除大鼠中，进行了检查愈伤组织形成和股骨骨折部位，正常骨痂形成，骨折愈合的过程，由维修或类似的骨强度支持的机械性能观察的不良影响。 4. 作用机序 巴多昔芬，是选择性雌激素受体调节剂（SERM）。这种药物是，结合到雌激素受体后，增强或抑制了根据组织的受体和活性。在骨，通过调节分化和破骨细胞功能的细胞因子，表明雌激素激动剂活性。此外，它显示了对脂质代谢的雌激素样作用。施用巴多昔芬一个（0.15〜1.5毫克/公斤/天）为一年到切除卵巢的老鼠，但子宫重量增加至溶剂对照组的约1.6倍于任何剂量的，在切除卵巢的猴子巴多昔芬（0.2〜25毫克/ kg /天）可能18个月给药，对生长的影响，和乳腺小叶组织重量子宫重量与本药物的给药未观察到。 适应病症 绝经后骨质疏松 用法用量 每日口服一次，每次为20mg。 包装规格 片剂：20毫克 100粒，140粒，500粒，700粒（PTP） 制造商： 辉瑞公司日本 完整处方资料附件：http://www.info.pmda.go.jp/go/pack/3999027F1020_1_05/ Viviant Tablets（Bazedoxifene acetate）醋酸巴多昔芬片/ビビアント錠20m Viviant Tablets 20mg（ビビアント錠20mg） Brand name : Viviant Tablets 20mg 　Active ingredient: Bazedoxifene acetate 　Dosage form: white to yellowish ash gray tablet, major axis 15.3 mm, minor axis 5.8 mm, thickness 5.2 mm 　Print on wrapping: ビビアント20mg, Viviant20mg, WY20 Effects of this medicine This medicine normalizes bone metabolic imbalance due to depressed secretion of female hormone (estrogen) in postmenopausal women. Consequently, improves the low bone mass and reduces the risk of bone fracture. Usually, used for treatment of postmenopausal osteoporosis. Before using this medicine, be sure to tell your doctor and pharmacist •If you ever experienced any allergic reaction (itch, rash etc.) to any medicine. If you have venous thromboembolism or a history of venous thromboembolism, antiphospholipid antibodies syndrome, a history of hypertriglyceridemia, or renal/liver dysfunction. If you are in a long-term bedridden or similar state, such as after a surgical operation or in a condition that requires long-term rest. •If you are pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>> •General dosage regimen: For adults, take 1 tablet (20 mg of the active ingredient) at a time, once a day. Strictly follow the instructions of your doctor/pharmacist. •If you missed a dose, take the missed dose as soon as possible. DO NOT take double doses to make up for the missed dose. •If you took too much of the medicine (more than ordered), check with your doctor/pharmacist. •Do not stop taking the medicine without the instructions of your doctor. Precautions while taking this medicine •Check with your doctor/pharmacist beforehand in case you are intending to be in a state of prolonged immobilization, such as travelling long distances by aircraft or by car. Possible adverse reactions to this medicine Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist: muscle spasm (muscle cramp), fibrocystic breast diseases (mastopathy, breast cyst), vasodilation (glow), leg cramp, etc. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •pain/swelling of the feet, sudden difficulty in breathing, shortness of breath, chest pain, sudden decrease of visual acuity [venous thromboembolism] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of the reach of children. Store away from direct sunlight, heat and humidity. •Discard the remainder. Do not store them. Pfizer Pharmaceuticals Inc.Internal Published: 10/2010 The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment. 巴多昔芬特点： 巴多昔芬(bazedoxifene)新一代SERM巴多昔芬，可竞争性抑制1713一雌二醇与雌激素受体ERoc和ER13的结合，对骨骼有雌激素激动剂活性，能改善脊椎和髋部的骨密度，故能显著降低骨质疏松症绝经妇女的椎骨骨折风险。其主要适应证为预防和治疗绝经期后骨质疏松症。目前进行的多中,L,III期临床研究显示，巴多昔芬联合雌激素可预防骨质丢失，且不会刺激乳腺或子宫。 对于具有正常或低BMD的健康绝经后妇女，SERM能在不刺激子宫内膜的情况下预防骨丢失和降低骨转换。在一项拥有了6847名绝经后骨质疏松症妇女的3年的RCT中（平均年龄66岁），每天20mg或40mg的巴多昔芬能分别使椎骨骨折的发生率降低42%和37%。但对非椎骨骨折无效。巴多昔芬治疗的耐受性与雷洛昔芬相似。与安慰剂组相比能使血管舒缩症状、VET和腿痛性痉挛的发生率增加。 巴多昔芬由惠氏原研，后转让给辉瑞制药，已经于2009年4月27通过欧洲药监局的批准在意大利和西班牙上市，商品名为Conbriza，2010年7月在日本上市，商品名为Viviant。