英文药名：Baraclude Tablets（Entecavir hydrate） 中文药名：博路定片（恩替卡韦水合物） 生产厂家：Bristol-Myers Squibb バラクルード錠0.5mg 治疗类别名称 抗病毒化疗药物 批准日期：2006年9月 欧文商標名 Baraclude Tablets 一般名 エンテカビル水和物（Entecavir Hydrate） 化学名 9-[(1S,3R,4S)-4-Hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]guanine monohydrate 分子式 C12H15N5O3・H2O 分子量 295.29 構造式 性状 恩替卡韦水合物是淡黄白色粉末白色。水，略溶于甲醇或乙醇（99.5）。 药效药理 1.作用机制 恩替卡韦是一种鸟嘌呤核苷类似物，对HBV DNA聚合酶和选择性的抑制活性强效（Ki值：0.0012μM）拥有。这种药物在细胞中，在与活性卡韦三磷酸改变磷酸化。 恩替卡韦三磷酸，通过与天然底物脱氧核苷三磷酸，HBV DNA聚合酶（1）启动;（2）在mRNA负链DNA合成反转录，及（3）加乙型肝炎病毒DNA的链竞争以抑制所有三种合成的功能活性的。磷酸α，β，在δ和ε和线粒体DNA聚合酶γ抑制效果的恩替卡韦三层细胞的DNA聚合酶是弱（Ki值：18至约160μM）。 2.抗病毒活性 恩替卡韦抑制乙肝病毒转染人肝HepG2细胞乙肝病毒DNA的合成，该EC50值为0.004μM4）。恩替卡韦为HIV-1的标准菌株和临床分离的EC 50值是在过量0.026〜10.mu.M的浓度，当在必要的HIV感染量的最小量测试中，观察到抑制活性小于1μM。在细胞培养研究中，恩替卡韦被选择以μM级的高浓度的M184I突变。此外，艾滋病病毒具有变异M184V表现出敏感性降低恩替卡韦。 当观察到恩替卡韦慢性感染土拨鼠天天在鸭乙型肝炎病毒感染鸭或每周重复给药的土拨鼠肝炎病毒，标志着病毒DNA含量（4〜8log10）减少。在使用土拨鼠，每周一次在0.5毫克/公斤（临床剂量为1mg当量）的恩替卡韦长期维持给药试验三年反复口服给药，结果，在给药期间的DNA的病毒量保持低于检测极限这是（PCR法）。此外，具有耐HBV DNA聚合酶也是任何在三年的给药动物的变化没有观察到，增加存活和抑制这些动物的肝癌发病已由恩替卡韦的治疗中。 3.耐药性 (1) 体外试验 在与HBV DNA聚合酶的氨基酸残基的特性的突变（rtM204V/ I，rtL180M）拉米夫定耐药HBV，但恩替卡韦灵敏度在1mg的施用减少到1/8或更小相比，野生型等离子体在细胞外浓度反映了中期恩替卡韦的浓度，细胞内三磷酸恩替卡韦被认为超越充分抑制拉米夫定耐药型HBV DNA聚合酶活性的浓度。在重组病毒编码rtN236T或阿德福韦rtA181V抗性突变，11易患恩替卡韦维持）。从无效获得乙肝病毒隔离治疗恩替卡韦和拉米夫定是不応患谁了敏感性阿德福韦体外，但观察到拉米夫定的敏感性。 (2) 体内试验（国内临床效果） 核苷类似物初治患者谁被给予最高148星期后81例（AI463-047，-053试验和连续性测试-060）和拉米夫定不応患人获得恩替卡韦164例（AI463-052测试和连续性测试-060）评价可能进行了研究恩替卡韦抗性相关基因突变（HBV DNA的重量为400拷贝/毫升或更多）样品（ETVr）（表8和。此外，例如核苷类似物未经治疗的患者164案件选自66和拉米夫定不応患的41案件出81例，其中施用的批准剂量为0.5mg和1mg的继续比在试验的开始，和其它情况下，直到迁移继续测试-060，施用低剂量。 应当指出，在海外有类似的趋势。 适应症 病毒的肝功能的乙型肝炎病毒的乙型肝炎增殖生长抑制伴随着异常已经证实B型慢性肝病。 用法与用量 饭前后两个多小时口服空腹。，每天一次，每次0.5mg口服给药。此外，对难治的患者配合拉米夫定给药，它建议口服给药每天一次1mg的如恩替卡韦。 包装规格 片：0.5毫克  PTP 70片 制造厂商 施贵宝有限公司 完整资料附件： http://www.info.pmda.go.jp/go/pack/6250029F1024_1_14/ Baraclude Tablets（Entecavir hydrate）恩替卡韦水合物 Baraclude Tablets 0.5mg（バラクルード錠0.5mg）  Brand name : Baraclude Tablets 0.5 mg 　Active ingredient: Entecavir hydrate 　Dosage form: white, triangular shaped film-coated tablet, perpendicular 8.4 mm, thickness 3.7 mm 　Print on wrapping: (Face) Baraclude 0.5 mg, BMS 1611, (Back) バラクルード 0.5 mg Effects of this medicine This medicine may lower the ability of HBV to multiply infect new liver cell and lower the amount of HBV in the body. It is usually used to treat chronic hepatitis B or hepatitis B with cirrhosis. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines. •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)) •In general, for adults, take one tablet (0.5 mg of entecavir) at a time, once daily on an empty stomach (avoid to take a medicine within 2 hours before and after meals). If other medicine (lamivudine) does not work well, the dosage may be adjusted to 2 tablets (1 mg) at a time, once daily. Strictly follow the instructions. •If you miss a dose, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at the same time. Keep your regular dosing schedule. Ask your doctor or pharmacist when you are not sure what to do. •If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist. •Do not stop taking this medicine unless your doctor instructs you to do so. In general, it is necessary to take this medicine for a long period of time. Strictly follow the instructions of your doctor or pharmacist, since your disease may worsen if you discontinue your medication by your own decision. Precautions while taking this medicine •Possible adverse reactions to this medicine The most commonly reported adverse reactions include headache, diarrhea, inflammation of nose and throat, back pain and sleeplessness. If any of these symptoms occur, consult with your doctor or pharmacist. 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. •general malaise, nausea, vomiting, itching, yellow discoloration of the white of eyes/skin/urine [hepatic function disorder, exacerbation of hepatitis after discontinuation] •general malaise, rash, itching of skin, shortness of breath, breathlessness [anaphylactoid symptoms] •general malaise, feeling queasy, vomiting, abdominal pain, breathlessness [lactic acidosis] 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 infants and children. Store at room temperature (1 to 30 degrees Celsius). Store away from light and moisture. •Discard the remainder. Do not store them. Ask your pharmacist or medical institution how to discard them. Bristol-Myers SquibbInternal Revised: 2/2016 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.