英文药名：PRADAXA KAPS(Dabigatran Etexilate) 中文药名：达比加群酯甲磺酸盐胶囊 药品说明 达比加群酯Pradaxa (dabigatran)由德国勃林格殷格翰公司开发，于2008年4月在德国和英国上市，2010年在美国上市，2011年在日本上市，用于伴有心律异常（心房纤维性颤动）的患者以预防中风和血液凝结。为近期成功开发的具有多种特点的新型抗凝血药物，这是继华法林之后50年来上市的首个新类别口服抗凝血药物，本品的上市，是抗凝血治疗领域和潜在致死性血栓预防领域的一项重大进展，具有里程碑意义。 血栓是人类健康的一大杀手，但与其他更加引人关注的疾病相比，普通民众对血栓造成的危害却知之甚少。仅静脉血栓栓塞症（VTE）每年就夺去欧盟地区50万人的生命，是该地区艾滋病、乳腺癌、前列腺癌和交通事故造成的总死亡人数的两倍多。 在美国，华法林（Warfarin）是目前唯一一只获得FDA批准，用来预防手术后VTE及心房颤动的口服抗血栓药物。 经过50多年的临床使用，已被证明是安全有效的。但是，华法林在使用时受到诸多限制，例如该药与许多常用药物及食品一起服用时会产生相互作用；该药的治疗作用必须由全科医生（GPs）利用国际标准化比率（INR）血液测试方法进行监测，以确保病人使用恰当而又安全的剂量。 新型药物的开发目标是，既要在疗效和安全性上与华法林媲美，又不会产生药物间的相互作用，而且最好不需治疗监测。 欧洲心脏病学会公布了长期抗凝治疗的随机评价，入选18113例卒中风险较高的房颤患者，比较不同剂量达比加群与常规剂量华法林的预防卒中的效果。随访1年，结果显示，与华法林相比，较高剂量达比加群（150mg，每日两次）可显著降低卒中风险34%；较低剂量达比加群（110mg，每日两次）预防卒中的效果与华法林类似，但大出血事件显著降低。因此达比加群在预防房颤患者卒中方面比华法林更有效，是近50年来最有希望的安全有效和令人信赖的口服抗凝药物，堪称房颤抗凝的新里程碑。这只口服的凝血酶抑制剂将远远超过同类药物，医生将会非常乐意使用此药来预防中风。RE-LY试验已经为我们显示了非常有希望的结果，与华法令相比，这只药物的疗效相当，并没有增加出血的风险和肝脏毒性，同时起效迅速和不需要监测凝血功能，这暗示着医生和患者将非常欢迎这只使用简单、可以替代华法令的药物。 达比加群酯是一种新型的合成的直接凝血酶抑制剂，是dabigatran的前体药物，属非肽类的凝血酶抑制剂。口服经胃肠吸收后，在体内转化为具有直接抗凝血活性的dabigatran。 dabigatran结合于凝血酶的纤维蛋白特异结合位点，阻止纤维蛋白原裂解为纤维蛋白，从而阻断了凝血瀑布网络的最后步骤及血栓形成。dabigatran可以从纤维蛋白一凝血酶结合体上解离，发挥可逆的抗凝作用。 达比加群酯口服用药后经胃肠道迅速吸收，用药后1h起效，2～3h即达血浆峰浓度，如果与食物同服，其血浆达峰时间后移。 总之，达比加群酯是直接凝血酶抑制剂，具有可以口服、强效、无需特殊用药监测、药物相互作用少等特点。体外、体内试验和临床各项研究均提示达比加群酯具有良好的疗效及药动学特性，临床应用前景乐观，其成功上市是抗凝血药物研究领域的一项重大突破。 适应证和用途 PRADAXA是一种直接凝血酶抑制剂适用于有非瓣膜性心房颤动患者中减低中风和全身栓塞的风险 剂量和给药方法 （1）对有CrCl>30 mL/min患者：150mg口服，每天2次 （2）对有CrCl 15-30 mL/min患者：75mg口服，每天2次 （3）指导患者不要咀嚼，弄碎，或打开胶囊 （4）复习对转换至或从其它口服或非肠道抗凝剂的建议 （5）当可能时在损伤性或手术操作前暂时停止PRADAXA，然后立即在开始 剂型和规格 胶囊：75mg和150mg 禁忌证 （1）活动病理性出血 （2）对PRADAXA严重超敏性反应史 警告和注意事项 出血的风险：PRADAXA可能引起严重和，有时，致命出血。及时评价失血的征象和症状暂时停止：避免治疗中过失以缩小中风的风险 P-gp诱导剂和抑制剂：避免利福平[rifampin]与PRADAXA同时给药因为对达比加群暴露的影响 不良反应 最常见不良反应(>15%)是胃炎-样症状和出血 在特殊人群中的使用 老年人使用：出血的风险随年龄增加 一般描述 达比加群酯甲磺酸盐，一种直接凝血酶抑制剂的化学名是β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate。分子量723.86(甲磺酸盐)，627.75(游离碱)。 MEDICATION GUIDE PRADAXA (pra dax' a) (dabigatran etexilate mesylate) capsulesRead this Medication Guide before you start taking PRADAXA and each time you get a refill. There may be new information. This Medication Guide does not take the place of talking with your doctor about your medical condition or your treatment. ----------------------------------------------------------------------------- What is the most important information I should know about PRADAXA? PRADAXA can cause bleeding which can be serious, and sometimes lead to death. This is because PRADAXA is a blood thinner medicine that lowers the chance of blood clots forming in your body. You may have a higher risk of bleeding if you take PRADAXA and: are over 75 years old have kidney problems have stomach or intestine bleeding that is recent or keeps coming back, or you have a stomach ulcer take other medicines that increase your risk of bleeding, including: aspirin or aspirin containing products long-term (chronic) use of non-steroidal anti-inflammatory drugs (NSAIDs) warfarin sodium (Coumadin®, Jantoven®) a medicine that contains heparin clopidogrel (Plavix®) prasugrel (Effient®) Tell your doctor if you take any of these medicines. Ask your doctor or pharmacist if you are not sure if your medicine is one listed above. PRADAXA can increase your risk of bleeding because it lessens the ability of your blood to clot. While you take PRADAXA: you may bruise more easily it may take longer for any bleeding to stop ----------------------------------------------------------------------------- Call your doctor or get medical help right away if you have any of these signs or symptoms of bleeding:unexpected bleeding or bleeding that lasts a long time, such as: unusual bleeding from the gums nose bleeds that happen often menstrual bleed or vaginal bleeding that is heavier than normal bleeding that is severe or you cannot control pink or brown urine red or black stools (looks like tar) bruises that happen without a known cause or get larger cough up blood or blood clots vomit blood or your vomit looks like "coffee grounds" unexpected pain, swelling, or joint pain headaches, feeling dizzy or weak Take PRADAXA exactly as prescribed. Do not stop taking PRADAXA without first talking to the doctor who prescribes it for you. Stopping PRADAXA may increase your risk of a stroke. PRADAXA may need to be stopped, if possible, for one or more days before any surgery, or medical or dental procedure. If you need to stop taking PRADAXA for any reason, talk to the doctor who prescribed PRADAXA for you to find out when you should stop taking it. Your doctor will tell you when to start taking PRADAXA again after your surgery or procedure. See "What are the possible side effects of PRADAXA?" for more information about side effects. ----------------------------------------------------------------------------- What is PRADAXA? PRADAXA is a prescription medicine used to reduce the risk of stroke and blood clots in people who have a medical condition called atrial fibrillation. With atrial fibrillation, part of the heart does not beat the way it should. This can lead to blood clots forming and increase your risk of a stroke. PRADAXA is a blood thinner medicine that lowers the chance of blood clots forming in your body. It is not known if PRADAXA is safe and works in children. ----------------------------------------------------------------------------- Who should not take PRADAXA? Do not take PRADAXA if you: currently have certain types of abnormal bleeding. Talk to your doctor, before taking PRADAXA if you currently have unusual bleeding. have had a serious allergic reaction to PRADAXA. Ask your doctor if you are not sure. ----------------------------------------------------------------------------- What should I tell my doctor before taking PRADAXA? Before you take PRADAXA, tell your doctor if you: have kidney problems have ever had bleeding problems have ever had stomach ulcers have any other medical condition are pregnant or plan to become pregnant. It is not known if PRADAXA will harm your unborn baby. are breastfeeding or plan to breastfeed. It is not known if PRADAXA passes into your breast milk. Tell all of your doctors and dentists that you are taking PRADAXA. They should talk to the doctor who prescribed PRADAXA for you, before you have any surgery, or medical or dental procedure. Tell your doctor about all the medicines you take, including prescription and nonprescription medicines, vitamins, and herbal supplements. Some of your other medicines may affect the way PRADAXA works. Certain medicines may increase your risk of bleeding. See "What is the most important information I should know about PRADAXA?" Especially tell your doctor if you take:rifampin (Rifater, Rifamate, Rimactane, Rifadin) Know the medicines you take. Keep a list of them and show it to your doctor and pharmacist when you get a new medicine. ----------------------------------------------------------------------------- How should I take PRADAXA? Take PRADAXA exactly as prescribed by your doctor. Do not take PRADAXA more often than your doctor tells you to. You can take PRADAXA with or without food. Swallow PRADAXA capsules whole. Do not break, chew, or empty the pellets from the capsule. If you miss a dose of PRADAXA, take it as soon as you remember. If your next dose is less than 6 hours away, skip the missed dose. Do not take two doses of PRADAXA at the same time. Your doctor will decide how long you should take PRADAXA. Do not stop taking PRADAXA without first talking with your doctor. Stopping PRADAXA may increase your risk of stroke. Do not run out of PRADAXA. Refill your prescription before you run out. If you plan to have surgery, or a medical or a dental procedure, tell your doctor and dentist that you are taking PRADAXA You may have to stop taking PRADAXA for a short time. See "What is the most important information I should know about PRADAXA?" If you take too much PRADAXA, go to the nearest hospital emergency room or call your doctor or the Poison Control Center right away. ----------------------------------------------------------------------------- What are the possible side effects of PRADAXA? PRADAXA can cause serious side effects.See "What is the most important information I should know about PRADAXA?" Allergic Reactions. In some people, PRADAXA can cause symptoms of an allergic reaction, including hives, rash, and itching. Tell your doctor or get medical help right away if you get any of the following symptoms of a serious allergic reaction with PRADAXA: chest pain or chest tightness swelling of your face or tongue trouble breathing or wheezing feeling dizzy or faint Common side effects of PRADAXA include:indigestion, upset stomach, or burning stomach pain Tell your doctor if you have any side effect that bothers you or that does not go away. These are not all of the possible side effects of PRADAXA. For more information, ask your doctor or pharmacist. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. ----------------------------------------------------------------------------- How should I store PRADAXA? Store PRADAXA at room temperature between 59°F to 86°F (15°C to 30°C). After opening the bottle, use PRADAXA within 30 days. Safely throw away any unused PRADAXA after 30 days. Store PRADAXA in the original package to keep it dry. Keep the bottle tightly closed. Keep PRADAXA and all medicines out of the reach of children. ----------------------------------------------------------------------------- General information about PRADAXA Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use PRADAXA for a condition for which it was not prescribed. Do not give your PRADAXA to other people, even if they have the same symptoms. It may harm them. This Medication Guide summarizes the most important information about PRADAXA. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about PRADAXA that is written for health professionals. ----------------------------------------------------------------------------- What are the ingredients in PRADAXA? Active ingredient: dabigatran etexilate mesylateInactive ingredients: acacia, dimethicone, hypromellose, hydroxypropyl cellulose, talc, and tartaric acid. The capsule shell is composed of carageenan, FD&C Blue No. 2, FD&C Yellow No. 6, hypromellose, potassium chloride, titanium dioxide, and black edible ink. 附件： 201011922485237.pdf  --------------------------------------------------------------- 注：以下产品不同规格和不同价格，购买时请以电话咨询为准！ --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: PRADAXA KAPS 150mg/cap 60caps/box 原产地英文药品名: DABIGATRAN ETEXILATE 原产地英文化合物名称: β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate 中文参考商品译名: PRADAXA胶囊剂 150毫克/胶囊 60胶囊/盒 中文参考药品译名: 达比加群酯 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ESPAÑA --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: PRADAXA KAPS 110mg/cap 60caps/box 原产地英文药品名: DABIGATRAN ETEXILATE 原产地英文化合物名称: β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate 中文参考商品译名: PRADAXA胶囊剂 110毫克/胶囊 60胶囊/盒 中文参考药品译名: 达比加群酯 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ESPAÑA --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: PRADAXA KAPS 110mg/cap 30caps/box 原产地英文药品名: DABIGATRAN ETEXILATE 原产地英文化合物名称: β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate 中文参考商品译名: PRADAXA胶囊剂 110毫克/胶囊 30胶囊/盒 中文参考药品译名: 达比加群酯 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ESPAÑA --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: PRADAXA KAPS 110mg/cap 10caps/box 原产地英文药品名: DABIGATRAN ETEXILATE 原产地英文化合物名称: β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate 中文参考商品译名: PRADAXA胶囊剂 110毫克/胶囊 10胶囊/盒 中文参考药品译名: 达比加群酯 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ESPAÑA --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: PRADAXA KAPS 75mg/cap 60caps/box 原产地英文药品名: DABIGATRAN ETEXILATE 原产地英文化合物名称: β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate 中文参考商品译名: PRADAXA胶囊剂 75毫克/胶囊 60胶囊/盒 中文参考药品译名: 达比加群酯 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ESPAÑA --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: PRADAXA KAPS 75mg/cap 30caps/box 原产地英文药品名: DABIGATRAN ETEXILATE 原产地英文化合物名称: β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate 中文参考商品译名: PRADAXA胶囊剂 75毫克/胶囊 30胶囊/盒 中文参考药品译名: 达比加群酯 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ESPAÑA --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: PRADAXA KAPS 75mg/cap 10caps/box 原产地英文药品名: DABIGATRAN ETEXILATE 原产地英文化合物名称: β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl] amino]iminomethyl] phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-,ethyl ester, methanesulfonate 中文参考商品译名: PRADAXA胶囊剂 75毫克/胶囊 10胶囊/盒 中文参考药品译名: 达比加群酯 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ESPAÑA