英文药名：Samsca（Tolvaptan tablets/granules 1%） 中文药名：托伐普坦片和颗粒 1% 生产厂家：大冢制药 药品介绍 托伐普坦(商品名:Samsca)是由Otsuka公司开发非肽类AVP2受体拮抗剂，仅需一日1次口服。用于治疗高容或等容性低钠血症伴心力衰竭、肝硬化、抗利尿激素分泌异常综合征。也是唯一获准治疗该症的新药。 サムスカ錠7.5mg／サムスカ錠15mg／サムスカ錠30mg／※サムスカ顆粒1％ 药物分类名称 V2受体拮抗剂 批准日期：2013年6月 欧文商標名 Samsca tablets 7.5mg Samsca tablets 15mg Samsca tablets 30mg Samsca granules 1% 一般名：トルバプタン〔Tolvaptan (JAN)〕 化学名：N-{4-[(5RS)-7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl]-3-methylphenyl}-2-methylbenzamide 構造式： 分子式：C26H25ClN2O3 分子量：448.94 性　状： 它是白色晶体或结晶粉末。微溶于甲醇或乙醇（99.5），几乎不溶于水。该产品的甲醇溶液（1→50）不显示旋光度。 熔点：224至228℃ 批准条件 随着肾脏体积增加和肾脏体积快速增加，抑制常染色体显性多囊性肾的进展 1.能够正确使用的常染色体显性的充分了解肾囊肿治疗的风险和这种药物，这种药物，包括定期检查选择或待施用肝功能和血清钠浓度只能由医生开出，进一步，作为医疗机构和确认分配之前规定由医生后做了准备药房，走生产销售的必要措施。 2.上市后，直到存储一定数量的情况下的数据，由代理来实现所有患者上市后调查管理，这种药物的安全性和有效性在早期阶段收集性别数据，并采取必要措施正确使用该药物。此外，定期报告累积的结果。 药用药理学 1.药理作用 （1）血管加压素V2-受体拮抗作用 托伐普坦是人加压素V2-受体表达细胞和大鼠，在犬肾膜制备，和标记的抗利尿激素V2-到以浓度依赖性方式抑制该受体的结合。此外，在人的后叶加压素V2-受体表达细胞，它没有显示出增加的cAMP产生本身的，因为它抑制了生产由后叶加压素的cAMP显示出具有后叶加压素V2-受体拮抗作用是的。人血管加压素V2受体的抑制常数为0.43±0.06 nmol/L. （2）利尿作用 Tolvaptan在清醒的大鼠和狗中以剂量依赖性方式增加尿量和降低尿渗透压。此时，与袢利尿剂不同，游离水清除率为正值，游离水排泄增加（水利尿作用）。 （3）抗水肿作用 托伐普坦在大鼠水肿模型，角叉菜胶和诱导的爪水肿的增强和组胺引起的毛细血管通透性剂量依赖性地抑制。我们还在患有唤醒性心力衰竭和减少预负荷的狗中显示出利尿作用。 （4）腹水减少效果 托伐普坦在大鼠肝硬化腹水模型，体重降低和腹围指示腹水。 （5）囊性肾脏进展的抑制作用 托伐普坦是，PCY小鼠是多囊肾疾病的动物模型，Pkd2WS25/-抑制肾体积的小鼠和大鼠PCK的增加。 2.作用机制 托伐普坦是用于加压素V2-受体拮抗作用和药理学特征的试剂，通过在肾集合管被水重吸收抑制血管加压素，选择性地排泄水，电解质排泄的增加显示利尿作用（水利尿作用）。此外，在多囊性肾中，通过加压素抑制细胞内cAMP的升高抑制了肾脏体积和肾囊肿的增加。 适应症 片剂： 7.5毫克 ●与其他利尿剂（如袢利尿剂）在心力衰竭不足时保留液体。 ●肝硬化时液体潴留与其他利尿剂如袢利尿剂效果不佳。 ●抑制常染色体显性多囊性肾的进展，肾容量增加，肾容量增加快。 15毫克 ●与其他利尿剂（如袢利尿剂）在心力衰竭不足时保留液体。 ●抑制常染色体显性多囊性肾的进展，肾容量增加，肾容量增加快。 30毫克 ●抑制常染色体显性多囊性肾的进展，肾容量增加，肾容量增加快。 ※颗粒1％ ※与其他利尿剂如袢利尿剂在心力衰竭不足时流利。 * 肝硬化中的液体储存对其他利尿剂如袢利尿剂不够有效。 * 抑制常染色体显性多囊性肾的进展，肾脏体积增加，肾脏体积增加速度快。 用法与用量 ●在心力衰竭时储存液体。 通常，每天一次口服给予15mg托伐普坦。 肝硬化液体积聚 通常，每天一次口服7.5mg托伐普坦。 ●在抑制常染色体显性多囊性肾的进展的情况下 通常，口服给药开始时，托伐普坦分为两个剂量（早晨45毫克，晚上15毫克），成人60毫克/天。如每天服用60毫克的剂量超过1周，如有耐受性，90毫克/天（早上60毫克，晚上30毫克），120毫克/天（早上90毫克，晚上30毫克） 逐步增加。另外，根据适当的耐受性增加或减少，最大剂量应高达每天120毫克。 包装 片剂 7.5毫克：[PTP] 20片（10片×2），100片（10片×10） 15毫克：[PTP] 20片（10片×2），100片（10片×10） 30毫克：[PTP] 10片（10片x 1） ※颗粒1％：[塑料瓶] 30克 制造供应商 大冢制药有限公司 注：以上中文资料不够完整，使用者以原资料为准。 完整资料附件：http://www.info.pmda.go.jp/go/pack/2139011D1022_1_02/ SAMSCA（Tolvaptan tablets サムスカ錠） SAMSCA tablets 15mg [Autosomal dominant polycystic kidney disease]（サムスカ錠15mg［常染色体显性多囊肾病］） Brand name : SAMSCA tablets 15mg [Autosomal dominant polycystic kidney disease] 　Active ingredient: Tolvaptan 　Dosage form: blue tablet, diameter 8mm, thickness 3.1mm 　Print on wrapping: （Front）サムスカ錠, Otsuka, 15mg（Back）サムスカ錠15mg SAMSCA tablets 30mg（サムスカ錠30mg）  Brand name : SAMSCA tablets 30mg 　Active ingredient: Tolvaptan 　Dosage form: blue square tablet, length of a side : 7.4 mm, thickness: 3.1 mm 　Print on wrapping: （Front）サムスカ錠, Otsuka, 30mg（Back）サムスカ錠30mg SAMSCA tablets 7.5mg [Autosomal dominant polycystic kidney disease]（サムスカ錠7.5mg［常染色体显性多囊肾病］） Brand name : SAMSCA tablets 7.5mg [Autosomal dominant polycystic kidney disease] 　Active ingredient: Tolvaptan 　Dosage form: blue tablet, major axis : 7.7 mm, minor axis: 4.4 mm, thickness: 2.6 mm 　Print on wrapping: （Front）サムスカ錠, Otsuka, 7.5mg（Back）サムスカ錠7.5mg Effects of this medicine This medicine inhibits the action of vasopressin in the kidney and lessens cystic enlargement. It is usually used to slow the progression of rapidly enlarging autosomal dominant polycystic kidney disease in which the kidneys has already become enlarged. 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 unable to sense thirst or have impaired fluid intake, hypernatremia or renal disorder, liver dysfunction or a history thereof, including chronic hepatitis and drug-induced liver dysfunction, coronary artery disease, cerebrovascular disease, hyperkalemia, hyponatremia, or dehydration symptom. •If you are pregnant, possibly 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, start with 8 tablets (60 mg of the active ingredient) a day in 2 divided doses, 6 tablets (45 mg) in the morning and 2 tablet (15 mg) in the evening. Take 60 mg a day for 1 week or longer. If you show tolerability (if you are able to continue treatment), the dose will be increased stepwise at intervals of at least 1 week, first to 12 tablets (90 mg: 8 tablets [60 mg] in the morning and 4 tablets [30 mg] in the evening) a day and then to 16 tablets (120 mg: 12 tablets [90 mg] in the morning and 4 tablets [30 mg] in the evening) per day. The dosage may be adjusted according to the tolerability, but it should not exceed 16 tablets (120 mg) a day. In the evening, take the medicine 4 hours before going to bed to avoid frequent urination during the night. Strictly follow the instructions. •If you miss a dose, take the missed dose as soon as you remember it. However, if it is close to the time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time. •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. Precautions while taking this medicine •If you feel thirst, drink enough water to prevent dehydration. Drink 1 or 2 glasses of water before going to bed and drink water whenever you urinate during the night. Always try to drink water as frequently as possible. •This medicine increases both urine volume and urination frequency and should therefore be used with caution as directed. •Women of childbearing potential should use contraception to avoid pregnancy while taking this medicine. Contact your doctor immediately if you discover that you are pregnant while on this medicine. •This medicine may cause syncope and dizziness and caution is therefore required to avoid falling accidents. In particular, you should refrain from working in high places or operating potentially hazardous machinery, including motor vehicles, while on this medicine. •Avoid drinking grapefruit juice since it may enhance the effect of this medicine. •Avoid taking health foods containing hypericum perforatum (St. John's wort) since it may reduce the therapeutic effect of this medicine. •As periodic hepatic function tests and serum sodium concentration measurements are necessary while on this medicine, follow the instructions of your doctor. Possible adverse reactions to this medicine The most commonly reported adverse reactions include thirst, frequent urination, excessive urination, headache, polydipsia and constipation. 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. •decrease of urine output, swelling, thirst [renal failure] •localized pain, pressured pain, erythema [thromboembolism] •mental confusion and hyperventilation, dehydration symptoms such as thirst, decreased consciousness (in serious cases, coma) [hypernatraemia] •general malaise, loss of appetite, yellowing in skin and white of eyes [liver dysfunction] •decreased blood pressure, hives, respiratory distress [shock, anaphylaxis] 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 moisture. •If there is a remainder, this is to be discarded. Do not store it. Ask your pharmacist or medical institution about how to discard it. Otsuka Pharmaceutical Co., Ltd.Internal Published: 3/2014 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