英文药名：Physuline（Mozavaptan Hydrochloride tablets） 中文药名：莫扎伐普坦片 生产厂家：大冢制药 フィズリン錠30mg 治疗类别名称 V2-受体拮抗剂 批准上市时间：2006年 欧文商標名 Physuline tablets 30mg 一般名： モザバプタン塩酸塩〔Mozavaptan Hydrochloride (JAN)〕 化学名： N-(4-{[(5RS)-5-(dimethylamino)-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl]carbonyl}phenyl)-2-methylbenzamide monohydrochloride 構造式： 分子式：C27H29N3O2・HCl 分子量：464.00 性 状： 它是一种白色的结晶性粉末。它易溶于二甲亚砜，它容易被微溶于甲醇和乙酸（100），和微溶于水，微溶于乙醇（99.5），并在己烷中几乎不溶。本产品（1→100）的甲醇溶液显示无旋光性。 融点： 約264℃（分解） 批准的条件 临床试验的患者是非常有限的，数据上市后，根据固定数目的情况下，直到它被集成在一起，以实现所有病例的利用效果的调查，此药物使用患者以及了解的背景资料，对这种药物的疗效和安全性等早期收集的数据，采取必要的措施，正确使用药物。 药效药理 1. 药理作用 (1) 加压素V2-受体拮抗剂 Mozabaputan盐酸，加压素V2-受体表达细胞和大鼠，在狗肾膜制剂，是标记的抗利尿激素的结合V2-至受体以依赖于浓度的方式抑制。 Mozabaputan盐酸在人加压素V2-受体表达细胞，表明没有cAMP产生增加本身，因为它抑制cAMP的产生由加压素，具有加压素V2-受体拮抗作用它已被证明。此外，观察到一些主要代谢物的加压素V2-受体拮抗作用。 抑制常数为人类加压素受体V2-，持平（9.42±0.85nM），M1（0.88±是0.11nm），M2（1.88±0.30nM），M3（6.59±0.50nM），M4（22.5±2.3纳米），是M5（24.3±3.0nM）。 (2) 利尿作用 Mozabaputan盐酸盐，清醒大鼠和狗的剂量依赖性增加尿量，降低尿渗透压。在清醒狗，不像呋是现有利尿，没有观察到对尿电解质排泄效果，观察到自由水清除增加。 (3) 在抗利尿激素分泌模型动物的行动综合征 Mozabaputan盐酸盐，在抗利尿激素分泌大鼠模型的综合征，表现为低钠血症的改善。 2. 作用机序 Mozabaputan盐酸盐是用于加压素V2-受体拮抗作用的药理学特征的药物，由肾脏血管加压素集合管抑制水的再吸收，选择性地排泄水，电解质排泄表明，不涉及在（水利尿作用）的增加利尿作用。 适应病症： V2阻抗剂:低钠血症治疗药，充血性心衰 剂量与用法 每日1次，每次30mg 包装规格 30mg*1片/盒 生产厂家： 大塚制药 完整处方资料附件：http://www.info.pmda.go.jp/go/pack/2139010F1029_1_10/ 莫扎伐普坦（Mozavaptan）—全球首个获批的非肽类血管加压素拮抗剂。本品由日本大塚制药株式会社研发，于2006年上市用于低钠血症的治疗，本品对血管加压素V2受体的选择性是V1受体的100倍。 本品为口服制剂，规格为30mg/片。由于本品在日本为罕见病用药，所以在获批的说明书中，本品的临床病例只有16例。其用法为每日1次，每次30mg。 PHYSULINE Tablets 30mg（フィズリン錠30mg）  Brand name : PHYSULINE Tablets 30mg 　Active ingredient: Mozavaptan hydrochloride 　Dosage form: white film-coated tablets, diameter: 6.1 mm, thickness: 2.9 mm 　Print on wrapping: ID Code: OG51, Description on the back: フィズリン錠 30mg Effects of this medicine This medicine normalizes potassium balance by acting on the kidneys to increase urination and excrete excess water from the body. It is usually used for the treatment of hyponatremia due to excessive fluid retention when restriction of fluid intake is ineffective. 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 have hepatic/renal dysfunction, hypotension, or hyperkalemia. If you have difficulty taking meals due to nausea associated with an underlying disease. •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 1 tablet (30 mg of the active ingredient) at a time, once daily after a meal. Strictly follow the instructions of your doctor and pharmacist. •In order to avoid nocturnal urination, take this medicine after breakfast or lunch. •If you miss a dose, take the dose as soon as possible. You should not 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 •Avoid taking this medicine when there is no restroom nearby, since you will need to urinate frequently for 6 hours after taking the medicine. •Be aware that your urination will increase in frequency and volume after taking this medicine. •Women of childbearing potential should use contraception to avoid pregnancy while taking this medicine. Contact your doctor immediately, if you are pregnant or suspect that you may be pregnant while on this medicine. •Take this medicine with continuing a therapy of restricting fluid intake (fluid restriction). Possible adverse reactions to this medicine The most commonly reported adverse reactions include thirst, decreased appetite, pollakiuria, malaise, and perioral edema. 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. No pertinent entries. 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. •Do not stop taking this medicine unless your doctor instructs you to do so. •If there is a remainder, this is to be discarded. Do not store it. Ask the pharmacist about how to discard it. Otsuka Pharmaceutical Co., Ltd.Internal Published: 9/2006 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.