福沙匹坦二甲葡胺EMEND INJECTION(Fosaprepitant DIMEGLUMINE)

药店国别： 产地国家：加拿大 处方药：是 所属类别： 150毫克/瓶 包装规格： 150毫克/瓶 计价单位：瓶 生产厂家中文参考译名： 生产厂家英文名：Merck & Co., Inc. 　原产地英文商品名：EMEND IV INJ 150MG/vial 原产地英文药品名：Fosaprepitant DIMEGLUMINE 　中文参考商品译名：EMEND IV注射剂 150毫克/瓶 中文参考药品译名：福沙匹坦二甲葡胺 曾用名： 简介：美国FDA批准默克公司的福沙吡坦二甲葡胺注射剂(fosaprepitantdimeglumine，Emend)上市，与其它止吐药联用静脉注射防治中等催吐和大剂量催吐的抗癌药化疗(包括大剂量顺铂)初始和反复用药引起的急性和迟后的恶心和呕吐。本品是阿瑞吡坦(aprepitant)口服制剂的前体药物，注射后在体内迅速转化成阿瑞吡坦。美国FDA批准福沙吡坦二甲葡胺注射剂上市是基于临床研究显示，本品115mg注射后与口服瑞吡阿坦胶囊125 mg呈生物等效性。 不良反应 为输注部位疼痛(7.6%)、输注部位硬结(1.5%)和头痛(3%)。由于福沙吡坦二甲葡胺注射后在体内转化成瑞吡阿坦，因此口服制剂出现的不良反应在注射剂中也会发生，如倦困、恶心、打呃、便秘、腹泻、食欲减退、头痛和掉发。 作用机制 福沙吡坦二甲葡胺与瑞吡阿坦属于称作人P物质/神经激肽1(NK-1)选择性高亲和性受体阻断剂，主要通过阻断大脑恶心和呕吐信号。瑞吡阿坦对5-羟色胺(5-HT3)、多巴胺和糖皮质激素受体极微弱或无亲和性。 适应症 用于治疗化疗诱导的恶心和呕吐及术后恶心和呕吐。瑞吡阿坦在动物模型上显示通过中枢神经作用抑制诸如顺铂等细胞毒化疗药物诱导的呕吐。瑞吡阿坦以动物和人正电子发射断层照相术(PET)研究表明，药物穿过血脑屏障并占据了脑NK-1受体。对动物和人的研究显示，瑞吡阿坦增大5-HT3受体阻断剂昂丹司琼和糖皮质激素地塞米松的止吐作用，抑制顺铂诱导的急性期和迟后期呕吐. 福沙匹坦二甲葡胺英文版说明书 EMEND 150 MG 10ML IV INJ VIAL 1'SEMEND INJECTION RxGeneric Name and Formulations:Fosaprepitant dimeglumine (prodrug of aprepitant) 115mg/vial, 150mg/vial; lyophilized pwd for IV infusion after reconstitution and dilution; contains polysorbate 80.Company:Merck & Co., Inc.Indications for EMEND INJECTION:In combination with other antiemetic agents to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of moderately to highly emetogenic cancer chemotherapy, including high-dose cisplatin.Adult:≥18yrs: Give with corticosteroid and 5-HT3 antagonist (see literature). Give approx. 30min prior to chemotherapy. Highly emetogenic: Single-dose regimen: 150mg IV over 20–30min on Day 1. Moderately or highly emetogenic: 3-Day regimen: 115mg IV over 15 min on Day 1, then Days 2 and 3: 80mg orally once daily in the AM.Children:<18yrs: not recommended.See Also:EMENDContraindications:Concomitant pimozide, cisapride.Warnings/Precautions:Not for chronic continuous use. Severe hepatic insufficiency. Pregnancy (Cat.B). Nursing mothers: not recommended.Interactions:See Contraindications. Monitor, and caution with, CYP3A4 substrates, including chemotherapy agents (eg, ifosfamide, vinblastine, vincristine); CYP3A4 inhibitors (eg, azole antifungals, macrolides, nefazodone, ritonavir, nelfinavir, diltiazem); and with CYP3A4 inducers (eg, carbamazepine, phenytoin, rifampin). Potentiates dexamethasone (reduce its dose by 50%), methylprednisolone (reduce its IV dose by 25% and its oral dose by 50%), midazolam, alprazolam, triazolam. May antagonize warfarin (closely monitor INR for 2 weeks after starting each regimen); phenytoin, tolbutamide, other CYP2C9 substrates; paroxetine, oral contraceptives (use alternative or backup method during and for 1 month after last dose).Adverse Reactions:Asthenia, fatigue, hiccups, ALT/AST increased, headache, constipation, anorexia, GI upset, eructation, hypotension, pruritus, pyrexia. Injection: inj site pain.How Supplied:Caps 40mg—1; Bi-fold pack (2 x 80mg)—1; Tri-fold pack (1 x 125mg + 2 x 80mg)—1; Vial—1