英文药名： Simulect(basiliximab) 中文药名： 注射用巴利昔单抗 舒莱 品牌药生产厂家：Novartis Pharma Schweiz AG 药品介绍； 舒莱是兼有人源性和鼠源性的嵌合性单克隆抗体，能抑制白介素-2介导的T淋巴细胞激活，抑制排斥反应过程中细胞免疫的关键通道,具有较强的互补免疫抑制作用,临床应用有较好的耐受性,用于预防首次肾移植术后早期急性器官排斥反应。 通用名：注射用巴利昔单抗 英文名：Basiliximab for Injection 汉语拼音：Zhusheyong Balixidankang 【成分】本品主要成分为巴利昔单抗。 【药物分类】免疫抑制剂 【性状】本药除活性成分外，还含有以下赋形剂 ：亚磷酸二氢钾、磷酸氢二钠、氧化钠、蔗糖、甘糖醇、甘氨酸等。本品不含防腐剂。外观为白色冻干物。 【药理作用】巴利昔单抗是一种鼠/人嵌合的单克隆抗体(1gG1K)。它能定向拮抗白细胞介素-2（IL-2）的受体α链（CD25抗原），CD25抗原在抗原的激发反应中，表达于T-淋巴细胞表面。激活的T-淋巴细胞对IL-2具极高的亲和力，巴利昔单抗则能特异地与激活的T-淋巴细胞上的CD25抗原结合，从而阻断T-淋巴细胞与IL-2结合，亦即阻断了使T-细胞增殖的信息。在血浆巴利昔单抗浓度超过0.2微克/毫升时，就能完全和稳定地阻断IL-2受体。当血药浓度降至0.2微克/毫升以下时，CD25抗原的表达约在1-2周内回复到治疗前水平。本品不会造成细胞因子释放或骨髓抑制。 临床研究 ：在多项安慰剂对照研究中，已证实了巴利昔单抗在肾移植中预防器官排斥的作用。二项重要的为期12个月的多中心研究显示，巴利昔单抗、环孢素微乳剂及皮质激素合用组与安慰剂组的对比表明，巴利昔单抗能显著减少急性排斥的发生。对268名接受巴利昔单抗的病人所作的抗个体基因型抗体的测试中，仅1例发生抗个体基因抗体反应。在另一项接受巴利昔单抗的172名病人的临床试验中，仅6例（3.5%）发生HAMA（人体抗鼠抗体）反应。 【药代动力学】已在肾移植病人中进行了单剂量和多剂量的药代动力学研究，其累积剂量为15-150 mg。 吸收 ：在静脉推注巴利昔单抗20 mg后的30分钟内，其血浆峰浓度为7.1±5.1 mg/L，随着单次剂量增加至60 mg的最高量时，其血药峰浓度及曲线下面积均成比例地增加。 分布 ：巴利昔单抗的稳态分布容积为8.6±4.1 L。其向人体各部位分布的范围和程度尚未全面研究。体外研究显示，巴利昔单抗仅与淋巴细胞以及巨噬细胞/单核细胞结合。 排泄 ：终未半衰期为7.2±3.2天，人体清除率为41±19 mL/小时。 在病人中的特点 ：在成人患者中，体重或性别对分布容积或清除率无具临床意义的影响。消除半衰期不受年龄（20-69岁）、性别或种族的影响。尚无巴利昔单抗用于新生儿或不足2岁幼儿的资料。一项对8名2-12岁的儿科肾移植病人的临床研究显示，其中央分布容积为1.7±0.6 L，半衰期为9.4±4.9天，清除率为20±4 mL/小时。清除率和分布容积不受年龄（2-12岁）、体重（9-37公斤）或体表面积（0.44-1.20平方米）的影响。 本品在成人肝移植病人中的特点是呈稳态分布，其分布容积为7.5±2.5 L，半衰期为4.1±2.1天，清除率为75±24 mL/小时，药物的消除，主要是药物经引流的腹水和手术后的出血而丢失。可以弥补这种较快清除率的是这些病人的受体饱和浓度阈值较低，为0.1 ug/mL。因此，在所推荐的巴利昔单抗剂量水平内，对IL-2Rα阻断的持续时间与在肾移植成人中所获得的时间相似。 【毒理研究】对敏感兔模型静脉注射巴利昔单抗，剂量高至4 mg/mL，未见局部刺激性。恒河猴静脉注射巴利昔单抗，剂量高达5 mg/kg，每周2次，共4周，未见毒性。而此最高剂量所产生的血药浓度已经是在肾移植病人中与其他免疫抑制剂联合应用的巴利昔单抗推荐剂量所产生的Cmax的20倍，在猕猴交媾后，即静脉推注巴利昔单抗，最高量达5 mg/kg，每周2次。于此用药后的100天胚胎器官发生期间，未见本品对母体、胚胎产生毒性或有致畸性。 在离体实验中，未见可能的致遗传突变性。 【适应症】巴利昔单抗用于预防首次肾移植术后早期急性器官排斥反应。本品通常与环孢素微乳剂及含皮质激素为基础的免疫抑制剂联合使用。 【用法用量】 成人 推荐剂量 ：标准总剂量为40 mg，分2次给予，每次20 mg。首次20 mg应于术前2小时内给予，第二次20 mg应于移植术后4天给予。如果发生术后并发症，如移植物失功等，则应停止第二次给药。 体重≥ (greater than or equal to) 40 kg的儿童 ，总量为40 mg，分2次给予，每剂20 mg。体重< 40 kg儿童 ：总量为20 mg，分2次给予，每剂10 mg。首次应于术前2小时内给予，第二次用药应于移植术后4天给予。如果发生术后并发症，如移植物失功等，则应停止第二次给药。 经配制后的巴利昔单抗，既可在20-30分钟内作静脉滴注，也可一次性静脉推注。 【不良反应】巴利昔单抗既不会增加因器官移植病人的基本疾病所导致的不良事件，也不会增加因同时服用免疫抑制剂或其它药物所发生的不良事件。在两项对照试验中，接受推荐用量的巴利昔单抗的363名病人的不良事件发生率与359名接受安慰剂的对照病人相比，两者无差别。两组最常见的不良事件（大于20%）为便秘、尿道感染、疼痛、恶心、外周性水肿、高血压、贫血、头痛以及高血钾。该结果与94名接受巴利昔单抗推荐剂量的非对照性试验的结果相似。在静脉注射巴利昔单抗期间及以后，未见细胞因子释放综合征出现，故不必使用激素预防。 【禁忌症】对巴利昔单抗以及处方中其它任何成分过敏者均禁用。 【注意事项】巴利昔单抗仅限于对器官移植术后进行免疫抑制治疗有经验的医师使用。除环孢素微乳剂及皮质激素外，巴利昔单抗与其它免疫抑制剂合用的经验有限。在所推荐的剂量范围内，巴利昔单抗在为数不多的病人中与硫唑嘌呤联合使用过。另外，一项应用巴利昔单抗的病人曾在移植术后的不同时间接受过马替麦考酚酯或抗体治疗，例如OKT3或ATG/ALG，而这些病人并未出现过度免疫抑制的症状。不过，除了环孢素微乳剂及皮质激素外，巴利昔单抗与其它免疫抑制剂合用时，有增加过度免疫抑制的可能。 对驾驶和操作机械能力的影响 本品对驾驶和操作机械的能力无影响。 【孕妇及哺乳期妇女用药】尚未在妊娠或哺乳妇女中进行本品的研究。由于巴利昔单抗是一种免疫球蛋白G(IgG1k)，它可以透过胎盘以及经乳汁排出，故妊娠妇女不应使用本品，除非本品对母亲的可能益处远超过对胎儿的潜在危险。妇女在接受第二次巴利昔单抗后的8周内，不应授乳。 【儿童用药】巴利昔单抗用于儿童的经验有限。推荐剂量见“用法用量”。 【老年患者用药】巴利昔单抗用于老年人的资料有限，但无证据显示老年人的用量与年轻人不同。 【药物相互作用】由于巴利昔单抗是一种免疫球蛋白，故不存在代谢后的药物与药物间的相互作用。在应用巴利昔单抗的病人中，其人体抗鼠抗体（HAMA）的反应罕见（3.5%）。但巴利昔单抗不能阻断随后用鼠抗淋巴细胞抗体处理后的反应。 【药物过量】在多个临床试验中，给予受试人单次剂量高达60 mg，以及在24天内多次累积剂量达150 mg，未见急性不良反应。在对恒河猴以巴利昔单抗5 mg/kg，每周2次的4周观察试验中，其血药浓度可达170 ug/mL，未见明显的不良反应，而所推荐的巴利昔单抗剂量水平用于人体时，其所产生的血药浓度一般低于10 ug/mL。 【用药须知】 每盒巴利昔单抗包装内另配1支5 mL注射用水。向瓶内加入5 mL注射用水，以配制静脉滴注/注射液，轻摇小瓶使粉末溶解。溶液一经配制，应尽快使用，在室温下可保存4小时 ；2-8°C 冰箱可保存24小时。若配制液于24小时内未被应用，则将其丢弃。 所配制的巴利昔单抗溶液是等渗的，可用作一次性静脉推注，也可用生理盐水或5%葡萄糖将它稀释至50 mL或以上，以用作静脉滴注。因无巴利昔单抗与其它静脉注射物质的配伍禁忌资料，故巴利昔单抗不应与其它药物/物质混合使用，且通常应使用单独的输液系统给药。 【贮藏/有效期】 冷藏条件下（2-8°C）运输和贮存。有效期3年。 Medication name Generic name: Basiliximab - Injection Brand name(s): Simulect Uses Basiliximab is used to prevent organ rejection in people who have received a kidney transplant. It is usually taken along with other medications (e.g., cyclosporine, corticosteroids) to allow your new organ to function normally. Basiliximab is an immunosuppressant drug known as a monoclonal antibody. It works by slowing down your body's defense system (immune system) to prevent your body from rejecting the new kidney after surgery (acute rejection). How to use This medication is given by injection into a vein by a health care professional. It is usually given in 2 doses. The first dose is given within 2 hours before the transplant surgery, and the second dose is given 4 days after surgery.Dosage is based on your age, weight, medical condition, and response to treatment.This medication is used with other medications (e.g., cyclosporine, corticosteroids) to prevent rejection of transplanted organs. Take all medications exactly as prescribed by your doctor. If you have any questions, ask your doctor or pharmacist. Precautions Before using basiliximab, tell your doctor or pharmacist if you are allergic to it; or to mouse proteins; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: certain infection (cytomegalovirus).Previous treatment with basiliximab may increase your risk of a serious allergic reaction (see Side Effects section). Before using this medication, tell your doctor or pharmacist if you have received basiliximab in the past. If you must stop using this drug due to an allergic reaction, do not use the drug again. Consult your doctor or pharmacist for more details.Before having surgery, tell your doctor or dentist that you are using this medication.Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose.Wash your hands well to prevent the spread of infections.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor. Women who may become pregnant should use effective birth control before beginning treatment with this drug, during use, and for 4 months after finishing treatment. Consult your doctor or pharmacist for more information.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding. Drug interactions Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval. Side effects Nausea, stomach pain, diarrhea, constipation, or pain/redness at the injection site may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.The use of medications that affect the immune system may lead to increased risk of infection or certain types of cancer. Tell your doctor right away if you have any serious side effects, including: fever, weakness, swollen glands, night sweats, unusual lumps, persistent cough/sore throat, sores around the mouth/genitals, pain with urination, vision changes, unexplained weight loss.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, unusually fast heartbeat, sneezing, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. Missed dose For the best possible benefit, it is important to receive each scheduled dose of this medication as directed. If you miss a dose, contact your doctor immediately to establish a new dosing schedule. Overdose If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center. Notes Laboratory and/or medical tests (e.g., kidney function) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details. Medical alert Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-800-854-1166 (USA) or 1-800-668-1507 (Canada). Storage Not applicable. This medication is given in a clinic and will not be stored at home. Photos by medication strength Click the "Photos" link to see sample photographs for a specific medication strength. Common strengths Simulect 10 mg IV Solution Simulect 20 mg IV Solution The photos shown are samples only. Not all photos of the drug may be displayed. Your medication may look different. If you have questions, ask your pharmacist. Important note HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs. Information last revised October 2010 Copyright(c) 2010 First DataBank, Inc. Intravenous Recon Soln Basiliximab| Kidney Transplant Rejection Prophylaxis|Renal Transplant Rejection Prophylaxis|Cardiac Transplant Rejection Prophylaxis|Heart Transplant Rejection Prophylaxis|Lung Transplant Rejection Prophylaxis| Prevent Kidney Transplant Rejection|Prevention of Cardiac Transplant Rejection|Prevention of Lung Transplant Rejection| Selected from NATIONAL DRUG DATA FILE (NDDF) data included with permission and copyrighted by First DataBank, Inc., 2012. This copyrighted material has been downloaded from a licensed data provider. The above information is intended to supplement, not substitute for, the expertise and judgment of your health care professional. You should consult your health care professional before taking any drug, changing your diet, or commencing or discontinuing any course of treatment. 舒莱是一种含有单克隆抗体——巴利昔单抗的治疗用药物，能够预防机体免疫系统对移植器官的排异。    对于易于发生排异的移植器官，在移植术的围手术期，两剂的舒莱将在最初的数周内，提供给移植器官更多的保护。   舒莱被指定用于成人和儿童的肾脏移植中。 作用原理   ·免疫系统保护机体对抗外来“入侵者（细菌或病毒）”。并将移植器官也认为“入侵者”进行攻击和排斥。   ·在免疫系统对抗入侵者的战役中，T淋巴细胞扮演了一个重要的角色。T淋巴细胞一般呈静止状态，当遇有入侵者产生的化学物质时，T淋巴细胞被激活。而刺激T淋巴细胞激活的一个重要化学物质是IL-2。舒莱阻断静息状态的T淋巴细胞的IL-2受体，使其不能转化为活性的T淋巴细胞。免疫反应因此被抑制，从而保护移植器官免受排异。   ·舒莱与静止状态的T淋巴细胞的IL-2受体的结合相当紧密。移植手术围手术期两剂的舒莱将提供给机体移植器官有效的保护作用达数周之久。