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 详细处方信息以本药内容附件PDF文件（20096200300223.pdf）的“原文Priscribing Information”为准
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部分中文赛尼哌处方资料（仅供参考）

【药物名称】赛尼哌 Zenapax

【制剂规格】每瓶注射液内含25 mg 达利珠单抗(5 mg/mL)，并含有以下赋形剂：聚山梨醇脂80，氯化钠，磷酸二氢钠，磷酸氢二钠，盐酸，氢氧化钠和注射用水。为澄清或淡乳白色液体。

【药理毒理】达利珠单抗是一种重组并人源化的IgGI（G亚型免疫球蛋白）抗TAC抗体。其功能类似于白细胞介素-2（IL-2）受体拮抗剂，与高亲和力的IL－2受体复合物（在激活的T细胞表面表达）的a－亚单位或TAC亚单位高特异性结合，从而抑制IL－2的结合和生物活性。使用本药可抑制IL－2介导的淋巴细胞激活，也即是抑制了移植排斥过程中细胞免疫反应的关键通道。采用推荐剂量时，达利珠单抗可使TAC受体饱和约120天。未发现影响其功效、安全性、血清达利珠单抗水平或任何其他临床相关参数的抗体。除了预期的暂时性TAC阳性细胞减少外，采用荧光活化细胞分检器（FACS）未观察到循环淋巴细胞总数或细胞表型的变化。临床试验显示，本药在降低由活检证实的移植后6个月内的急性排斥发生率方面明显优于安慰剂，具有统计学意义，并且未观察到反跳排斥。在一III期临床研究中观察到，本药组病人的移植后6个月和12个月的存活率比安慰剂组显著增高，具有统计学意义。在移植后6个月时，以肾小球滤过率来评价肾功能，本药治疗组的肾功能明显优于安慰剂组。本药治疗组接受抗淋巴细胞抗体治疗急性排斥反应的病人少于安慰剂组。

【药 动 学】临床试验中，每14天用1 mg/kg本药治疗异体肾移植病人，总共5个剂量，平均血清峰浓度（平均值±标准差）在第一（21±14 mg/mL）和第五剂量（32±22 mg/mL）间上升。第五次剂量前的血清浓度谷值为7.6±4.0 mg/mL。5－10 mg/mL的血清水平对于TAC受体的完全饱和和阻断激活的T淋巴细胞反应是必需的。为达到和维持使TAC受体饱和的血清水平，可每14天给1 mg/kg的推荐剂量一次。推荐的给药方案保证了在移植后3个月内维持血清受体饱和浓度，这3个月也正是移植后最关键的时期。估计达利珠单抗的半衰期在异体肾移植病人中为270－919小时（平均480小时），与报道的人体IgG的半衰期相同，后者为432－552小时（平均480小时），这充分说明达利珠单抗是人源化蛋白质。人群药代动力学分析说明，达利珠单抗系统清除率受总体重，年龄，性别，蛋白尿和种族的影响。体重对系统清除率的影响支持以mg/kg为本药的剂量单位，推荐的剂量方案使药物暴露程度保持在有大范围人口学特性的病人群中参照暴露程度的30%以内，对于异体肾移植的病人不需要基于其他协变指数（性别，蛋白尿，种族和年龄）作剂量调整。

【适 应 证】预防肾移植后急性排斥反应的发生，可与包含环孢素和皮质类固醇激素的免疫抑制方案一起使用。

【不良反应】
    对本药安全性的研究是通过比较在原有的环孢素和皮质类固醇激素并加用硫唑嘌呤或霉酚酸酯的免疫抑制方案中，加用本药和安慰剂的两组病人而进行的。
　　本药没有明显毒性，与安慰剂相比，它不增加免疫抑制方案的毒性。报导的不良反应与移植过程及免疫抑制方案中的药物有关。药物相关不良反应，可参照环孢素，皮质类固醇激素，硫唑嘌呤或霉酚酸酯的处方信息。根据报道，95%使用安慰剂治疗的病人及96%使用本药治疗的病人出现不良反应。据报道，44.4%使用安慰剂的病人及39.9%使用本药治疗的病人，发生严重不良反应。据报道，在移植术后的前6个月，3.4%使用安慰剂治疗的病人及0.6％使用本药治疗的病人死亡。移植后12个月的死亡率，使用安慰剂组为4.4%，本药治疗组为1.5%。
　　最常报道的不良反应为胃肠道紊乱，其发生率在使用本药组（67%）和安慰剂组（68%）相仿。本药不增加感染发生率（安慰剂组成为72%，而本药治疗组为68%）。据报道，使用本药治疗组和安慰剂组发生感染的类型相似。据报道，安慰剂组发生巨细胞病毒感染的发生率为16%，而本药治疗组为13%。加用本药不会增加移植后淋巴组织增生紊乱的例数，该发生率在安慰剂组和本药治疗组均小于1%。使用本药后未观察到细胞因子释放综合征

【相互作用】在临床试验中，本药与下列用于移植的药物合用不会增加不良反应的发生：环孢素，霉酚酸酯、更昔洛韦，阿昔洛韦，他克莫司，硫唑嘌呤，抗胸腺细胞免疫球蛋白，CD-3（OKT3）和皮质类固醇激素。本药和霉酚酸酯的活性代谢产物霉酚酸之间，没有药代动力学的相互影响。

【用法用量】推荐剂量为1 mg/kg，加入0.9％生理盐水50 mL中，由周围或中央静脉输入15分钟以上。本药首剂应在移植前24小时内给药，以后每隔14天给药1次，5次为一疗程。每次给药必须在预定给药时间的前后一天内进行。严重肾损害的病人不必进行剂量调整。 本药的最大承受剂量在病人中还没有确定，也没能在动物实验中获得。1.5 mg/kg的剂量用于骨髓移植受者，未发生任何相关的不良反应。在单剂量毒性研究中，125 mg/kg的剂量给老鼠静脉注射，未产生明显毒性。 本药不能直接注射，而应在静脉给药前用0.9%氯化钠溶液50mL稀释。当混合溶液时，不要摇荡，应轻轻翻转以防止起泡沫，因为药品不含有任何抗微生物防腐剂和制菌剂，所以必须小心保持本药配好溶液无菌。本药为一种无色液体，盛放于一次性瓶内，打开后，任何未使用的部分都应被丢弃。胃肠外药物制剂在给药前应肉眼检查是否有颗粒物质或变色，一旦灌注液准备好，应在4小时内进行静脉输入。如果需保存更长时间（最多24小时），则应保存在2-8℃环境中。其他药物或物质不应加在本药稀释液中或和本药稀释液同时从同一条静脉通路输入。

【注意事项】
    已知对达利珠单抗或此产品的任何成分具有高敏感性的病人禁止使用。 严重肝损害的病人：没有关于严重肝损害病人的资料。
　　对妊娠和哺乳的影响：未进行过本药对动物生殖影响的研究。尚不知道本药治疗是否会损伤胎儿或影响生殖功能。因为IgG能通过胎盘屏障，育龄妇女使用本药治疗必须根据个案对其潜在利弊进行权衡，育龄妇女在用药期间和最后一次给药后4个月内必须使用避孕方法以防怀孕。
　　现尚不知道本药是否会被分泌到人乳中，因为许多药物可被分泌到人乳中并具有潜在的不良反应，因此必须根据药物对哺乳妇女的重要性来确定是停止哺乳还是停止用药。
　　对老年人的影响：老年病人（65岁以上）使用本药的临床经验有限，因为做肾移植的老年病人很少。
　　对儿童的影响：儿科病人使用本药的安全性和功效尚无资料支持。

Zenapax
Generic Name: Daclizumab (da-KLYE-zue-mab)
Brand Name: Zenapax

Zenapax is used for:
Preventing organ rejection in kidney transplant patients in combination with other medicines. It may also be used for other conditions as determined by your doctor.

Zenapax is a monoclonal antibody and immunosuppressive agent. It works by blocking the activation of the immune system, which decreases the risk of the body rejecting a transplanted organ.

Do NOT use Zenapax if:
•you are allergic to any ingredient in Zenapax
Contact your doctor or health care provider right away if any of these apply to you.

Before using Zenapax:
Some medical conditions may interact with Zenapax. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
•if you are pregnant, planning to become pregnant, or are breast-feeding
•if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
•if you have allergies to medicines, foods, or other substances
•if you have diabetes or an infection

Some MEDICINES MAY INTERACT with Zenapax. However, no specific interactions with Zenapax are known at this time.

This may not be a complete list of all interactions that may occur. Ask your health care provider if Zenapax may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Zenapax:
Use Zenapax as directed by your doctor. Check the label on the medicine for exact dosing instructions.
•Zenapax is administered as an intravenous (IV; into a vein) infusion only in a medical setting.
•If Zenapax contains particles or is discolored, or if the vial is cracked or damaged in any way, do not use it.
•If you miss a dose of Zenapax, contact your doctor immediately.

Ask your health care provider any questions you may have about how to use Zenapax.

Important safety information:
•Zenapax may cause dizziness or blurred vision. Do not drive, operate machinery, or do anything else that could be dangerous until you know how you react to Zenapax. Using Zenapax alone, with certain other medicines, or with alcohol may lessen your ability to drive or perform other potentially dangerous tasks.
•Before you have any medical or dental treatments, emergency care, or surgery, tell the doctor or dentist that you are using Zenapax.
•Zenapax may lower your body's ability to fight infection. Prevent infection by avoiding contact with people with colds or other infections. Notify your doctor of any signs of infection, including fever, sore throat, rash, or chills.
•Women of childbearing age should use effective birth control methods (eg, condoms, diaphragms, spermicide) before beginning treatment with Zenapax and continue to use birth control for 4 months after completing therapy.
•Diabetes patients - Zenapax may affect your blood sugar. Check blood sugar levels closely and ask your doctor before adjusting the dose of your diabetes medicine.
•LAB TESTS, including complete blood cell counts, may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.
•Use Zenapax with extreme caution in CHILDREN. Safety and effectiveness have not been confirmed.
•PREGNANCY and BREAST-FEEDING: It is unknown if Zenapax can cause harm to the fetus. If you become pregnant, discuss with your doctor the benefits and risks of using Zenapax during pregnancy. It is unknown if Zenapax is excreted in breast milk. Do not breast-feed while taking Zenapax.

Possible side effects of Zenapax:
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:
Back pain; constipation; coughing; diarrhea; difficult or painful urination; dizziness; fever; gas; generalized weakness; headache; impaired wound healing without infection; increase or decrease in blood pressure; leg cramps; muscle pain; nausea; night sweats; pain; reaction at the injection site; stomach fullness; stomach pain; swelling; swelling of the legs and feet; tiredness; tremors; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); abnormal heartbeat; chest pain; difficulty swallowing; fast heartbeat; fainting; fluid in the lungs; hoarseness; infection; unusual bruising or bleeding; urinary tract bleeding; weakened immune system.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

If OVERDOSE is suspected:
Proper storage of Zenapax:
Zenapax is usually handled and stored by a health care provider. If you are using Zenapax at home, store Zenapax as directed by your pharmacist or health care provider. Keep Zenapax out of the reach of children and away from pets.

General information:
•If you have any questions about Zenapax, please talk with your doctor, pharmacist, or other health care provider.
•Zenapax is to be used only by the patient for whom it is prescribed. Do not share it with other people.
•If your symptoms do not improve or if they become worse, check with your doctor.

This information is a summary only. It does not contain all information about Zenapax. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

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 详细处方信息以本药内容附件PDF文件（20096200300223.pdf）的“原文Priscribing Information”为准
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