英文药名:Enbrel(Etanercept) 中文药名:恩利（依那西普注射剂） 生产厂家：辉瑞（惠氏） 给药说明 依那西普是一种人源TNF-α受体抗体融合蛋白，可溶性抗肿瘤坏死因子融合蛋白，是肿瘤坏死因子(TNF-α)拮抗剂，通过抑制TNF-α可以起到控制炎症、阻断病情进展的作用，它属DMARD类药物，是抗风湿病的生物制剂；用于活动性类风湿关节炎，牛皮癣及关节性牛皮癣，幼年特发性关节炎，活动性强直性脊柱炎。 通用名为注射用重组人II型TNF-α受体抗体融合蛋白。该药于1998年经美国FDA批准用于治疗类风湿性关节炎，2002年批准用于治疗银屑病性关节炎，2004年批准用于治疗寻常性银屑病。 药品英文名 Etanercept 药品别名 Enbrel  恩利 药物剂型 冻干粉针剂：每小瓶含本品25mg  50mg。 药理作用 TNF是内源性炎症介质，其在类风湿性关节炎(RA)病变过程中可能与破坏关节组织的炎症密切相关，对风湿性关节炎起着十分重要的作用。在RA病人关节腔的积液中，TNF浓度明显高于正常人。本品特异性与TNFA和TNFB结合，阻断其与细胞表面的TNF受体作用，从而缓解关节炎症状。在心力衰竭病人中，静脉注射本品1mg/m2或4mg/m2后，血浆TNF-α水平下降85%。 药动学 皮下注射本品25mg，达峰时间约为72小时，峰浓度(Cmax)为12µg/mL，平均半衰期115小时，清除率为89mL/h。连续使用本品6个月(1周2次，25mg/次)，血药浓度可达平均3µg/mL。 适应证 本品用于缓解风湿性关节炎症状。用于减轻活动性银屑病性关节炎的症状，阻止中到重度类风湿性关节炎结构性损伤。 禁忌证 孕妇禁用，哺乳期妇女如用本品应停止哺乳。 注意事项 本品引发的过敏反应报道较少，少于0.5%。本品有可能加重感染，引发致死性的败血症。使用本品的患者如同时患有细菌感染，用药需格外小心。本品应冷藏保存，不可冷冻。 不良反应 约37%的患者在皮下注射本品时会发生局部刺激，但这一反应较轻，不影响治疗。其他不良反应有呼吸道感染、头痛、鼻炎、咳嗽和腹痛等。 用法用量 皮下注射，25mg/次，1周2次。也可与甲氨蝶呤联合使用。 专家点评 在一项180名患者参与的双盲多中心对照试验中，治疗组给以本品0.25，2或16mg/m2，对照组使用安慰剂。3个月后，试验组结果显示，本品的治疗作用呈剂量依赖性，在最高剂量组，有75%的患者的症状得到改善，而安慰剂组这一比例仅有14%。本品在使用过程中也未见抗原反应。在与甲氨蝶呤的对比试验中发现，使用本品的患者关节功能恢复得更好，而症状较甲氨蝶呤组更轻。 Enbrel (etanercept) Prefilled Syringes DESCRIPTION ENBREL® (etanercept) is a dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. Etanercept is produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system. It consists of 934 amino acids and has an apparent molecular weight of approximately 150 kilodaltons. ENBREL® single-use prefilled syringes are available in 25 mg (0.51 mL of a 50 mg/mL solution of etanercept) and 50 mg (0.98 mL of a 50 mg/mL solution of etanercept) dosage strength. IMPORTANT SAFETY INFORMATION What is the most important information I should know about ENBREL? ENBREL is a medicine that affects your immune system. ENBREL can lower the ability of your immune system to fight infections. Serious infections have happened in patients taking ENBREL. These infections include tuberculosis (TB) and infections caused by viruses, fungi, or bacteria that have spread throughout the body. Some patients have died from these infections. Your doctor should test you for TB before you take ENBREL and monitor you closely for TB before, during, and after ENBREL treatment, even if you have tested negative for TB. There have been some cases of unusual cancers reported in children and teenage patients who started using TNF blockers before 18 years of age. Also, for children, teenagers, and adults taking TNF blockers, including ENBREL, the chances of getting lymphoma or other cancers may increase. Patients with RA and psoriasis may be more likely to get lymphoma. Before starting ENBREL, tell your doctor if you: Have any existing medical conditions Are taking any medicines, including herbals Think you have, are being treated for, have signs of, or are prone to infection. You should not start taking ENBREL if you have any kind of infection, unless your doctor says it is okay Have any open cuts or sores Have diabetes or an immune system problem Have TB or have been in close contact with someone who has had TB Were born in, lived in, or traveled to countries where there is more risk for getting TB. Ask your doctor if you are not sure Live or have lived in certain parts of the country (such as, the Ohio and Mississippi River valleys, or the Southwest) where there is a greater risk for certain kinds of fungal infections, such as histoplasmosis. These infections may develop or become more severe if you take ENBREL. If you don't know if histoplasmosis or other fungal infections are common in the areas where you live or have lived, ask your doctor. Have or have had hepatitis B Have heart failure Develop symptoms such as persistent fever, bruising, bleeding, or paleness while taking ENBREL Use the medicine Kineret® (anakinra), Orencia® (abatacept), or Cytoxan® (cyclophosphamide) Have or develop a serious nervous disorder, seizures, any numbness or tingling, or a disease that affects your nervous system such as multiple sclerosis Are scheduled to have surgery Have recently received or are scheduled for any vaccines. All vaccines should be brought up-to-date before starting ENBREL. Patients taking ENBREL should not receive live vaccines. Are allergic to rubber or latex Are pregnant, planning to become pregnant, or breastfeeding Have been around someone with chicken pox What are the possible side effects of ENBREL? ENBREL can cause serious side effects including: Infections, including serious infections like TB; hepatitis B can become active if you already have had it; nervous system problems, such as multiple sclerosis, seizures, or inflammation of the nerves of the eyes; blood problems (some fatal); new or worsening heart failure; new or worsening psoriasis; allergic reactions; autoimmune reactions, including a lupus-like syndrome and autoimmune hepatitis. Common side effects include: Injection site reactions, upper respiratory infections (sinus infections), and headache. In a medical study of patients with JIA, infection, headache, abdominal pain, vomiting, and nausea occurred more frequently than in adults. The kinds of infections reported were generally mild and similar to those usually seen in children. Other serious adverse reactions were reported, including serious infection and depression/personality disorder. These are not all the side effects with ENBREL. Tell your doctor about any side effect that bothers you or does not go away. If you have any questions about this information, be sure to discuss them with your doctor. You are encouraged to report negative side effects of prescription drugs to the FDA. INDICATIONS Moderate to Severe Rheumatoid Arthritis (RA) ENBREL is indicated for reducing signs and symptoms, keeping joint damage from getting worse, and improving physical function in patients with moderate to severe rheumatoid arthritis. ENBREL can be taken with methotrexate or used alone. In medical studies, ENBREL was shown to be effective in about 2 out of 3 adults with RA who used it, and has been shown to begin working in as few as 2 weeks, with most patients receiving benefit within 3 months. In an RA medical study, 55% of patients had no progression of joint damage. Moderate to Severe Polyarticular Juvenile Idiopathic Arthritis (JIA) ENBREL is indicated for reducing signs and symptoms of moderately to severely active polyarticular juvenile idiopathic arthritis (JIA) in children ages 2 years and older. In a medical study, ENBREL was shown to be effective in about 3 out of 4 children with JIA who used it. For these JIA patients, ENBREL has been shown to begin working in approximately 2 to 4 weeks. Psoriatic Arthritis ENBREL is indicated for reducing signs and symptoms, keeping joint damage from getting worse, and improving physical function in patients with psoriatic arthritis. ENBREL can be used in combination with methotrexate in patients who do not respond adequately to methotrexate alone. In a medical study, ENBREL was shown to be effective in about 50% of psoriatic arthritis patients who used it. Clinical responses were apparent at the time of the first visit (4 weeks) and were maintained through 6 months of therapy. Ankylosing Spondylitis (AS) ENBREL is indicated for reducing signs and symptoms in patients with active ankylosing spondylitis. In a medical study, ENBREL was shown to be effective in about 3 out of 5 adults with AS who used it. Clinical responses were seen at 2 weeks in 46% of patients, with 59% of patients receiving benefit within 8 weeks. Moderate to Severe Plaque Psoriasis ENBREL is indicated for the treatment of adult patients (18 years or older) with chronic moderate to severe plaque psoriasis who are candidates for systemic therapy or phototherapy. In medical studies, nearly half of patients saw a significant improvement in their plaque psoriasis within 3 months of using ENBREL. Overall, 3 out of 4 patients saw improvement. ENBREL can work fast; many patients saw improvement within 2 months. ENBREL has been shown to be effective through 12 months of therapy. ENBREL Rx Generic Name and Formulations: Etanercept 25mg; per vial (pwd for SC inj after reconstitution; preservative-free; diluent contains benzyl alcohol); 50mg/mL prefilled syringe (soln for SC inj; preservative free); 50mg/mL prefilled syringe SureClick autoinjector (soln for SC inj; preservative-free). Company: Amgen, Inc. Indications for ENBREL: To reduce signs/symptoms, induce major clinical response, inhibit progression of structural damage, and improve physical function in patients with moderately to severely active rheumatoid arthritis; to reduce signs/symptoms, inhibit progression of structural damage of active arthritis, and improve physical function in patients with psoriatic arthritis; for both: may be used with or without methotrexate in patients who have not responded adequately to methotrexate alone. To reduce signs/symptoms of: ankylosing spondylitis, and of moderately to severely active polyarticular juvenile idiopathic arthritis (JIA). Adult Dose for ENBREL: Use prefilled syringe. Inject 50mg SC once weekly into thigh, abdomen, or upper arm; rotate inj sites. Children's Dose for ENBREL: Inject SC into thigh, abdomen, or upper arm; rotate inj sites. <2yrs: not recommended. JIA: <63kg: 0.8mg/kg per week; max 50mg/week. ≥63kg: may use 50mg prefilled syringe or SureClick autoinjector. Pharmacological Class: Tumor necrosis factor (TNF) blocker. Contraindications: Sepsis. Warnings/Precautions: Increased risk of serious or fatal infections (eg, TB, bacterial sepsis, invasive fungal [treat empirically if develops], or other pathogens). Active infections: do not initiate therapy. Chronic or history of recurring infections. Conditions that predispose to infection (eg, diabetes, immunosuppression). Travel to, or residence in, areas with endemic TB or mycoses. Test/treat latent TB and HBV infection prior to initiating therapy. Monitor closely if new infection, active TB (even if initial latent test is negative), reactivation of HBV, or blood dyscrasias occurs; discontinue if serious or opportunistic infection, sepsis, HBV reactivation, or hematological abnormality develops. Suspend if significant exposure to varicella occurs (consider varicella prophylaxis). Discontinue if lupus-like syndrome with antibody formation or serious hypersensitivity reaction occurs. CNS demyelinating disorders (eg, multiple sclerosis, myelitis, optic neuritis), seizures. Heart failure. Malignancies. Attempt to complete childhood immunizations first. Wegener's granulomatosis patients receiving immunosuppressive agents: not recommended. Moderate to severe alcoholic hepatitis. Latex allergy (syringe). Supervise 1st dose. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended. Interactions: Concurrent cyclophosphamide, anakinra, abatacept, live vaccines, other TNF blockers: not recommended. Immunosuppressants increase risk of infection. Adverse Reactions: Inj site reactions, infections (eg, sepsis, osteomyelitis, cellulitis, pneumonia, pyelonephritis), antibody formation, respiratory disorders; worsening psoriasis; rare: CNS demyelinating disorders, pancytopenia, aplastic anemia, tuberculosis, malignancies (eg, lymphoma; esp. children), others. Children: also varicella, headache, GI disturbances. How Supplied: Multi-use vials—4 (w. supplies); Single-use prefilled syr (1mL)—4 (w. needles); Single-use prefilled SureClick autoinjector—4 (w. needles) 日批准依那西普用于类风湿关节炎治疗 惠氏日本公司和Takeda Pharmaceutical公司于2005年1月25日宣布，日本厚生省批准依那西普（etanercept，Enbrel）用于治疗对现有药物应答不足的类风湿性关节炎（RA）患者。 至此，本品已在全球70多个国家上市。 本品为一靶向肿瘤坏死因子（TNF）的完全人源化单克隆抗体药物，可缓解对传统抗关节炎药物应答不足的RA患者的体征和症状。其于1998年首次获得FDA批准用于治疗疼痛性关节疾病，长期安全性和疗效已在临床上得到了证明。本品可以单用治疗RA，以每周皮下注射2次的方式给药，在日本由惠氏公司和Takeda Pharmaceutical公司共同销售。本品最常见不良反应有注射部位反应、感染和头痛。 RA为一种可致残的慢性疾病。在日本大约有70万RA患者。严重的RA会引起机体免疫系统攻击关节内衬和结缔组织，致使关节疼痛和肿胀。如果不进行及时有效的治疗，还可能导致疲乏、残疾、畸形、器官损伤，甚至早死。在日本，畿患RA的女性患者人数是男性患者的4倍之多。RA可以在所有的年龄段包括儿童时期发病，其高发年龄段为25～50岁 --------------------------------------------------------------- 注：以下产品不同的产地和不同的价格，购买时请认请咨询 --------------------------------------------------------------- 产地国家: 加拿大 原产地英文商品名: ENBREL 25mg/vial 4vials/box 原产地英文药品名: ETANERCEPT 中文参考商品译名: 恩利 25毫克/瓶 4瓶/盒 中文参考药品译名: 依那西普 生产厂家中文参考译名: IMMUNEX 生产厂家英文名: IMMUNEX --------------------------------------------------------------- 产地国家: 加拿大 原产地英文商品名: ENBREL 50mg/vial 4vials/box 原产地英文药品名: ETANERCEPT 中文参考商品译名: 恩利 50毫克/瓶 4瓶/盒 中文参考药品译名: 依那西普 生产厂家中文参考译名: IMMUNEX 生产厂家英文名: IMMUNEX --------------------------------------------------------------- 产地国家: 香港 原产地英文商品名: ENBREL 50mg/vial 4vials/box 原产地英文药品名: ETANERCEPT 中文参考商品译名: 恩利 50毫克/瓶 4瓶/盒 中文参考药品译名: 依那西普 生产厂家中文参考译名: IMMUNEX 生产厂家英文名: IMMUNEX --------------------------------------------------------------- 产地国家: 香港 原产地英文商品名: ENBREL 25mg/vial 4vials/box 原产地英文药品名: ETANERCEPT 中文参考商品译名: 恩利 25毫克/瓶 4瓶/盒 中文参考药品译名: 依那西普 生产厂家中文参考译名: IMMUNEX 生产厂家英文名: IMMUNEX --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: ENBREL 25mg/25ml/vial 4vials/box 原产地英文药品名: ETANERCEPT 中文参考商品译名: 恩利 25毫克/25毫升/瓶 4瓶/盒 中文参考药品译名: 依那西普 生产厂家中文参考译名: IMMUNEX 生产厂家英文名: IMMUNEX --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: ENBREL 25mg/0.5ml/syringe 4syringes/Box 原产地英文药品名: ETANERCEPT 中文参考商品译名: 恩利 25毫克/0.5毫升/注射器 4注射器/盒 中文参考药品译名: 依那西普 生产厂家中文参考译名: IMMUNEX 生产厂家英文名: IMMUNEX --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: ENBREL 50MG/ML/SYRINGE 4SYRINGES/BOX 原产地英文药品名: ETANERCEPT 中文参考商品译名: 恩利 50毫克/毫升/注射器 4注射器/盒 中文参考药品译名: 依那西普 生产厂家中文参考译名: IMMUNEX 生产厂家英文名: IMMUNEX