制造商：
基因泰克公司
药理分类：
白细胞介素-6受体抑制剂
活性成分（补）：
用tocilizumab 20mg/mL;溶液稀释后的静脉输液，不含防腐剂。
指示（补）：
中度至严重，类风湿关节炎患者活动谁也进行了充分的反应到≥1 TNF阻断剂。可与甲氨蝶呤或的DMARDs。
药理作用：
白细胞介素-6（IL - 6的）是由单核细胞和血液中的淋巴细胞和在关节滑膜和血管内皮细胞，导致全身和局部的IL - 6的生产，如类风湿关节炎患者的炎症过程的影响。用tocilizumab结合具体可溶性和膜结合的IL - 6受体，并已被证明能够抑制这些受体通过的IL - 6介导的信号。
临床试验：
的疗效和安全性进行评估的tocilizumab五个随机，双盲的病人的研究“18岁的类风湿关节炎。用tocilizumab给予作为单一疗法（研究一）与甲氨蝶呤（MTX）（研究II和III）或患者（研究四）其他DMARDs与不足，针对这些药品，或与甲氨蝶呤联合相结合的患者，每4周反应不足与肿瘤坏死因子拮抗剂（研究五）。主要终点是患者的比例在24周谁取得了ACR20反应。在所有的研究，以tocilizumab 8mg/kg治疗的患者在24周显着ACR20，ACR50，比甲氨蝶呤或安慰剂治疗的患者和ACR70反应率。反应不足或TNF拮抗剂治疗的DMARDs以tocilizumab 4mg/kg治疗的患者相比有较低的反应治疗的患者以tocilizumab 8mg/kg率。
法律分类：
接收
成人：
给曾经有60分钟的静脉输注，每4个星期。最初4mg/kg，可能会增加到8mg/kg临床反应为基础。不要一开始如果非国大<2000/mm3，血小板<100000/mm3，或ALT / AST的> 1.5xULN。如果减少剂量4mg/kg肝酶升高，白细胞减少，或血小板减少发生（见文献）。
儿童：
不推荐。
警告/注意事项：
非洲人国民大会<500立方毫米，血小板<五点零零零万立方毫米，或ALT / AST的> 5xULN：不推荐。监视器中性粒细胞，血小板，肝功能检查每4-8个星期。积极肝疾病或损伤：不推荐。乙型肝炎病毒或丙型肝炎病毒感染。风险增加严重或致命的感染（如结核病，细菌性败血症，侵入性真菌）。主动感染：不给治疗。长期或经常性或机会性感染的历史。条件，易患感染。旅游，或居住在，与TB或真菌病流行地区。测试和治疗潜伏性结核病治疗开始之前。密切监测，如果新的感染发展;停止造成严重感染或败血症或伺机发展。监测血脂4-8周后开始，然后每隔6个月。免疫抑制。中枢神经系统脱髓鞘疾病。恶性肿瘤。老人。妊娠（Cat.C）。哺乳母亲：不推荐。
互动（补）：
与风险增加（如肿瘤坏死因子拮抗剂，白细胞介素1受体拮抗剂，抗CD20单克隆抗体，选择性共刺激调节剂）伴随免疫抑制剂感染。避免使用活疫苗。注意与CYP3A4底物药物（如口服避孕药，洛伐他汀，阿托伐他汀）。监测华法令，环孢素，茶碱，这是细胞色素P450基板与其他药物的治疗指数狭窄。
不良反应（补）：
上呼吸道感染，鼻咽炎，头痛，高血压，ALT升高，输液反应，白细胞减少，血小板减少，胃肠穿孔，增加脂质。
如何提供：
一次性使用瓶（80mg/4mL，
200mg/10mL，400mg/20mL）-1，4
最后更新：
2/12/2010
Manufacturer:
Genentech, Inc.
Pharmacological Class:
Interleukin-6 receptor inhibitor
Active Ingredient(s):
Tocilizumab 20mg/mL; soln for IV infusion after dilution; preservative-free.
Indication(s):
Moderately-to severely-active rheumatoid arthritis in patients who have had an inadequate response to ≥1 TNF blocker. May be used with methotrexate or DMARDs.
Pharmacology:
Interleukin-6 (IL-6) is produced by monocytes and lymphocytes in the bloodstream and by synovial and endothelial cells in the joints, leading to systemic and local production of IL-6 in patients affected by inflammatory processes such as rheumatoid arthritis. Tocilizumab binds specifically to both soluble and membrane-bound IL-6 receptors, and has been shown to inhibit IL-6-mediated signaling through these receptors.
Clinical Trials:
The efficacy and safety of tocilizumab was assessed in five randomized, double-blind studies in patients >18 years with active rheumatoid arthritis. Tocilizumab was given every 4 weeks as monotherapy (Study I), in combination with methotrexate (MTX) (Studies II and III) or other DMARDs (Study IV) in patients with an inadequate response to those drugs, or in combination with MTX in patients with an inadequate response to TNF antagonists (Study V). The primary endpoint was the proportion of patients who achieved an ACR20 response at week 24. In all studies, patients treated with tocilizumab 8mg/kg had statistically significant ACR20, ACR50, and ACR70 response rates versus MTX- or placebo-treated patients at week 24. Patients with inadequate response to DMARDs or TNF antagonist therapy treated with tocilizumab 4mg/kg had lower response rates compared to patients treated with tocilizumab 8mg/kg.
Legal Classification:
Rx
Adults:
Give once every 4 weeks as a 60-minute IV infusion. Initially 4mg/kg, may increase to 8mg/kg based on clinical response. Do not start if ANC<2000/mm3, platelets <100000/mm3, or ALT/AST >1.5xULN. Reduce dose to 4mg/kg if elevated liver enzymes, neutropenia, or thrombocytopenia occur (see literature).
Children:
Not recommended.
Warnings/Precautions:
ANC <500mm3, platelets <50000mm3, or ALT/AST >5xULN: not recommended. Monitor neutrophils, platelets, liver function tests every 4–8 weeks. Active hepatic disease or impairment: not recommended. HBV or HCV infection. Increased risk of serious or fatal infections (eg, TB, bacterial sepsis, invasive fungal). Active infections: do not give therapy. Chronic or history of recurring or opportunistic infections. Conditions that predispose to infection. Travel to, or residence in, areas with endemic TB or mycoses. Test for and treat latent TB prior to starting therapy. Monitor closely if new infection develops; discontinue if serious or opportunistic infection or sepsis develop. Monitor lipids 4–8 weeks after initiation, then every 6 months. Immunosuppression. CNS demyelinating disorders. Malignancies. Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.
Interaction(s):
Increased risk for infection with concomitant immunosuppressants (eg, TNF antagonists, IL-1R antagonists, anti-CD20 monoclonal antibodies, selective co-stimulation modulators). Avoid live vaccines. Caution with CYP3A4 substrate drugs (eg, oral contraceptives, lovastatin, atorvastatin). Monitor warfarin, cyclosporine, theophylline, other drugs that are CYP450 substrates with narrow therapeutic indices.
Adverse Reaction(s):
Upper respiratory tract infections, nasopharyngitis, headache, hypertension, increased ALT; infusion reactions, neutropenia, thrombocytopenia, gastrointestinal perforations, increased lipids.
How Supplied:
Single-use vials (80mg/4mL,
200mg/10mL, 400mg/20mL)—1, 4