英文药名：DOCEFREZ LYOPH（DOCETAXEL） 中文药名：多西他赛粉剂 药品说明 CHMP推荐批准Docefrez粉剂治疗乳腺癌、非小细胞肺癌、前列腺癌、胃腺癌及头颈部癌 人用医疗产品委员会（CHMP）推荐批准Sun Pharmaceutical Industries Europe B．V公司的Docefrez（I）20mg和80mg粉针剂用于治疗乳腺癌、非小细胞肺癌、前列腺癌、胃腺癌及头颈部癌。 分类名称 一级分类：抗肿瘤药物 二级分类：抗代谢药 三级分类：    药品英文名 Docetaxei   药品别名 多西紫杉、多西紫杉醇、多烯紫杉醇、紫杉特尔、Taxotere  DOCEFREZ  LYOPH   药物剂型 1.多西他赛注射剂：20mg/支，80mg/支(各附有1.5ml、6ml溶剂)。避光贮藏，放置于2～8℃下保存。 2.多西他赛注射液：20mg/0.5ml，20mg/1ml，20mg/2ml，80mg/2ml，80mg/8ml。2～8℃，密闭，遮光贮存。 3.DOCEFREZ LYOPH粉剂： 20MG/瓶，80MG/瓶。2～8℃，密闭，遮光贮存。 药理作用 本品为细胞周期特异性抗肿瘤药，可特异性作用于M期细胞。本品可促进小管聚合成为稳定的微管，并抑制其解聚，以显著减少小管的数量，也可通过破坏微管的网状结构，抑制细胞有丝分裂，从而达到抗肿瘤的目的。   药动学 静滴本品100mg/m2后(滴注时间为1h)，平均血药峰浓度(Cmax)为3.7µg/ml，稳态分布容积为113L。本品可分布于全身各脏器，以肝脏、胆汁、肠、胃中含量较高，中枢神经系统中含量极少。蛋白结合率高于95%。主要在肝脏代谢，三相半衰期(α、β、γ)分别为4min、36min及11.1h。本品主要以代谢产物形式随粪便排泄(占给药量的75%)，经尿液排出仅占6%，仅有小部分以药物原形排出体外。   适应证 用于治疗晚期乳腺癌、非小细胞肺癌。也有报道用于治疗头颈部癌、小细胞肺癌、胃癌、卵巢癌等肿瘤。 禁忌证 1.对本品有严重过敏史者禁用。 2.严重白细胞低下者禁用。 3.严重肝功能不全者禁用。 4.本品的妊娠安全性分级为D级，孕妇用药后，对其胎儿有潜在危害，并有流产的可能性，因此孕妇禁用。 5.本品注射液可能含有聚山梨酯80，对其有严重过敏史者不能使用。   注意事项 1.肝功能不全者、严重衰弱者、严重水潴留者、严重感觉神经疾病患者慎用。 2.本品用于儿童的安全性尚未确定。 3.尚不清楚本品能否分泌人乳汁，哺乳期妇女的用药安全性尚未确定，用药前应停止哺乳。 4.配制本品时，粉针剂应先以指定溶剂溶解，再以生理盐水或5%葡萄糖注射液稀释后使用(配制后浓度不超过0.74mg/ml)。工作台表面应覆盖可丢弃的塑料薄膜，操作者应穿戴防护衣服及手套。若皮肤接触了药液，应立即用肥皂和水彻底清洗；如眼睛或黏膜接触了药液，立即用水彻底清洗。配制好的药液应立即使用。 5.在使用本品的最初几分钟内，可能发生过敏反应，应具备相应的急救设施。为预防液体潴留和过敏反应，推荐在用药前1天开始口服地塞米松(每天16mg，连用4～5天)。 6.如用药后仅发生面部潮红或局部皮肤反应，则不需要停止治疗。如发生严重过敏反应(血压下降超过2.67kPa、支气管痉挛或全身皮疹/红斑)，则需立即停止给药，并给予对症治疗。已发生过严重不良反应者，不能再次使用本品。 7.使用本品治疗时如出现严重的周围神经病变、严重的或累积性皮肤反应，或严重的中性粒细胞减少(低于0.5×109/L，并持续7天或7天以上)，建议下1个疗程减量给药。 8.当血胆红素高于正常值上限、氨基转移酶高于正常上限1.5倍、ALP高于正常上限2.5倍时，应停用本品治疗。 9.药物过量时，可能表现为中性粒细胞减少、皮肤反应和感觉异常。目前尚无特效解毒药。 10.治疗过程中应定期检测血常规、肝功能、血电解质、血肌酐、神经系统及超声心动图。   不良反应 1.血液系统：可见贫血、白细胞减少及血小板减少，其中中性粒细胞减少为剂量限制性毒性。 2.消化系统：恶心、呕吐、腹泻、黏膜炎、便秘、肝功能损害。 3.代谢/内分泌系统：使用本品后，可见体重增加，发生率约为13%。当累积量达400mg/m2时，可出现下肢水肿，甚至发展为全身水肿，体重可增加3kg以上。极少数患者可出现胸腹腔积液、心包积液。停止治疗后，液体潴留一般可逐渐消失。 4.皮肤：部分患者可发生指(趾)甲改变、色素沉着，甚至指甲脱落。 5.过敏反应：轻度过敏反应表现为皮肤瘙痒及潮红、皮疹、发热、寒战等，皮疹主要见于手、足，亦可在手臂、面部和胸部出现，常于用药后1周内发生；严重过敏反应不多见，主要表现为支气管痉挛、呼吸困难和低血压。 6.其他：肌肉关节疼痛、感染、头痛、感觉障碍，尚可见溢泪、脱发、乏力、注射部位反应及心血管毒性报道。   用法用量 1.单药治疗：每次75～100mg/m2，静滴1h，每3周1次。 2.联合用药：一般每次75mg/m2，每3周1次。   药物相应作用 1.本品与环磷酰胺、依托泊苷、氟尿嘧啶联合给药有协同作用，对放疗也有增敏作用。 2.本品与紫杉醇之间具有不完全交叉耐药性，与顺铂和氟尿嘧啶无交叉耐药。 3.与顺铂合用，导致神经病变的危险性增加。 4.伊曲康唑可抑制本品代谢，增加本品毒性。 5.体外研究表明，细胞色素P450 3A4抑制剂可能干扰本品代谢，当与此类药物(如酮康唑、红霉素、环孢素等)合用时，应特别谨慎。 6.给予托泊替康治疗3天后再使用本品，可使本品的清除率降低达50%。两者合用时，建议在第1天给予本品，第1～4天给予托泊替康。 7.用药期间接种活疫苗，将增加感染活疫苗的危险，故用药期间不能接种活疫苗。化疗停止至少3个月后才能接种活疫苗。 完整处方附件：http://druginserts.com/lib/rx/meds/docefrez/page/5/ 1 INDICATIONS AND USAGE1.1 Breast CancerDOCEFREZ is indicated for the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy. 1.2 Non-Small Cell Lung CancerDOCEFREZ as a single agent is indicated for the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of prior platinum-based chemotherapy. 1.3 Prostate CancerDOCEFREZ in combination with prednisone is indicated for the treatment of patients with androgen independent (hormone refractory) metastatic prostate cancer. 2 DOSAGE AND ADMINISTRATIONFor all indications, toxicities may warrant dosage adjustments [see Dosage and Administration (2.7)]. 2.1 Breast Cancer ◦For locally advanced or metastatic breast cancer after failure of prior chemotherapy, the recommended dose of DOCEFREZ is 60 mg/m2 to 100 mg/m2 administered intravenously over 1 hour every 3 weeks. 2.2 Non-Small Cell Lung Cancer◦For treatment after failure of prior platinum-based chemotherapy, docetaxel was evaluated as monotherapy, and the recommended dose is 75 mg/m2 administered intravenously over 1 hour every 3 weeks. A dose of 100 mg/m2 in patients previously treated with chemotherapy was associated with increased hematologic toxicity, infection, and treatment-related mortality in randomized, controlled trials [see Boxed Warning, Dosage and Administration (2.7), Warnings and Precautions (5), Clinical Studies (14)]. 2.3 Prostate Cancer◦For hormone-refractory metastatic prostate cancer, the recommended dose of DOCEFREZ is 75 mg/m2 every 3 weeks as a 1 hour intravenous infusion. Prednisone 5 mg orally twice daily is administered continuously [see Dosage and Administration (2.7)]. 2.6 Premedication RegimenAll patients should be premedicated with oral corticosteroids (see below for prostate cancer) such as dexamethasone 16 mg per day (e.g., 8 mg twice daily) for 3 days starting 1 day prior to DOCEFREZ administration in order to reduce the incidence and severity of fluid retention as well as the severity of hypersensitivity reactions [see Boxed Warning, Warnings and Precautions ( 5.4)]. This regimen was evaluated in 92 patients with metastatic breast cancer previously treated with chemotherapy given docetaxel at a dose of 100 mg/m2 every 3 weeks. [see Warnings and Precautions (5.4)]. 2.7 Dosage Adjustments During TreatmentBreast Cancer Patients who are dosed initially at 100 mg/m2 and who experience either febrile neutropenia, neutrophils <500 cells/mm3 for more than 1 week, or severe or cumulative cutaneous reactions during DOCEFREZ therapy should have the dosage adjusted from 100 mg/m2 to 75 mg/m2. If the patient continues to experience these reactions, the dosage should either be decreased from 75 mg/m2 to 55 mg/m2 or the treatment should be discontinued. Conversely, patients who are dosed initially at 60 mg/m2 and who do not experience febrile neutropenia, neutrophils <500 cells/mm3 for more than 1 week, severe or cumulative cutaneous reactions, or severe peripheral neuropathy during DOCEFREZ therapy may tolerate higher doses. Patients who develop ≥grade 3 peripheral neuropathy should have DOCEFREZ treatment discontinued entirely. Non-Small Cell Lung Cancer Monotherapy with DOCEFREZ for NSCLC treatment after failure of prior platinum-based chemotherapy Patients who are dosed initially at 75 mg/m2 and who experience either febrile neutropenia, neutrophils <500 cells/mm3 for more than one week, severe or cumulative cutaneous reactions, or other grade 3/4 non-hematological toxicities during DOCEFREZ treatment should have treatment withheld until resolution of the toxicity and then resumed at 55 mg/m2. Patients who develop ≥grade 3 peripheral neuropathy should have DOCEFREZ treatment discontinued entirely. Prostate Cancer Combination therapy with DOCEFREZ for hormone-refractory metastatic prostate cancer DOCEFREZ should be administered when the neutrophil count is ≥1,500 cells/mm3. Patients who experience either febrile neutropenia, neutrophils <500 cells/mm3 for more than one week, severe or cumulative cutaneous reactions or moderate neurosensory signs and/or symptoms during DOCEFREZ therapy should have the dosage of DOCEFREZ reduced from 75 to 60 mg/m². If the patient continues to experience these reactions at 60 mg/m², the treatment should be discontinued. Combination Therapy with Strong CYP3A4 inhibitors: [see Drug Interactions (7), Clinical Pharmacology (12.3)]. 2.8 Administration PrecautionsDOCEFREZ is a cytotoxic anticancer drug and, as with other potentially toxic compounds, caution should be exercised when handling and preparing DOCEFREZ solutions. The use of gloves is recommended. Please refer to [see How Supplied/ Storage and Handling (16.3)]. If DOCEFREZ lyophilized powder, reconstituted solution, or infusion solution should come into contact with the skin, immediately and thoroughly wash with soap and water. If DOCEFREZ lyophilized powder, reconstituted solution or infusion solution should come into contact with mucosa, immediately and thoroughly wash with water. Contact of the DOCEFREZ reconstituted solution with plasticized PVC equipment or devices used to prepare solutions for infusion is not recommended. In order to minimize patient exposure to the plasticizer DEHP (di-2-ethylhexyl phthalate), which may be leached from PVC infusion bags or sets, the DOCEFREZ infusion solution should be stored in bottles (glass, polypropylene) or plastic bags (polypropylene, polyolefin) and administered through polyethylene-lined administration sets. DOCEFREZ (Lyophilized Powder for Injection and Diluent) DOCEFREZ for Injection requires reconstitution with Diluent and one further dilution with infusion solution prior to administration. Please follow the preparation instructions provided below. The table below provides the fill range of the Diluent, the volume of Diluent to be added for the reconstitution and the concentration of the reconstituted solution for DOCEFREZ 20 mg and DOCEFREZ 80 mg (See Table 1). PACKAGE LABEL.PRINCIPAL DISPLAY PANEL-DOCEFREZ-20MG-LABELNDC 47335-285-40 DocefrezTM (Docetaxel) for Injection 20 mg For Intravenous Infusion Only Each Docefrez for Injection vial contains a slight overfill to deliver 20 mg of Docetaxel per 0.8 mL after reconstitution Rx ONLY (click image for full-size original) PACKAGE LABEL.PRINCIPAL DISPLAY PANEL-DOCEFREZ-20MG-CARTONNDC 47335-285-41 DocefrezTM (Docetaxel) for Injection 20 mg* For Intravenous Infusion Only *Each Docefrez for Injection vial contains a slight overfill to deliver 20 mg of Docetaxel per 0.8 mL after reconstitution Each carton contains: One vial of Docefrez (docetaxel) for Injection 20 mg One vial of DILUENT for Docefrez 20 mg Rx ONLY (click image for full-size original) PACKAGE LABEL.PRINCIPAL DISPLAY PANEL-DILUENT-20MG-LABELNDC 47335-287-40 DILUENT for DocefrezTM 20 mg 1.13 mL Single Use Vial-Discard Unused Portion. Rx ONLY (click image for full-size original) PACKAGE LABEL.PRINCIPAL DISPLAY PANEL-DOCEFREZ-80MG-LABELNDC 47335-286-40 DocefrezTM (Docetaxel) for Injection 80 mg For Intravenous Infusion Only Each Docefrez for Injection vial contains a slight overfill to deliver 80 mg of Docetaxel (24 mg/mL after reconstitution) (click image for full-size original) PACKAGE LABEL.PRINCIPAL DISPLAY PANEL-DOCEFREZ-80MG-CARTONNDC 47335-286-41 DocefrezTM (Docetaxel) for Injection 80 mg* For Intravenous Infusion Only *Each Docefrez for Injection vial contains a slight overfill to deliver 80 mg of Docetaxel (24 mg/mL after reconstitution) Each carton contains: One vial of Docefrez (docetaxel) for Injection 80 mg One vial of DILUENT for Docefrez 80 mg Rx ONLY (click image for full-size original) PACKAGE LABEL.PRINCIPAL DISPLAY PANEL-DILUENT-80MG-LABELNDC 47335-288-40 DILUENT for DocefrezTM 80 mg 4.21 mL Rx ONLY (click image for full-size original) label-diluent-80mg --------------------------------------------------------------- 注：以下产品来同规格和不同价格，购买时请以电话咨询为准！ --------------------------------------------------------------- 原产地英文商品名: DOCEFREZ LYOPH POWDER 80MG/VIAL 原产地英文药品名: DOCETAXEL 中文参考商品译名: DOCEFREZ LYOPH粉剂 80毫克/瓶 中文参考药品译名: 多西他赛 生产厂家中文参考译名: SUN PHARMA GLOBAL 生产厂家英文名: SUN PHARMA GLOBAL --------------------------------------------------------------- 原产地英文商品名: DOCEFREZ LYOPH POWDER 20MG/VIAL 原产地英文药品名: DOCETAXEL 中文参考商品译名: DOCEFREZ LYOPH粉剂 20毫克/瓶 中文参考药品译名: 多西他赛 生产厂家中文参考译名: SUN PHARMA GLOBAL 生产厂家英文名: