简介：

部分中文 CLOLAR 处方信息（仅供参考）
英文名称: Clofarabine
药品名称：氯法拉滨
又名：Clofarabine，Clolar，卢伐拉滨，克罗拉滨
美国Bioenvision公司开发, Genzyme公司生产，04.12.28FDA快速审评通道批准本品上市。现本品未申请进口，原料制剂均为3.1类。Bioenvision公司于2006年5月宣布，欧盟委员会已经批准其clofarabine（Evoltra）上市。用于治疗急性淋巴细胞性白血病。本品适用范围为复发的或对至少2种疗法无应答且没有其它疗法可选用的儿科急性淋巴细胞性白血病患者。此外，本品还可用于初次诊断为白血病的21岁及以下患者。
适应症、用法用量：
用于1～21岁顽固性或复发性急性淋巴细胞白血病（ALL）患者，患者此前至少接受过2种优先使用的疗法。本品先用5％葡萄糖注射液或0.9％NaCl注射液稀释。儿童推荐剂量为52mg/m2，每天输注2小时，连续5天。器官功能回复到基线后，治疗周期循环，大约每2～6周一次。
本品结合了氟达拉滨和克拉屈滨 的优点，既抑制DNA聚合酶，又抑制核糖核酸还原酶，是目前唯一可以特异性用于儿童白血病的药物；治疗白血病有效率高。两次常规化疗无应答的患者, 对该药的总反应率为31%；病人耐受性好，无不可预知的不良反应；具有潜在广谱抗肿瘤特性。
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药品英文名
Clofarabine
药理作用
本药为脱氧腺苷类似物，与其他脱氧腺苷类似物(如克拉屈滨、氟达拉滨)相比，本药除可促进细胞凋亡外，还通过抑制核糖核苷酸还原酶和DNA多聚酶而起抗肿瘤作用。本药还可对抗细菌的嘌呤核苷磷酸化酶(PNP)而减少药物毒性，尤其是其他嘌呤脱氧腺苷类似物常见的神经毒性。
药动学
本药静脉滴注后，血药峰浓度在滴注结束时出现。蛋白结合率为47%，主要与白蛋白结合，分布容积为172L/m2。主要通过脱氧胞苷激酶在细胞内磷酸化而转变为细胞毒活性形式，仅0.2%在肝脏代谢。49%～60%以原形从肾脏排泄，总清除率为28.8L/(h·m2)。清除半衰期为5.2h，三磷酸代谢物的清除半衰期超过24小时。
适应证
1.用于复发性或抵抗性急性淋巴细胞白血病(国外资料)。
2.与阿糖胞苷联用，对急性髓样白血病和骨髓增生异常综合征的老年患者有效(国外资料)。
禁忌证
尚不明确。
注意事项
1.慎用：
(1)低血压或脱水患者。
(2)肝功能不全患者。
(3)肾功能不全(使用本药5日内避免使用肾毒性药物)患者。
(4)骨髓抑制导致的继发感染(如严重败血症)患者。
(5)可能出现肿瘤溶解综合征(ATLS)的患者(可导致系统性炎症反应综合征或毛细血管漏综合征、器官功能障碍)。
(6)孕妇。
(7)哺乳期妇女。
2.药物对妊娠的影响：本药对人类胎儿有不良影响，但妊娠妇女在危及生命或严重疾病时较安全的药物不能使用或无效的情况下，也可应用本药。建议育龄妇女用药期间应避免怀孕。美国药品和食品管理局(FDA)对本药的妊娠安全性分级为D级。
3.药物对哺乳的影响：哺乳期妇女用药应权衡利弊；治疗期间应停止哺乳。
4.用药前后及用药时应当检查或监测：
(1)治疗期间及治疗后应监测全血细胞计数及分类。
(2)用药前应测定肝、肾功能，用药的5日内应经常复查肝、肾功能。
(3)应监测尿酸浓度，以尽早发现肿瘤溶解综合征和高尿酸血症。
(4)用药的5日内严密监测血压。
(5)静脉滴注过程中严密监测呼吸功能。
5.本药不能与其他药物通过同一静脉通道给药。
6.本药使用前应用5%的葡萄糖注射液或0.9%的氯化钠注射液稀释。
7.用药过程中出现任何原因引起的低血压都应停药。如低血压为一过性的或可自行恢复，则可以较低剂量重新开始给药。治疗的第1～3日，使用皮质激素(如氢化可的松100mg/m2)，可预防SIRS或毛细血管漏发生。用药过程中一旦出现SIRS或毛细血管漏的症状或体征，应立即停药并给予支持治疗。一旦患者情况稳定和器官功能恢复，可以较低剂量重新开始给药
不良反应
1.心血管系统：
(1)可见心动过速、高血压、低血压，有一过性左室收缩功能不良的报道。
(2)有4例儿科患者出现毛细血管漏综合征和系统性炎症反应综合征(SIRS)，症状包括快速发作的呼吸窘迫、心动过速、低血压和肺水肿，胸腔积液、心包积液和多器官功能衰竭。
2.中枢神经系统：可见头痛、乏力、疲倦、头晕、嗜睡、震颤、焦虑、抑郁、易激惹，少见兴奋。
3.代谢/内分泌系统：可见水肿、体重减轻，有白血病细胞快速分解所致的继发性高尿酸血症的报道，可使用别嘌醇预防高尿酸血症。
4.呼吸系统：可引起鼻出血、呼吸困难、呼吸窘迫、咳嗽、胸腔积液等。
5.肌肉骨骼系统：有关节痛、后背痛、肌肉痛、肢体疼痛的报道。
6.泌尿生殖系统：可见血尿和血清肌酸酐升高。
7.肝脏：可引起可逆性肝毒性，表现为丙氨酸氨基转移酶升高、天门冬氨酸氨基转移酶、胆红素升高、肝肿大、黄疸。
8.胃肠道：可见恶心、呕吐、食欲缺乏、腹痛、腹泻、便秘、牙龈出血、咽喉痛，有胰腺炎的个案报道。
9.血液：最常见贫血、白细胞减少、血小板减少、中性粒细胞减少和发热伴中性粒细胞减少。
10.皮肤：可见皮炎、皮肤干燥、红斑、淤斑、瘙痒、斑丘疹、注射部位疼痛、一过性面部潮红、掌-足-红肿疼痛综合征，有皮疹和口炎的报道。
11.其他：可引起疼痛、发热、寒战、感染性疾病。
用法用量
1.成人常规剂量：静脉滴注：
(1)复发性或抵抗性急性淋巴细胞白血病：先前至少接受过2种治疗方案的患者(年龄在1～21岁之间)，一日52mg/m2，滴注时间超过2h，连续5日；待器官功能恢复或返回基线水平后，每2～6周重复治疗1次。
(2)急性髓样白血病和骨髓增生异常综合征：一项未公布的初步研究表明，一日52mg/m2，滴注时间1h，持续5日；4h后给予阿糖胞苷(每日1g/m2)静脉滴注2h，持续5日，对新近诊断为急性髓样白血病和高危骨髓增生异常综合征的老年患者有积极作用。一个诱导过程后，52%的患者有全面反应，还有13%的患者有全面反应但血小板没有恢复。
2.儿童常规剂量：静脉滴注：
(1)复发性或抵抗性急性淋巴细胞白血病：同成人。
(2)复发性和抵抗性急性髓样白血病：一日52mg/m2，滴注2h以上，连续5日；根据毒性和患者的反应每2～6周重复治疗。已有肝功能不全者可能需要调整剂量。
药物相应作用
尚不明确。Clolar(clofarabine injection)
Preface
Clolaris the brand name of the medication Clofarabine, a medicine used to treat cancer. Clolar is currently indicated to treat acute lymphoblastic leukemia (ALL) in pediatric patients aged 1 to 21 years old that has relapsed after at least two prior treatments. This is the only indication of Clolar, and it cannot be used for treatment of new ALL cases and for other types of cancer. Clolar is indicated for pediatric refractory ALL based on its response rate alone and there were no trials showing that it can extend survival or improve disease-related symptoms.
Acute lymphoblastic leukemia is a type of blood and bone marrow cancer. ALL happens when too many stem cells from the bone marrow becomes lymphoblasts (hence, the term ‘lymphoblastic’), B lymphocytes and T lymphocytes. These cells are not normal, and not able to hunt and fight infectious pathogens well. Also, the sudden drastic increase of these cells create less room for red blood cells, white blood cells and platelets, reducing their number and causing hallmark symptoms like anaemia, frequent infections and bleeding tendencies. The huge numbers of useless, cancerous cells spreads in via bloodstream and lymph vessels to lymph nodes and other organs to cause complications. ALL is termed ‘acute’ because it progresses fairly quickly in short amount of time and can cause death in a few months. ALL is the most common form of blood cancer in children. When treated early, ALL treatment can be successful. If ALL recurs or relapses after one or two treatments, it is already considered a refractory case because it does not respond to usual medications. Only medicines like Clolar are found to cause good response to refractory cases of ALL.
Clolar is manufactured and owned by Genzyme Corporation, a biotechnology company based in Cambridge, Massachusetts which is now a fully owned subsidiary of the French-owned Sanofi S.A. Clolar first entered the market after receiving approval from the United States Food and Drug Administration (FDA) on December 2004. Clolar is classified as an orphan medication and thus not widely available in most pharmacies, even in countries where it is approved.
CANCER TREATMENT MEDS dispenses Clolar and delivers it to customers on a prescription-only basis. We are a premier internet pharmacy specializing on orphan medicines such as Clolar, and we deliver to most countries. We are your best source of Clolar; order it now at CANCER TREATMENT MEDS!
There is no information indicating the use of Clolar for sarcomas. Clolar is exclusively indicated to treat pediatric cases of refractory ALL. There is no research study or clinical trials supporting the use of Clolar for sarcoma-type cancers or for soft-tissue sarcoma. There is also no documented off-label use of Clolar to treat sarcomas.
Clolar medication and use
Clolar medication is used to treat ALL cases in persons below 21 years old that has recurred despite two previous treatments. Pediatric cases of ALL are usually treated with chemotherapy, radiotherapy or a combination of the two. In case of remission, high-dose treatment of chemotherapy with radiotherapy plus stem cell support is indicated to improve chances of cure or prolong remission. If despite second treatment there is still another remission of ALL, Clolar can now be considered to be used for treatment.
Clolar is supplied in a single-use vial containing 20 mg of Clofarabine dissolved in 20 mL 0.9% sodium chloride injection, USP. The recommended dosage of Clolar is 52 mg/m2 of patient’s body surface area, which will be computed by your oncologist.
To administer, Clolar must be first filtered through a sterile 0.2 micron syringe filter, then diluted to intravenous fluids 5% Dextrose Injection, USP, or 0.9% Sodium Chloride Injection, USP prior to infusion to achieve final concentration between 0.15 mg/mL and 0.4 mg/mL. Diluted Clolar must be used within 24 hours, and stored at room temperatures 15 C- 30 C. Your doctor or nurse will prepare Clolar for you. Clolar must be infused through an exclusive intravenous line; no other medicines must be infused in this line to prevent drug incompatibilities.
Clolar infusions are given for over 2 hours for 5 consecutive days. Then a waiting period of 2 to 5 weeks is initiated until organ function tests results return to baseline, and Clolar is infused again. During Clolar infusion days, your kidney, heart and liver functions are closely monitored and supportive care such as intravenous fluids and antihyperuremic treatmentare provided. If your creatinine clearance is goes down to between 30 – 60 mg/minute, Clolar dosage is reduced by 50%.
Furthermore, additional medications such as anti-emetics and prophylactic steroids are given during Clolar infusions.
Clolar dosage may be adjusted if the following toxicities occur:
•For grade 3 neutropenia lasting ≥ 4 weeks, Clolar dose is reduced by 25% for the next cycle•Clolar dose is withheld if the patient develops significant infection, which is then restarted when it subsides•Withhold Clolar dose in any event of Grade 3 non-infectious non-hematological toxicity, but not including momentary elevations in serum transaminase and/or bilirubin, and nausea and vomiting controlled by antiemetic therapy. When these toxicities subside, re-administer Clolar with 25% dose reduction•If there is any event of Grade 4 non-infectious  non-hematological toxicity, discontinue Clolar administration•If systemic inflammatory response syndrome (SIRS) occur or capillary leak occurs, discontinue Clolar administration•If there is Grade 3 or higher creatinine and bilirubin increases, discontinue Clolar administration. If organ functions returns to baseline and becomes stable, re-administer Clolar at the next scheduled dose with a 25% dose reductionClolar chemical structure
Clolar has a chemical structure formula C10H11ClFN5O3 and molecular weight of 303.677 g/mol. Clolar, in its vial, appears as a clear and colourless liquid. Clolar in vials is sterile and preservative-free, and therefore can only be used once.
According to a study involving 40 ALL patients aged 2 to 19 years of age, Clolar is 47% bound to plasma proteins and concentrations were seen over wide range of body surface areas. Clolar has a half-life of 2.5 hours in the body, and 49-60% of it is excreted in the urine unchanged. The pathways of Clolar to the hepatic (liver) system are not yet known.
Clolar definition
Clolar is the brand name of the medication Clofarabine. Clofarabine is a medication indicated to treat pediatric cases of recurrent or refractory ALL.
Clolar classification
Clolar is classified as an antineoplastic medication working as a purine nucleoside metabolic inhibitor indicated for treatment of ALL.

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