福达华注射剂fludarabine(Fludara Injection 50mg/2ml)

产地国家:美国

处方药:是

所属类别: 50毫克/2毫升/瓶

包装规格: 50毫克/2毫升/瓶

计价单位:瓶

生产厂家英文名:Berlex Laboratories Inc.

原产地英文商品名:Fludara Injection 50mg/2ml/Vial

原产地英文药品名:Fludarabine

中文参考商品译名:Fludara注射剂 50毫克/2毫升/瓶

中文参考药品译名:氟达拉滨

简介

注射用磷酸氟达拉滨,适应症为用于B细胞性慢性淋巴细胞白血病(CLL)患者的治疗,这些患者至少接受过一个标准的包含烷化剂的方案的治疗,但在治疗期间或治疗后,病情并没有改善或仍持续进展。

商品名称:FLUDARA 50MG

英文名:FLUDARABINE

中文名:福达华(氟达拉滨冻晶注射剂)

药理毒理:药效学本药系阿糖腺苷的2-氟,5-磷酸化衍生物。阿糖腺苷是一种合成的嘌呤类抗代谢药,虽然它是一种有效的抗病毒药,但由于它的低溶解度和腺嘌呤脱氨基酶的快速脱氨基作用,使体内抗肿瘤活性受到限制,因此可作为一种潜在的抗癌药。本药是在阿糖腺苷的嘌呤环第2位上以氟原子取代和第5’位上加上一个磷酸基而形成,提高了其溶解度,并可抵抗腺嘌呤脱氨基酶的脱氨基作用。本药在体内被血清磷酸酶去磷酸化成为2-氟-阿糖腺苷(9-β-D-阿拉伯呋喃糖-2-氟腺嘌呤)后,可被细胞摄取,然后被转化为有活性的三磷酸盐。该代谢产物是DNA合成的竞争性抑制剂。

已有的数据表明,本药能抑制几种酶的活性,包括DNA聚合酶、核糖核酸还原酶、腺苷甲硫氨酸转移酶。曾有报道,本药对T细胞的作用强于B细胞;但是,临床治疗B细胞性恶性瘤有效。临床前研究显示,本药对和L白血病、CD乳腺癌、LX-1人类异种皮移植癌和其它动物及人类的肿瘤细胞有较强的抗肿瘤活性。在Ⅰ期试验时,本药的剂量限制性毒性反应是骨髓抑制,高剂量时可见神经毒性。本药治疗慢性淋巴细胞性白血病和非霍奇金淋巴瘤中的作用较强。

药动学:用于慢性淋巴细胞性白血病时,静脉注射后7-21周可起效。口服给药1.1-1.2小时可达血药峰浓度,曲线下面积为 1760-3016(ng·h)/ml;静脉给药曲线下面积为3060(ng·h)/ml;皮下给药曲线下面积为4.56(ng·h)/ml。多次静脉给药药效可维持65-91周;对非霍奇金淋巴瘤患者,多次给药药效可维持2-20个月。本药口服后生物利用度为54%-56%,皮下给药的生物利用度为静脉注射的1.05倍。本药分布半衰期为57分钟,分布容积为98L/m2。代谢产物为2-氟-阿糖腺苷(有活性)和2-氟-腺嘌呤-5-三磷酸盐。约40% 经肾排泄,总体清除率为8.9L/(m2·h)。原型药物的清除半衰期为10.3-20小时。

适应症:用于B细胞性慢性淋巴细胞白血病(CLL)患者的治疗,这些患者至少接受过一个标准的包含烷化剂的方案的治疗,但在治疗期间或治疗后,病情并没有改善或仍持续进展。

禁忌症

1.禁忌症(1)对本药过敏者(国外资料)。(2)严重肾功能不全(肌酐清除率小于30ml/min)的患者。(3)失代偿性溶血性贫血的患者。(4)孕妇。(5)哺乳期妇女。

2.慎用(1)骨髓抑制者(国外资料)。(2)肾功能不全者(国外资料)。(3)有免疫缺陷的患者。(4)有机会性感染病史的患者。(5)肝功能不全者。

3.药物对儿童的影响儿童用药的安全性与有效性尚未确定。

4.药物对妊娠的影响国内资料中建议孕妇禁用本药,用药期间及停药后6个月内应避免怀孕;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。

5.药物对哺乳的影响尚不确定本药是否能分泌入乳汁,但在动物试验中,本药及其代谢产物可进入乳汁,因此,哺乳期妇女用药时应停止哺乳。

6.用药前后及用药时应当检查或监测治疗期间应定期(一周至少1次)监测全血细胞计数。

不良反应:以下不良反应的发生频率(常见≥1%,不常见>;0.1%但<;1%)主要源于临床试验资料,而没有考虑与本药的因果关系。罕见的不良反应(低于0.1%)主要源于上市后的报道。

1.心血管系统可见水肿,罕见心衰和心律失常。

2.中枢神经系统(1)常见周围神经病,少见精神混乱,罕见昏迷和焦虑不安。(2)有研究发现,高剂量本药与严重的神经毒性(如失明、昏迷和死亡)相关。静脉内给药4倍于推荐剂量(一日96mg/m2,连用5-7日)后,36%的患者出现了严重的中枢神经系统毒性。而应用推荐剂量患者,严重的中枢神经系统症状(如昏迷和焦虑不安)罕见或(精神混乱)少见。

3.呼吸系统常见肺炎。

4.泌尿生殖系统罕见出血性膀胱炎的报道。

5.肝脏少见肝酶和胰腺相关酶的改变。

6.胃肠道(1)常见胃肠异常(如恶心、呕吐、食欲缺乏、腹泻和胃炎)。(2)有报道,本药不良反应主要是与血小板减少相关的消化道出血。

7.血液(1)大多数患者可见血液学改变(如白细胞减少、血小板减少和贫血)。骨髓抑制可能是严重和有累积效应的。本药对减少T淋巴细胞数目长时间的影响可能导致机会感染危险性的增加[包括潜伏病毒的活化(如进行性多灶性脑白质病)]。(2)在实体瘤患者的Ⅰ期临床研究中发现,粒细胞数目降到最低的中位时间是13日(范围是3-25日),血小板是16日(范围是2-32日)。大多数患者的基础造血功能有损伤,可能是基础疾病的原因或是以前用骨髓抑制药物的结果。

8.皮肤(1)常见皮肤红斑。罕见Stevens-Johnson综合征或毒性表皮坏死(Lyells综合征)的报道。(2)有患者在用药后,既往的皮肤癌病变出现可逆性的恶化或骤然爆发的报道。

9.眼常有视觉障碍的报道。罕见病例中会出现视神经炎、视神经病变和失明。

10.过敏反应少见因过敏所致的呼吸困难和咳嗽的反应(肺浸润、肺炎和肺间质纤维化)。

11.其它(1)有出现肿瘤溶解综合征的报道,具体包括高尿酸血症、高磷酸血症、低钙血症、代谢性酸中毒、高钾血症、血尿、尿酸结晶尿和肾衰竭。腰疼和血尿可以是该综合征的首发症状。鉴于这种综合征在用药后的第1周就可出现,建议对高危人群应及早采取预防措施。(2)有患者在用药后,出现致命的自身免疫现象(如自身免疫性溶血性贫血、自身免疫性血小板减少、血小板减少性紫癜、天疱疮、Evans综合征)的报道。大多数溶血性贫血的患者在再次接受本药治疗后,可出现症状的反复。此时应停药,输血(辐射后血液)并使用肾上腺皮质激素制剂进行治疗。

国外不良反应参考

1.心血管系统在临床试验(n=133)中,水肿发生率为8%-19%。

2.中枢神经系统(1)在临床试验(n=133)中,可见虚弱无力(9%-65%)、感觉异常(4%-12%);激动、精神混乱和昏迷也有报道。还有周围神经病变的报道和“垂腕症”的个案报道。(2)有使用高剂量本药(一日100-150mg/m2,连用5-7日),引起严重的迟发神经毒性的报道。表现为视野缺损、构音困难、感觉异常、虚弱无力及癫痫发作,甚至发展为双侧皮质盲、意识混乱、痉挛性瘫痪和昏迷。中枢神经系统进行性脱髓鞘可能是导致神经毒性反应的原因。(3)在36位接受过至少1个疗程、一日剂量不超过96mg/m2、连用5-7日的患者中,有13位出现严重的中枢神经系统毒性,其中11位患者出现了视觉缺失。精神状态的恶化和进行性脑病也有发生。此13名患者全部死亡。(4)有引起脑白质炎的报道。常见的症状有单侧轻偏瘫和共济失调,并有患者死亡的个案报道。(5)有引起嗜睡和(或)疲倦的报道。

3.呼吸系统(1)在临床试验(n=133)中,可见肺炎(16%-22%)、咳嗽(10%-44%)、呼吸困难(9%-22%)、鼻窦炎(不超过5%)、咽炎(不超过9%)及上呼吸道感染(2%-16%)。(2)过敏时可见呼吸困难、咳嗽和间质性肺浸润。(3)其它尚有急性呼吸窘迫综合征、呼吸窘迫、肺出血、肺纤维化和呼吸衰竭。(4)有患者用药(一日25mg/m2,连用3日,一月1次)10个疗程后,出现了严重的呼吸系统合胞病毒(RSV)肺部感染的个案报道。

4.肌肉骨骼系统(1)有出现肌无力的报道,但尚不清楚这是否为一种神经毒性的前驱症状。(2)在临床试验(n=133)中,4%-16%的患者出现肌痛。(3)有出现骨髓4维化的个案报道,但与本药的关系尚不明确。

5.泌尿生殖系统在临床试验(n=133)中,可见排尿困难(3%-4%)和感染(2%-15%)。极少有出现出血性膀胱炎的报道。

6.肝脏有联合使用环磷酰胺(首日1000mg/m2)和本药(20mg/m2,连用5日)3个疗程,治疗非霍奇金淋巴瘤,由于腺病毒感染而发生严重的爆发性肝功能衰竭的个案报道。

7.胃肠道(1)在临床试验(n=133)中,可见恶心和(或)呕吐(31%-36%)、腹泻(13%-15%)、畏食(7%-34%)、口腔炎(低于9%)和胃肠道出血(3%-13%)。(2)有引起假性肠梗阻的个案报道。

8.血液(1)中性粒细胞减少症和血小板减少症是最常见不良反应,具有剂量限制性。少见淋巴细胞减少症和贫血症的报道。有本药引起全血血细胞减少(可持续2个月到1年),并导致致死的报道。(2)有引起自身免疫性贫血并致死的报道。多数患者再次用药时,会引起溶血复发。(3)有引起嗜酸粒细胞增多症的报道。(4)有引起嗜血细胞综合征,并导致患者死亡的个案报道。(5)有引起骨髓纤维化的个案报道。

9.皮肤(1)有患者静脉给药(25mg/m2,连用5日)后,出现副肿瘤性天疱疮[表现为结膜炎、水肿,四肢末端、颜面部和(或)躯干部表皮水疱]的报道。(2)在临床试验(n=133)中,15%的患者可见皮疹。

10.眼(1)在临床试验(n=133)中,3%-15%的患者出现视力障碍。(2)有报道,本药(尤其是高剂量)导致的神经毒性综合征中,可见视力模糊、复视、畏光,甚至发展为失明。

11.其它(1)在临床试验(n=133)中,出现了发热(69%)、寒战(11%-19%)、乏力(10%-38%)、感染(33%-44%)及疼痛(20%-22%)。(2)有患者静脉给药后,先出现发热,然后出现肺炎的个案报道。(3)有1例瓦尔登斯特伦巨球蛋白血症白人女性患者,用药6个月后,出现隐球菌性脑膜炎和颅内结核瘤的报道。(4)有出现移植物抗宿主病、疱疹病毒感染的报道。(5)对595例使用过本药的患者进行了平均时间长达7.4年的随访,其中23例出现继发的恶性肿瘤。继发肿瘤分别为肺癌(n=6)、霍奇金淋巴瘤 (n=5)、结肠癌(n=4)、膀胱癌(n=2)、头颈部肿瘤(n=2)、肝癌(n=1)、白血病(n=1)、中枢神经系统肿瘤(n=10和肉瘤 (n=1)。(6)据报道,在接受过本药治疗的患者中,曾出现过腰痛和血尿,这可能是肿瘤溶解综合征的症状。肿瘤溶解综合征可能包括了高尿酸血症、高磷血症、低钙血症、代谢性酸中毒、高钾血症、血尿、尿酸盐结晶和肾功能不全。

注意事项:药物-药物相互作用。

1.用药期间接种活疫苗(如轮状病毒疫苗),可使免疫应答降低,导致患者被活疫苗感染。建议用药期间不应接种活疫苗。白血病缓解患者在结束化疗至少3个月后,方能接种活疫苗。

2.与喷司他丁合用,可增加发生严重肺毒性的风险。不推荐两药合用。3.腺苷吸收抑制药(如双嘧达莫)可减弱本药的疗效。

用法与用量:成人常规剂量静脉滴注一日25mg/m2,持续30分钟,连用5日。然后停药23日(即 28日为1个疗程)。疗程取决于疗效及患者对药物的耐受性(一般至少需6个疗程)。肾功能不全时剂量对肾功能不全患者的剂量应作相应的调整。肌酐清除率为 30-70ml/min时,剂量应减少50%,且应严密检测血液学改变以评价药物的毒性。若肌酐清除率小于30ml/min,应禁用本药。

国外用法用量参考:成人常规剂量静脉滴注一日25mg/m2,持续约30分钟,连用5日。28日后继续下1个疗程。用药剂量应根据血液或非血液毒性进行调整。建议在达到最佳治疗效果后,应再给药3个疗程。肾功能不全时剂量中度肾功能能损害[肌酐清除率为30-70ml/(min·1.73m的患者,用量应降低20%-50%;严重肾功能损害[肌酐清除率小于30ml/(min·1.73m)]的患者,不推荐使用本药。

规格:50mg/瓶

贮存:室温(最高温度30℃)保存。

有效期:暂定两年

批准文号:注册证号H20080009

生产厂家:拜耳医药保健有限公司广州分公司

英文版说明书

Fludarabine Injection(floo dare’ a been)IMPORTANT WARNING:Fludarabine injection must be given under the supervision of a doctor who is experienced in giving chemotherapy medications for cancer.Fludarabine injection can cause a decrease in the number of blood cells made by your bone marrow.This decrease may cause you to develop dangerous symptoms and may increase your risk of having a serious or life-threatening infection. Your doctor may prescribe other medications to decrease the risk that you will develop a severe infection during your treatment.Tell your doctor if you have or have ever had a low number of any type of blood cells in your blood or any condition that affects your immune system and if you have ever developed an infection because your blood cell levels were too low. If you experience any of the following symptoms, call your doctor immediately: shortness of breath; fast heartbeat; headache; dizziness; pale skin; extreme tiredness; unusual bleeding or bruising; black, tarry, or bloody stool; vomit that is bloody or that looks like coffee grounds; and fever, chills, cough, sore throat, difficult, painful, or frequent urination, or other signs of infection.Fludarabine injection can also cause damage to the nervous system .If you experience any of the following symptoms, call your doctor immediately: seizures, agitation, confusion, and coma (loss of consciousness for a period of time).Fludarabine injection may cause serious or life-threatening conditions in which the body attacks and destroys its own blood cells.Tell your doctor if you have ever developed this type of condition after receiving fludarabine in the past.If you experience any of the following symptoms, call your doctor immediately: dark urine, yellow skin, tiny red or purple dots on the skin, nosebleeds, heavy menstrual bleeding, blood in the urine, coughing up blood, or difficulty breathing due to bleeding in the throat.In a clinical study, people with chronic lymphocytic leukemia who used fludarabine injection along with pentostatin (Nipent) were at high risk of developing serious lung damage.In some cases, this lung damage caused death. Therefore, your doctor will not prescribe fludarabine injection to be given along with pentostatin (Nipent).Keep all appointments with your doctor and the laboratory. Your doctor will order certain tests to check your body’s response to fludarabine injection.Talk to your doctor about the risks of receiving fludarabine injection.Why is this medication prescribed?Fludarabine injection is used to treat chronic lymphocytic leukemia (CLL; a type of cancer of the white blood cells) in adults who have already been treated with at least one other medication and have not gotten better. Fludarabine injection is in a class of medications called purine analogs.It works by slowing or stopping the growth of cancer cells in your body.How should this medicine be used?Fludarabine injection comes as a powder to be added to fluid and injected over 30 minutes intravenously (into a vein) by a doctor or nurse in a medical office or hospital outpatient clinic.It is usually injected once a day for 5 days in a row.This treatment period is called a cycle, and the cycle may be repeated every 28 days for several cycles.Your doctor may need to delay your treatment or adjust your dose if you experience certain side effects. Be sure to tell your doctor how you are feeling during your treatment with fludarabine injection.Other uses for this medicineFludarabine injection is also sometimes used to treat non-Hodgkin’s lymphoma (NHL; cancer that begins in a type of white blood cell that normally fights infection) and mycosis fungoides (a type of lymphoma that affects the skin). Talk to your doctor about the risks of using this medication for your condition.This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.What special precautions should I follow?Before receiving fludarabine injection,tell your doctor and pharmacist if you are allergic to fludarabine, any other medications, or any of the ingredients in fludarabine injection. Ask your pharmacist for a list of the ingredients.tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.Be sure to mention the medication listed in the IMPORTANT WARNING section or cytarabine(Cytosar-U, DepoCyt). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.tell your doctor if you have or have ever had kidney disease.Also tell your doctor about all the other chemotherapy medications you have received and if you have ever been treated with radiation therapy (cancer treatment that uses waves of high energy particles to kill cancer cells). Before you receive chemotherapy or radiation therapy in the future, tell your doctor that you have been treated with fludarabine.you should know that fludarabine injection may interfere with the normal menstrual cycle (period) in women and may stop sperm production in men.However, you should not assume that you or your partner cannot become pregnant.If you are pregnant or breast-feeding, you should tell your doctor before you beginreceiving this medication. You should not plan to have children while receiving fludarabine injection or for at least 6 months after treatments. Use a reliable method of birth control to prevent pregnancy during this time. Talk to your doctor for further details.Fludarabine injection may harm the fetus.if you are having surgery, including dental surgery, tell the doctor or dentist that you are receiving fludarabine injection.you should know that fludarabine injection may cause tiredness, weakness, confusion, agitation, seizures, and vision changes. Do not drive a car or operate machinery until you know how this medication affects you.talk to your doctor before you receive any vaccinations during your treatment with fludarabine injection.you should know that you may develop a serious or life-threatening reaction if you need to receive a blood transfusion during your treatment with fludarabine injection or at any time after your treatment. Be sure to tell your doctor that you are receiving or have received fludarabine injection before you receive a blood transfusion.What special dietary instructions should I follow?Unless your doctor tells you otherwise, continue your normal diet.What side effects can this medication cause?Fludarabine injection may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:loss of appetitenauseavomitingconstipationdiarrheamouth soreshair lossnumbness, burning, pain, or tingling in the hands, arms, feet, or legsmuscle or joint painheadachedepressionsleep problemsSome side effects can be serious. If you experience any of these symptoms or those listed in the IMPORTANT WARNING section, call your doctor immediately:chest pain or discomfortfast or irregular heartbeathearing losspain along the side of the bodyswelling of the arms, hands, feet, ankles, or lower legsrashhivesdifficulty breathing or swallowingpeeling or blistering skinFludarabine injection may cause other side effects. Call your doctor if you have any unusual problems while receiving this medication.If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online or by phone [1-800-332-1088].In case of emergency/overdoseIn case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.Symptoms of overdose may include:unusual bruising or bleedingfever, chills, cough, sore throat, or other signs of infectiondelayed blindnesscomaWhat other information should I know?Ask your doctor or pharmacist if you have any questions about fludarabine injection.It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital.It is also important information to carry with you in case of emergencies.Brand namesFludaraOther names2-Fluoro-ara-A Monophosphate, 2-Fluoro-ara AMP, FAMP

 

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