英文药名: Procytox (cyclophosphamide tablets) 中文药名: 环磷酰胺片 药品名称 中文别名：环磷氮芥，安道生，癌得星，癌得散。 外文名：Cyclophosphamide, Cytoxan, En-doxan, Neosar, Procytox, Sendoxan, Cyclophos-phan, Cytophosphan, Genoxal。 药理作用 CTX为HN2的衍生物，其作用与HN2类似，但抗瘤谱比HN2广，毒性亦比HN2小，亦为细胞周期非特异性药物，但对G2期作用显著。本品在体外无活性，在体内经肝微烂漫混合功能氧化酶P450活化后方具有烷化活力。首先是其环N原子邻近的C被氧化，生成4-羟基环烯磷酰胺，自发开环生成醛磷酰胺（aldophosphoramide），4-羟基环磷酰胺与醛磷酰胺两者维持动态平衡，经可溶性酶分别氧化成4-酮基环磷酰胺和羧基磷酰胺，后两者无细胞毒作用，是从尿中排泄的失活性产物，约占CTX用量的80%。未经氧化的醛磷酰胺可自发生成丙烯醋和磷酰胺氮芥（PM），PM是CTX的活性代谢物，具有烷化活性和细胞毒作用。4-羟基环磷酰胺和醛磷酰胺不具有烷化活性，是一种转运型化合物，将高度极性的PM转运到细胞内和血液循环中，PM和DNA形成交叉联结，影响DNA功能，抑制肿瘤细胞生长与繁殖。CTX在临床上的耐药机制正在研究中，许多学者认为与多药耐药基因及P糖蛋白有关。 药动学 本品口服后易被吸收，迅速分布全身，生物利用度为74%~97%，血液浓度1小时后达高峰，与血浆蛋白结合不足20%。在肝脏转化释放出磷酰胺氮芥，半衰期为4~6.5小时；48小时内由肾脏排出50%~70%，68%为代谢物，32%为原形。静脉给药60mg/kg后，血浆峰浓度500umol/L,血浆半衰期为3~10小时。环磷酰胺能少量通过血脑屏障，脑脊液中的浓度仅为血浆的20%。 适应症 本品为目前广泛应用的烷化剂之一。 （1）非霍奇金淋巴瘤：单用有效率为55%~65%，联合用药可选CHOP方案。 （2）小细胞肺癌：单用有效率为38%，联合用药可选COMVP方案。 （3）乳腺癌：单药有效率为33%，联合用药可选CAF方案。 （4）对卵巢癌、多发性骨髓瘤、神经母细胞瘤、睾丸肿瘤、胸腺癌等均有一定疗效。 （5）对儿童急性淋巴细胞性白血病、慢性淋巴细胞性白血病等有较好疗效。 （6）用于宫颈癌、头颈部癌、结肠癌、前列腺癌及肉瘤术后化疗，可提高远期生存率。 （7）作为免疫抑制剂，可用于流行性出血热、肾移植；对Weger肉芽肿及激素耐药的系统性坏死血管炎可作为首选药。 用法用量 成人： 静脉注射，每次15~20mg/kg，或600mg/m2，每周1次，总量8~12g为1疗程；冲击疗法，一般每次不超过1500mg，用生理盐水稀释，由皮管缓慢注射，每周1次，冲击2~3次，治疗无效则停药。 口服，每日2~4mg/kg或50~200mg，作维持治疗，总量10~15g；用于免疫抑制，可每日1.5~3mg，分1~2次口服，连服4~6周。 动脉注射：每次200~400mg，每日或隔日1次，总量8~10g。 儿童： 静脉注射，每次2~6mg/kg，每日或隔日1次，2~3g为1疗程；冲击疗法，每次10~20mg/kg,每周1次，或分2次，以生理盐水20ml稀释后缓慢注射。 口服，每日2~8mg/kg，分2次口服。 任何疑问，请遵医嘱！ 不良反应 （1）骨髓抑制：以白细胞下降为最常见，在用药后的8~15日达到最低点，但恢复较快，一般在用药后18~25日即可恢复正常；血小板减少不常出现。 （2）胃肠道反应：常见有食欲下降，恶心，呕吐，少见腹泻，偶可引起口腔炎、胃肠粘膜溃疡，口因部感觉异常。 （3）泌尿系统反应：5%~15%的患者可能出现出血性膀胱炎，表现为尿频、尿急、尿痛等，停药后可恢复，但膀胱损伤是永久性的；大剂量静脉注射时可引起少尿、血尿、蛋白尿等，系本品代谢物丙烯醛对尿路刺激所致，治疗白血病或淋巴瘤时因破坏大量瘤细胞，易发生高尿酸血症及尿酸性肾痛。 （4）心脏毒性：高剂量时可产生心肌坏死，可能引起心脏毒性，出现急性心衰而致死，多发生于首次给药15日内；放射治疗、与色霉素合用均可促使心脏毒性发生。 （5）肝脏毒性：有时可出现肝功能损害，黄疸等。 （6）皮肤反应：损害毛囊，造成脱发；皮炎，皮肤和甲术色素沉着，指甲变形，荨麻疹等。 （7）其它反应：头晕，不安，幻视，久用可致闭经或精子减少，个别可发生肺纤维化，长期使用可发生继发性肿瘤。 禁忌症 （1）孕妇及哺乳妇女禁用。 （2）肝肾功能损害、感染、骨髓抑制、痛风、泌尿系结石和曾接受放疗或化疗患者慎用。 注意事项 （1）使用本品采用大剂量冲击或中等剂量间歇给药比小剂量连续给药疗效好。 （2）当使用冲击疗法或大剂量给药时，应注意膀胱刺激症状，应鼓励患者多饮水，大量补液，碱化尿液，每日尿量保持在2000~3000ml，以减轻刺激。 （3）本品与别嘌呤醇合用，有可能加重其骨髓抑制；与苯二氮卓类药物同用时，可能使肝药酶受诱导，使本品代谢产物增多，毒性增加。本品还可增加血清尿酸水平，与阿霉素同用可增加心脏毒性。 （4）本品溶解度小，应强力摇匀，必须在完全溶解后才能注射用。 规格 片剂：25mg/片，50mg/片。   Cyclophosphamide review

Cyclophosphamide is a drug used for the treatment of various types of cancer. Aside from being a cytotoxic drug, Cyclophosphamide is immunosuppressive since it can suppress the immune system.

Cyclophosphamide is marketed under the brand name Cytoxan. It is available in tablet form as well as a powder used for intravenous injection. It is prescribed to individuals who are suffering from certain types of cancer such as ovarian, breast, and leukemia. It is also known to cure nephritic syndrome, an ailment of the kidneys among children.

The initial dosage of Cyclophosphamide is at least 40 mg injected in a stretch of 3-5 days divided in various doses. The usual dosage for oral use is 1-5 mg/kg per day. The dosage is then adjusted depending on the tumor’s response to the medication and its side effects.

Cyclophosphamide should be taken as prescribed by a physician. While using Cyclophosphamide, patients should drink more water and urinate more frequently. This should help the kidneys in removing the drug from the system and lowering the chances of occurrence of side effects.

Patients should not stop using Cyclophosphamide until the prescribed schedule of a physician, or even if they experience nausea or vomiting.

This drug usually works a month or two before producing positive results. The effects also hinge on the illness being treated.

One of the most common side effects is nausea. Doctors usually prescribe another medication to reduce this side effect.

Users may also experience bleeding and inflammation of the bladder wall, or haemorrhagic cystitis characterized by blood in the urine. To reduce the chances of this side effect, patients are advised to drink more water, preferably up to 10 glasses a day.

This drug can also have an effect on the blood count of the patient. It can also result to hair loss, irregular menstrual periods, and mouth ulcers. In case a patient develops these symptoms after using Cyclophosphamide, he or she should immediately inform a doctor.

Patients who came into close contact with a person with chicken pox are advised to stop using Cyclophosphamide and immediately consult a doctor. This case usually requires a special, antiviral treatment since chicken pox can be severe among people who are undergoing treatment with Cyclophosphamide.

Since Cyclophosphamide may affect the bladder and the blood, doctors may have to arrange for a blood and urine examination before allowing the patient to start treatment with Cyclophosphamide. Regular examinations are also required while the patient takes Cyclophosphamide. Patients should not take Cyclophosphamide unless they are undergoing regular blood and urine examinations.

Certain medications may interact negatively with other drugs. Patients should make it a point to inform their physicians if they are beginning to take new drugs while taking Cyclophosphamide.

Taking Cyclophosphamide may lead to a decrease in fertility among women and men; so young users are advised to use this medication with caution.

Pregnant women should never take this drug. Cyclophosphamide may also be passed on to infants so breastfeeding mothers should not take this medication.

Cyclophosphamide has the following structural formula:

Brand name(s): Clafen, Claphene, Cyclophosphamid, Cyclophosphamidum, Cyclophosphan, Cyclophosphane, Cyclophosphoramide, Cyclostin, Cyklofosfamid, Cytophosphan, Cytoxan, Endoxan, Endoxan R, Endoxana, Endoxanal, Endoxane, Enduxan, Genoxal, Hexadrin, Lyophilized Cytoxan, Mitoxan, Neosar, Procytox, Semdoxan, Sendoxan, Senduxan, Zyklophosphamid