激素和细胞毒药物--环磷酰胺Cyclophosphamide (Cytoxan, Endoxan, CTX) 

【化学名称】对-［双-(β-氯乙基)胺基］-β-苯丙氨酸。

【别名】癌得星、安道生、CTX。

【药理及作用】本品属细胞毒类药物，主要是通过杀伤免疫细胞，阻止其增殖而抑制免疫反应。主要用于经常复发的肾病综合征和激素依赖型肾病综合征。与激素同用，有可能减少激素的副作用。
本品在体外无活性，进入体内被肝脏或肿瘤内存在的过量的磷酰胺酶或磷酸酶水解，变为活化作用型的磷酰胺氮芥而起作用。其作用机制与氮芥相似，与DNA发生交叉联结，抑制DNA的合成，也可干扰RNA的功能，属细胞周期非特异性药物。本品抗瘤谱广，对多种肿瘤有抑制作用。

【药代动力学】环磷酰胺口服易吸收，迅速分布全身，约1小时后达血浆峰浓度，在肝脏转化释出磷酰胺氮芥，其代谢产物约50%与蛋白结合。静注后血浆半衰期4～6小时，48小时内经肾脏排出50%～70%，其中68%为代谢产物，32%为原形。 　　

【适应症】本品为目前广泛应用的抗癌药物，对恶性淋巴瘤、急性或慢性淋巴细胞白血病、多发性骨髓瘤有较好的疗效，对乳腺癌、睾丸肿瘤、卵巢癌、肺癌、头颈部鳞癌、鼻咽癌、神经母细胞瘤、横纹肌肉瘤及骨肉瘤均有一定的疗效。

【用法】每天每千克体重2-3毫克，可分为两次口服。亦可将两天的剂量加入注射用生理盐水内，隔日静脉注射1次。累积量不超过每千克体重150毫克。

【不良反应】骨髓抑制：白细胞减少较血小板减少为常见，最低值在用药后1～2周，多在2～3周后恢复。对肝功有影响。胃肠道反应：包括食欲减退、恶心及呕吐，一般停药1～3天即可消失。泌尿道反应：当大剂量环磷酰胺静滴，而缺乏有效预防措施时，可致出血性膀胱炎，表现为膀胱刺激症状、少尿、血尿及蛋白尿，系其代谢产物丙烯醛刺激膀胱所致，但环磷酰胺常规剂量应用时，其发生率较低。其他反应尚包括脱发、口腔炎、中毒性肝炎、皮肤色素沉着、月经紊乱、无精子或精子减少及肺纤维化等。

【禁忌】抗癌药物，必须在有经验的专科医生指导下用药。凡有骨髓抑制、感染、肝肾功能损害者禁用或慎用。对本品过敏者禁用。妊娠及哺乳期妇女禁用。

【注意】
1.本品早期副作用有骨髓抑制（白细胞减少等），感染，出血性膀胱炎，脱发，胃肠道反应；远期副作用有生殖系统功能损害（主要为睾丸生精能力损害，停经及卵巢纤维化较少见），发生恶性肿瘤。
2.用药期间，特别是用药后1-2周，定期检查血白细胞，如白细胞≤3Χ109/升，应减少本药的剂量或暂停使用。以免其代谢产物停留在膀胱内时间过长，而引起出血性膀胱炎。

【孕妇及哺乳期妇女用药】有致突变、致畸胎作用，可造成胎儿死亡或先天畸形，妊娠妇女禁用。本品可在乳汁中排出，在开始用药时必须中止哺乳。 　　

【药物相互作用】环磷酰胺可使血清中假胆碱酯酶减少，使血清尿酸水平增高，因此，与抗痛风药如别嘌呤醇、秋水仙碱、丙磺舒等同用时，应调整抗痛风药物的剂量。此外也加强了琥珀胆碱的神经肌肉阻滞作用，可使呼吸暂停延长。环磷酰胺可抑制胆碱酯酶活性，因而延长可卡因的作用并增加毒性。大剂量巴比妥类、皮质激素类药物可影响环磷酰胺的代谢，同时应用可增加环磷酰胺的急性毒性。 　　

【贮藏】遮光，密闭，在30℃以下保存。

【制剂】
片剂
注射剂

【原产地英文商品名】CYTOXAN 500mg/12mls/vial
【原产地英文药品名】CYCLOPHOSPHAMIDE
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·CYTOXAN 500毫克/12毫升/瓶
·CYTOXAN 500毫克/毫升/瓶
·CYTOXAN 2克/12毫升/瓶
·CYTOXAN 2克/毫升/瓶
·CYTOXAN 1克/12毫升/瓶
·CYTOXAN 1克/毫升/瓶
【中文参考药品译名】环磷酰胺
【生产厂家中文参考译名】百特
【生产厂家英文名】BAXTER HLTHCARE

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【原产地英文商品名】CYCLOPHOSPHAMIDE(CYTOXAN GENERIC)500mg/vial
【原产地英文药品名】CYCLOPHOSPHAMIDE
【中文参考商品译名:
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·环磷酰胺(CYTOXAN仿制药)1克/瓶
·环磷酰胺(CYTOXAN仿制药)2克/瓶
·环磷酰胺(CYTOXAN仿制药)500毫克/瓶
【中文参考药品译名:环磷酰胺
【生产厂家中文参考译名:百特
【生产厂家英文名:BAXTER HLTHCARE

GENERIC NAME: cyclophosphamide

BRAND NAME: Cytoxan

DRUG CLASS AND MECHANISM: Cyclophosphamide is a drug that is used primarily for treating several types of cancer. In order to work, cyclophosphamide first is converted by the liver into two chemicals, acrolein and phosphoramide. Acrolein and phosphoramide are the active compounds, and they slow the growth of cancer cells by interfering with the actions of deoxyribonucleic acid (DNA) within the cancerous cells. It is, therefore, referred to as a cytotoxic drug. Unfortunately, normal cells also are affected, and this results in serious side effects. Cytoxan also suppresses the immune system and is also referred to as immunosuppressive.

GENERIC AVAILABLE: Yes

PRESCRIPTION: Yes

PREPARATIONS: Powder for intravenous injection (100 mg), tablets of 25 and 50 mg.

STORAGE: Powder and tablets should be stored at room temperature, 15-30�C (59-86�F). Solutions prepared with bacteriostatic water are usable up to 24 hours if stored at room temperature and up to 6 days if stored in the refrigerator.

PRESCRIBED FOR: Cyclophosphamide is used for the treatment of several types of cancers and often in combination with other drugs to treat breast cancer, leukemia and ovarian cancer. It also is approved for treating nephrotic syndrome (a disease of the kidneys) in children. Unapproved uses include the treatment of Wegener's granulomatosis, severe rheumatoid arthritis, lupus erythematosus, advanced mycosis fungoides, and a number of forms of vasculitis.

DOSING: The usual initial dose for adults and children is 40-50 mg/kg administered intravenously over 3-5 days in divided doses. The usual oral dose is 1-5 mg/kg daily. Subsequent maintenance doses are adjusted based on the response of the tumor to treatment and the side effects.

DRUG INTERACTIONS: Allopurinol (Zyloprim) enhances the ability of cyclophosphamide to reduce production of blood cells from the bone marrow. (See below.)

Cyclophosphamide increases the occurrence of heart failure that is caused by doxorubicin (Adriamycin), increases the action of blood thinners such as coumarin (Coumadin), and decreases the effects of quinolone antibiotics (Cipro).

PREGNANCY: Use of cyclophosphamide during pregnancy may affect the fetus. Fetuses exposed to cyclophosphamide may be born with missing fingers, toes and a poorly-developed heart. Exposure in the second or third trimester may be less risky.

NURSING MOTHERS: Cyclophosphamide is excreted in breast milk and could cause serious problems in the nursing infant.

SIDE EFFECTS: Side effects of cyclophosphamide include hair loss, vomiting, diarrhea, mouth sores, sterility and jaundice.

Cyclophosphamide causes kidney failure, and it also may affect the heart and lungs. Cyclophosphamide suppresses production of blood cells from the bone marrow, including white blood cells (leukopenia), red blood cells (anemia) and platelets (thrombocytopenia). Leukopenia reduces the ability of the body to fight infection, thrombocytopenia impairs the ability of blood to clot, and anemia reduces the ability of blood to carry oxygen.

Cyclophosphamide also may cause inflammation of the urinary bladder with bleeding (hemorrhagic cystitis). This can result in lower abdominal pain from the bladder, problems urinating due to blood clots, and anemia due to loss of blood.