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英文药名: CeeNU (Lomustine Capsules)
中文药名: 洛莫司汀胶囊
品牌药生产厂家: Bristol Meyers Squibb
药品名称
洛莫司汀 Lomustine (CCNU)
别名：罗氮芥、罗莫司丁、环己亚硝脲、氯乙环己亚硝脲
规格
(1) 10mg (2) 40mg (3) 100mg
本品主要成份为：洛莫司汀。
其化学名称为：N-(2-氯乙基)-N′-环己基-N-亚硝基脲。
药理毒理
本品为细胞周期非特异性药，对处于G2－S边界，或S早期的细胞最敏感，对G2期亦有抑制作用。动物实验表明其与BCNU机理相似。
本品进入人体后，其分子从氨甲酰胺键处断裂为两部分：一为氯乙胺部分，将氯解离，形成乙烯碳正离子，发挥烃化作用，致使DNA链断裂，RNA及蛋白质受到烃化，这些主要与抗瘤作用有关；另一为氨甲酰基部分变为异氰酸酯．或再转化为氨甲酸，以发挥氨甲酰化作用，主要与蛋白质，特别是与其中的赖氨酸末端氨基等反应。据认为这主要与骨髓毒性作用有关，氨甲酰化作用还可破坏一些酶蛋白，使DNA受烃化破坏后较难于修复，有助于抗癌作用。
本品虽具烷化剂作用。但与一般烷化剂无交叉耐药性，与长春新碱、甲基苄肼及抗代谢药物亦无交叉耐药性。对小鼠和兔子的试验表明该药物有致癌性。
药代动力学
口服易吸收，体内迅速变为代谢产物。器官分布以肝（胆汁）。肾脾为多，次为肺、心、肌肉、小肠、大肠等。能透过血脑屏障，数分钟后脑脊液中药物浓度为血浆浓度的15～30%，可经胆汁排人肠道，形成肝肠循环，故药效持久。血浆蛋白结合率为50％（代谢物）。T1/2为16～18小时，其持久存在可能引起迟发性骨髓抑制。在肝内代谢完全，排泄于胆汁。有肠肝循环，故药效持久。在尿、血浆、脑脊液均无原形药存在。口服24小时内，本品的50％以代谢物形式从尿中排泄，但4日排泄量小于75%；从粪中排泄少于5%，从呼吸道排出约10％。因其脂溶性强，可有效透过血脑屏障。脑脊液中药物浓度为血浆中的50%或更高。
适应症
本品脂溶性强，可通过血脑屏障，进入脑脊液，常用于脑部原发肿瘤（如成胶质细胞瘤）及继发性肿瘤；治疗实体瘤，如联合用药治疗胃癌、直肠癌及支气管肺癌、恶性淋巴瘤等。
用法用量
100～130mg/m2，顿服，每6～8周一次，3次为一疗程。
任何疑问，请遵医嘱！
不良反应
口服后6小时内可发生恶心、呕吐，可持续2～3天，预先用镇静药或甲氧氯普胺并空腹服药药可减轻；少数患者发生胃肠道出血及肝功能损害。骨髓抑制，服药后3～5周可见血小板减少，白细胞降低可在服药后第1及第4周先后出现两次，第6～8周才恢复；但骨髓抑制有累计性。偶见全身性皮疹，有致畸胎的可能，亦可能抑制睾丸或卵巢功能，引起闭经或精子缺乏。
禁忌
有肝功能损害、白细胞低于4×109／l、血小板低于80×109／l者禁用。合并感染时应先治疗感染。
注意事项
1、因可引起突变和畸变，孕妇及哺乳期妇女应禁用。
2、对诊断的干扰：本品可引起肝功能一时性异常。
3、下列情况慎用：骨髓抑制、感染、肾功能不全、经过放射治疗或抗癌药治疗的患者或有白细胞低下史者。
4、用药期间应注意随访检查血常规及血小板、血尿素氮、血尿酸、肌酐清除率、血胆红素、丙氨酸氨基转移酶等。
5、病人宜睡前与止吐药、安眠药共服，用药当天不能饮酒。
6、治疗前和治疗中应检查肺功能。
孕妇及哺乳期妇女用药
本药有致癌、致畸作用，故妊娠及哺乳期妇女禁用。
儿童用药
100-130mg/m2，顿服，每6～8周重复。
药物相互作用
以本品组成联合化疗方案时，应避免合用有严重降低白细胞和血小板的抗癌药。
药物过量
尚无药物可对抗药物过量，如出现严重骨髓抑制，白细胞过低可使用粒细胞集落刺激因子。
Description:
Ceenu, ingredient lomustine, is an antineoplastic used to treat certain cancer.
WARNING:
Lomustine has caused serious blood disorders (e.g., bone marrow suppression, thrombocytopenia). These problems have an increased chance of occurring as more doses are used. Notify your doctor immediately if you have symptoms of an infection such as persistent fever or sore throat, easy bruising or bleeding, or unusual fatigue. Your doctor will monitor you and perform blood tests weekly for at least 6 weeks after each dose. Your dose may be adjusted accordingly. Some medicines or medical conditions may interact with this medicine. INFORM YOUR DOCTOR OR PHARMACIST of all prescription and over-the-counter medicine that you are taking. DO NOT TAKE THIS MEDICINE if you are also taking cimetidine. ADDITIONAL MONITORING OF YOUR DOSE OR CONDITION may be needed if you are taking aminoglycoside antibiotics. Inform your doctor of any other medical conditions, allergies, pregnancy, or breast-feeding. Contact your doctor or pharmacist if you have any questions or concerns about taking this medicine.
How to Use This Medicine:
Follow the directions for using this medicine provided by your doctor. THIS MEDICINE IS TAKEN BY MOUTH usually as a single dose which is not repeated for at least 6 weeks. There may be 2 or more different types of capsules in the container you receive. Ask your doctor, nurse, or pharmacist any questions you have about this medicine. TAKE THIS MEDICINE ON AN EMPTY STOMACH to reduce nausea and vomiting. DO NOT DRINK ALCOHOL on the day you take this medicine. IF NAUSEA, VOMITING, OR LOSS OF APPETITE OCCUR, ask your doctor, nurse, or pharmacist for ways to lessen these effects. STORE THIS MEDICINE at room temperature in a tightly-closed container, away from heat and light.
Cautions:
KEEP ALL DOCTOR AND LABORATORY APPOINTMENTS while you are being treated with this medicine. THIS MEDICINE LOWERS YOUR RESISTANCE to infection. To prevent infection, avoid contact with people who have colds or other infections. Do not touch your eyes or the inside of your nose unless you have thoroughly washed your hands first. THIS MEDICINE MAY REDUCE THE NUMBER OF BLOOD CELLS NEEDED FOR CLOTTING. To prevent bleeding, avoid situations where bruising or injury may occur. CHECK WITH YOUR DOCTOR BEFORE HAVING IMMUNIZATIONS (VACCINATIONS) while you are using this medicine. THE USE OF BIRTH CONTROL is recommended while taking this medicine. THIS MEDICINE HAS BEEN SHOWN TO CAUSE HARM to the human fetus. IF YOU PLAN ON BECOMING PREGNANT, discuss with your doctor the benefits and risks of using this medicine during pregnancy. THIS MEDICINE IS EXCRETED IN BREAST MILK. DO NOT BREAST-FEED while taking this medicine.
Possible Side Effects:
SIDE EFFECTS, that may go away during treatment, include nausea or vomiting, loss of appetite, or occasional hair loss. If they continue or are bothersome, check with your doctor. CHECK WITH YOUR DOCTOR AS SOON AS POSSIBLE if you experience shortness of breath; unusual bruising or bleeding; sores on the mouth or lips; fever or chills; dry cough; sore throat; or confusion. If you notice other effects not listed above, contact your doctor, nurse, or pharmacist.
Overdose:
If overdose is suspected, contact your local poison control center or emergency room immediately.
Additional Information: DO NOT SHARE THIS MEDICINE with others for whom it was not prescribed. DO NOT USE THIS MEDICINE for other health conditions. KEEP THIS MEDICINE out of the reach of children.
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