替莫唑胺Temodar(temozolomide for Injection)

产地国家：加拿大

处方药：是

所属类别： 100毫克／支

包装规格： 100毫克／支

计价单位：盒

生产厂家英文名：Merck

原产地英文商品名：Temodar Powder for Solution for Injection 100mg/vial

原产地英文药品名：TEMOZOLOMIDE

中文参考商品译名：Temodar注射用粉剂 100毫克/支

中文参考药品译名：替莫唑胺

简介

【制造商】先灵葆雅 ( Schering-Plough )

【成份】Temozolomide

【适应症】本品用于治疗 :新诊断的多形性胶质母细胞瘤，开始先与放疗联合治疗，随后作为辅助治疗；常规治疗后复发或进展的多形性胶质母细胞瘤或间变性星形细胞瘤。

【用量】新诊断的多形性胶质母细胞瘤的成人患者：同步放化疗期：口服本品，75mg/m2/日，共42天，同时接受放疗。随后接受6个周期的本品辅助治疗。根据患者耐受程度可暂停用药，但无需降低剂量。

辅助治疗期：同步放化疗期结束后4周，进行6个周期的本品单药辅助治疗。

起始剂量 ：150mg/m2/日，共5天，然后停药23天。一周期为28天。从第2周期开始，根据前1周期不良反应，剂量可增至200mg/m2/日，或减至100 mg/m2。

常规治疗后复发或进展的多形性胶质母细胞瘤或间变性星形细胞瘤患者：成人患者：以前曾接受过化疗者的起始剂量是150 mg/m2/日，共5天。 成人 没有接受过其他化疗者的起始剂量为200mg/m2/日，均连用5天，28天为一个周期。治疗可继续到病变出现进展，最多为2年。

儿童患者：在以前接受过化疗3岁或以上的患儿，每28天周期中本品口服起始剂量是 150mg/m2/日，共5天。如果没有出现毒性，下个周期的剂量增至200 mg/m2/日.治疗可继续到病变出现进展，最多为2年。

全部患者：应空腹（进餐钱至少一小时）服用本品。服用本品前后可使用止吐药。如果服药后出现呕吐，不能打开或咀嚼本品，应用一杯水整粒吞服。如果胶囊有破损，应避免皮肤或粘膜与胶囊内粉状内容物接触。

【FDA妊娠分级】D级:有明确证据显示，药物对人类胎儿有危害性，但尽管如此，孕妇用药后绝对有益（例如用该药物来挽救孕妇的生命，或治疗用其他较安全的药物无效的严重疾病）。

【禁忌】对本药或达卡巴嗪过敏、妊娠期、严重骨髓抑制的患者禁用。

【注意事项】对于接受42-49天合并治疗者需要预防卡氏肺囊虫性肺炎发生。男性患者在治疗过程及治疗结束后6个月之内应避孕，在接受该治疗之前应冰冻保存精子。严重肝功能异常或肾功能异常者慎用。本药不应用于哺乳期妇女。目前尚无3岁以下多形性胶质母细胞瘤患儿使用该药的临床经验。

【儿童用药】尚无3岁以下多形性胶质母细胞瘤患儿使用该药的临床经验；对于3岁以上胶质瘤儿童患者，使用该药的临床经验有限。

【老年患者用药】与年轻患者相比，老年患者（>70岁）中性粒细胞减少及血小板减少的可能性较大。

【孕妇及哺乳期妇女用药】对妊娠期妇女使用该药尚未进行研究。在用大鼠和兔所进行的临床前研究中，给药150mg/m2曾有致畸和/或胎儿毒性的报道。因此替莫唑胺不应常规用于妊娠期妇女，如果妊娠期内必须使用该药，应将可能对胎儿造成的潜在风险告知病人。对于可能怀孕的妇女，应劝阻其在接受替莫唑胺治疗或在终止替莫唑胺治疗后6个月内怀孕。替莫唑胺是否可经母乳分泌尚不可知，因此替莫唑胺胶囊不应用于哺乳期妇女。

【不良反应】轻中度胃肠道功能紊乱，具有自限性，或标准止吐药易于控制。骨髓抑制（一般在开始几个周期的第21-28天），通常在1-2周内迅速恢复。其他不良反应包括：口腔念珠菌病、感染，血象异常，体重降低，焦虑、抑郁、情绪不稳定、失眠、头痛、惊厥、头晕等神经系统症状，视力障碍，听力损害、耳鸣，下肢浮肿、出血、深静脉血栓形成，咳嗽、呼吸困难，脱发、皮肤干燥，肌无力，尿失禁，疲乏、发热、疼痛、过敏反应、放射损伤、味觉异常，SGPT升高。

【药物相互作用】同时服用丙戊酸，替莫唑胺清除率轻度降低。与其他可导致骨髓抑制的的药物联合应用时，骨髓抑制可能加重。

【药物过量】在患者中已进行了剂量为500，750，1000和1250 mg/m2(每治疗周期服药5天的总剂量)的临床评价。剂量限制性毒性为血液学毒性，在任一剂量下均有报道，但在较高剂量时较为严重。1患者5天中每天过量服用2000mg，所报道的不良事件为全血细胞减少症、发热、多器官衰竭及死亡。在服药超过5天（最长达64天）的患者中所发生的不良事件包括骨髓抑制（伴随或不伴随感染），某些严重且持久的病例最终死亡。在药物过量事件中，应进行血液学评价。必要时应采取支持性措施。

【药理作用】替莫唑胺为咪唑并四嗪类具有抗肿瘤活性的烷化剂。在体循环生理pH状态下，迅速转化为活性产物MTIC（3-甲基-(三嗪-1-)咪唑-4-甲酰胺）。MTIC的细胞毒作用主要表现为DNA分子上鸟嘌呤第6位氧原子上的烷基化以及第7位氮原子的烷基化。通过甲基化加成物的错配修复，发挥细胞毒作用。

【药代动力学】临床前数据提示本品能迅速通过血脑屏障，进入脑脊液。成年患者口服本品后，被迅速吸收，最早在服药后20分钟就可达到血药峰浓度（平均时间为0.5-1.5小时）。血浆清除率、分布容积和半衰期都与剂量无关。本品的蛋白结合率低(10-20%)，因此估计不会与蛋白结合率高的药物发生相互作用。口服14C-本品后7天内粪便内排泄的14C为0.8%，表明药物是完全吸收的。口服后，24小时尿内的原形药占剂量的5%-10%左右，其余是以AIC（4-氨基-5-咪唑-盐酸羧酰胺）形式或其他极性代谢物排泄到尿中。本品药代动力学的群体分析表明本品血浆清除率与年龄、肾功能或吸烟无关。儿科患者的AUC比成人患者高，但是儿童和成人每周期的最大耐受剂量(MTD) 都是1000mg/m2。

英文版说明书

Temodar DescriptionThis medication is used to treat certain types of brain cancer. It is a chemotherapy drug that works by slowing cancer cell growth. In some patients, temozolomide decreases the size of brain tumors.OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.This medication may also be used to treat other types of cancer (such as bone cancer).Temodar DirectionsRead the Patient Information Leaflet provided by your pharmacist before you start using temozolomide and each time you get a refill. If you have any questions about the information or if you are not certain which days of the treatment cycle to take your medication, consult your doctor or pharmacist.Take this medication by mouth, usually once daily or as directed by your doctor. To reduce nausea and vomiting, take it on an empty stomach (1 hour before or 3 hours after a meal) or at bedtime, unless otherwise directed by your doctor. To make sure the amount of medicine in your body is kept at a constant level, take it at the same time every day in relation to a meal (e.g., always 1 hour before the evening meal or always 3 hours after the evening meal).Swallow the capsules whole with a full glass of water (8 ounces or 240 milliliters). The dosage is based on your medical condition, body size, and response to therapy.Do not crush, chew, or open the capsules. If the capsules are accidentally opened or damaged, avoid inhaling the medication, and do not let it touch the skin or mucous membranes (e.g., inside the nose). If contact occurs, flush the area with water. Since this drug can be absorbed through the skin, women who are pregnant or who may become pregnant should not handle this medication.Do not increase your dose or take this medication more often without your doctor's approval. Your condition will not improve any faster and the risk of serious side effects may be increased.Temodar CautionsBefore taking temozolomide, tell your doctor or pharmacist if you are allergic to it; or to dacarbazine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney problems, liver problems, decreased bone marrow function, blood cell disorders (e.g., anemia, leukopenia, thrombocytopenia).Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine.To lower the chance of getting cut, bruised or injured, use caution with sharp objects like safety razors or nail cutters, and avoid activities such as contact sports. Use a soft-bristle toothbrush to lower the risk of bleeding gums.Wash your hands well to prevent the spread of infections.The elderly may be more sensitive to the side effects of this drug, especially the increased risk of infection and easy bruising/bleeding.Women may be more sensitive to the side effects of this drug, especially the increased risk of infection and easy bruising/bleeding.This medication is not recommended for use during pregnancy. It may harm an unborn baby. It is recommended that men and women use two effective forms of birth control (e.g., condoms and birth control pills) during treatment with this drug and for some time afterwards. Consult your doctor for more details and to discuss reliable forms of birth control.It is not known if this drug passes into breast milk. Due to the potential risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.Temodar Side EffectsNausea, vomiting, loss of appetite, constipation, tiredness, weakness, and headache may occur. Nausea and vomiting can be quite severe. Drug therapy may be necessary to prevent or relieve nausea and vomiting. Not eating before your treatment may help relieve vomiting. Changes in diet and lifestyle, such as eating several small meals or limiting activity, may help lessen some of these effects. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.Temporary hair loss may occur. Normal hair growth should return after treatment has ended.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor immediately if any of these unlikely but serious side effects occur: mouth sores, swelling of the ankles/feet, easy bleeding or bruising, shortness of breath.This medication can lower the body's ability to fight an infection. Notify your doctor promptly if you develop any signs of an infection such as: fever, chills, persistent sore throat, cough, burning/painful/frequent urination.Although temozolomide is used to treat cancer, very rarely in some patients it may increase the risk of developing another form of cancer (of the bone marrow). Consult your doctor for more details. Tell your doctor immediately if you develop: swollen glands, unexplained or sudden weight loss, night sweats.A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.Temodar Active IngredientsTemozolomide.