英文药名：TEMODAL Infusion(Temozolomide) 中文药名：替莫唑胺冻干粉注射剂 生产厂家：MSD有限公司 テモダール点滴静注用100mg 治疗类别名称 抗肿瘤药 商標名 TEMODAL Infusion 100mg 一般名 テモゾロミド（JAN） Temozolomide（JAN） 化学名 3-Methyl-4-oxo-3,4-dihydroimidazo［5,1-d］［1,2,3,5］ tetrazine-8-carboxamide 構造式 分子式 C6H6N6O2 分子量 194.15 性　状 白中的细红或浅黄棕色粉末，微溶于二甲亚砜，水，甲醇，丙酮，或乙腈微溶，在乙醇（95）非常微溶。 熔点 约206℃（分解） 分配系数（1-辛醇/水系统） 20.8至22.4 用0.1mol/L磷酸盐缓冲液（pH7.0） 22.0 加0.1mol/L盐酸试液 20.8 水 22.4 条件批准 由于案件审理在日本该药已经非常有限，上市后，直至有关一定数量的病例数据集成，通过实现对一切案件的使用，调查结果，随着了解这种药物的使用患者的背景资料，数据早来收集这些药物的安全性和有效性，采取必要的措施，正确使用此药。 药效药理 替莫唑胺是一价烷基化剂在生理pH条件下分解成非酶MTIC，是甲基重氮离子，通过甲基化的DNA的表现出抗肿瘤活性。 1. 抗肿瘤作用 替莫唑胺显示出在体外对人恶性胶质瘤来源的细胞抑制细胞生长的作用。此外，替莫唑胺被允许延长在从颅内移植小鼠衍生的人恶性胶质瘤细胞的存活时间（体内）。 2，作用机制 替莫唑胺引起DNA损伤通过甲基化DNA的鸟嘌呤的6-位氧原子，示出了细胞增殖的抑制效果通过诱导细胞周期阻滞和细胞凋亡（体外）。 适应症 恶性胶质瘤 用法与用量 本药物一般在90分钟静脉内给药。 1. 在最初的情况下， 在与辐射的组合，通常在成人的体表面积的75毫克/米2给药42天每日一次，休息4周。然后，在仅此剂，150毫克/平方米（体表面积），每天一次给药5天作为，接着停药23天。28日和1次，下面可提高到200毫克一次/平方米。 2. 在复发的情况下 通常，在成人注射150毫克/平方米（体表面积），每天一次给药5天作为，接着停药23天。28天及1凉爽，可提高到一次在下一凉爽200毫克/平方米。 包装规格 静脉滴注 100毫克：1瓶 制造厂商 MSD有限公司 完整处方资料附件：http://www.info.pmda.go.jp/go/pack/4219404D1027_1_09/ Temodar: Intravenous drip infusion effective for malignant glioma On January 20, 2010, injection formulation of antineoplastic agent temozolomide (trade name: 100 mg for intravenous infusion of Temodar) acquired manufacturing approval. As a drug containing temozolomide as the main ingredient, capsule preparations were approved for the indication of "malignant glioma" in July 2006, but the injectable instillation approved this time is equivalent to the capsule preparation and bioequivalence Has been verified, it has been approved for the same indication as capsule formulation. Malignant glioma is a generic term for tumors with high malignancy among tumor groups classified as gliomas of brain tumors. Since this malignant glioma develops in the brain tissue and develops while invading the surrounding brain tissues, it combines surgical operation, postoperative radiotherapy, and postoperative adjuvant chemotherapy to preserve brain function Treatment is done. Nimustine hydrochloride (trade name: Nidran), ranimustine (trade name: Cimelin), interferon beta (trade name: Feron, IFN beta motida), etc. are used in adjuvant chemotherapy, and in 2005 nimustine Three drug combination therapy (PAV therapy) of hydrochloride, procarbazine hydrochloride (trade name: procarbazine hydrochloride), vincristine sulfate (trade name: Oncovin) (PAV therapy) is effective against glioma with malignant astrocytoma or oligodendroglioma component Have been approved for treatment. Capsule formulation of temozolomide is a drug approved for the first time in 19 years as an antineoplastic drug having a brain tumor-related indication in the country, and is currently being used in combination with local radiation and subsequent monotherapy, recurrent malignant glia It is widely used as a remedy for tumors. Temozolomide is classified as an alkylating drug among antineoplastic drugs, it becomes methyldiazonium ion in vivo without requiring metabolism in the liver, and methylation of DNA causes DNA damage. This induces cell cycle arrest and apoptosis and suppresses cell proliferation. In addition, temozolomide is a medicine characterized by its ease of passing through the blood-brain barrier and good transferability to cerebrospinal fluid. Temozolomide drip infusion preparation is a useful treatment option for cases where it is difficult to take a capsule preparation due to nausea/vomiting due to elevation of intracranial pressure, tumor infiltration into the brainstem, and the like. Overseas, capsules and injectable preparations have been approved in 90 countries around the world since approval by the EU (European Union) in 1991, and drip injection preparations have been approved in 33 countries. The approval of temozolomide injectable formulation will expand treatment options in patients with malignant glioma. In addition, since the injectable instillation approved this time has been confirmed to be bioequivalent to conventional capsule preparations, clinical trials with a primary objective of examining new efficacy and safety for malignant glioma Has not been done. Therefore, as with capsule formulations, careful attention should be paid to the development of serious side effects such as bone marrow suppression such as leukopenia and platelet reduction, pneumocystis pneumonia, infection, interstitial pneumonia, cerebral hemorrhage, anaphylactoid symptoms, etc. is necessary.