替莫唑胺注射液temozolomide(TEMODAR Injection)

产地国家：日本 处方药：是 所属类别： 100毫克/瓶 包装规格： 100毫克/瓶 计价单位：瓶 生产厂家英文名：MSD Co., Ltd. 原产地英文商品名：TEMODAL Infusion100mg/vial 原产地英文药品名：Temozolomide 中文参考商品译名：TEMODAL100毫克/瓶 中文参考药品译名：替莫唑胺

简介：

部份中文替莫唑胺处方资料(仅供参考)通用名：注射用替莫唑胺英文名：TEMODAR(temozolomide for Injection)商標名TEMODAL Infusion 100mg开发品种 替莫唑胺原料、注射用替莫唑胺药物分类名称抗肿瘤药规格制剂 规格：100mg 适应症：多形性胶质母细胞瘤或间变性星形细胞瘤。 用法与用量：该药物经90分钟静脉内施用。1. 初治者结合照射，通常成年人每天接受75mg/m 2的体表面积，持续42天，休息4周，作为替莫唑胺。 此后，作为替莫唑胺的150mg/m2(体表面积)每天一次，用该药单独给药5天，取出23天。 第二天每天可以增加到200毫克/平方米，这个第28天有1个疗程。2. 复发者通常，在成年人中，作为替莫唑胺的150mg / m 2(体表面积)每天一次施用5天，并且撤回23天。 我们可以将这个剂量每天一次增加到200毫克/平方米，一天是一次用药。 产品特点：替莫唑胺是先灵-葆雅(Schering-Plough)公司生产的治疗脑胶质瘤和恶性黑色素瘤的抗癌新药。它是一类称之为咪唑四嗪新型物质的第一个化合物，由于其毒性小、耐受性好而在胶质细胞瘤治疗中迈出重要的一步。由于其毒副作用低，也就可以较长时间用药，提高了长期疗效，病人的身体和精神状态均得到明显改善，提高了病人的生活质量。 常规化疗(BCNU、CCNU)耐药后用替莫唑胺仍然有效，而且这两类药物不仅无交叉耐药性且有协同增效作用。其延长此类病人的病情无进展存活时间比丙卡巴肼(procarbazine)标准治疗要长。因此，替莫唑胺是目前相对最好的治疗脑胶质瘤和恶性黑色素瘤的药物。 替莫唑胺优势： 1.替莫唑胺针对性强、特异性高，可透过血脑屏障，是治疗脑胶质瘤及转移瘤的特效药。由于其毒副作用低，可以较长时间用药，提高了病人的生活质量和治疗效果。 2.替莫唑胺治疗脑胶质瘤效果显著，同时具有延长生存时间、提高生存质量的作用，是治疗脑胶质瘤，特别是多形性胶质母细胞瘤或间变性星形细胞瘤的一线用药。它的上市改变了国内尚没有针对胶质瘤疗效较好的化疗药的现状。 3.常规化疗耐药后用替莫唑胺仍然有效，不仅无交叉耐药性且有协同增效作用。另外，替莫唑胺对白血病、黑色素瘤、淋巴瘤和实体瘤也有较好的疗效。目前，国内用于临床的只有口服替莫唑胺胶囊，虽然其口服后完全吸收、生物利用度高、组织分布好、可透过血脑屏障。 副作用：恶心、呕吐、乏力、便秘和轻度的骨髓抑制等。由于恶心、呕吐造成药物吸收不全，通常在服药前先服用止吐药，给患者带来极大的痛苦和经济负担。 另外，手术后病人常不适用固体药物，再加上传统的临床用药习惯，替莫唑胺静脉注射剂将更适合病人临床使用，提高病人用药的顺应性，还可满足临床医生的用药习惯。另外，替莫唑胺在水中不稳定，故将其制成冻干粉针，从而提高制剂的稳定性。 国内外上市情况替莫唑胺是由M..F.G Stevens、E.S Newlands等研制，1992年转让给先灵-葆雅(Schering-Plough)公司生产的。1997年10月在欧盟CPMP一致推荐下得到批准，并于1998年在欧洲上市。1999年1月美国FDA专家顾问小组一致推荐要加速替莫唑胺的批准并于1999年8月11日通过FDA批准在美国上市。同时该公司已向16个国家包括加拿大、澳大利亚、新西兰、瑞士、挪威、南非和巴西等国家提出上市申请。注射用替莫唑胺于2009年2月27日通过FDA批准在美国上市。 包装：100mg

英文版说明书：

Intravenous drip infusion effective for malignant gliomaOn 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 validated, 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 tissue, in order to preserve brain function, a combination of surgical operation, postoperative radiation therapy, and postoperative adjuvant chemotherapy 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 drug that is characterized by its ease of passing through the blood-brain barrier and good migration 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, even in administration by drip injection, as with capsule formulation, pay attention to the development of serious side effects such as leukopenia and platelet reduction such as myelosuppression, pneumocystis pneumonia, infection, interstitial pneumonia, cerebral hemorrhage, anaphylactoid symptoms is necessary.