第七章抗肿瘤药.docVIP

第七章 抗肿瘤药 （Antineoplastic Agents） 本文档由【中文word文档库】提供，转载分发敬请保留本信息； 中文word文档库免费提供海量范文、教育、学习、政策、报告和经济类word文档。 要求： 了解烷化剂类药物的发展；熟悉烷化剂类药物的结构类型和作用机理；掌握盐酸氮芥、环磷酰胺、顺铂的结构、理化性质、体内代谢及作用特点；熟悉塞替派、卡莫司汀、白消安的结构及临床应用；了解金属铂配合物的发展及构效关系；熟悉环磷酰胺、卡莫司汀的合成方法。了解抗代谢药物的发展；熟悉抗代谢药物的设计原理及作用机理；掌握氟尿嘧啶、巯嘌呤的结构、理化性质及临床应用；熟悉盐酸阿糖胞苷和甲氨喋呤的结构及临床应用；熟悉氟尿嘧啶和巯嘌呤的合成方法。了解抗肿瘤抗生素的发展及作用机理；熟悉米托蒽醌的结构特点、设计思想及作用。了解抗肿瘤植物药及衍生物的发展和作用机理；熟悉喜树碱类、长春碱类及紫杉烷类抗肿瘤药物的结构特点及临床应用。Facts and figures Along with heart disease, cancer is the largest cause of death in the developed world. Cancer affects 1 in 3 people and is responsible for 25% of all deaths. Cancer cells are formed when normal cells lose the normal regulatory mechanisms that control growth and multiplication. They lose differentiation and become immortal. Causes As many as 30% of cancers are though to be caused by smoking. Another 30% are diet related. At least 15% are related to viruses, e.g. cervical cancer(宫颈癌 ) caused by human papillomavirus(乳头状病毒 ) . Treatment of Cancer Treatment: Surgery, radiotherapy and chemotherapy Selectivity is a big problem for most anticancer drugs, as identifying targets that are unique to cancer cells is not easy. Many drugs rely on the fact that cancer cells have a significantly raised metabolism relative to normal cells. They accumulate nutrients, cell building blocks and drugs more easily, and are thus more prone to the cytotoxic affects of a cancer drug. Other normal cells in the body which grow rapidly, such as bone marrow cells, are adversely affected resulting in severe toxic side effects from many chemotherapy regimes. Common side effects include a depressed immune system, leading to infection, impaired wound healing, sterility, hair loss, kidney damage and depression of growth in children. 第一节 生物烷化剂 Bioalkylating Agents 分类 氮芥类 亚硝基脲类 甲磺酸酯及多元醇类 金属铂配合物类 二、盐酸氮芥 Chloromethine hydrochloride 化学名：N-甲基-N-（2-氯乙基）-2-氯乙胺盐酸盐 英文名：N-Methyl-N-(2-chloroethyl)-2-chloroethylamine hydrochloride 本品为白色粉末，有吸湿性，对皮肤、粘膜有腐蚀性。易溶于水与乙醇，m