第六章面板数据模型电子教案.ppt

单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,*,第六章 非甾体抗炎药,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,白加黑,通用名：美息伪麻片商品名：白加黑【主要成份】每片含 日用片 夜用片作用分类,对乙酰氨基酚 325mg 325mg解热镇痛苯胺类,盐酸伪麻黄碱 30mg 30mg减轻鼻充血拟肾上腺,氢溴酸右美沙芬 15mg 15mg镇咳药吗啡烃类,盐酸苯海拉明 0 25mg抗H1抗过敏氨基醚类,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,泰诺,成份：,对乙酰氨基酚,325mg,盐酸伪麻黄碱,30mg,氢溴酸右美沙芬,15mg,马来酸氯苯那敏,2mg,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,新康泰克,成份,盐酸伪麻黄碱（,）,90mg,马来酸氯苯那敏（扑尔敏,）4mg,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,常用感冒药,银得菲,对乙酰胺基酚325，盐酸伪麻黄碱30，马来酸氯苯那敏2,感康,金钢烷胺100，对乙酰胺基酚250，人工牛黄10，咖啡因15,速效伤风胶囊,成分：扑热息痛250毫克，咖啡因15毫克，扑尔敏3毫克，人工牛黄10毫克,感冒通,双氯灭痛,15,毫克，扑尔敏,2.5,毫克，人工牛黄,15,毫克,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,本章目标,1.掌握解热镇痛药与非甾体抗炎药的结构类型。,2.掌握阿司匹林、对乙酰氨基酚、布洛芬的结构及性质。,3.理解阿司匹林、对乙酰氨基酚的合成。,4.熟悉阿司匹林、对乙酰氨基酚在体内的代谢.,5.了解抗痛风药的分类及临床用途。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,思考,为什么解热镇痛药和非甾体抗炎药在同一章里学习？,解热镇痛药和非甾体抗炎药这两类药的区别是什么？,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,解热、镇痛、抗炎作用机制,选择性地抑制中枢或外周前列腺素的合成，对各种原因引起的发热有效；,对慢性钝痛有效，,不易产生耐受性及成瘾性，,对急性锐痛及内脏痉挛性绞痛无效；,大多数药物有抗炎抗风湿作用；,部分药物还有抗痛风作用。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,解热镇痛药,指主要具有解热镇痛作用，且部分兼有良好抗炎抗风湿作用的一类药物；,非甾体抗炎药,指主要具有抗炎抗风湿作用，且兼有良好解热镇痛作用的一类药物。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,第一节 解热镇痛药,作用,解热,使发热的体温降至正常,镇痛,对慢性钝痛有良好的作用,常见的牙痛、头痛、神经痛、肌肉痛、关节痛等,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,解热镇痛药的作用部位,作用于下丘脑的体温调节中枢,使发热的体温降至正常,对正常的体温无影响,作用于外周抑制环氧酶,常见的慢性钝痛有良好的作用。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,分类（按化学结构）,水杨酸类,（阿司匹林）,苯胺类,（对乙酰氨基酚）,吡唑酮类,（安乃近）,发现都较早,临床上应用的时间较久,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,水杨酸类及吡唑酮类,都具有良好的解热镇痛、抗炎抗风湿作用；,苯胺类,只有解热镇痛作用而无抗炎抗风湿作用；,吡唑酮类,毒副作用大。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,一,.,水杨酸类,本类药物有：阿司匹林铝、赖氨匹林、阿司匹林精氨酸盐、阿司匹林等。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,发现过程,公元前15世纪，咀嚼柳树皮可减轻疼痛。,1838年首次从植物中提取得到Salicylic Acid,1860年人工合成,开辟了一条工业生产的道路。,1875年水杨酸钠作为临床上使用。,乙酰水杨酸1853年合成，1899年开始药用,。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,阿司匹林（Aspirin）,化学名为2-(乙酰氧基)苯甲酸,又名,乙酰水杨酸,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,以,水杨酸,为原料，,醋酐,为,酰化剂,，进行,酰化反应,制得。,实验室,常用,硫酸,作催化剂，50-60水浴加热约半小时即得。,合成方法,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,工业合成,工业上,用,醋酸,作催化剂，加热温度70-75，8小时完成制备。,杂质,未反应的原料,产品储存水解产生的水杨酸,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,鉴别方法,遇湿气,酚酯键,即缓慢水解，生成水杨酸和醋酸，可嗅到醋酸味。,PH升高和加热会加快水解反应的进行，用氢氧化钠或碳酸钠加热水解，冷却，然后再酸化，不仅可嗅到,醋酸味,，并且有,水杨酸白色沉淀,析出。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,应置于密封容器内,在阴凉干燥处贮存。,制备过程中酰化不完全或贮存中水解产生的,水杨酸,，遇空气易被氧化成一系列,有色醌类物质，出现淡黄、红棕、深棕至黑色。,失去治疗作用，产生毒性。,贮存方式,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,检查法,用铁盐产生紫堇色，检查游离水杨酸的存在,水溶液加热放冷，,加入三氯化铁，呈紫堇色,加碳酸钠溶液加热放冷，与稀硫酸反应,析出白色沉淀，并发出醋酸气,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,老药新用,用于心血管系统疾病的预防和治疗,最近研究还表明，对结肠癌有预防作用,其应用范围不断扩大。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,临床应用,镇痛、解热,抗炎、抗风湿,关节炎,抗血栓,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,不良反应,对胃粘膜有刺激作用,可引起胃及十二指肠出血等症,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,二.苯胺类,乙酰苯胺,（退热冰）,对乙酰氨基苯乙醚,（非那西汀）,对乙酰氨基酚,（扑热息痛）等，,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,苯胺类药物代表,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,对乙酰氨基酚,扑热息痛,N-(4-羟基苯基)乙酰胺,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,合成方法,以,硝基苯酚钠,为原料，在,盐酸酸性条件,下用,铁粉,还原生成对氨基苯酚，再用,醋酸酰化,制得。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,合成,杂质检查-对氨基酚,与亚硝酰铁氰化钠试液,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,贮存方式,水溶液在,PH6时,最稳定，在酸性或碱性条件下易水解生成,对氨基酚,，进一步,氧化生成醌亚胺类化合物，颜色逐渐变为粉红色、棕色至黑色。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,理化性质,白色结晶或结晶性粉末，无臭，味微苦。熔点168-172。,稳定,在空气中稳定,水溶液中与PH有关,水解,对氨基酚,鉴别,三氯化铁,亚硝酸钠，再与-萘酚，呈红色（重氮化偶合反应),Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,临床,临床用于发热、多种慢性钝痛，适合儿童及不能耐受阿司匹林的患者应用，无抗炎抗风湿作用。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,第二节 非甾体抗炎药,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,炎症,机体对感染的一种防御机制,主要表现为红肿、疼痛等,常见疾病类型,风湿性疾病,关节炎,类风湿性疾病,类风湿性关节炎,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,解热镇痛药与非甾体抗炎药,解热镇痛药,除苯胺类外，具有抗炎作用,非甾体抗炎药,都具有镇痛作用,通过抑制PG合成酶而起镇痛和抗炎作用,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,吲哚乙酸,-吲哚美辛,芳基烷酸,-布洛芬,1，2-苯并噻嗪,3，5-吡唑烷二酮,邻氨基苯甲酸,分类（化学结构）,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,一.吲哚乙酸类,吲哚美辛抗炎镇痛效果好，但毒副反应也较严重。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,吲哚美辛,消炎痛,化学名：2-甲基-1-（4-氯苯甲酰基）-5-甲氧基-1H-吲哚-3-乙酸,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,发现-吲哚美辛,偶然性,美籍华人：沈宗瀛先生,消炎痛,的出现也并不偶然，它不过是我们大量抗炎研究工作的必然报酬罢了,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,理化性质,水解性,酰胺强酸强碱水解,水解产物,对氯苯甲酸,5-甲氧基-2-甲基吲哚-3-乙酸,5-甲氧基-2，3 二甲基吲哚,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,鉴别方法,1.溶于稀氢氧化钠溶液中与重铬酸钾试液共热，冷却，再加硫酸酸化并缓缓加热，呈,紫色,。,2.与亚硝酸钠试液共热，冷却，再加盐酸酸化，呈,绿色,，放置后渐变为,黄色,。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,具有抗炎、解热及镇痛作用，作用机理为通过,对环氧化酶的抑制而减少前列腺素的合成。,羧基对抗炎作用是必要的基团，且在一定范围内，羧基的酸性愈强，抗炎作用也愈强。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,临床应用,强效非甾体抗炎药，但毒副作用也严重。,主要用于治疗不宜用阿司匹林的风湿和类风湿性关节炎、骨关节炎等患者；,用于癌症引起的发热及其他不易控制的发热；,用于急性痛风等。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,二芳基烷酸类,芳基乙酸类,芳基丙酸类,毒性较小，临床应用较广泛。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,芳基烷酸类药物代表,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,布洛芬（Ibuprofen）,异丁苯丙酸,-甲基,-4-（2-甲基丙基）苯乙酸,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,布洛芬理化性质,酸性,pKa=5.2,溶于氢氧化钠和碳酸钠,鉴别反应,异羟肟酸铁盐反应,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,异羟肟酸铁盐反应,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,药效,镇痛、抗炎、解热作用。,作用机制,-通过,对环氧酶的抑制而减少前列腺素的合成,，减轻因前列腺素引起的组织充血、肿胀、降低周围神经,痛觉,的敏感性。,-通过,下丘脑体温调节中心,起,解热,作用。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,临床应用,用于治疗风湿性及类风湿性关节炎、骨关节炎、神经炎、咽喉炎、红斑狼疮等；,用于发热；,用于轻、中度钝痛。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,三.1，2-苯并噻嗪类,新型非甾体抗炎药,作用时间持久。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,吡罗昔康（炎痛昔康）,弱酸性,分子结构中含烯醇式羟基，具有弱酸性。,鉴别反应,溶于氯仿中加三氯化铁试液，呈,玫瑰红色。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,临床应用,用于治疗风湿性及类风湿性关节炎、骨关节炎、急性肌肉骨骼损伤、急性通风等。,消炎镇痛作用强于消炎痛。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,四.3，5-吡唑烷二酮类,1949年,保泰松,最早用于临床，但毒副反应大，已很少用。,1961年发现了,羟布宗,等，抗炎抗风湿作用较弱，但具有,较强的排尿酸作用。主要用于治疗痛风、风湿和类风湿关节炎等。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,五.邻氨基苯甲酸类,毒副反应较多，临床很少应用。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,第三节 抗痛风药,痛风病是由于体内嘌呤核苷酸分解代谢过甚，使终产物尿酸生成过多，而导致高尿酸血症，并且尿酸盐在关节或泌尿道析出，引起通风性关节炎、通风性肾病及尿路结石等一类疾病的,总称,。,根据作用特点可分为,抗痛风发作药,、,尿酸排泄剂,、,尿酸合成阻断剂,三类。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,一.痛风发作药,作用,-轻度促进尿酸排泄,消除痛风发作引起的疼痛,临床应用,主要用于治疗急性痛风发作。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,二尿酸排泄剂,能显著抑制肾小管对原尿中尿酸的重吸收，可使尿中尿酸的排泄量增加，而致血浆中尿酸浓度降低，痛风病得到缓解。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,三尿酸合成阻断剂,作用,可抑制黄嘌呤氧化酶活性，使次黄嘌呤转为黄嘌呤,受阻断，黄嘌呤转变为尿酸相应受阻，尿酸合成减少。,临床应用,用于治疗慢性原发性痛风及痛风性肾病，对急性痛风无效。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,2003年处方量TOP200,2003排名,商品名,通用名,中文名,19,lbuprofen,lbuprofen,布洛芬,23,Celebrex,Celecoxib,塞利西布,29,VIOXX,Rofecoxib,罗非西布,73,Naproxen,Naproxen,萘普生,173,Mobic,Meloxicam,美洛昔康,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,2003年通用名药销量TOP200,排名,通用名,金额,中文名,21,Naproxen,$338,104,萘普生,39,lbuprofen,$248,800,布洛芬,69,Diclofenac Sodium,$130,781,双氯芬酸钠,124,Piroxicam,$61,456,吡罗昔康,154,Indomethacin,$41,620,吲哚美辛,200,Ketoprofen,$27,933,酮洛芬,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,非甾类抗炎药的局限,在减少发炎及减轻疼痛方面十分有效,常规治疗用药,不能预防或阻止慢性关节炎的病理过程,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,思考题,1.概述解热镇痛药和非甾体抗炎药的主要结构类型，并各举1-2类药物，试说出典型药物临床如何选用？,2.写出阿司匹林、对乙酰氨基酚、布洛芬的化学结构及鉴别方法。,3.阿司匹林及对乙酰氨基酚在贮存过程中颜色加深的原因是什么？应如何防止？,4.过量对乙酰氨基酚进入体内为什么可能引起肝坏死或肾损害？,5.,比较解热镇痛药与镇痛药。,Evaluation only.,Created with Aspose.Slides for.NET 3.5 Client Profile 5.2.0.0.,Copyright 2004-2011 Aspose Pty Ltd.,