解热镇痛药和非甾体抗炎药 .pptxVIP

第六章 解热镇痛药和非甾体抗炎药;定义及内容;第一节 解热镇痛药;定义及内容;阿司匹林 Aspirin;阿司匹林的历史;阿司匹林的作用机理;阿司匹林;;阿司匹林的作用;阿司匹林的代谢;阿司匹林的制备;?对乙酰氨基酚 Paracetamol ;苯胺类解热镇痛药发展历史;扑热息痛的合成;;第二节 非甾体抗炎药NSAID;定义和内容;非甾体抗炎药分类;吡唑酮类;邻氨基苯甲酸类;1、2-苯并噻嗪类;苯乙酸类;芳基丙酸类;一、吡唑酮类;一、吡唑酮类发展历程;一、吡唑酮类发展历程;一、吡唑酮类发展历程;一、吡唑酮类发展历程;Phenylbutazone的???效关系;;羟布宗具有潜在的芳伯氨基;邻氨基苯甲酸类;邻氨基苯甲酸类的特点;吲哚乙酸类;吲哚美幸的特点;吲哚美幸的衍生药物;芳基丙酸类;芳基丙酸类;代表药物;芳基丙酸类镇痛抗炎药构效关系;Ibuprofen的体内代谢;Ibuprofen的合成;萘普生 Naproxen;萘普生 Naproxen的构效关系;衍生物 萘普酮 Nambumetone;Naproxen的合成路线如下：;苯乙酸类;;Diclofenac Sodium 同类芳基乙酸类药物;Diclofenac Sodium的合成;1、2-苯并噻嗪类;吡罗昔康 Piroxicam的特点;吡罗昔康 Piroxicam的衍生物;;COX-2 抑制剂;选择性环氧酶-2抑制剂（Selective Cycloxygenase-2 Inhibitors）;选择性环氧酶-2抑制剂（Selective Cycloxygenase-2 Inhibitors）;选择性环氧酶-2抑制剂（Selective Cycloxygenase-2 Inhibitors）;选择性环氧酶-2抑制剂（Selective Cycloxygenase-2 Inhibitors）;塞来昔布（Celebrex）;塞来昔布（Celebrex）西乐葆;塞来昔布的市场情况;“万络”风波;;结果;影响：;中国医药报 2007年11月13日报道;其它西布类药物;Valdecoxib (marketed as Bextra) Report serious adverse events to FDAs MedWatch at 1-800-FDA-1088; FDA Alert [04/07/05]: FDA has requested that Pfizer voluntarily withdraw Bextra from the United States market. Pfizer has agreed to suspend sales and marketing of Bextra in the United States, pending further discussion with the Agency. At this time, the Agency has concluded that the overall risk versus benefit profile of Bextra is unfavorable. This conclusion is based on the potential increased risk for serious cardiovascular (CV) adverse events, which appears to be a class effect of non-steroidal anti-inflammatory drugs (NSAIDs) (excluding aspirin), an increased risk of serious skin reactions (e.g., toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme) compared to other NSAIDs, and the fact that Bextra has not been shown to offer any unique advantages over the other available NSAIDs. ;Vioxx的召回、引起不良反应的机制;RofecoxibBrand name: vioxx中文名:罗非昔布;vioxx召回的原因;　最初引起学术界对Rofecoxib心血管安全性的关注，是起源于2000年11月发表于英国医学杂志的名为VIGOR的Rofecoxib胃肠道终点研究，该研究显示Rofecoxib心血管事件的发生率显著高于萘普生。;最近由美国ＦＤＡ 资深科学家Graham等，对140万例病人的病历进