Chpt 19 NSAIDs解热镇痛药.pptVIP

下载本文档

1
0
约 38页
2017-09-17 发布于浙江
举报
版权申诉

Chpt 19 NSAIDs解热镇痛药.ppt

1、原创力文档（book118）网站文档一经付费（服务费），不意味着购买了该文档的版权，仅供个人/单位学习、研究之用，不得用于商业用途，未经授权，严禁复制、发行、汇编、翻译或者网络传播等，侵权必究。。
2、本站所有内容均由合作方或网友上传，本站不对文档的完整性、权威性及其观点立场正确性做任何保证或承诺！文档内容仅供研究参考，付费前请自行鉴别。如您付费，意味着您自己接受本站规则且自行承担风险，本站不退款、不进行额外附加服务；查看《如何避免下载的几个坑》。如果您已付费下载过本站文档，您可以点击这里二次下载。
3、如文档侵犯商业秘密、侵犯著作权、侵犯人身权等，请点击“版权申诉”（推荐），也可以打举报电话：400-050-0827(电话支持时间：9:00-18:30)。
4、该文档为VIP文档，如果想要下载，成为VIP会员后，下载免费。
5、成为VIP后，下载本文档将扣除1次下载权益。下载后，不支持退款、换文档。如有疑问请联系我们。
6、成为VIP后，您将拥有八大权益，权益包括：VIP文档下载权益、阅读免打扰、文档格式转换、高级专利检索、专属身份标志、高级客服、多端互通、版权登记。
7、VIP文档为合作方或网友上传，每下载1次，网站将根据用户上传文档的质量评分、类型等，对文档贡献者给予高额补贴、流量扶持。如果你也想贡献VIP文档。上传文档

Biosynthesis of Prostaglandins 1. COX-1 (constitutive expression 组成型表达) Pharmacological Actions of NSAIDs 1. Antipyretic Effect (解热作用） Decrease high fever body temperature to normal level, have no effect on normal body temperature. Mechanism : prostaglandins in hypothalamus(下丘脑）↓ → set point of temperature ↓ → perspiration↑→ heat loss↑→ normal temperature 3. Anti-inflammatory Effect（抗炎作用） All NSAIDs but acetaminophen can significantly alleviate inflammation Mechanism: locally inhibit the synthesis of PGs 4. Inhibition of Platelet Aggregation（抗血小板作用） (only for Aspirin) Aspirin decreases the formation of TXA2, so can inhibit thrombosis. Aspirin（阿司匹林） is an irreversible COX inhibitor, while other NSAIDs are reversible inhibitors. Inhibition of COX by Aspirin Medications that NSAIDs provide Analgesia（镇痛） Antipyresis（解热） Anti-Inflammatory effects（抗炎，对乙酰氨基酚无此作用） Antiplatelet（抗血小板，仅限阿司匹林） Aspirin (Acetylsalicylic Acid) A nonselective inhibitor of both COX isoforms Weak acid with a pKa of 3.5 – rapidly absorbed from the stomach and upper GIT T1/2 = 15 min –hydrolyzed to acetic acid and salicylate Salicylate is bound to albumin, but the binding is saturable so that the unbound fraction increases as total concentration increases. Alkalinization of the urine increases the rate of excretion of free salicylate and its water-soluble conjugates. 1. ANALGESIC EFFECTS Aspirin is most effective in reducing pain of mild to moderate intensity through its effects on inhibiting PGs production. Aspirin is valuable for the relief of mild to moderate pain (e.g., headache, toothache, arthritis, dysmenorrhea(痛经), neuralgia, and myalgia（肌肉痛）). Aspirin is not effective for severe visceral（内脏的） pain. 2. ANTIPYRETIC EFFECTS Aspirins antipyretic effect is mediated by COX inhibition in the central nervous system. Antipyretic therapy is reserved for patients in whom fever in itself may be deleterious and for those who experience considerable relief when fever is lowered. Aspirin 3. ANTI-