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1、Antipyretic-analgesic and Antipyretic-analgesic and Antiinflammatory DrugsAntiinflammatory Drugs non-steroidal anti-inflammatory non-steroidal anti-inflammatory drugs (NSAIDS)drugs (NSAIDS)Aspirin and other salicylates（阿司匹林及水杨酸类）（阿司匹林及水杨酸类）Aniline derivatives（苯胺类衍生物）（苯胺类衍生物）Indole derivatives（吲哚类衍生物
2、）（吲哚类衍生物）Propionic acid derivatives（丙酸类衍生物）（丙酸类衍生物）Others (烯醇酸类，灭酸类，杂环芳基乙酸类，茚乙酸类，烯醇酸类，灭酸类，杂环芳基乙酸类，茚乙酸类，吡唑酮类，以及选择性吡唑酮类，以及选择性COX-2抑制剂抑制剂)Classification of NSAIDs :作作作作用用用用机机机机制制制制通过抑制环氧酶（通过抑制环氧酶（通过抑制环氧酶（通过抑制环氧酶（PGPG合成酶）发挥作用合成酶）发挥作用合成酶）发挥作用合成酶）发挥作用 COX-1 COX-2SynthesisintrinsicinducedFunctionsphysiolog
3、ical:gastrointestinal protectionplatelet aggregation regulationvascular resistance regulationrenal blood flow regulationphysiological: production of PG elevated during pregnancypathological:producing proteinase, PG, and other inflammatory mediators Characteristics comparison between COX-1 and COX-2
4、Pharmacological effectu antipyretic action:inhibit PG biosynthesis in hypothalamic region, lower the set-point; reduce elevated temperature,normal body temperature is only slightly affected.Pharmacological effectu analgesia: moderate Pharmacological effectuanti-inflammatory effects: inhibit PG biosy
5、nthesis inhibition of leukocyte and platelet adhesionSalicylates 水杨酸类水杨酸类 A Aspirinspirin 阿司匹林阿司匹林(Acetyl salicylic acid (Acetyl salicylic acid 乙酰水杨酸乙酰水杨酸) )Actions:antipyretic and analgesiclower the body temperature of febrile patientsmanage low to moderate superficial pains, especially inflammatio
6、naryantirheumatic 抗抗风湿风湿obvious in acute rheumatic fever急性急性风湿热风湿热 and rheumatic arthritis风湿性关节炎风湿性关节炎antithromboticulow doses (40 mg/d) of aspirin can irreversibly inhibit TXA2 production in platelets without markedly affecting PGI2 production in the endothelial cells currently employed in the prop
7、hylactic and treatment of platelet highly-aggregated ularge doses (more than 300 mg/d), PGI2 production in the endothelial cells can also be inhibited_血栓素血栓素(TXA(TXA2 2) )为血小板释放和聚集的诱导物为血小板释放和聚集的诱导物,PGI,PGI2 2 与与 TXATXA2 2 有生理有生理拮抗作用拮抗作用,血小板中的血小板中的coxcox对阿司匹林的敏感性比血管中的高对阿司匹林的敏感性比血管中的高抑制血小板血小板血小板血小板中的C
8、OX-1小剂量小剂量小剂量小剂量 血小板中TXA2 抑制血小板聚集和血栓形成抑制血管壁细胞血管壁细胞血管壁细胞血管壁细胞中COX-1大剂量大剂量大剂量大剂量促进血栓形成前列环素(PGI2)小剂量小剂量aspirinaspirin用于防止血栓形成用于防止血栓形成 抑制血小板聚集作用抑制血小板聚集作用Prevent gestational hypertensionlocal applicationAdverse effects of aspirinAdverse effects of aspirinGI tract: most common epigastric discomfort, gastr
9、ic ulceration and bleedingAllergic reactionnettle rash荨麻疹荨麻疹, angioneurotic edema血管神经性血管神经性水肿水肿 aspirin asthma 阿司匹林哮喘阿司匹林哮喘 is rareDisturbance of blood coagulationplatelet aggregation inhibited and bleeding time prolongedSalicylism水杨酸反应水杨酸反应 (intoxication)headache, dizziness, tinnitus, nausea, vomit
10、ing, convulsions, coma.iv. sodium bicarbonate enhances the elimination of salicylateLiver systemReyes syndrome 瑞夷综合征瑞夷综合征fulminating hepatitis with cerebropathyduring viral infections, encountered in childrenAniline 苯胺类苯胺类 Acetaminophen 对乙酰氨基酚对乙酰氨基酚 （paracetamol扑热息痛）扑热息痛）analgesic and antipyretic ef
11、fect is the same as aspirin, but no significant antiinflammatory effectit dose not cause GI irritationacute intoxication can cause damage of liver对乙酰氨基酚对乙酰氨基酚对氨苯乙醚对氨苯乙醚非那西丁非那西丁NHCOCH3OC2H5NHCOCH3OHNH2OC2H5 Indomethacin Indomethacin（吲哚美辛）（吲哚美辛）One of the most potent inhibitors of COXHigh potency of a
12、nti-inflammatory, analgesic, and antipyretic activityUsed for ankylosing spondylitis (强直性脊柱炎强直性脊柱炎SA)，Osteoarthritis (骨关节炎骨关节炎OA) and gout (痛风痛风)Effective in treating patent ductus arteriosus （动脉导（动脉导管未闭）管未闭）Propionic acid derivatives Propionic acid derivatives 丙酸类丙酸类naproxen 萘普生萘普生ibuprofen 布洛芬（芬必得
13、）布洛芬（芬必得）fenoprofen 非诺洛芬非诺洛芬powerful antiinflammatory effect used for acute arthritic and ankylosing spondylitisGI effects are generally less than that of aspirin and indomethacinCOX-2 Selective InhibitorsCelecoxib 塞来昔布塞来昔布(西乐葆西乐葆)Indications: osteoarthritis 骨关节炎骨关节炎, rheumatoid arthritis 类风湿性关节炎类风湿
14、性关节炎, odontalgia 牙痛牙痛GI adverse effects and gastroduodenal ulcers are less药名药名成份成份新康泰克新康泰克盐酸伪麻黄碱、扑尔敏盐酸伪麻黄碱、扑尔敏速效伤风胶囊速效伤风胶囊对乙酰氨基酚、扑尔敏、咖啡因、人工牛黄对乙酰氨基酚、扑尔敏、咖啡因、人工牛黄感康感康金刚烷胺、对乙酰氨基酚、人工牛黄、咖啡因金刚烷胺、对乙酰氨基酚、人工牛黄、咖啡因康必得康必得对乙酰氨基酚、葡萄糖酸锌、盐酸伪麻黄碱、对乙酰氨基酚、葡萄糖酸锌、盐酸伪麻黄碱、板蓝根浸膏粉板蓝根浸膏粉 日夜百服宁日夜百服宁对乙酰氨基酚，氢溴酸右美沙芬，扑尔敏对乙酰氨基酚，氢溴
15、酸右美沙芬，扑尔敏 泰诺感冒片泰诺感冒片对乙酰氨基酚、盐酸伪麻黄碱、氢溴酸右美沙对乙酰氨基酚、盐酸伪麻黄碱、氢溴酸右美沙芬、扑尔敏芬、扑尔敏 快克快克金刚烷胺，对乙酰氨基酚，人工牛黄，咖啡因，金刚烷胺，对乙酰氨基酚，人工牛黄，咖啡因，扑尔敏。扑尔敏。美息伪麻片（白加美息伪麻片（白加黑）黑）日服片：每片含对乙酰氨基酚、盐酸伪麻黄碱、日服片：每片含对乙酰氨基酚、盐酸伪麻黄碱、氢溴酸右美沙芬氢溴酸右美沙芬 夜服片：日服片盐酸苯海夜服片：日服片盐酸苯海拉明拉明25mg25mg 药物药物 解解 热热 镇镇 痛痛 抗炎抗风湿抗炎抗风湿阿司匹林阿司匹林 + + + + +扑热息痛扑热息痛 + + -+ + -布洛芬布洛芬 + + + + +消炎痛消炎痛 + + + + +保泰松保泰松 + + + + +炎痛喜康炎痛喜康 + + + + +常用解热镇痛药作用强度比较常用解热镇痛药作用强度比较
