药理学教学课件：6 antipyretic-analgesic agents

Antipyretic-analgesicandAntiinflammatoryDrugs

non-steroidalanti-inflammatorydrugs(NSAIDS)

Aspirinandothersalicylates（阿司匹林及水杨酸类）Anilinederivatives（苯胺类衍生物）Indolederivatives（吲哚类衍生物）Propionicacidderivatives（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，吡唑酮类，以及选择性COX-2抑制剂)ClassificationofNSAIDs:作用机制通过抑制环氧酶（PG合成酶）发挥作用COX-1COX-2SynthesisintrinsicinducedFunctionsphysiological:gastrointestinalprotectionplateletaggregationregulationvascularresistanceregulationrenalbloodflowregulationphysiological:productionofPGelevatedduringpregnancypathological:producingproteinase,PG,andotherinflammatorymediatorsCharacteristicscomparisonbetweenCOX-1andCOX-2Pharmacologicaleffect

antipyreticaction:inhibitPGbiosynthesisinhypothalamicregion,lowertheset-point;reduceelevatedtemperature,normalbodytemperatureisonlyslightlyaffected.Pharmacologicaleffect

analgesia:

moderate

Pharmacologicaleffectanti-inflammatoryeffects:inhibitPGbiosynthesisinhibitionofleukocyteandplateletadhesionSalicylates水杨酸类

Aspirin

阿司匹林

(Acetylsalicylicacid乙酰水杨酸)Actions:antipyreticandanalgesiclowerthebodytemperatureoffebrilepatientsmanagelowtomoderatesuperficialpains,especiallyinflammationaryantirheumatic抗风湿obviousinacuterheumaticfever急性风湿热andrheumaticarthritis风湿性关节炎antithromboticlowdoses(40mg/d)ofaspirincanirreversiblyinhibitTXA2productioninplateletswithoutmarkedlyaffectingPGI2productionintheendothelialcellscurrentlyemployedintheprophylacticandtreatmentofplatelethighly-aggregated

largedoses(morethan300mg/d),PGI2productionintheendothelialcellscanalsobeinhibited血栓素(TXA2)为血小板释放和聚集的诱导物,PGI2与

TXA2有生理拮抗作用,血小板中的cox对阿司匹林的敏感性比血管中的高抑制血小板中的COX-1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中COX-1大剂量促进血栓形成前列环素(PGI2)↓小剂量aspirin用于防止血栓形成

抑制血小板聚集作用PreventgestationalhypertensionlocalapplicationAdverseeffectsofaspirinGItract:mostcommonepigastricdiscomfort,gastriculcerationandbleedingAllergicreactionnettlerash荨麻疹,angioneuroticedema血管神经性水肿aspirinasthma‘阿司匹林哮喘’israreDisturbanceofbloodcoagulationplateletaggregationinhibitedandbleedingtimeprolongedSalicylism水杨酸反应(intoxication)headache,dizziness,tinnitus,nausea,vomiting,convulsions,coma.iv.sodiumbicarbonateenhancestheeliminationofsalicylateLiversystemReye’ssyndrome瑞夷综合征fulminatinghepatitiswithcerebropathyduringviralinfections,encounteredinchildrenAniline苯胺类

Acetaminophen对乙酰氨基酚

（paracetamol扑热息痛）analgesicandantipyreticeffectisthesameasaspirin,butnosignificantantiinflammatoryeffectitdosenotcauseGIirritationacuteintoxicationcancausedamageofliver对乙酰氨基酚对氨苯乙醚非那西丁NHCOCH3OC2H5NHCOCH3OHNH2OC2H5Indomethacin（吲哚美辛）OneofthemostpotentinhibitorsofCOXHighpotencyofanti-inflammatory,analgesic,andantipyreticactivityUsedforankylosingspondylitis(强直性脊柱炎SA)，Osteoarthritis(骨关节炎OA)andgout(痛风)Effectiveintreatingpatentductusarteriosus（动脉导管未闭）Propionicacidderivatives丙酸类naproxen萘普生ibuprofen布洛芬（芬必得）fenoprofen非诺洛芬powerfulantiinflammatoryeffectusedforacutearthriticandankylosingspondylitisGIeffectsaregenerallylessthanthatofaspirinandindomethacinCOX-2SelectiveInhibitorsCelecoxib塞来昔布(西乐葆)Indications:osteoarthritis骨关节炎,rheumatoidarthritis类风湿性关节炎,odontalgia牙痛GIadverseeffectsandgastroduodenalulcersareless药名成份新康泰克盐酸伪麻黄碱、扑尔敏速效伤风胶囊对乙酰氨基酚、扑尔敏、咖啡因、人工牛黄感康金刚烷胺、对乙酰氨基酚、人工牛黄、咖啡因

康必得对乙酰氨基酚、葡萄糖酸锌、盐酸伪麻黄碱、板蓝根浸膏粉日夜百服宁对乙酰氨基酚，氢溴酸右美沙芬，扑尔敏泰诺感冒片对乙酰氨基酚、盐酸伪麻黄碱、氢溴酸右美沙芬、扑尔敏快克金刚烷胺，对乙酰氨基酚，人工牛黄，咖啡因，扑尔敏。

美息伪麻片（白加黑）日服片：每片含对乙酰氨基酚、盐酸伪麻黄碱、氢溴酸右美沙芬夜服片：日服片＋盐酸苯海拉明25mg

药物解热镇痛抗炎抗风湿阿司匹林++++++