藥理學(xué)教學(xué)課件：6 antipyretic-analgesic agents

Antipyretic-analgesicandAntiinflammatoryDrugs

non-steroidalanti-inflammatorydrugs(NSAIDS)

Aspirinandothersalicylates（阿司匹林及水楊酸類）Anilinederivatives（苯胺類衍生物）Indolederivatives（吲哚類衍生物）Propionicacidderivatives（丙酸類衍生物）Others(烯醇酸類，滅酸類，雜環(huán)芳基乙酸類，茚乙酸類，吡唑酮類，以及選擇性COX-2抑制劑)ClassificationofNSAIDs:作用機(jī)制通過(guò)抑制環(huán)氧酶（PG合成酶）發(fā)揮作用COX-1COX-2SynthesisintrinsicinducedFunctionsphysiological:gastrointestinalprotectionplateletaggregationregulationvascularresistanceregulationrenalbloodflowregulationphysiological:productionofPGelevatedduringpregnancypathological:producingproteinase,PG,andotherinflammatorymediatorsCharacteristicscomparisonbetweenCOX-1andCOX-2Pharmacologicaleffect

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

analgesia:

moderate

Pharmacologicaleffectanti-inflammatoryeffects:inhibitPGbiosynthesisinhibitionofleukocyteandplateletadhesionSalicylates水楊酸類

Aspirin

阿司匹林

(Acetylsalicylicacid乙酰水楊酸)Actions:antipyreticandanalgesiclowerthebodytemperatureoffebrilepatientsmanagelowtomoderatesuperficialpains,especiallyinflammationaryantirheumatic抗風(fēng)濕obviousinacuterheumaticfever急性風(fēng)濕熱andrheumaticarthritis風(fēng)濕性關(guān)節(jié)炎antithromboticlowdoses(40mg/d)ofaspirincanirreversiblyinhibitTXA2productioninplateletswithoutmarkedlyaffectingPGI2productionintheendothelialcellscurrentlyemployedintheprophylacticandtreatmentofplatelethighly-aggregated

largedoses(morethan300mg/d),PGI2productionintheendothelialcellscanalsobeinhibited血栓素(TXA2)為血小板釋放和聚集的誘導(dǎo)物,PGI2與

TXA2有生理拮抗作用,血小板中的cox對(duì)阿司匹林的敏感性比血管中的高抑制血小板中的COX-1小劑量血小板中TXA2↓抑制血小板聚集和血栓形成抑制血管壁細(xì)胞中COX-1大劑量促進(jìn)血栓形成前列環(huán)素(PGI2)↓小劑量aspirin用于防止血栓形成

抑制血小板聚集作用PreventgestationalhypertensionlocalapplicationAdverseeffectsofaspirinGItract:mostcommonepigastricdiscomfort,gastriculcerationandbleedingAllergicreactionnettlerash蕁麻疹,angioneuroticedema血管神經(jīng)性水腫aspirinasthma‘阿司匹林哮喘’israreDisturbanceofbloodcoagulationplateletaggregationinhibitedandbleedingtimeprolongedSalicylism水楊酸反應(yīng)(intoxication)headache,dizziness,tinnitus,nausea,vomiting,convulsions,coma.iv.sodiumbicarbonateenhancestheeliminationofsalicylateLiversystemReye’ssyndrome瑞夷綜合征fulminatinghepatitiswithcerebropathyduringviralinfections,encounteredinchildrenAniline苯胺類

Acetaminophen對(duì)乙酰氨基酚

（paracetamol撲熱息痛）analgesicandantipyreticeffectisthesameasaspirin,butnosignificantantiinflammatoryeffectitdosenotcauseGIirritationacuteintoxicationcancausedamageofliver對(duì)乙酰氨基酚對(duì)氨苯乙醚非那西丁NHCOCH3OC2H5NHCOCH3OHNH2OC2H5Indomethacin（吲哚美辛）OneofthemostpotentinhibitorsofCOXHighpotencyofanti-inflammatory,analgesic,andantipyreticactivityUsedforankylosingspondylitis(強(qiáng)直性脊柱炎SA)，Osteoarthritis(骨關(guān)節(jié)炎OA)andgout(痛風(fēng))Effectiveintreatingpatentductusarteriosus（動(dòng)脈導(dǎo)管未閉）Propionicacidderivatives丙酸類naproxen萘普生ibuprofen布洛芬（芬必得）fenoprofen非諾洛芬powerfulantiinflammatoryeffectusedforacutearthriticandankylosingspondylitisGIeffectsaregenerallylessthanthatofaspirinandindomethacinCOX-2SelectiveInhibitorsCelecoxib塞來(lái)昔布(西樂(lè)葆)Indications:osteoarthritis骨關(guān)節(jié)炎,rheumatoidarthritis類風(fēng)濕性關(guān)節(jié)炎,odontalgia牙痛GIadverseeffectsandgastroduodenalulcersareless藥名成份新康泰克鹽酸偽麻黃堿、撲爾敏速效傷風(fēng)膠囊對(duì)乙酰氨基酚、撲爾敏、咖啡因、人工牛黃感康金剛烷胺、對(duì)乙酰氨基酚、人工牛黃、咖啡因

康必得對(duì)乙酰氨基酚、葡萄糖酸鋅、鹽酸偽麻黃堿、板藍(lán)根浸膏粉日夜百服寧對(duì)乙酰氨基酚，氫溴酸右美沙芬，撲爾敏泰諾感冒片對(duì)乙酰氨基酚、鹽酸偽麻黃堿、氫溴酸右美沙芬、撲爾敏快克金剛烷胺，對(duì)乙酰氨基酚，人工牛黃，咖啡因，撲爾敏。

美息偽麻片（白加黑）日服片：每片含對(duì)乙酰氨基酚、鹽酸偽麻黃堿、氫溴酸右美沙芬夜服片：日服片＋鹽酸苯海拉明25mg

藥物解熱鎮(zhèn)痛抗炎抗風(fēng)濕阿司匹林++++++