藥理學(xué)英文版教學(xué)課件：Chapter 19 Antipyretic-analgesic-Anti-inflammatory Drugs

Non-steroidalAnti-inflammatoryDrugs,NSAIDs

HistoryofNSAIDsCase1P134§1IntroductiontoNSAIDsI.COMMONAction&MechanismInhibitthecycloxygenase(COX,環(huán)氧酶)Decreasethesynthesisofprostaglandins(PGs,前列腺素)RelatedPathwaysPAF(血小板活化因子)+CharacteristicsofCOX-1,COX-21.Antipyretic(解熱，退燒）effectOnlydeclinethetemperatureoffeverpatients,notnormalperson’s.Commonpharmacologicaleffects2.Analgesic（止痛）effectPG=Paininducer&painintensifier3.Anti-inflammatoryaction4.OtheractionsInhibitthesynthesisofTXA2inplatelet,inhibitthethrombosis（血栓）.InhibitthetumordevelopmentDelaytheonsetofAlzheimer’sdiseaseII.ShareAdversereactions1.gastrointestinereaction:COX-1inhibition2.skinrash3.kidneydamage4.liverdamage5.Cardiovascularreaction6.effectsonblood7.CNS:headache,dizziness,sleepy8.inhibittheprotectiveabilityofthebodyClassificationofNSAIDsNon-selectiveCOXinhibitorsSelectiveCOX2inhibitors§2commonusedNSAIDs

Non-selectiveNSAIDs一、salicylates水楊酸類二、anilines苯胺類：acetaminophen三、indoles吲哚類：indomethacin四、aryloxyaceticacid芳基乙酸類：diclofenic五、Phenylpropionicacid芳基丙酸類：iboprofen六、烯醇酸類：Piroxicam(吡羅昔康)七、吡唑酮類：phenylbutazone保泰松八、烷酮類：Mabumetone(奈丁美酮)九、異丁芬酸類：Sulindac(舒林酸)I.salicylates(水楊酸類)

Aspirin(乙酰水揚酸,阿斯匹林)Apro-drugforsalicylicacid

Pharmacokineticsp.oreadilyabsorbedinstomachandsmallintestine;quicklyhydrolyzedintosalicylicacidandwidelydistributed;metablizedinliverandexcretedinurineKinetics:<1g,1storder>1g,0orderPharmacologicaleffects&clinicaluses1.antipyretics,analgesics,antirheumaticeffects2.anti-plateleteffect:inhibitplateletsaggregationandthrombosis.TXA2inplateletPGI2inbloodvesselSmallamountforpreventionofthrombosis3.otherapplicationspediatrics---Kawasakidiseases（川崎氏病）Alzheimer‘sdiseasesAdversereaction1.gastrointestinereaction:Directdrugstimulation,localPGsIndirecteffect—CTZ2.bleedingtendency:3.salicylicacidreaction:headache,tinnitus4.allergicreaction:aspirinasthma5.Reye’ssyndrome:liver6.kidneydamageII.Anilines(苯胺類)Acetaminophen(對乙酰氨基酚)，paracetamol（撲熱息痛）InhibitPGssynthesisinCNSbetterthanthatinperipheraltissuesHavegoodantipyreticeffectbutbadanti-inflammatoryeffectsFirstchoiceforchildrenIII、Pyrazolone(吡唑酮類)Phenybutazone(保泰松)、Metamizole（安乃近）IV.Indoles(吲哚類)Indomethacin(吲哚美辛,消炎痛)ThestrongestCOXinhibitoreverfound,mayalsoinhibitphospholipaseA&CMoreadversereactionsSulindac(舒林酸)V.Phenylpropionicacid(芳基丙酸類)Ibuprofen(布洛芬)：芬必得（fenbid）Naproxen（萘普生）VI.Aryloxyaceticacid(芳基乙酸類)Diclofenic(雙氯芬酸，p139)SelectiveCOX-2inhibitorsDecreasetheriskofgastro-intestinaldamagebutmayincreasetheriskofcardiovascularsystemreactionCelecoxib(塞來昔布)Rofecoxib(羅非昔布)nimesulide（尼美舒利）Gout(痛風(fēng))SuppressantsDrugclassificationbasedonpharmacologicaleffects1.inhibitthesynthesisofuri