解热镇痛抗炎药x.ppt

解热镇痛抗炎药,1,谢谢聆听,2019-11-8,objecter,掌握解热镇痛抗炎药的一般药理.阿司匹林、对乙酰氨基酚、吲哚美辛的药理作用、临床应用、不良反应和药物的相互作用。熟悉布洛芬、双氯芬酸、选择性COX-2抑制药的药理作用特点。了解其他解热镇痛抗炎药的作用特点。,2,谢谢聆听,2019-11-8,Introduction,definitionp.1851）havestrongantipyretic(解热)、2）analgesic、3）anti-inflammatory(抗炎)4）antirheumatic(抗风湿)effects.non-steroidalanti-inflammatorydrugs(NSAIDs非甾体抗炎药),3,谢谢聆听,2019-11-8,awidevarietyofdrugs,chemicalstructurearevarious.,Anti-inflammatorydrugs,NSAIDsaspirin(阿司匹林）,SAIDshydrocortisone(氢化可的松）,4,谢谢聆听,2019-11-8,mechanism,Membranephospholipids,PLA2,Arachidonicacid,COX,LTs(白三烯),PGG2,PGH2,vessel,PGI2,PGF,PGE,platelet,TXA2,SAIDs(),NSAIDs(),甾体激素,非甾体抗炎药,5,谢谢聆听,2019-11-8,【commonness】,一、antipyreticaction1）pyretic,细菌毒素病毒等,粒细胞吞噬、处理,产生、释放,内热原,CNSPG合成与释放,体温调定点,370C,发热,aspirin,2）antipyreticmechanism,6,谢谢聆听,2019-11-8,3）characters,1、temperaturenormal(patientswithfever);2、theactionindependentofenvironmenttemperature;3、mainlyinfluencedispelfever.,（散热）,7,谢谢聆听,2019-11-8,Meaningofpyretic,advantages：recovery，diagnose；disadvantages：highfeverordurativefeverconsumephysicalforce，CNSfunctiondisorders.T39c(especiallywean!),Notice,8,谢谢聆听,2019-11-8,二、analgesicaction,Characteristics：1）moderateanalgesics，Inflammatorypainwell,butsevereorcolicpainuseless.2）noaddiction，norespiratorydepression.,9,谢谢聆听,2019-11-8,Mechanismofanalgesic,局部释放,致痛物质BK、PG等,（+）,痛觉感受器,痛觉增敏,疼痛,NSAIDs,NSAIDsCOXPGanalgesic,组织损伤局部炎症,10,谢谢聆听,2019-11-8,2）(-)COXPGSsynthesize；3)sensitizetoinflammatorymediators.,(1)Functionarysite-mainlyperipheral；,11,谢谢聆听,2019-11-8,三、Antiinflammation,IntheinflammatoryreactionPGsproduce:vasodilation;vascularpermeability;tissueoedema,NSAIDs()COX,Cellularadhesionmolecule(细胞粘附分子),12,谢谢聆听,2019-11-8,Cyclooxygenase,COX,COX-1structuraltype结构型参与血管舒张、血小板聚集、胃粘膜血流、胃粘液分泌及肾功能的调节；COX-2derivationaltype诱导型一般在正常组织较少表达，而在炎症部位呈诱导性表达，是产生PGE2等炎症介质的关键酶。,13,谢谢聆听,2019-11-8,NSAIDs对COX-1和COX-2作用的比较（IC50：mol/L）药物COX-1COX-2COX-2/COX-1吡罗昔康0.00150.906600阿司匹林1.6277.0173吲哚美辛0.0281.68068布洛芬4.872.815.16美洛昔康0.2140.1710.08萘普生9.55.00.58萘丁美酮7.01.00.143尼美舒利100.070.007塞来昔布150.040.0027罗非昔布0.0180.00150.0833,14,谢谢聆听,2019-11-8,ClassificationaccordingtoselectivityofCOX,NSAIDs,Non-selectivityCOXinhibitorsaspirin,.,selectiveCOX-2inhibitorscelecoxib,nimesulide,塞来昔布,尼美舒利,15,谢谢聆听,2019-11-8,1non-selectiveCOXinhibitors,Classification水杨酸类aspirin，sodiumsalicylate；苯胺类acetaminophen；有机酸类indomethacin，ibuprofen；吡唑酮类phenylbutazone；,16,谢谢聆听,2019-11-8,Usualdrugs,aspirin阿司匹林acetylsalicylicacid乙酰水杨酸,17,谢谢聆听,2019-11-8,【pharmacokinetics】,1、absorbrapidly，distributionwide;2、metabolism-liver;3、non-linearityelimination,dosaget1/2(1g,t1/21530h)；4、excretion-kidney,urinepHinfluenceitsexcrete.,18,谢谢聆听,2019-11-8,【actionsanduses】,1.antipyretic、analgesicandanti-rheumaticeffectsusuallyusedfor:variousinflammatorypain;rheumaticarthritisfirstchoice;3-5g/d,qid.,风湿性关节炎,19,谢谢聆听,2019-11-8,2.treatmentofthrombosis(血栓病),aspirin,Lowdose(-),PlateletTXA2synthesize,PLTcongregate,therapeuticeffect,Largedose(-),VesselCOXPGI2-effect,血栓素A2,20,谢谢聆听,2019-11-8,highselectivity75100mg/dpreventthrombosis.(血栓形成),21,谢谢聆听,2019-11-8,【adversereactions】,22,谢谢聆听,2019-11-8,1、gastrointestinalsymptoms,themostcommonreaction,induceoraggravate(加重)ulcer；directstimulation,(-)parietalcellCOX-1PGE2usedwithmisoprostol(米索前列醇)pepticulceroccur,23,谢谢聆听,2019-11-8,2、cruordrawback（凝血障碍）prolongedbleedingtimepreventionandcure：vitamineK3、anaphylaxis（过敏反应）asthmaofaspirin，Adrinefficacy!,24,谢谢聆听,2019-11-8,4、salicylatereaction（水杨酸反应）overdosage(5g/d)GIsymptoms+CNSsymptoms1)withdrawalatonce;2)iv.gtt.NaHCO3excretion.5、renaldamagePGE2、PGI2mediatedeffects(-).,25,谢谢聆听,2019-11-8,Acetaminophen对乙酰氨基酚(paracetamol扑热息痛),【characteristics】1、antipyretic、analgesicaspirinwithoutantiinflammation;2、mostlyusefor：headache、fevercanttakeaspirin;3、adversereactionmild,overdosage-hepaticdamage.,26,谢谢聆听,2019-11-8,Indomethacin（吲哚美辛,消炎痛）,【characteristics】1.OneofthemostpotentCOXinhibitors；2.Antiinflammatory、antipyreticandanalgesiceffectsareremarkable；,27,谢谢聆听,2019-11-8,3.Usedin:rheumatoidarthritis,(风湿性关节炎)stiffnessofosteoarthritis.(强直性骨关节炎)4.Adversereactions:severe;cross-irritability(交叉过敏性)withaspirin.,28,谢谢聆听,2019-11-8,Othersp.190-191,Ibuprofen布洛芬Diclofenac双氯芬酸Piroxicam吡罗昔康Phenylbutazone保泰松Nabumetone萘丁美酮,29,谢谢聆听,2019-11-8,2selectiveCOX-2inhibitorsP.192,Celecoxid（塞来昔布）Rofecoxib（罗非昔布）nimesulide（尼美舒利）new-typeNSAIDs,selective(-)COX-2,adversereactionsnon-selectiveNSAIDs.,30,谢谢聆听,2019-11-8,31,谢谢聆听,2019-11-8,抗感冒药常用的复方制剂,快克醋氨酚250mg金刚烷胺100mg氯苯那敏2mg人工牛黄10mg咖啡因15mg,白+黑,白片,黑片,醋氨酚0.325g0.325g伪麻黄碱30mg30mg右美沙芬15mg15mg苯海拉明25mg,32,谢谢聆听,2019-11-8,泰诺,扑尔敏,对乙酰氨基酚,咖啡因,非那西丁,2,常用抗感冒药组方（Mg/片）,325,右美沙芬,伪麻黄碱,苯丙醇胺,苯海拉明,1530,康泰克450,克感敏