解热镇痛抗炎药课件

解热镇痛抗炎药1谢谢观赏2019-6-29解热镇痛抗炎药1谢谢观赏2019-6-29objecter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谢谢观赏2019-6-29objecter掌握解热镇痛抗炎药的一般药理.阿司匹林、对Introduction[definition]p.185

1）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谢谢观赏2019-6-29Introduction[definition]awidevarietyofdrugs,chemicalstructurearevarious.Anti-inflammatorydrugsNSAIDs

aspirin(阿司匹林）SAIDshydrocortisone(氢化可的松）4谢谢观赏2019-6-29awidevarietyofdrugs[mechanism]MembranephospholipidsPLA2ArachidonicacidCOXLTs(白三烯)PGG2,PGH2vesselPGI2PGF,PGEplateletTXA2SAIDs(–)NSAIDs(–)甾体激素非甾体抗炎药5谢谢观赏2019-6-29[mechanism]Membranephosphol【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aspirin㈠2）antipyretic

mechanism6谢谢观赏2019-6-29【commonness】一、antipyreticact3）characters

1、

temperaturenormal(patientswithfever);2、theactionindependentofenvironmenttemperature;3、mainlyinfluencedispelfever.（散热）7谢谢观赏2019-6-293）characters1、temperatureMeaningofpyretic

advantages：

recovery，diagnose；

disadvantages：highfeverordurativefeverconsumephysicalforce，CNSfunctiondisorders.T>39ºc(especiallywean!)Notice8谢谢观赏2019-6-29Meaningofpyreticadvantages：二、analgesicactionCharacteristics：

1）

moderateanalgesics，Inflammatorypainwell,butsevereorcolicpainuseless.2）noaddiction，

norespiratorydepression.9谢谢观赏2019-6-29二、analgesicactionCharacterisMechanismofanalgesic局部释放致痛物质BK、PG等（+）痛觉感受器痛觉增敏疼痛NSAIDs㈠NSAIDs㈠COXPGanalgesic组织损伤局部炎症10谢谢观赏2019-6-29Mechanismofanalgesic局部释放致痛物2）(-)COXPGSsynthesize；3)sensitizetoinflammatorymediators.(1)Functionarysite----mainlyperipheral；11谢谢观赏2019-6-292）(-)COXPGSsynthesize；三、AntiinflammationIntheinflammatoryreaction

PGsproduce:vasodilation;vascularpermeability;tissueoedema……NSAIDs(–)COXCellularadhesionmolecule

(细胞粘附分子)12谢谢观赏2019-6-29三、AntiinflammationIntheinflaCyclooxygenase,COXCOX-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谢谢观赏2019-6-29Cyclooxygenase,COXCOX-1sNSAIDs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＞100.07＜0.007

塞来昔布150.040.0027罗非昔布0.0180.0015＜0.083314谢谢观赏2019-6-29NSAIDs对COX-1和COX-2作用的比较（IC50：ClassificationaccordingtoselectivityofCOXNSAIDsNon-selectivityCOXinhibitorsaspirin,…….selectiveCOX-2inhibitorscelecoxib,nimesulide…塞来昔布尼美舒利15谢谢观赏2019-6-29Classificationaccordingtose§1non-selectiveCOXinhibitorsClassification水杨酸类aspirin，sodiumsalicylate；苯胺类acetaminophen；有机酸类indomethacin，ibuprofen；吡唑酮类phenylbutazone；

……16谢谢观赏2019-6-29§1non-selectiveCOXinhibitorUsualdrugsaspirin阿司匹林acetylsalicylicacid乙酰水杨酸17谢谢观赏2019-6-29Usualdrugsaspirin17谢谢观赏2019-6【pharmacokinetics】1、absorbrapidly，distributionwide;2、metabolism---liver;3、non-linearityelimination,dosaget1/2(>1g,t1/215~30h)；4、excretion---kidney,

urinepHinfluenceitsexcrete.18谢谢观赏2019-6-29【pharmacokinetics】1、absorbrap【actionsanduses】

1.antipyretic、analgesic

and

anti-rheumaticeffects

usuallyusedfor:

variousinflammatorypain;

rheumaticarthritisfirstchoice;

3-5g/d,qid.风湿性关节炎19谢谢观赏2019-6-29【actionsanduses】1.anti2.treatmentofthrombosis(血栓病)aspirinLowdose(-)PlateletTXA2synthesizePLTcongregatetherapeuticeffectLargedose(-)VesselCOXPGI2-----effect血栓素A220谢谢观赏2019-6-292.treatmentofthrombosis(血highselectivity75~100mg/dpreventthrombosis.

(血栓形成)21谢谢观赏2019-6-29highselectivity21谢谢观赏2019-6-【adversereactions】22谢谢观赏2019-6-29【adversereactions】22谢谢观赏21、gastrointestinalsymptoms

themostcommonreaction,induceoraggravate(加重)ulcer；

directstimulation,(-)parietalcellCOX-1PGE2

usedwithmisoprostol(米索前列醇)pepticulceroccur23谢谢观赏2019-6-291、gastrointestinalsymptoms2、cruordrawback（凝血障碍）

prolongedbleedingtime

preventionandcure：vitamineK3、anaphylaxis（过敏反应）

asthmaofaspirin，

Adr

—

inefficacy!24谢谢观赏2019-6-292、cruordrawback（凝血障碍）24谢谢观赏24、salicylatereaction（水杨酸反应）

overdosage(>5g/d)GIsymptoms+CNSsymptoms1)withdrawalatonce;2)iv.gtt.NaHCO3excretion.5、renaldamagePGE2、PGI2mediatedeffects(-).

……

25谢谢观赏2019-6-294、salicylatereaction（水杨酸反应）25Acetaminophen

对乙酰氨基酚

(paracetamol扑热息痛)【characteristics】1、antipyretic、analgesic

≈aspirin

withoutantiinflammation;2、mostlyusefor：headache、fevercan’ttakeaspirin;3、adversereactionmild,

overdosage-----hepaticdamage.26谢谢观赏2019-6-29Acetaminophen对乙酰氨基酚

(parIndomethacin（吲哚美辛,消炎痛）【characteristics】1.OneofthemostpotentCOXinhibitors；2.Antiinflammatory、antipyreticandanalgesiceffectsareremarkable；27谢谢观赏2019-6-29Indomethacin（吲哚美辛,消炎痛）【chara3.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谢谢观赏2019-6-293.Usedin:rheumatoidarthritOthers

p.190-191Ibuprofen布洛芬Diclofenac双氯芬酸Piroxicam吡罗昔康Phenylbutazone保泰松Nabumetone萘丁美酮

……29谢谢观赏2019-6-29Othersp.190-19§2selectiveCOX-2inhibitorsP.192

Celecoxid（塞来昔布）

Rofecoxib

（罗非昔布）

nimesulide（尼美舒利）

new-type

NSAIDs,selective(-)COX-2,adversereactions<non-selectiveNSAIDs.

30谢谢观赏2019-6-29§2selectiveCOX-2inhibitors31谢谢观赏2019-6-2931谢谢观赏2019-6-29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25mg32谢谢观赏2019-6-29抗感冒药常用的复方制剂快克醋氨酚250mg金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

212630100氨基比林APC35162乙酰水杨酸226.8去痛片

12650150感冒灵325030药物33谢谢观赏2019-6-29泰诺扑尔敏对乙酰咖啡因非那2常用抗感冒药组方（Mg/三九感冒灵颗粒维C银翘片……34谢谢观赏2019-6-29三九感冒灵颗粒34谢谢观赏2019-6-291、试比较解热镇痛药与镇痛药在镇痛方面的作用和应用。2、试比较解热镇痛药与氯丙嗪在影响体温方面的作用和应用。思考题35谢谢观赏2019-6-291、试比较解热镇痛药与镇痛药在镇痛方面的作用和应用。思考36谢谢观赏2019-6-2936谢谢观赏2019-6-29Thankyougoodbye37谢谢观赏2019-6-29Thankyougoodbye37谢谢观赏2019-6解热镇痛抗炎药38谢谢观赏2019-6-29解热镇痛抗炎药1谢谢观赏2019-6-29objecter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。39谢谢观赏2019-6-29objecter掌握解热镇痛抗炎药的一般药理.阿司匹林、对Introduction[definition]p.185

1）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)40谢谢观赏2019-6-29Introduction[definition]awidevarietyofdrugs,chemicalstructurearevarious.Anti-inflammatorydrugsNSAIDs

aspirin(阿司匹林）SAIDshydrocortisone(氢化可的松）41谢谢观赏2019-6-29awidevarietyofdrugs[mechanism]MembranephospholipidsPLA2ArachidonicacidCOXLTs(白三烯)PGG2,PGH2vesselPGI2PGF,PGEplateletTXA2SAIDs(–)NSAIDs(–)甾体激素非甾体抗炎药42谢谢观赏2019-6-29[mechanism]Membranephosphol【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aspirin㈠2）antipyretic

mechanism43谢谢观赏2019-6-29【commonness】一、antipyreticact3）characters

1、

temperaturenormal(patientswithfever);2、theactionindependentofenvironmenttemperature;3、mainlyinfluencedispelfever.（散热）44谢谢观赏2019-6-293）characters1、temperatureMeaningofpyretic

advantages：

recovery，diagnose；

disadvantages：highfeverordurativefeverconsumephysicalforce，CNSfunctiondisorders.T>39ºc(especiallywean!)Notice45谢谢观赏2019-6-29Meaningofpyreticadvantages：二、analgesicactionCharacteristics：

1）

moderateanalgesics，Inflammatorypainwell,butsevereorcolicpainuseless.2）noaddiction，

norespiratorydepression.46谢谢观赏2019-6-29二、analgesicactionCharacterisMechanismofanalgesic局部释放致痛物质BK、PG等（+）痛觉感受器痛觉增敏疼痛NSAIDs㈠NSAIDs㈠COXPGanalgesic组织损伤局部炎症47谢谢观赏2019-6-29Mechanismofanalgesic局部释放致痛物2）(-)COXPGSsynthesize；3)sensitizetoinflammatorymediators.(1)Functionarysite----mainlyperipheral；48谢谢观赏2019-6-292）(-)COXPGSsynthesize；三、AntiinflammationIntheinflammatoryreaction

PGsproduce:vasodilation;vascularpermeability;tissueoedema……NSAIDs(–)COXCellularadhesionmolecule

(细胞粘附分子)49谢谢观赏2019-6-29三、AntiinflammationIntheinflaCyclooxygenase,COXCOX-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。50谢谢观赏2019-6-29Cyclooxygenase,COXCOX-1sNSAIDs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＞100.07＜0.007

塞来昔布150.040.0027罗非昔布0.0180.0015＜0.083351谢谢观赏2019-6-29NSAIDs对COX-1和COX-2作用的比较（IC50：ClassificationaccordingtoselectivityofCOXNSAIDsNon-selectivityCOXinhibitorsaspirin,…….selectiveCOX-2inhibitorscelecoxib,nimesulide…塞来昔布尼美舒利52谢谢观赏2019-6-29Classificationaccordingtose§1non-selectiveCOXinhibitorsClassification水杨酸类aspirin，sodiumsalicylate；苯胺类acetaminophen；有机酸类indomethacin，ibuprofen；吡唑酮类phenylbutazone；

……53谢谢观赏2019-6-29§1non-selectiveCOXinhibitorUsualdrugsaspirin阿司匹林acetylsalicylicacid乙酰水杨酸54谢谢观赏2019-6-29Usualdrugsaspirin17谢谢观赏2019-6【pharmacokinetics】1、absorbrapidly，distributionwide;2、metabolism---liver;3、non-linearityelimination,dosaget1/2(>1g,t1/215~30h)；4、excretion---kidney,

urinepHinfluenceitsexcrete.55谢谢观赏2019-6-29【pharmacokinetics】1、absorbrap【actionsanduses】

1.antipyretic、analgesic

and

anti-rheumaticeffects

usuallyusedfor:

variousinflammatorypain;

rheumaticarthritisfirstchoice;

3-5g/d,qid.风湿性关节炎56谢谢观赏2019-6-29【actionsanduses】1.anti2.treatmentofthrombosis(血栓病)aspirinLowdose(-)PlateletTXA2synthesizePLTcongregatetherapeuticeffectLargedose(-)VesselCOXPGI2-----effect血栓素A257谢谢观赏2019-6-292.treatmentofthrombosis(血highselectivity75~100mg/dpreventthrombosis.

(血栓形成)58谢谢观赏2019-6-29highselectivity21谢谢观赏2019-6-【adversereactions】59谢谢观赏2019-6-29【adversereactions】22谢谢观赏21、gastrointestinalsymptoms

themostcommonreaction,induceoraggravate(加重)ulcer；

directstimulation,(-)parietalcellCOX-1PGE2

usedwithmisoprostol(米索前列醇)pepticulceroccur60谢谢观赏2019-6-291、gastrointestinalsymptoms2、cruordrawback（凝血障碍）

prolongedbleedingtime

preventionandcure：vitamineK3、anaphylaxis（过敏反应）

asthmaofaspirin，

Adr

—

inefficacy!61谢谢观赏2019-6-292、cruordrawback（凝血障碍）24谢谢观赏24、salicylatereaction（水杨酸反应）

overdosage(>5g/d)GIsymptoms+CNSsymptoms1)withdrawalatonce;2)iv.gtt.NaHCO3excretion.5、renaldamagePGE2、PGI2mediatedeffects(-).

……

62谢谢观赏2019-6-294、salicylatereaction（水杨酸反应）25Acetaminophen

对乙酰氨基酚

(paracetamol扑热息痛)【characteristics】1、antipyretic、analgesic

≈aspirin

withoutantiinflammation;2、mostlyusefor：headache、fevercan’ttakeaspirin;3、adversereactionmild,

overdosage-----hepaticdamage.63谢谢观赏2019-6-29Acetaminophen对乙酰氨基酚

(parIndomethacin（吲哚美辛,消炎痛）【characteristics】1.OneofthemostpotentCOXinhibitors；2.Antiinflammatory、antipyreticandanalgesiceffectsareremarkable；64谢谢观赏2019-6-29Indomethacin（吲哚美辛,消炎痛）【chara3.Usedin:rheumatoidarthritis,(风湿性关节炎)

stiffnessofosteoarthritis.

(强直性骨关节炎)4.Adversereactions:severe;

cross-irritability(