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1、解热镇痛抗炎药Antipyretic analgesic and anti-inflammatory drugs,北京协和医学院基础医学院药理学系 叶菜英,Antipyretic analgesic and anti-inflammatory drugs,These drugs relieve the pain associated with inflammation,including that from arthritis and gout.Antipyretic,analgesic,and antiinflammatory drugs.They produce their anti-in
2、flammatory action through a different mechanism,not as glucocorticoid.Classed into non-steroidal anti-inflammatordrugs(NSAIDs)in 1974.,virusbacteriaBacterial productendotoxinTDAg-Ab,external fever,phagocyte（GC）,endogenous pyrogen,hypothalamus,PL,unsaturated fatty acid,PGS,PG,TEMP SET cells,febrile,a
3、ntipyretic analgesic,inhibition,Antipyretic action,Febrile:endogenous pyrogen CNSrelease PG thermotaxic center FebrileAntipyretil:inhibit PG synthetase，decrease synthesis of PG hypothermy,Antipyretic action,depression bradykinin pain sensorantipyretic analgesic painstimulus PG PG synthesis sensitiza
4、tion depression,Analgesic action,Mechanisms:Effect on periphery,inhibit the synthesis of prostaglandins and prevent bradykinin from stimulating pain receptors,also inhibit the recognition of pain impulses centrally and peripherally.,Analgesic action,Anti-inflammatory action Mechanisms:Inhibit a prim
5、ary pathway in PG synthesis.Summary:Inhibit the PG synthesis to antipyretil,analgesic and anti-inflammatory,解热镇痛抗炎药分类,水杨酸类：阿司匹林等苯胺类：对乙酰氨基酚（扑热息痛）等吡唑酮类：保泰松、羟基保泰松等芳基烷酸类：布洛芬、炎痛喜康等,阿斯匹林,解热镇痛消炎药 水杨酸类 阿斯匹林,Aspirin,【physiological disposition】：Oral,absorbed from gutdistribution,metabolismkenosis(enter articu
6、lar cavity,CSF),【Pharmacological action】Atipyretic:temperature drop qiucklyAnalgesic:medium intensityAnti-rheumatic:inhibit antigen-antibody reaction,antibody formation,antigen antibody union，blood sedimentation,relieve flare of articulus.,Aspirin,【Clinical Indications】Antipyretic analgesic and anti
7、 inflammatory Headache,toothache,algomenorrhea,neuralgiacourbature,arthralgia.Fever Acute rheumatism,rheumatoid arthritis,Aspirin,Aspirin,【Pharmacological action&Clinical Indications】Effect on thrombosis：Inhibit cycloxygenase cyclo-oxygenase，reduce TXA2 synthesis Inhibit PA effect on thromboxane syn
8、thesis aspirin TXA2synthetase PM phospholipid AA endoperoxide TXA2 thrombosis PA platelet releasion Clinical Indications:low dose,long term use could prevent CHDthrombosis,cerebral thrombosis,Aspirin,【Untoward reaction】Gastrointestinal tract reactionBlock blood coagulationNS reaction:salicylism,naus
9、ea,vomiting,dizziness,tinnitus,acouesthesiaAnaphylactic responseNephrotoxicity,Paracetamol&Phenacetin,Strong antipyretic analgesic effect;weak anti-rheumatic effect.(inhibition for center epoxidase is stronger than that for external epoxidase),【Pharmacological action】,Phenacetin,Paracetamol,P-aminop
10、henetole,Aniline Paracetamol,Phenacetin,【Pharmacokinetics】Oral,absorbhepatic metabolism kenosis 60combine with GA de-ET（7080）Paracetamol35combine with H2SO4,fail barehydroxidePhenacetin de-AcP-aminophenetole hydroxidehemoglobin oxidation metahemoglobin toxic metabolin,Paracetamol&Phenacetin,【Untowar
11、d Reaction】Allergy occasionally:rash,drug fever,M.M damageOverdose(1015gday)acute poisoninghepatonecrosisOverdosemethemoglobinemia,cyanosis,hypoxia,HAKidney damage,Phenylbutazone(保泰松),Strong anti-inflammatory,anti-rheumatic effects,but weak atipyretil,analgesic effects.,【Pharmacologic action】,Pyrazo
12、ketone,Primary used to rheumatism and rheumatoid arthritis,【Physiological disposition】Oral to absorb,penetration synovia membranethe concentration in synovia intermembrance space is 50%of that in blood(high concentration in joint tissue),Phenylbutazone(保泰松),Pyrazoketone,【Side effects】Stomach intesti
13、ne reactionWater-sodium retention Anaphylactic responsLiver&kidney damageThyromegaly and myxedema,Phenylbutazone(保泰松),Indometacin,【Untoward Reaction】,One of the most potent inhibitors of COX isozymes;Effects on inflammatory,atipyretil analgesic and rheumatism significantly;Use to the cases which dif
14、ficult to cure above-mentioned.,Lots of untoward reaction,high incidence rate,Stomach intestine reaction(ulcer),CNS reaction,Inhibit hematopoietic system,anaphylactic response,Organic acids,Brufen&Fenbid,【Pharmacologic action】Less stomach intestine reactions,good tolerance.99%combine with plasma-alb
15、uminenter synovial membrane tune slowly,keep high concentration.Effect is similar with aspirin,stronger than paracetamol.Used to rheumatism and rheumatoid arthritis.Light dyspepsia,rash occasionally.,Compound preparation(67 types),ColdrineCompound Aminopyrine Phenacetin TabletsAPC Pseudoephedrine+Paracetamol+Dextromethorphan+Chlorphenamine MaleateParacetamolCompound Chlorphenamine Maleate【Essential component】APC:aspirin paracetamol caffeineSomedon:aminophenazone PAC caffeine,Thanks!,Thanks!,
