神经系统药理—吴希美(解热镇痛药.ppt

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1、Chapter27Antipyretic-AnalgesicandAntiinflammatoryDrugsA.GeneralPharmacologicalproperties1.Inhibitionofprostaglandinsynthesisinhibitingcyclooxygenase(COX，环氧酶),decreasingthesynthesisofPGsandTXA2,resultingantipyretic,analgesic,andanti-inflammatoryeffectsnon-steroidalanti-inflammatorydrugs(NSAIDs,非甾体抗炎药

2、）。2.AntipyreticeffectsInhibitionofPGE2productioninthehypothalamusinducedbyendogenouspyregensafterpathologicalstimulitemperaturenotes:symptomaticcontrolonly,notbeindicatedinallpatientswithfever.Theeffectonbodytemperatureisdifferentfromthatofchlorpromazine.A.GeneralPharmacologicalpropertiesCompariso

3、nofpropertiesoftwotypesofdrugs3.AnalgesiceffectsAnalgesiceffectisresultedfrominhibitionofPGE2production.Effectiveonthepainoflowtomoderateintensityrelatedtoinflammatoryresponses.PGE2:apainstimulantandhyperalgesicagentTheanalgesiceffectisdifferentfromopioidanalgesics.A.GeneralPharmacologicalproperties

4、Comparisonofpropertiesoftwotypesofdrugs4.Anti-inflammatoryeffectsPGsinduceinflammatoryresponses.InhibitionofPGproductioncanrelieveinflammatoryresponses,suchascongestion,exudation,pain.Theeffectisdifferentfromthatofglucocorticosteroids.A.GeneralPharmacologicalpropertiesComparisonofpropertiesoftwotype

5、sofdrugs5.COX-1/COX-2andselectivityofthedrugsCOX-1:constructive;involvedinphysiologicregulatoryfunctionsinGItract,kidney,etc.;inhibitionofCOX-1isrelatedtotheadverseeffects.COX-2:inducible;involvedinpathologicalresponsessuchasinflammation,andpregnancy;inhibitionofCOX-2isrelatedtothetherapeuticeffects

6、.A.GeneralPharmacologicalproperties（－）（＋）（＋）（－）B.SalicylatesAspirin阿司匹林Acetylsalicylicacid乙酰水杨酸Aspirin阿司匹林Salicylicacid水杨酸Salicylicsodium水杨酸钠Aspirin阿司匹林1.ADMEtransformedtosalicylicacidforminthebodyhepaticmetabolismisprimarilyconjugation.excretionfromurine,theexcretionofunchangedformsofaspirinisincre

7、asedinthealkalinizedurine.largerdoses(>1g/d):non-linearelimination,zeroorderkineticprocess,easiertoaccumulationandintoxication.B.Salicylates2.Pharmacologicaleffectsandclinicaluses(1)Antipyretic,analge