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1、CholinergicmimicagentsLinYuanPhD,ProfDept.Pharmacology胆碱受体激动药乙酰胆碱药理作用毛果芸香碱（1）药理作用（2）临床应用抗胆碱酯酶药和胆碱酯酶复活药易逆性抗胆碱酯酶药（1）作用机制（2）药理作用 （3）新斯的明的临床应用难逆性抗胆碱酯酶药（1）毒理作用机制（2）急性中毒胆碱酯酶复活药碘解磷定碘解磷定的药理作用及临床应用期末考试/临床执业医师药理学考试大纲知识整合乙酰胆碱小剂量与大剂量效应的不同；外源性与内源性乙酰胆碱产生的效应一样吗？乙酰胆碱长时间与短时间产生的效应一样吗？如何区分肌无力危象（Myasth
2、enicCrisis）和胆碱能危象（CholinergicCrisis）Objective:TounderstandtheclassificationofCholinergicmimicagents;pharmacologiceffectsofAcetylcholine(ACh);ExtendedAnalysis:endogenousandexogenousACh;AChinlowandhighdose(speciallyinorganophosphateintoxication),Shorttime/longtimeexposure.pharmacologi
3、caleffectsandmajorclinicalusesofpilocarpine,neostigmine.ExtendedAnalysis:identificationofMyasthenicCrisisandCholinergicCrisistreatmentoforganophosphateintoxication.ExtendedAnalysis:forthetreatmentofglaucoma,whichofthefollowingdrugshaslessADR,pilocarpineorphysostigmine.Q-1HowareCholi
4、nergicmimicagentsclassified(1)Direct-actingagents:directlybindtoandactivatethemuscarinicornicotiniccholinergicreceptors.Direct-actingagentscanbefurthersub-classifiedintoMreceptoragonist,e.g.,pilocarpine(毛果芸香碱，代表药物）;MandNreceptoragonist,e.g.,AcetylcholineandCarbachol.(2)Indirect-acti
5、ngagents:producetheircholinergiceffectsbyinhibitingtheactionofacetylcholinesterase.Reversible:e.g.,neostigmine(新斯的明）Irriversible:organophosphate,e.g.,Insecticides（杀虫剂，乐果，敌敌畏等）.Acetylcholine(ACh)Classification(Mreceptoragonist,M/Nreceptoragonist)Compareendogenous/exogenousAChAChlowdo
6、se/highdose(speciallyinorganophosphateintoxication),Shorttime/longtime.ACh5μg500μgACh5μgAtropine(Adrenergicfibers)：(Cholinergicfibers)：N1N2MαβN1N1Q-2Describepharmacologicaleffects,clinicalapplicationandmajoradverseeffectsofMreceptoragonist,e.g.,pilocarpine.Pharmacologicaleffects(1)S
7、timulatesthesecretionofsweatandsaliva.(2)Decreaseofcardiacfunction(rate,conduction)(3)Contractionofthesmoothmuscleoftheirissphincterciliarymuscle(睫状肌),resultin(a)miosis;(b)Accommodationspasm*（调节痉挛）(c)Decreaseofocularpressure*Aspasmofaccommodationisaconditioninwhichtheciliarymuscleof
8、theeyeremainsinacon
