神经系统药理魏尔清（传出药理概论 拟胆碱药课件

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1、Part2ParasympathomimeticsCholinoceptoragonists:M,NAnticholinesteraseinhibitorsAMuscarinicreceptoragonistsAMuscarinicreceptoragonists1.CholineEsters(胆碱酯类)Acetylcholine乙酰胆碱Carbachol卡巴胆碱Methacholine醋甲胆碱Bethanecholchloride氯贝胆碱2.NaturalAlkaloids(生物碱类)Pilocarpine毛果芸香碱（

2、匹罗卡品）Muscarine毒蕈碱Pilocarpine毛果芸香碱（匹罗卡品）Pilocarpine毛果芸香碱AMuscarinicreceptoragonists1.Pharmacologicaleffects（1）EyesMiosis（缩瞳）:contractionofsphinctermuscleofirisLowingintraocularpressure（降低眼内压）:enlargingangleofanteriorchamber,increasingdrainageofaquoushumorSpasmofac

3、commodation（调节痉挛）:contractionofciliarymuscle,contractionfornearvisionAMuscarinicreceptoragonistsIris,cilliarymuscles,andSchelemmcanalAqueoushumordrainagePilocarpineAtropine（2）Promotingsecretionofexocrineglands（外分泌腺体）especiallyinsweat,salivaryandtearglandsAMuscari

4、nicreceptoragonists2.Clinicaluses（1）OphthamologicalusesGlaucoma:narrow-orwide-anglesIritis:miotics/mydriaticsBOXGlaucomaAcutecongestiveglaucoma（narrow-angle）Chronicsimpleglaucoma（wide-angle）AMuscarinicreceptoragonists（2）SystemicuseDrymouth:radiotherapyAntidotefor

5、atropinepoisoningAMuscarinicreceptoragonists3.Adverseeffects（1）Local(eye):pain,tears（2）Systemic:secretionofexocrineglands,treatedwithatropineAMuscarinicreceptoragonistsBAnticholinesterases1.Reversibleanticholinesterases2.Irreversibleanticholinesterasesanionicsite

6、esteraticsiteAcetylcholinesteraseisthemechanismofterminatingACheffectsB-1ReversibleanticholinesterasesActionofacetylcholinesteraseAcetylcholinese:structureforinteractionwithsubstrateB-1ReversibleanticholinesterasesNeostigmine新斯的明Neostigmine新斯的明1.Pharmacologicalef

7、fectsbindingtoAChE,butslowlyhydrolysisinhibitingAChEactivityPropertiesofEffectsstrongereffectonskeletalmusclesAChE(-),AChrelease,stimulatingNMreceptoreffectiveonGItractandurinarybladdermorepolarandcannotenterCNSrelativelyineffectiveonCVS,glands,eyeB-1Reversiblean

8、ticholinesterasesEffectofneostigmineonAChEActionofneostigmineonacetylcholinesterase2.Clinicaluses(1)Myastheniagravis（重症肌无力）:symptomatictreatment,overdose:choli