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1、Part3CholinoceptorAntagonistsAMuscarinicreceptorantagonistsActionsitesofcholinoceptorantagonistActionsitesofcholinoceptorantagonistNMAtropine阿托品Scopolamine东莨菪碱Anisodamine山莨菪碱Atropine-likealkaloidsAMuscarinicreceptorantagonists1.Pharmacologicaleffects(1)Inhibitionofexocri
2、neglandsecretionsalivary,sweatglandstear,respiratorytractglandsrelativelyineffective:GItract(2)EyemydriasisriseinintraocularpressureparalysisofaccommodationAtropine阿托品pilocarpineatropineDurationsoftheactionatropine-likedrugsoneye(3)Antispamodicactiononsmoothmusclesensiti
3、ve:GI,urinarybladder(spasmodicstate)relativelyinsensitive:bileduct,urinarytract,bronchialtractinsensitive:uterus(4)HeatHR↓:becauseofM1blockade;HR↑:ifvagaltone↑A-Vconduction:ifvagaltone↑AMuscarinicreceptorantagonists(5)BloodvesselsandbloodpressureTherapeuticdoses:noremark
4、ableeffectLargerdoses:vasodilatationintheskin(indirect)andinsepticshock(6)CentralstimulationLargerdosesAMuscarinicreceptorantagonists2.Clinicaluses(1)SpasmsofsmoothmusclesGI,biliaryorrenalcolic,enuresis(2)InhibitingexocrineglandsecretionPreanestheticmedication,over-secre
5、tion(3)OphthalmologyAcuteiritisoriridocyclitis:mydriatics/mioticsMeasurementoftherefraction:childrenAMuscarinicreceptorantagonists(4)Bradyarrhythmiasinusornodalbradycardia,A-Vblock(5)Septicshock(6)AntidotefororganophosphatepoisoningAMuscarinicreceptorantagonists3.Adverse
6、effects(1)Sideeffects(2)CentraltoxicityLethaldose:80~130mg(adults),10mg(child)butnotincludingthecaseoftreatingorganophosphatetoxicationAMuscarinicreceptorantagonists(3)DetoxicationSymptomatictreatment:diazepam,etc.Physostigmine(毒扁豆碱)orpilocarpine(毛果芸香碱)(4)Contraindicatio
7、nsglaucoma,prostatauxe,feverAMuscarinicreceptorantagonistsActionsandclinicalusesPeripheraleffectsaresimilartoatropine;buthasstrongercentraleffects(depression)Pre-anestheticmedication,preventionofmotionsickness,Parkinson’sdiseaseScopolamine东莨菪碱AMuscarinicreceptorantagonis
8、tsActionsandclinicalusesPrimarilyactsonthesmoothmusclesofperipheralorgans;weakinCNS,glands,eyeSepticsho