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1、 Cholinoceptor-activating drugCholinoceptor-activating drugAcetylcholine receptor stimulantsCholinesterase inhibitorsMimic acetylocholineAcetylcholine receptor stimulantsClassified by their spectrum of action depending on the receptor typeActivate muscarinic receptor Activate nicotinic receptorMusca
2、rinic receptor stimulantsCholine esters:acetylcholine,methacholine,carbachol,bethanecholAlkaloid:pilocarpine,arecolineAcetylcholineCardiovascular system:Vessel:dilation via EDRFNegative chronotropic effectNegative dromotropic effectNegative inotropic effectAcetylcholineGastrointestinal tract:increas
3、e motility,stimulate secretionUrinary bladder:detrusor contraction,trigone and sphincter relaxationGlands:stimulate secretionEye:contract sphincter muscle of iris,contract ciliary muscle for near visionAcetylcholineA large dose of Ach after administration of atropine can activate nicotinic receptorN
4、1:ganglionN2:neuromuscular junctionActivate NN receptorAll ganglion are activatedSympathetic effects:increase in blood pressureParasympathetic effects:glands secret,contract smooth muscleexcite adrenal gland medullaOverdose:excitement inhibitionActivate Nm receptorNeuromuscular end plateSkeletal mus
5、cle ContractionmethacholineSelectively activate muscarinic receptorStronger effects on cardiovascular system Clinical uses:sjogrens syndromeAsthma,ulcer,anoxemiaothersCarbachol:pharmacodynamics is similar to Ach,uses for glaucomaBethanechol:more selective to M receptor Alkaloid Including pilocarpine
6、,arecoline,muscarine,oxotremorinepilocarpinePharmacodynamics:Eye:miosis,ocular pressure reduction,accommodationGlands:secretion（动眼神经的胆碱能神经支配）（动眼神经的胆碱能神经支配）毛果芸香碱激动毛果芸香碱激动 瞳孔括约肌瞳孔括约肌 缩瞳缩瞳 阿托品阻断阿托品阻断 瞳孔开大肌瞳孔开大肌 扩瞳扩瞳（去甲状腺素能神经支配）（去甲状腺素能神经支配）虹膜虹膜(包括瞳孔括约肌和瞳孔开大肌包括瞳孔括约肌和瞳孔开大肌 )毛果芸香碱的缩瞳作用毛果芸香碱的缩瞳作用 受体受体 M受体受体
7、狭窄时眼内狭窄时眼内压增高，闭压增高，闭角型青光眼角型青光眼（急，慢型（急，慢型充血性青光充血性青光眼）眼）变性或硬化变性或硬化时眼内压增时眼内压增高高 开角性开角性青光眼（慢青光眼（慢性单纯性青性单纯性青光眼）光眼）睫状体上皮睫状体上皮 细胞分泌细胞分泌血管血管渗出渗出 房水房水 瞳孔瞳孔 前前房房前房角间隙前房角间隙小梁网小梁网巩膜静脉窦巩膜静脉窦血流血流 毛果芸香碱的降低眼内压作用毛果芸香碱的降低眼内压作用 间隙扩大间隙扩大,房房水入循环水入循环毛果芸香碱收毛果芸香碱收缩瞳孔括约肌缩瞳孔括约肌 缩瞳虹膜拉紧缩瞳虹膜拉紧 虹膜根部变薄虹膜根部变薄毛果芸香碱毛果芸香碱收缩睫状肌收缩睫状肌扩张
8、小血管扩张小血管阿托品扩瞳，虹膜退向四周，前房角阿托品扩瞳，虹膜退向四周，前房角间隙变窄，房水回流受阻，眼内压升高间隙变窄，房水回流受阻，眼内压升高 降低眼内压降低眼内压正常时晶体较扁平正常时晶体较扁平受睫状肌控制受睫状肌控制环状肌环状肌辐射状肌辐射状肌(瞳孔括约肌瞳孔括约肌)动眼神经兴奋动眼神经兴奋或毛果芸香碱或毛果芸香碱动眼神经胆动眼神经胆碱能神经碱能神经阿阿托托品品向瞳孔中心收缩悬韧向瞳孔中心收缩悬韧带，睫状小带放松带，睫状小带放松睫状肌松弛而退向睫状肌松弛而退向外缘，悬韧带拉紧外缘，悬韧带拉紧(瞳孔开大肌瞳孔开大肌)去甲肾上腺素能去甲肾上腺素能神经支配神经支配 对眼对眼调节无重要意义调
9、节无重要意义只视近物只视近物(调节痉挛调节痉挛)只视远物只视远物(调节麻痹调节麻痹)晶状体变扁晶状体变扁屈光度降低屈光度降低晶状体变凸晶状体变凸屈光度增加屈光度增加毛果芸香碱的调节痉挛作用毛果芸香碱的调节痉挛作用外外界界睫状肌起点睫状肌起点悬韧带悬韧带Clinical usesGlaucomaIritisMuscarine Direct acting muscarinic receptor:toxic reactionnicotineContributes to increased risk of vascular disease and sudden coronary deathContri
10、butes to high incidence of ulcer recurrence with peptic ulcer AnticholinesteraseAnticholinesterase agentsagentsAcetylcholinesteraseAch=AchE Ach-AchE choline+AcAchE Acetate+AcheThe entire process takes place in 150ms AchENerve terminal,synaptic cleft,effectorsMost chlinergic synapses are richly suppl
11、ied with AchE,the half-life of Ach is very shortAnticholinesterase agentsBinds to AchE complexThe covalent bond is resistance to the second process,and this step is prolongedclassificationHydration process is prolonged for 30 minutes to 6 hoursHydration process is prolonged for hundreds of hoursAnti
12、cholinesterase agentsPharmacodynamics:Eye:miosis,ocular pressure reduction,accommodationGastrointerase systems:contract,increase secretionAnticholinesterase agentsNeuromuscular junction:Therapeutic concentration:prolong and intensify the actions of Ach;activate skeletal muscle directlyHigher concent
13、ration:fibrillation of muscle fibersAnticholinesterase agentsRespiratory,urinary tract:contractCardiovascular system:increase activation in ganglia and at acetylcholine receptors on neruoeffector cells(HR ,BP )Anticholinesterase agentsGlands:secretCNSLow concentration:activation of EEG,subjective al
14、erting responseHigh concentration:coma,respiratory arrestClinical usesMyasthenia gravisIleus,GlaucomaDetoxifcationAlzheimiers diseasecholinergic crisisNeostigmineInhibit AchE and thereby increase the concentration of endogenous AchAct at neuromuscular junction and smooth muscle Selectively Myastheni
15、a gravisIleus,PyridostigminePharmacodynamics is similar to NeostigmineTake effect slowly Myasthenia gravisIleus,physostigmineEyeCNS:toxic reactionglaucomaEdrophonium chloride:Use for diagnosisAmbenonium chloride:GalanthamineDemecarium bromideOrganophosphatesBinds to AchE complexThe covalent bond is stable and hydrolyzes in water at a very slow rateAging:more stable and more difficult to splitToxic symptomActivate M receptorActivate N receptorCNSDiagnosisPreventionDetoxifcationAtropinePAM