胆碱受体阻断药的分类胆碱受体阻断药的分类McholinoceptorblockingdrugsMcholinoceptorblockingdrugsNN11CholinoceptorBlockingDrugsCholinoceptorBlockingDrugs(ganglionicblockingdrugs(ganglionicblockingdrugs))NN22CholinoceptorBlockingDrugsCholinoceptorBlockingDrugs(Skeletalmusclerelaxants)(Skeletalmusclerelaxants)第一节第一节M-CholinoceptorBlockingDruM-CholinoceptorBlockingDrugsgs阿托品阿托品(Atropine)(Atropine)Abelladonnaalkaloid,hasahighaffiniAbelladonnaalkaloid,hasahighaffinityforMreceptors,whereitbindscompetyforMreceptors,whereitbindscompetitively,preventingacetylcholinefromtitively,preventingacetylcholinefrombindingtothatsite.bindingtothatsite.竞争性拮抗竞争性拮抗AchAch对对MM受体的激动作用,大剂量受体的激动作用,大剂量阻断阻断NN受体。受体。PharmacologicaleffectsPharmacologicaleffects11、解除平滑肌痉挛:松驰多种内脏平滑肌、解除平滑肌痉挛:松驰多种内脏平滑肌特点特点::(1)(1)对过度活动或痉挛的平滑肌松驰作用较对过度活动或痉挛的平滑肌松驰作用较显著。显著。(2)(2)胃肠胃肠>>膀胱膀胱>>胆囊胆囊,,胆管胆管,,输尿管输尿管,,支气管支气管,,子宫子宫2.2.抑制腺体分泌抑制腺体分泌唾液腺唾液腺((口干口干),),汗腺汗腺((皮肤干燥皮肤干燥)>)>呼吸呼吸道腺体道腺体>>胃腺。大剂量也抑制胃的分泌机能胃腺。大剂量也抑制胃的分泌机能Salivarygland(drymouth),sweatglanSalivarygland(drymouth),sweatgland(drynessoftheskin)>bronchialsecrd(drynessoftheskin)>bronchialsecretorygland(dischargedecreased)>stometorygland(dischargedecreased)>stomachgland(Largedosagemayinhibittheachgland(Largedosagemayinhibitthesecretoryfunctionofthestomach)secretoryfunctionofthestomach)3.Eye:itblocksallcholinergicactivityo3.Eye:itblocksallcholinergicactivityontheeye,resultingindilationofpupil,ntheeye,resultingindilationofpupil,unresponsivenesstolightandinabilitytounresponsivenesstolightandinabilitytofocusfornearvision.Inpatientswithglafocusfornearvision.Inpatientswithglaucoma,intraocularpressuremayrisedangerucoma,intraocularpressuremayrisedangerously.ously.(1)(1)散瞳散瞳(mydriasis)(mydriasis)::??(2)(2)眼内压升高:眼内压升高:??(3)(3)调节麻痹调节麻痹(cycloplegia)(cycloplegia)::??睫状肌松弛,拉紧悬韧带,使晶状体睫状肌松弛,拉紧悬韧带,使晶状体变扁平,屈光度降低,以致视近物模变扁平,屈光度降低,以致视近物模糊,视远物清楚。糊,视远物清楚。4.Cardiovascularsystem:4.Cardiovascularsystem:AtropineproducesAtropineproducesdivergentdivergenteffeffectsonthecardiovascularsystectsonthecardiovascularsystem,dependingonthedose.em,dependingonthedose.((11))Atlowdose(0.4-0.6mg),itrAtlowdose(0.4-0.6mg),itresultsintheblockadeofesultsintheblockadeof突触前膜突触前膜((presynapticpresynapticmembranemembrane))的的M1M1受体,受体,ththuspermittingincreasedAchrelease.uspermittingincreasedAchrelease.心率减慢。心率减慢。((22))WithhigherdoseofatropineWithhigherdoseofatropine(atleastof1mg),thecardiacM-re(atleastof1mg),thecardiacM-receptorsontheSAceptorsontheSA((sinoatrialsinoatrial))nonodede窦房结窦房结areblocked,andthecardiareblocked,andthecardiacrateincreasesmoderately.acrateincreasesmoderately.迷走神经张力高的青年,心率加快作用迷走神经张力高的青年,心率加快作用显著,对婴幼儿和老年人的心率影响很显著,对婴幼儿和老年人的心率影响很小。小。(3)(3)扩张血管,改善微循环扩张血管,改善微循环:治疗量对血管:治疗量对血管和血压无明显影响,大剂量解除小血管痉挛,和血压无明显影响,大剂量解除小血管痉挛,改善微循环和重要器官的血流供应...