第八章M胆碱受体阻断药

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DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC(cholinoceptorblockingdrugs)第八章MMMM胆碱受体阻断药DepartmentDepartmentDepartmentDepartmentofofofofpathophysiologypathophysiologypathophysiologypathophysiologyJNMCJNMCJNMCJNMCDepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC目的要求掌掌握掌握阿托品的药理作用、作用机制、临床应用及不良反应。熟悉熟悉了解了解东茛菪碱、山茛菪碱的作用特点和临床应用。溴丙胺太林、贝那替秦、哌仑西平的作用特点。DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC胆碱受体阻断药分类胆碱受体阻断药分类1.1.1.1.1.1.1.1.MMMMMMMM受体阻断药受体阻断药阿托品、山莨菪碱、东莨菪碱阿托品、山莨菪碱、东莨菪碱2.N2.N2.N2.N2.N2.N2.N2.N11111111受体阻断药:受体阻断药:美加明、咪噻吩美加明、咪噻吩3.N3.N3.N3.N3.N3.N3.N3.N22222222受体阻断药:受体阻断药:筒箭毒碱筒箭毒碱DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC颠茄、曼陀罗、莨菪阿托品唐古特莨菪樟柳碱唐古特莨菪山莨菪碱洋金花东莨菪碱第一节第一节第一节第一节阿托品和阿托品类生物碱阿托品和阿托品类生物碱阿托品和阿托品类生物碱阿托品和阿托品类生物碱DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC••颠茄曼陀罗莨菪第一节第一节第一节第一节阿托品和阿托品类生物碱阿托品和阿托品类生物碱阿托品和阿托品类生物碱阿托品和阿托品类生物碱DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC曼陀罗洋金花DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC•曼陀罗DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC阻断MMMM受体大剂量:阻断NNNN1111受体atropineatropineatropineatropine阿托品(atropineatropineatropineatropine)[作用机制]DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC特点随剂量增加,依次作用•腺体→眼→心脏→平滑肌→血管→CNSCNSCNSCNSatropineatropineatropineatropineDepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMCatropineatropineatropineatropine��抑制腺体分泌:抑制腺体分泌:��唾液腺、汗腺唾液腺、汗腺��泪腺、泪腺、呼吸道腺体呼吸道腺体��胃液分泌胃液分泌��胃酸分泌胃酸分泌[[[[[[[[药理作用及临床应用药理作用及临床应用]]]]]]]]强弱DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC••眼睛:眼睛:––扩瞳扩瞳––升高眼内压升高眼内压––调节麻痹调节麻痹DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC(1)扩瞳扩瞳扩瞳扩瞳虹膜平滑肌示意图atropineatropineatropineatropineDepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC•(2)眼内压升高眼内压升高眼内压升高眼内压升高房水出路((((箭头示房水流出方向))))atropineatropineatropineatropine睫状肌M-R(-)M-R(-)M-R(-)M-R(-)→睫状肌松弛而退向外缘→悬韧带拉紧→晶状体变扁平→屈光度减低→视近物不清,适于视远物晶状体(3)(3)(3)(3)调节麻痹调节麻痹调节麻痹调节麻痹睫状肌悬韧带图8-5调节麻痹示意图atropineatropineatropineatropineM胆碱受体激动药和阻断药对眼的作用atropineatropineatropineatropineDepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC��松弛内脏平滑肌松弛内脏平滑肌胃肠道尿道和膀胱平滑肌胆道、输尿管和支气管子宫平滑肌atropineatropineatropineatropine[[[[[[[[药理作用及临床应用药理作用及临床应用]]]]]]]]强弱DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMCnotice•阿托品对痉挛状态平滑肌松弛作用明显•对括约肌作用不稳定,取决于机能状态DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC对心脏的作用心率小量(0.4~0.6mg):少数人减慢较大量(1~2mg):加快房室传导:(-)(-)(-)(-)突触前膜的MMMM1111-R(-R(-R(-R(负反馈))))↖(-)(-)(-)(-)窦房结的MMMM2222-R-R-R-R加速加速加速加速atropineatropineatropineatropineDepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC血管机制:(与MMMM受体阻断无关)治疗量无明显变化大剂量血管扩张改善微循环体温升高的代偿性散热反应直接扩张血管作用atropineatropineatropineatropineDepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC中枢神经系统(CNS)兴奋atropineatropineatropineatropine治疗量中枢作用不明显较大量轻度兴奋延髓呼吸中枢(1-2mg)(1-2mg)(1-2mg)(1-2mg)更大量兴奋大脑(烦躁、谵妄)(2-5mg)(2-5mg)(2-5mg)(2-5mg)DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC中枢神经系统(CNS)兴奋•中毒量((((>10mg)10mg)10mg)10mg)幻觉、定向障碍、运动兴奋、惊厥•严重中毒兴奋转为抑制,循环和呼吸衰竭DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC临临临临床床床床应应应应用用用用药药药药理理理理作作作作用用用用抗休克缓慢型心律失常内脏绞痛膀胱刺激症状虹膜睫状体炎验光检查眼底全麻前全麻前全麻前全麻前给药给药给药给药严重盗严重盗严重盗严重盗汗流涎汗流涎汗流涎汗流涎兴奋(毒性)大剂量扩张血管加快心率房室传到加快解除平滑肌痉挛扩瞳眼压调解麻痹抑制腺体分泌CNSCNSCNSCNS血管血压心脏平滑肌眼腺体药理作用与临床应用有机有机有机有机磷中磷中磷中磷中毒解毒解毒解毒解救救救救atropineatropineatropineatropineDepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC[[[[不良反应不良反应不良反应不良反应]]]]1.1.1.1.副作用副作用副作用副作用口干、视物模糊口干、视物模糊口干、视物模糊口干、视物模糊阿托品2.2.2.2.使用过量使用过量使用过量使用过量呼吸加深加快、高热、谵妄、惊厥等。3.3.3.3.严重中毒严重中毒严重中毒严重中毒中枢抑制,昏迷和呼吸麻痹等。DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC阿托品的副作用阿托品瞳孔放大DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNMCJNMC阿托品的副作用阿托品视物模糊DepartmentDepartmentDepartmentDepartmentofofofofPharmacologyPharmacologyPharmacologyPharmacologyJNMCJNMCJNM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