胆碱R阻断药.ppt

Click to edit Master title style,Click to edit Master text styles,Second level,Third level,Fourth level,Fifth level,*,*,1,Chapter 8,胆碱受体阻断剂,（,I,）,M-R,阻断剂,Cholinoceptor blocking drugs,M-R blocking drugs,2,Instructional objectives,1.,阐述阿托品的作用、用途、不良反应、禁忌症；,2,.,比较山莨菪碱和东莨菪碱的作用特点及用途；,3,.,列举阿托品的合成代用品；,4,.,列举肌松药的分类及代表药。,3,M-R,阻断药,muscarinic blocking drugs,抗胆碱药,anticholinegics,副交感神经阻断药,parasympatholytics,Muscarinic blocking drugs,have no intrinsic activity,and they can produce effects only by blocking the activation of muscarinic receptors by muscarinic agonists or by neuronally released ACh.,4,图,5-2,传出神经分类模式图,5,1,阿托品和阿托品类生物碱,Atropine,atropine-like alkaloid,存在于颠茄、曼陀罗、莨菪中,颠茄,Atropa belladonna,曼陀罗,莨菪,阿托品,Atropine,东莨菪碱,Sco,p,olamine,山莨菪碱,Ani,s,odamine,中枢作用：氧桥,，羟基,东莨菪碱,阿托品山莨菪碱,7,【,Mechanism of action,】(,作用机理,),1.,（,-,）,M-R,2.,large dose,:,（,-,）,N,N,-R,【,Pharmacological actions,】,（,药理作用,）,gland(,腺体,),eye,smooth muscle,(,平滑肌,),heart,CNS,阿托品,Atropine,8,1.,腺体（,glands,）,（,-,）,腺体分泌,（,inhibits the secretion of glands,）,汗腺,(,sweat gland,),、,唾液腺,(,salivary gland,),泪腺,(,lachrymal,),、,呼吸道腺体,胃壁细胞,(,gastric parietal cells,),9,2.,眼（,eye,）,(1),扩瞳（,mydriasis,）,atropine,Please compare,atropine,with,pilocarpine,(,-,),瞳孔括约肌,M,-,R,开大肌功能占优势,瞳孔扩大,(,dilate the pupil,),10,(2),升高眼压,(,increase intraocular pressure,),Atropine,扩瞳,虹膜退向四周边缘,根部变厚,前房角间隙,房水回流,眼内压,。,(3),调节麻痹,（,paralysis accommodation,）,Atropine,(,-,),睫状肌,M-R,睫状肌松驰,悬韧带拉紧,晶状体扁平,视远物清楚,，近物模糊。,12,summary,Muscarinic agonist,Pilocarpine,Muscarinic antagonist,Atropine,Mi,o,sis,缩瞳,intraocular pressure,眼内压,Spasm of,accommodation,调节痉挛,lacrimal secretion,泪腺分泌,Mydriasis,扩瞳,intraocular pressure,眼内压,pa,r,alysis of,accommodation,调节麻痹,lacrimal secretion,泪腺分泌,13,3.,平滑肌,（,smooth muscle,）,松弛内脏平滑肌,Relaxes visceral smooth muscle.,Characteristics,(,特点,),(1),作用强度与平滑肌的功能状态有关；,(2),作用强度顺序,：,胃肠道,膀胱,输尿管,胆管、支气管,、,子宫。,14,4,.,心脏,（,Heart,）,(1),心率,（,heart rate,HR,）,治疗量（,therapeutic dose,）：,HR,大剂量,（,higher,dose,）,：,HR,解除了迷走神经对心脏的抑制。,(2),房室传导,:,促进房室传导,(,Block vagal effects on the sinoatrial node directly.,),15,5.,血管与血压,(,Vessels,blood pressure,),Therapeutic dose,-,无明显作用,原因：多数血管缺乏胆碱能神经支配,Large dose-,-,扩张血管,6.CNS,兴奋,抑制,-atropine blush,（,脸红,）,The mechanism is unknown.,There is little effect on blood pressure.,Excitation followed by depression.,16,【,Clinical Uses,】,1.,缓解内脏绞痛（,releves visceral colic pain,）,解痉药,胃肠绞痛,(,gastric and intestinal colic pain,),膀胱刺激症状,(,bladder irritating symptoms,),胆绞痛,(,gallbladder colic pain,),肾绞痛,(,renal colic pain,),合用哌替啶,17,2,.,抑制腺体分泌,Inhibition of the secretion of the glands,(1),麻醉前给药,（,premedication,）,(2),盗汗,（,severe night sweat,）,(3),流涎,(,salivation,),3.,眼科,(,ophthalmologic disorders,),(1),虹膜睫状体炎,(,Iridocyclitis,),(3),验光配镜,(2),扩瞳，检查眼底,18,4.,缓慢型心律失常,(1),心动过缓,(,Bradycardia,),(2),迷,走,N,过度兴奋所致传导阻滞,Note:,at too large dose,：,HR,oxygen consumption(,耗氧量,),the risk of ventricular fibrillation,（,心室纤颤,）,19,5.,抗休克,（,Anti-shock,）,暴发型流脑、中毒性菌痢、中毒性肺炎,感染性休克,(,infectious shock,),解除小血管痉挛，改善微循环。,In large dose,atropine can abolish the vessel spasm and improve microcirculation.,6.,有机磷酸酯中毒,Organophosphate intoxication,20,【,Adverse reaction,】(,不良反应,),口干,、,皮肤干燥、体温；,心动过速,眼内压、视力模糊；,便秘,、,排尿困难；,腺,眼,平,心,【,Contraindication,】,禁忌症,CNS,青光眼,(,Glaucoma,),，,前列腺肥大。,Summary,Atropine,腺,眼,平,心血管,CNS,作用,(,-,),分泌,用途,麻醉前给药,盗汗,流涎,不良反应,口干,体温,禁忌症,发热,扩瞳,眼内压,调节麻痹,虹膜炎,检查眼底验光,眼内压,视力模糊,青光眼,松弛,内脏绞痛,便秘,尿潴留,前列腺肥大,HR,血管扩张,心动过缓传导阻滞,心动过速,心动过速,先兴奋后抑制,有机磷中毒,感染性休克,22,山莨菪碱,(,anisodamine,654-2),1.,解痉、扩血管作用强；,2.,抑制腺体分泌、扩瞳作用弱,；,3.,主要用于感染性休克、内脏平滑肌绞痛；,4.,不良反应、禁忌症同,atropine,。,23,东莨菪碱,（,scopolamine,）,1.,外周抗胆碱作用,腺,(,gland,),atropine,心血管系统,atropine,眼,(,eye,),【,Pharmacological actions,】,（,药理作用,）,24,1.,麻醉前给药,（,premedication,）,2.,晕动病,(,motion sickness,),3.,帕金森氏病,（,Parkinsons disease,）,【,Clinical Uses,】,（,临床用途,）,25,2,阿托品的合成代用品,合成扩瞳药,(,synthetic mydriatics,),后马托品 托吡卡胺,合成解痉药,(,synthetic spasmolytics,),溴丙胺太林（普鲁本辛）,选择性,M,1,受体阻断剂,哌仑西平,pirenzepine,26,Chapter 9,胆碱受体阻断剂,（,II,）,N-R,阻断剂,Cholinoceptor blocking drugs,N-R blocking drugs,27,1,神经节阻滞药,(,ganglion,ic,blockers,),(,-,)N,N,-,R (,-,)postganglial fibres of sympathetic and parasympathetic nerves,美加明,樟磺咪芬,【,Mechanism,】(,机理,),【,Clinical Uses,】(,临床用途,),控制性降压,(,controlled hypotension,),28,除极化型肌松药,Depolarizing muscular relaxants,【,Classification,】(,分类,),2,骨骼肌松驰药,(,肌松药,),Skeletal muscular relaxants,非除极化型肌松药,Non-depolarizing muscular relaxants,琥珀胆碱,筒箭毒碱,29,一,、,去极化型肌松药（非竞争性肌松药）,琥珀胆碱,succinylcholine,【,Mechanism,】,作用机理,Depolarizing muscular relaxants,司可林,scoline,琥珀胆碱,（）,N,M,-R,后膜持久去极化,肌松,N-M,接头处的兴奋传递过程,轴突末稍,AP,Ca,2,内流,释放,ACh,终板电位（,EPP,）,肌细胞膜爆发,AP,31,1.,作用快、强、短；,2.,肌松前有短时肌震颤；,3.,过量中毒时不可用新斯的明解救,:,(1),无效,;(2),加重中毒,;,4.,青光眼、高钾血症禁用。,【,Characteristics,】,特点,【,Clinical Uses,】(,临床用途,),1.,气管内插管、气管镜、食管镜检查；,2.,辅助麻醉。,32,筒箭毒碱,(,-,),N,M,-,R,竞争性对抗,ACh,的作用,肌松,二,、,非除化型肌松药（竞争性肌松药）,筒箭毒碱,d-tubocurarine,Non-depolarizing muscular relaxants,【,Mechanism,】,作用机理,33,【,Characteristics,】,特点,1.,作用时间长，连用蓄积；,2,.,过量可用新斯的明解救；,3.,阻断,N,节，释放组胺；,4,.,禁用于重症肌无力、支气管哮喘、严重休克。,阿曲库铵 泮库溴铵,P 75,表,9-2,34,拟胆碱药,M-R,激动药,抗,ChE,药,抗胆碱药,M-R,阻断药,N-R,阻断药,pilocarpine,neostigmine,atropine,筒箭毒碱 阿曲库铵,