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1、Guangdong University of TechnologyGuangdong University of Technology轻工化工学院Chapter 8 Cholinoceptor blocking drugs胆碱受体阻断药胆碱受体阻断药Guangdong University of TechnologyGuangdong University of Technology轻工化工学院Cholinoceptor blocking drugs：Anticholinergic drugs(抗胆碱药)can combine with cholinergic receptors and i
2、nhibit Ach or cholinergic drugs to combine with the receptors.They are divided into M-cholinoceptor blocking drugs and N-cholinoceptor blocking drugs.Guangdong University of TechnologyGuangdong University of Technology轻工化工学院 1 M-cholinoceptor blocking drugs：Atropine and atropine like biological alka
3、loid(阿托品和阿托品类生物碱阿托品和阿托品类生物碱)Atropine 阿托品阿托品(存在于颠茄存在于颠茄、曼陀罗、莨菪中、曼陀罗、莨菪中)颠颠茄茄曼曼陀陀罗罗belladonnaGuangdong University of TechnologyGuangdong University of Technology轻工化工学院 1、（）、（）M-R（阻断（阻断M-受体）受体）2、large dose,toxic dose:（）（）N1-R,（）（）CNS 选择性：选择性：（）（）M-R（）（）N1-Rmechanism of actionGuangdong University of Tec
4、hnologyGuangdong University of Technology轻工化工学院 gland eye smooth muscle heart CNS sweat gland汗腺、汗腺、salivary gland唾液腺唾液腺 lachrymal泪腺、泪腺、bronchial gland 呼吸道腺体呼吸道腺体 gastric parietal cells胃壁细胞胃壁细胞Pharmacological Effects一、一、glands：decrease the secretionGuangdong University of TechnologyGuangdong Universi
5、ty of Technology轻工化工学院二、二、eye 1)mydriasis 扩瞳扩瞳 atropine（）（）瞳孔括约肌瞳孔括约肌M-R 开大肌功能占开大肌功能占 优势优势瞳孔扩大瞳孔扩大Guangdong University of TechnologyGuangdong University of Technology轻工化工学院atropine（）瞳（）瞳孔括约肌孔括约肌M-R扩瞳扩瞳虹膜退向外缘虹膜退向外缘前前房角间隙变小房角间隙变小 房水房水回流回流 眼内压眼内压 2)increase intraocular pressure升高眼压升高眼压Guangdong Univers
6、ity of TechnologyGuangdong University of Technology轻工化工学院3）paralysis of accommodation 调节麻痹调节麻痹Atropine：睫状肌睫状肌M-R睫状肌松驰睫状肌松驰 悬韧悬韧带拉紧带拉紧晶状体扁平晶状体扁平屈光度屈光度 视远物清、视远物清、近物模糊近物模糊Guangdong University of TechnologyGuangdong University of Technology轻工化工学院characteristics1)作用强度与作用强度与SM紧张度成正比紧张度成正比 对痉挛的对痉挛的SM作用最强作用
7、最强2)selectivity to smooth muscle：gastrointestinal tract urinary bladder膀胱、膀胱、尿尿道道 Biliary tract 胆管、胆管、ureter 输尿管、输尿管、bronchia支气管、支气管、uterus子宫子宫三、三、smooth muscle：relaxation Guangdong University of TechnologyGuangdong University of Technology轻工化工学院 1、HR：1)therapeutic dose HR （）突触前膜（）突触前膜M1-R 负反馈负反馈 Ac
8、h释放释放 特点：特点：a.短时、轻度短时、轻度(每分钟减少每分钟减少4-8次次)b.部分病人出现部分病人出现 四、四、Cardiovascular system：（一）（一）HeartGuangdong University of TechnologyGuangdong University of Technology轻工化工学院2、A(atria)-V(ventricle)conduction（房室传导）：（房室传导）：atropine (一一)M-R conduction2)larger dose HR（）窦房结起搏点（）窦房结起搏点M2-R 解除了迷走神经对心脏解除了迷走神经对心脏的抑
9、制，强度与迷走神经张力水平有关。的抑制，强度与迷走神经张力水平有关。因此年青人心率变化明显。因此年青人心率变化明显。Guangdong University of TechnologyGuangdong University of Technology轻工化工学院 Therapeutic dose-no significant effect 原因：多数血管缺乏胆碱能神经支配原因：多数血管缺乏胆碱能神经支配 （二）（二）Vessel and blood pressure 血管和血压血管和血压Larger dose-dilate cutaneous vessel(皮肤血管扩张皮肤血管扩张)，war
10、m and flush(热，潮红热，潮红)机理：不明机理：不明，与（），与（）M-R无关无关 possible reason：1)atropine secretion of sweat gland T 代偿性散热反应代偿性散热反应 2)atropine dilate the blood vessel directlyGuangdong University of TechnologyGuangdong University of Technology轻工化工学院 0.5-1.0mg-increase the frequency of respiration 1.0-5.0mg-stimulat
11、e cerebrum(大脑大脑)-restlessness(焦躁不安焦躁不安)10mg-hallucination(幻觉幻觉),delirium(精神错乱精神错乱)and convulsion(惊厥惊厥)五、五、CNS excitation depressionGuangdong University of TechnologyGuangdong University of Technology轻工化工学院1、Relaxation of smooth muscle spasm:Atropine is used to treat visceral colic pain(内脏内脏绞痛绞痛)【Cli
12、nical Uses】胃肠绞痛胃肠绞痛膀胱刺激症状膀胱刺激症状胆、肾绞痛胆、肾绞痛也可用于遗尿症，因也可用于遗尿症，因Atropine可松弛膀胱逼尿肌可松弛膀胱逼尿肌治疗时要与哌治疗时要与哌替啶合用替啶合用Guangdong University of TechnologyGuangdong University of Technology轻工化工学院1)Iridocyclitis(虹膜睫状体炎虹膜睫状体炎)：虹膜括约肌和睫状肌休息虹膜括约肌和睫状肌休息 充分，有助于炎症消退充分，有助于炎症消退 与缩瞳药合用：防止粘连与缩瞳药合用：防止粘连2)Optical examination 验光配镜：
13、准确测定屈光度验光配镜：准确测定屈光度 特点：调节麻痹作用持久特点：调节麻痹作用持久(2-3天天)成人少用成人少用 小儿验光用：睫状肌调节功能强小儿验光用：睫状肌调节功能强 3、eye：Guangdong University of TechnologyGuangdong University of Technology轻工化工学院2、Inhibition of the secretion of the glands 制止腺体分泌：制止腺体分泌：1)preanesthetic medication全麻前给药全麻前给药：decrease the respiratory and salivator
14、y(唾液唾液)gland secretionprevent the side effect of general anesthetics(防止分泌物阻塞呼吸道及吸入性肺炎防止分泌物阻塞呼吸道及吸入性肺炎)2)severe night sweat and salivation(严重盗汗和流涎严重盗汗和流涎)Guangdong University of TechnologyGuangdong University of Technology轻工化工学院Bradycardia(心动过缓心动过缓)，S-A blockade，A-V blockade by hyperfunction(机能亢进机能亢进
15、)of vagal nerves（迷走神经）（迷走神经）4、Cardiovascular disorderAttention:too large dose：induce the increase of HR and oxygen consumption and increase the risk of ventricular(心室）心室）fibrillation（纤维颤动）（纤维颤动）.Guangdong University of TechnologyGuangdong University of Technology轻工化工学院 5.Antishock:infectious shock 暴
16、发型流行性脑脊髓膜炎、中毒性菌痢、中毒性肺炎暴发型流行性脑脊髓膜炎、中毒性菌痢、中毒性肺炎 Large dose of atropine-abolish the vessel spasm,dilate peripheral vessel,improve microcirculation(微循环微循环)Attention:Atropine is not used to the shock patient accompany with fever and tachycardia(心动过速心动过速).Guangdong University of TechnologyGuangdong Univer
17、sity of Technology轻工化工学院As early as possibleAtropinization（阿托品化）（阿托品化）RepeatedlyCombination with reactivators6.Organophosphate intoxicationGuangdong University of TechnologyGuangdong University of Technology轻工化工学院Side effect（0.4-0.6mg）：dry mouth、blurred vision视力模糊视力模糊、tachycardia、mydriasis、dryness o
18、f skin and flush，difficulty in urination,constipation(便秘便秘).adverse action Toxic effects：action of cardiovascular system,（）（）CNScontraindication:Glaucoma，prostatauxe (前列腺肥大前列腺肥大)Guangdong University of TechnologyGuangdong University of Technology轻工化工学院anisodamine (山莨菪碱山莨菪碱，654-2)1.similar effects to
19、 that of atropine,but the intensity is only 1/20-1/10 to that of atropine 2.cant pass the BBB,no effects on CNS3.relieve the spasm of the smooth muscle,especially to GI tracts4.clinical Uses:colic pain绞痛绞痛(gastrointestinal)and infectious toxic shock 感染中毒性休克感染中毒性休克Guangdong University of TechnologyGu
20、angdong University of Technology轻工化工学院scopolamine（东莨菪碱）（东莨菪碱）1.Peripheral(外周外周)effect is similar to atropine gland,eyeatropine cardiovascular systematropine2.depress CNS low dosage:sedation 镇静镇静 large dosage:hypnotic 催眠催眠3.Clinical Uses 1)preanesthesia 2)motion sickness(晕动病晕动病)3)ParkinsonismGuangdon
21、g University of TechnologyGuangdong University of Technology轻工化工学院substitutive atropine阿托品的合成代用品阿托品的合成代用品合成扩瞳药合成扩瞳药 homatropine 后马托品、后马托品、tropicamide 托吡卡胺托吡卡胺合成解痉药合成解痉药 propantheline bromide 溴丙胺太林（普鲁本辛）溴丙胺太林（普鲁本辛）选择性选择性M受体亚型阻断剂受体亚型阻断剂 pirenzepine 哌仑西平哌仑西平 (M1-R)Guangdong University of TechnologyGuan
22、gdong University of Technology轻工化工学院2 Cholinoceptor blocking drugs N-R blocking drugs Guangdong University of TechnologyGuangdong University of Technology轻工化工学院ganglion blockade 神经节阻滞药神经节阻滞药(-)N1-R (-)postganglial fibres of sympathetic and parasympathetic nervesMecamylamine 美加明美加明Trimethaphan camsyl
23、ate 樟磺咪芬樟磺咪芬mechanismclinical usage控制性降压控制性降压:麻醉时控制性降压，以减少手术区出血。麻醉时控制性降压，以减少手术区出血。adverse effect 多、严重多、严重 Guangdong University of TechnologyGuangdong University of Technology轻工化工学院skeletal muscular relaxants 骨骼肌松驰药骨骼肌松驰药(肌松药肌松药)Depolarizing muscular relaxants 除极化型肌松药除极化型肌松药Nondepolarizing muscular r
24、elaxants 非除极化型肌松药非除极化型肌松药classificationGuangdong University of TechnologyGuangdong University of Technology轻工化工学院 一、一、Depolarizing muscular relaxants 除极化型肌松药（非竞争性肌松药）除极化型肌松药（非竞争性肌松药）suxamethonium 琥珀胆碱琥珀胆碱,又名又名scoline司可林司可林mechanismsuxamethonium （）（）N2-R 后膜持久后膜持久去极化去极化 N2-R 不能对不能对ACh起反应起反应 肌松肌松Guangd
25、ong University of TechnologyGuangdong University of Technology轻工化工学院Characteristics2、骨骼肌先收缩后放松、骨骼肌先收缩后放松 Relaxation order:neck（颈颈）shoulderabedomenlimbs3、it is hydrolyzed by pseudocholinesterase（假胆碱酯酶假胆碱酯酶）in the blood a)过量中毒时不可用新斯的明解救过量中毒时不可用新斯的明解救(人工呼吸机人工呼吸机)b)遗传性遗传性ChE缺陷，有机磷中毒不可使用该药缺陷，有机磷中毒不可使用该药1
26、、iv，the effect is quick,strong and short Guangdong University of TechnologyGuangdong University of Technology轻工化工学院4.对喉肌松弛作用强，对喉肌松弛作用强，用于气管镜、食道镜操作。用于气管镜、食道镜操作。5.青光眼、高钾血症禁用。青光眼、高钾血症禁用。肌肉持久去极化，肌肉持久去极化，K+释放增加释放增加眼外骨骼肌收缩，眼外骨骼肌收缩，升高眼内压升高眼内压Guangdong University of TechnologyGuangdong University of Technol
27、ogy轻工化工学院mechanism d-tubocurarine (-)N2-R 竞争性对抗竞争性对抗ACh的作用的作用 肌松肌松二、二、nondepolarizing muscular relaxants 非除化型肌松药（竞争性肌松药）非除化型肌松药（竞争性肌松药）d-tubocurarine筒箭毒碱筒箭毒碱Guangdong University of TechnologyGuangdong University of Technology轻工化工学院1、po cannot be absorbed iv the effect is quick,strong,short2、Relaxati
28、on order:head,neck shoulder,limbs intercostal muscle (肋间肌肋间肌)diaphragm(膈肌膈肌)出现呼吸肌麻痹，出现呼吸肌麻痹，人工呼吸人工呼吸+新斯的明新斯的明3、禁用于重症肌无力、支气管哮喘、严重休克。、禁用于重症肌无力、支气管哮喘、严重休克。儿童不宜使用儿童不宜使用(发生高敏反应较多发生高敏反应较多)。Characteristics促进组胺释放促进组胺释放Guangdong University of TechnologyGuangdong University of Technology轻工化工学院 思考：思考：阿托品解救有机磷酸酯类中毒时，阿托品过量阿托品解救有机磷酸酯类中毒时，阿托品过量引起阿托品中毒，能否用新斯的明、毒扁豆碱、引起阿托品中毒，能否用新斯的明、毒扁豆碱、毛果芸香碱解救？毛果芸香碱解救？琥珀胆碱、筒箭毒碱过量引起的中毒能否使用琥珀胆碱、筒箭毒碱过量引起的中毒能否使用新斯的明新斯的明进行解救，行解救，为什么？什么？