胆碱受体阻断药课件

Chapter8

Cholinoceptorblockingdrugs胆碱受体阻断药Cholinoceptorblockingdrugs：

Anticholinergicdrugs(抗胆碱药)cancombinewithcholinergicreceptorsandinhibitAchorcholinergicdrugstocombinewiththereceptors.

TheyaredividedintoM-cholinoceptorblockingdrugsandN-cholinoceptorblockingdrugs.

§1M-cholinoceptorblockingdrugs：

Atropineandatropinelikebiologicalalkaloid(阿托品和阿托品类生物碱)Atropine阿托品(存在于颠茄、曼陀罗、莨菪中)颠茄曼陀罗belladonnagland>eye

>smoothmuscle

>heart>CNS

sweatgland汗腺、salivarygland唾液腺>lachrymal泪腺、bronchialgland呼吸道腺体>gastricparietalcells

胃壁细胞PharmacologicalEffects一、glands↓：

decreasethesecretion二、eye1)mydriasis

扩瞳

atropine→（－）瞳孔括约肌M-R→开大肌功能占优势→瞳孔扩大atropine→（－）瞳孔括约肌M-R→扩瞳→虹膜退向外缘→前房角间隙变小→房水回流↓→眼内压2)increaseintraocularpressure

升高眼压3）paralysisofaccommodation调节麻痹Atropine：睫状肌M-R↓→睫状肌松驰→悬韧带拉紧→晶状体扁平→屈光度→视远物清、近物模糊1、HR：

1)therapeuticdoseHR

（－）突触前膜M1-R→负反馈→Ach释放↑特点：a.短时、轻度(每分钟减少4-8次)

b.部分病人出现

四、Cardiovascularsystem：（一）Heart2、A(atria)-V(ventricle)conduction（房室传导）：

atropine→(一)M-R→conduction↑2)largerdoseHR↑

（－）窦房结起搏点M2-R→解除了迷走神经对心脏的抑制，强度与迷走神经张力水平有关。因此年青人心率变化明显。0.5-1.0mg----

increasethefrequencyofrespiration1.0-5.0mg---stimulatecerebrum(大脑)---restlessness(焦躁不安)

>10mg---hallucination(幻觉),delirium(精神错乱)andconvulsion(惊厥)五、CNSexcitationdepression1、Relaxationofsmoothmusclespasm:Atropineisusedtotreatvisceralcolicpain

(内脏绞痛)【ClinicalUses】胃肠绞痛>膀胱刺激症状>胆、肾绞痛也可用于遗尿症，因Atropine可松弛膀胱逼尿肌治疗时要与哌替啶合用1)Iridocyclitis(虹膜睫状体炎)：虹膜括约肌和睫状肌休息充分，有助于炎症消退与缩瞳药合用：防止粘连2)

Opticalexamination

验光配镜：准确测定屈光度特点：调节麻痹作用持久(2-3天)成人少用小儿验光用：睫状肌调节功能强

3、eye：Bradycardia(心动过缓)，S-Ablockade，A-Vblockadebyhyperfunction(机能亢进)ofvagalnerves（迷走神经）4、CardiovasculardisorderAttention:toolargedose：inducetheincreaseofHRandoxygenconsumptionandincreasetheriskofventricular(心室）

fibrillation（纤维颤动）.5.Antishock:infectiousshock

暴发型流行性脑脊髓膜炎、中毒性菌痢、中毒性肺炎

Largedoseofatropine-----abolishthevesselspasm,dilateperipheralvessel,improvemicrocirculation(微循环)Attention:

Atropineisnotusedtotheshockpatientaccompanywithfeverandtachycardia(心动过速).AsearlyaspossibleAtropinization（阿托品化）RepeatedlyCombinationwithreactivators

6.Organophosphateintoxicationanisodamine(山莨菪碱，654-2)1.similareffectstothatofatropine,buttheintensityisonly1/20-1/10tothatofatropine2.can’tpasstheBBB,noeffectsonCNS3.relievethespasmofthesmoothmuscle,especiallytoGItracts4.clinicalUses:colicpain绞痛

(gastrointestinal)andinfectioustoxicshock感染中毒性休克scopolamine（东莨菪碱）Peripheral(外周)effectissimilartoatropinegland,eye>atropinecardiovascularsystem<atropine2.depressCNSlowdosage:sedation镇静

largedosage:hypnotic催眠3.ClinicalUses1)preanesthesia2)motionsickness(晕动病)3)Parkinsonismsubstitutiveatropine

阿托品的合成代用品合成扩瞳药

homatropine后马托品、

tropicamide托吡卡胺合成解痉药

propanthelinebromide

溴丙胺太林（普鲁本辛）选择性M受体亚型阻断剂

pirenzepine哌仑西平(M1-R)ganglionblockade

神经节阻滞药(-)N1-R→(-)postganglialfibresofsympatheticandparasympatheticnervesMecamylamine美加明Trimethaphancamsylate樟磺咪芬mechanismclinicalusage控制性降压:麻醉时控制性降压，以减少手术区出血。adverseeffect

多、严重

skeletalmuscularrelaxants

骨骼肌松驰药(肌松药)Depolarizingmuscularrelaxants

除极化型肌松药Nondepolarizingmuscularrelaxants

非除极化型肌松药classification4.对喉肌松弛作用强，用于气管镜、食道镜操作。5.青光眼、高钾血症禁用。肌肉持久去极化，K+释放增加眼外骨骼肌收缩，升高眼内压mechanismd-tubocurarine→(-)N2-R竞争性对抗ACh的作用肌松二、nondepolarizingmuscularrelaxants

非除化型肌松药（竞争性肌松药）

d-tubocurarine筒箭毒碱1、pocannotbeabsorbedivtheeffectisquick,strong,short2、Relaxationorder:head,neck→shoulder,limbs→intercos