N受体阻滞剂-山东大学药理学英文课件

Chapter7Cholinoceptor-BlockingDrugs(Ⅱ)-N-Cholinoceptorblockers

ZhangbinInstituteofPharmacologySchoolofMedicineShandongUniversityNicotiniccholinoceptor-blockingdrugsNN-Rantagonists(ganglionicblockingdrugs)NM-Rantagonists(neuromuscularblockingdrugs)(Skeletalmusclerelaxants)Section1NN-Rantagonists

(ganglionicblockingdrugs)Mecamylamine(美卡拉明，美加明)Trimethaphan〔樟磺咪酚，曲美芬〕NN-Rantagonists[Characteristics]Co-innervationanddominanttheoryBloodvessel:vasodilation,peripheralresistancedecrease,bloodpressuredecrease.Glands,eye,GI,bladder:drymouth,mydriasis,constipation,urinaryretention[Clinicaluse]

HBPSection2NM-Rantagonists

〔Skeletalmusclerelaxants〕(neuromuscularblockingdrugs)Depolarizingskeletalmusclerelaxants——

succinylcholineNondepolarizingskeletalmusclerelaxants

——

D-tubocurarineDepolarizingskeletalmusclerelaxantsMechanism:Two-phaseblock

Phase1:durabledepolarizingblock

Phase2:NMreceptordesensitizationDepolarizingskeletalmusclerelaxants[CharacteristicsofAction]〔1〕Musclefasciculation(肌束震颤)〔2〕Tachyphylaxis(快速耐受性)〔3〕Can’tbeantagonizedbyAChEI〔4〕havenoganglionicblockingactionsattherapeuticdose(5)rapidonsetandshortdurationsuccinylcholine(琥珀胆碱,scoline,司可林)(1)Onsetrapid(1’),Emax2’,shortduration(5’)(2)Neckandlimbs(3)pseudocholinesterase[Uses]1.assistantagentsofanesthetics2.bronchialcannulation，bronchoscopyoesophagoscop(食道镜)Adversereactions(1)

asphyxy(窒息):respiratorymuscleparalysis:geneticpseudo-ChElowpatientsanti-AChEagentslocalanestheticsandaminoglycosides(2)Musclefasciculation(3)ElevationofextracellularK+(4)CVS:complex(5)Malignanthyperpyrexia(恶性高热):idiosyncrasy〔特异质反响)(6)increasehistaminereleaseMalignanthyperpyrexia在并用琥珀胆碱和强挥发性全麻药〔氟烷、异氟烷〕时引起的高代谢反响，体温极度升高。是一种常染色体显性遗传。(钙释放通道基因变异，骨骼肌对钙呈高反响性，引起剧烈的肌肉收缩、代谢提高)丹曲林钠(肌松剂):其主要作用部位是骨骼肌的肌浆网，通过抑制肌浆网释放钙离子而减弱肌肉收缩。Nondepolarizingmuscularrelaxants

(competitiveneuromuscularblockers)Mechanisms:NM-R

competitiveantagonistCharacteristicsofAction

(1)nofasciculation(2)AntagonizedbyAChEI(3)slowonsetandlongduration(4)NNblockadeattherapeuticdosed-tubocurarine(筒箭毒碱)[[Actions]

musclerelaxantblockganglionic

releasehistamine[Uses]assistantagentsofanestheticsOtherdrugsbenzylisoquinolines(苄基异喹啉类)Atracurium〔阿曲库铵〕Doxacurium〔多