膽堿受體阻斷藥課件

膽堿受體阻斷藥CholinoceptorBlockingDrugs成都大學(xué)醫(yī)護(hù)學(xué)院藥理教研室王躍锜原創(chuàng)膽堿受體阻斷藥CholinoceptorBlocking1

MuscarinicCholinoceptorBlockingDrugs

毒蕈堿型受體阻斷藥，M受體阻斷藥2NicotinicCholinoceptorBlockingDrugs

煙堿型受體阻斷藥，N受體阻斷藥IntroductiontoCholinoceptorBlockingDrugs

膽堿受體阻斷藥1MuscarinicCholinoceptorBloMuscarinicCholinoceptorBlockingDrugs毒蕈堿型受體阻斷藥，M受體阻斷藥ReceptorTypeOtherNamesLocation部位M1

Nerves神經(jīng)M2

CardiacM2

Heart,nerves,smoothmuscle心臟，神經(jīng)，平滑肌M3

Glands,smoothmuscle,endothelium腺體，平滑肌，內(nèi)皮細(xì)胞M4

CNS中樞神經(jīng)系統(tǒng)M5

CNSNM

Muscletype,endplatereceptor肌肉型，終板受體Skeletalmuscleneuromuscularjunction骨骼肌神經(jīng)肌肉接頭NN

Neuronaltype,ganglionreceptor神經(jīng)元型，神經(jīng)節(jié)受體postganglioniccellbody,dendrites突觸后細(xì)胞，樹突MuscarinicCholinoceptorBlockAtropine阿托品tertiaryaminealkaloidestersoftropicacid莨菪酸的叔胺生物堿酯Propantheline丙胺太林,普魯本辛Quaternaryamineantimuscarinicagents季胺類化合物Atropine阿托品tertiaryaminealkMosttertiaryantimuscarinicdrugs（叔胺類抗膽堿藥）

arewellabsorbedfromthegut（消化道）

andconjunctivalmembranes（結(jié)膜）.Incontrast,only10–30%ofadoseofaquaternaryantimuscarinicdrug（季胺類抗膽堿藥）

isabsorbedafteroraladministration（口服）,reflectingthedecreasedlipidsolubilityofthechargedmolecule（帶電荷的分子）.Absorption吸收

MosttertiaryantimuscarinicdDistribution分布

Atropineandtheothertertiaryagents(叔胺類抗膽堿藥)arewidelydistributedinthebody.SignificantlevelsareachievedintheCNS(中樞神經(jīng)系統(tǒng))within30minutesto1hour,andthiscanlimitthedosetoleratedwhenthedrugistakenforitsperipheraleffects.Scopolamine（東莨菪堿）israpidlyandfullydistributedintotheCNSwhereithasgreatereffectsthanmostotherantimuscarinicdrugs.Incontrast,thequaternaryderivatives（季胺類抗膽堿藥）arepoorlytakenupbythebrainandthereforearerelativelyfree—atlowdoses—ofCNSeffects.Distribution分布AtropineandAfteradministration,theelimination消除ofatropinefromthebloodoccursinapproximately15hours.About50%ofthedoseisexcretedunchangedintheurine尿.Mostoftherestappearsintheurineashydrolysis水解andconjugationproducts結(jié)合物.Thedrug‘seffectonparasympathetic副交感functiondeclinesrapidlyinallorgansexcepttheeye.Effectsontheiris瞳孔andciliarymuscle睫狀肌persistformorethan72hours.MetabolismandExcretion代謝與消除Afteradministration,theelimAtropinecausesreversible(surmountable可逆的)blockadeatmuscarinicreceptors;thatis,blockadebyasmalldoseofatropinecanbeovercomebyalargerconcentrationofacetylcholine乙酰膽堿

orequivalentmuscarinicagonistM受體阻斷藥.Tissues組織mostsensitivetoatropinearethesalivary唾液腺,bronchial支氣管,andsweatglands汗腺.Secretionofacidbythegastricparietalcells胃壁細(xì)胞

istheleastsensitive.Pharmacodynamics藥效作用Atropinecausesreversible(suAtropineishighlyselective選擇性formuscarinicreceptorsM型受體.Itspotency效力atnicotinicreceptorsN型受體ismuchlower.Atropinedoesnotdistinguish區(qū)分

amongtheM1,M2,andM3subgroups亞型

ofmuscarinicreceptors.Incontrast,otherantimuscarinicdrugsaremoderatelyselectiveforoneoranotherofthesesubgroups.Atropineishighlyselective選CentralNervousSystem中樞神經(jīng)系統(tǒng)

Inthedosesusuallyused,atropine阿托品

hasminimalstimulanteffects興奮效應(yīng)

ontheCNS,andaslower,longer-lastingsedative鎮(zhèn)靜effectonthebrain.Scopolamine東莨菪堿hasmoremarkedcentraleffects,producingdrowsiness嗜睡whengiveninrecommendeddosagesandamnesia失憶insensitiveindividuals.Intoxicdoses中毒劑量,scopolamine,andtoalesserdegreeatropine,cancauseexcitement興奮,agitation

焦躁,hallucinations幻覺,andcoma昏迷.Pharmacodynamics:藥效

器官效應(yīng)OrganSystemEffectsCentralNervousSystem中樞神經(jīng)系統(tǒng)PEye眼前房角變窄睫狀肌松弛擴(kuò)瞳畏光，調(diào)節(jié)麻痹房水回流受阻淚腺分泌減少，眼干澀Eye眼前房角變窄淚腺分泌減少，眼干澀CardiovascularSystem心血管系統(tǒng)心率上升，房室傳導(dǎo)加快CardiovascularSystem心率上升，房室傳導(dǎo)RespiratorySystem呼吸系統(tǒng)支氣管分泌減少，支氣管擴(kuò)張RespiratorySystem呼吸系統(tǒng)支氣管分泌減GastrointestinalTract消化道Blockadeofmuscarinicreceptorshasdramaticeffectsonmotility運(yùn)動

andsomeofthesecretory分泌functionsofthegut腸道.AntimuscarinicdrugsM型抗膽堿藥

havemarkedeffectsonsalivarysecretion唾液分泌;

drymouthoccursfrequentlyinpatientstakingantimuscarinicdrugs.Gastricsecretion胃酸分泌isblockedlesseffectively.Gastrointestinalsmoothmusclemotility胃腸平滑肌運(yùn)動isaffectedfromthestomach胃tothecolon結(jié)腸.Ingeneral,thewallsoftheviscera內(nèi)臟

arerelaxed,andbothtone張力

andpropulsivemovements蠕動arediminished.Therefore,gastricemptyingtime胃排空時間

isprolonged,andintestinaltransittimeislengthened.GastrointestinalTract消化道GenitourinaryTract泌尿道Theantimuscarinicactionofatropineanditsanalogs同類藥

relaxessmoothmuscleoftheureters輸尿管

andbladderwall膀胱壁andslowsvoiding排尿.

SweatGlands汗腺體溫上升，皮膚血流增加散熱降低皮膚變干汗液減少GenitourinaryTractSweatGlanOphthalmologicDisorders

眼科Accuratemeasurementofrefractiveerror屈光不正

inuncooperativepatients,eg,youngchildren,requiresciliaryparalysis睫狀肌麻痹.Also,ophthalmoscopicexamination眼底鏡檢查oftheretina視網(wǎng)膜isgreatlyfacilitatedbymydriasis散瞳.Therefore,antimuscarinicagents,administeredtopicallyaseyedrops眼藥水orointment眼膏,areveryhelpfulindoingacompleteexamination.Foradultsandolderchildren,theshorter-actingdrugsarepreferred（如后馬托品，托吡卡胺）.Foryoungerchildren,thegreaterefficacyofatropineissometimesnecessary.Asecondophthalmologicuseistopreventsynechia(adhesion粘連)formationinuveitis葡萄膜炎andiritis虹膜炎.Clinicalapplications臨床應(yīng)用OphthalmologicDisorders眼科ClAntimuscarinicDrugsUsedinOphthalmology眼科使用的M型抗膽堿藥DrugDurationofEffect(days)作用持續(xù)時間UsualConcentration(%)常用濃度Atropine阿托品7–100.5–1Scopolamine東莨菪堿3–70.25Homatropine后馬托品1–32–5Tropicamide托吡卡胺0.250.5–1AntimuscarinicDrugsUsedinORespiratoryDisorders呼吸系統(tǒng)Theuseofatropine阿托品becamepartofroutinepreoperativemedication術(shù)前給藥whenanesthetics麻醉suchasether乙醚wereused,becausetheseirritant刺激性anestheticsmarkedlyincreasedairwaysecretions分泌andwereassociatedwithfrequentepisodesoflaryngospasm喉痙攣.Preanesthetic麻醉前injectionofatropine阿托品

orscopolamine東莨菪堿

couldpreventthesehazardouseffects.RespiratoryDisorders呼吸系統(tǒng)CardiovascularDisorders

心血管系統(tǒng)Markedreflexvagaldischarge迷走神經(jīng)反射性興奮

sometimesaccompaniesthepainofmyocardialinfarction心肌梗塞(eg,vasovagalattack血管迷走神經(jīng)性發(fā)作)andmayimpaircardiacoutput心輸出.Parenteral注射atropineorasimilarantimuscarinicdrugisappropriatetherapyinthissituation.Rareindividualswithoutotherdetectablecardiacdiseasehavehyperactivecarotidsinusreflexes頸動脈竇反射andmayexperiencefaintness眩暈

orevensyncope昏厥asaresultofvagaldischarge迷走興奮

inresponsetopressureontheneck,eg,fromatightcollar.Suchindividualsmaybenefitfromtheuseofatropineorarelatedantimuscarinicagent.CardiovascularDisorders心血管系GastrointestinalDisorders

消化道Antimuscarinicagentscanprovidesomereliefinthetreatmentofmildorself-limitedconditionsofhypermotility胃腸平滑肌過度興奮.UrinaryDisorders

泌尿系統(tǒng)Atropineandotherantimuscarinicdrugshavebeenusedtoprovidesymptomaticreliefinthetreatmentofurinaryurgency尿急causedbyminorinflammatorybladderdisorders膀胱炎.GastrointestinalDisorders消化CholinergicPoisoning

膽堿能中毒Severecholinergicexcessisamedicalemergency,especiallyinruralcommunitieswherecholinesteraseinhibitorinsecticides殺蟲劑arecommonlyusedandincultureswherewildmushrooms毒蘑菇arecommonlyeaten.Thepotentialuseofcholinesteraseinhibitorsaschemicalwarfare“nervegases“神經(jīng)毒氣

alsorequiresanawarenessofthemethodsfortreatingacutepoisoning.CholinergicPoisoning膽堿能中毒Overdoses過量ofatropineoritscongeners同類藥aregenerallytreatedsymptomatically對癥治療.Poisoncontrolexpertsdiscouragetheuseofphysostigmine毒扁豆堿oranothercholinesteraseinhibitor膽堿酯酶抑制藥toreversetheeffectsofatropineoverdosebecausesymptomaticmanagementismoreeffectiveandlessdangerous.Symptomatictreatmentmayrequiretemperaturecontrolwithcoolingblanketsandseizure癲癇controlwithdiazepam安定.Artificialrespiratorysupportisneededinrespiratorydepression.AntimuscarinicPoisoning抗膽堿藥中毒Overdoses過量ofatropineoritsContraindicationstotheuseofantimuscarinicdrugsarerelative相對禁忌,notabsolute.Obviousmuscarinicexcess,especiallythatcausedbycholinesteraseinhibitors膽堿酯酶抑制藥,canalwaysbetreatedwithatropine.Antimuscarinicdrugsarecontraindicatedinpatientswithglaucoma青光眼,especiallyangle-closureglaucoma急性閉角型青光眼.Inelderlymen,antimuscarinicdrugsshouldalwaysbeusedwithcautionandshouldbeavoidedinthosewithahistoryofprostatichyperplasia

前列腺肥大.Contraindications禁忌癥Contraindicationstotheuseo1Ganglionicblockingdrugs

神經(jīng)節(jié)阻斷藥2Skeletalmuscularrelaxants

骨骼肌松弛劑Nicotiniccholinoceptor

blockingdrugs煙堿型受體阻斷藥N受體阻斷藥1GanglionicblockingdrugsNicGanglionicblockingdrugs

神經(jīng)節(jié)阻斷藥GanglionPreganglionicfiberPostganglionicfiberGanglionicblockingdrugs

神經(jīng)節(jié)阻Mecamylamine美加明andtrimethaphan咪噻吩isoccasionallyusedinthetreatmentofhypertensiveemergencies高血壓危象anddissectingaorticaneurysm主動脈夾層動脈瘤;inproducinghypotension低血壓,whichcanbeofvalueinneurosurgery神經(jīng)手術(shù)toreducebleedingintheoperativefield.Clinicalapplications臨床應(yīng)用Mecamylamine美加明andtrimethaphaNeuromuscularblockingdrugsinterferewithtransmissionattheneuromuscularendplate終板.Thesecompoundsareusedprimarilyasadjuncts輔助用藥duringgeneralanesthesia全身麻醉tofacilitatetrachealintubation氣管插管andoptimizesurgicalconditionswhileensuringadequateventilation通氣.Skeletalmuscularrelaxants

骨骼肌松弛劑NeuromuscularblockingdrugsiMechanismofneuromuscularblocked作用機(jī)制Mechanismofneuromuscularblo1Nondepolarizingmuscularrelaxants(d-tubocurarine筒箭毒堿)

非除極化肌松藥2Depolarizingmuscularrelaxants(succinylcholine琥珀酰膽堿)

除極化肌松藥1Nondepolarizingmuscularrel筒箭毒堿Nondepolarizingmuscularrelaxants非除極化肌松藥筒箭毒堿Nondepolarizingmuscularr膽堿受體阻斷藥課件Duringanesthesia麻醉,administrationoftubocurarine筒箭毒堿initiallycausesmotorweakness,followedbytheskeletalmusclesbecomingflaccid松弛的andinexcitabletoelectricalstimulation.Ingeneral,largermuscles(eg,abdominal腹肌,trunk軀干,diaphragm)橫隔膜aremoreresistanttoneuromuscularblockadeandrecovermorerapidlythansmallermuscles(eg,facial面部,foot,hand).Thediaphragm膈肌

isusuallythelastmuscletobeparalyzed麻痹.Whenadministrationofmusclerelaxantsisdiscontinued,recoveryofmusclesusuallyoccursinreverseorder,withthediaphragmregainingfunctionfirst.Clinicalapplications臨床應(yīng)用Duringanesthesia麻醉,administr乙酰膽堿Depolarizingmuscularrelaxants

除極化肌松藥琥珀酰膽堿乙酰膽堿Depolarizingmuscularrela膽堿受體阻斷藥課件Followingtheadministrationofsuccinylcholine琥珀酰膽堿,transientmusclefasciculations肌束震顫

occuroverthechest胸部andabdomen腹部within30seconds.Asparalysis麻痹developsrapidly(<90seconds),thearm,neck,andlegmusclesareinitiallyrelaxedfollowedbytherespiratorymuscles呼吸肌.Asaresultofsuccinylcholine‘srapidhydrolysis水解bycholinesteraseintheplasma血漿(andliver),thedurationofneuromuscularblocktypicallylastslessthan10minutes.Clinicalapplications臨床應(yīng)用FollowingtheadministrationoTubocurarine筒箭毒堿Succinylcholine琥珀酰膽堿PhaseIPhaseIIEffectofneostigmine新斯的明的影響AntagonisticAugmented1

AntagonisticInitialexcitatoryeffectonskeletalmuscle骨骼肌初始的表現(xiàn)NoneFasciculations肌束震顫NoneTubocurarineSuccinylcholine琥A63-year-oldarchitect,complainsofurinarysymptomstohisfamilyphysician.Hehashypertensionandthelast8years,hehasbeenadequatelymanagedwithathiazidediuretic噻嗪類利尿藥andanangiotensin-convertingenzymeinhibitor.Duringthesameperiod,hedevelopedthesignsofbenignprostatichypertrophy,whicheventuallyrequiredprostatectomy前列腺切除torelievesymptoms.Henowcomplainsthathehasanincreasedurgetourinateaswellasurinaryfrequency,andthishasdisruptedthepatternofhisdailylife.Whattreatmentstepswouldyouinitiate?CaseStudyA63-year-oldarchitect,complA53-year-oldwomancomestoseeyouforaconsultation.SheisscheduledtotakeaCaribbeancruisein2weeksbutisconcernedaboutseasickness.Shehasbeenonboatsbeforeandisverysensitivetomotionsickness.Afriendmentionedtoherthatthereisapatchthatiseffectiveforthisproblem.Sheisingoodhealthandtakesnomedicationsregularly.Herexaminationisnormal.Youprescribeascopolaminetransdermalpatchforher.

·Whatisthemechanismofactionofscopolamine?

·Whatarethecommonsideeffectsofthismedication?

·Whataresomerelativecontraindicationstoitsuse?CaseStudyA53-year-oldwomancomestosMechanismofactionofscopolamine:Competitiveantagonistofmuscariniccholinoreceptorsinthevestibularsystemandthecentralnervoussystem(CNS).

Commonsideeffects:Mydriasis,drymouth,tachycardia,urinaryretention,confusion,drowsiness.

Relativecontraindications:Glaucoma,urinaryobstruction,heartdisease.

ANSWERSTOCASEMechanismofactionofscopola膽堿受體阻斷藥CholinoceptorBlockingDrugs成都大學(xué)醫(yī)護(hù)學(xué)院藥理教研室王躍锜原創(chuàng)膽堿受體阻斷藥CholinoceptorBlocking1

MuscarinicCholinoceptorBlockingDrugs

毒蕈堿型受體阻斷藥，M受體阻斷藥2NicotinicCholinoceptorBlockingDrugs

煙堿型受體阻斷藥，N受體阻斷藥IntroductiontoCholinoceptorBlockingDrugs

膽堿受體阻斷藥1MuscarinicCholinoceptorBloMuscarinicCholinoceptorBlockingDrugs毒蕈堿型受體阻斷藥，M受體阻斷藥ReceptorTypeOtherNamesLocation部位M1

Nerves神經(jīng)M2

CardiacM2

Heart,nerves,smoothmuscle心臟，神經(jīng)，平滑肌M3

Glands,smoothmuscle,endothelium腺體，平滑肌，內(nèi)皮細(xì)胞M4

CNS中樞神經(jīng)系統(tǒng)M5

CNSNM

Muscletype,endplatereceptor肌肉型，終板受體Skeletalmuscleneuromuscularjunction骨骼肌神經(jīng)肌肉接頭NN

Neuronaltype,ganglionreceptor神經(jīng)元型，神經(jīng)節(jié)受體postganglioniccellbody,dendrites突觸后細(xì)胞，樹突MuscarinicCholinoceptorBlockAtropine阿托品tertiaryaminealkaloidestersoftropicacid莨菪酸的叔胺生物堿酯Propantheline丙胺太林,普魯本辛Quaternaryamineantimuscarinicagents季胺類化合物Atropine阿托品tertiaryaminealkMosttertiaryantimuscarinicdrugs（叔胺類抗膽堿藥）

arewellabsorbedfromthegut（消化道）

andconjunctivalmembranes（結(jié)膜）.Incontrast,only10–30%ofadoseofaquaternaryantimuscarinicdrug（季胺類抗膽堿藥）

isabsorbedafteroraladministration（口服）,reflectingthedecreasedlipidsolubilityofthechargedmolecule（帶電荷的分子）.Absorption吸收

MosttertiaryantimuscarinicdDistribution分布

Atropineandtheothertertiaryagents(叔胺類抗膽堿藥)arewidelydistributedinthebody.SignificantlevelsareachievedintheCNS(中樞神經(jīng)系統(tǒng))within30minutesto1hour,andthiscanlimitthedosetoleratedwhenthedrugistakenforitsperipheraleffects.Scopolamine（東莨菪堿）israpidlyandfullydistributedintotheCNSwhereithasgreatereffectsthanmostotherantimuscarinicdrugs.Incontrast,thequaternaryderivatives（季胺類抗膽堿藥）arepoorlytakenupbythebrainandthereforearerelativelyfree—atlowdoses—ofCNSeffects.Distribution分布AtropineandAfteradministration,theelimination消除ofatropinefromthebloodoccursinapproximately15hours.About50%ofthedoseisexcretedunchangedintheurine尿.Mostoftherestappearsintheurineashydrolysis水解andconjugationproducts結(jié)合物.Thedrug‘seffectonparasympathetic副交感functiondeclinesrapidlyinallorgansexcepttheeye.Effectsontheiris瞳孔andciliarymuscle睫狀肌persistformorethan72hours.MetabolismandExcretion代謝與消除Afteradministration,theelimAtropinecausesreversible(surmountable可逆的)blockadeatmuscarinicreceptors;thatis,blockadebyasmalldoseofatropinecanbeovercomebyalargerconcentrationofacetylcholine乙酰膽堿

orequivalentmuscarinicagonistM受體阻斷藥.Tissues組織mostsensitivetoatropinearethesalivary唾液腺,bronchial支氣管,andsweatglands汗腺.Secretionofacidbythegastricparietalcells胃壁細(xì)胞

istheleastsensitive.Pharmacodynamics藥效作用Atropinecausesreversible(suAtropineishighlyselective選擇性formuscarinicreceptorsM型受體.Itspotency效力atnicotinicreceptorsN型受體ismuchlower.Atropinedoesnotdistinguish區(qū)分

amongtheM1,M2,andM3subgroups亞型

ofmuscarinicreceptors.Incontrast,otherantimuscarinicdrugsaremoderatelyselectiveforoneoranotherofthesesubgroups.Atropineishighlyselective選CentralNervousSystem中樞神經(jīng)系統(tǒng)

Inthedosesusuallyused,atropine阿托品

hasminimalstimulanteffects興奮效應(yīng)

ontheCNS,andaslower,longer-lastingsedative鎮(zhèn)靜effectonthebrain.Scopolamine東莨菪堿hasmoremarkedcentraleffects,producingdrowsiness嗜睡whengiveninrecommendeddosagesandamnesia失憶insensitiveindividuals.Intoxicdoses中毒劑量,scopolamine,andtoalesserdegreeatropine,cancauseexcitement興奮,agitation

焦躁,hallucinations幻覺,andcoma昏迷.Pharmacodynamics:藥效

器官效應(yīng)OrganSystemEffectsCentralNervousSystem中樞神經(jīng)系統(tǒng)PEye眼前房角變窄睫狀肌松弛擴(kuò)瞳畏光，調(diào)節(jié)麻痹房水回流受阻淚腺分泌減少，眼干澀Eye眼前房角變窄淚腺分泌減少，眼干澀CardiovascularSystem心血管系統(tǒng)心率上升，房室傳導(dǎo)加快CardiovascularSystem心率上升，房室傳導(dǎo)RespiratorySystem呼吸系統(tǒng)支氣管分泌減少，支氣管擴(kuò)張RespiratorySystem呼吸系統(tǒng)支氣管分泌減GastrointestinalTract消化道Blockadeofmuscarinicreceptorshasdramaticeffectsonmotility運(yùn)動

andsomeofthesecretory分泌functionsofthegut腸道.AntimuscarinicdrugsM型抗膽堿藥

havemarkedeffectsonsalivarysecretion唾液分泌;

drymouthoccursfrequentlyinpatientstakingantimuscarinicdrugs.Gastricsecretion胃酸分泌isblockedlesseffectively.Gastrointestinalsmoothmusclemotility胃腸平滑肌運(yùn)動isaffectedfromthestomach胃tothecolon結(jié)腸.Ingeneral,thewallsoftheviscera內(nèi)臟

arerelaxed,andbothtone張力

andpropulsivemovements蠕動arediminished.Therefore,gastricemptyingtime胃排空時間

isprolonged,andintestinaltransittimeislengthened.GastrointestinalTract消化道GenitourinaryTract泌尿道Theantimuscarinicactionofatropineanditsanalogs同類藥

relaxessmoothmuscleoftheureters輸尿管

andbladderwall膀胱壁andslowsvoiding排尿.

SweatGlands汗腺體溫上升，皮膚血流增加散熱降低皮膚變干汗液減少GenitourinaryTractSweatGlanOphthalmologicDisorders

眼科Accuratemeasurementofrefractiveerror屈光不正

inuncooperativepatients,eg,youngchildren,requiresciliaryparalysis睫狀肌麻痹.Also,ophthalmoscopicexamination眼底鏡檢查oftheretina視網(wǎng)膜isgreatlyfacilitatedbymydriasis散瞳.Therefore,antimuscarinicagents,administeredtopicallyaseyedrops眼藥水orointment眼膏,areveryhelpfulindoingacompleteexamination.Foradultsandolderchildren,theshorter-actingdrugsarepreferred（如后馬托品，托吡卡胺）.Foryoungerchildren,thegreaterefficacyofatropineissometimesnecessary.Asecondophthalmologicuseistopreventsynechia(adhesion粘連)formationinuveitis葡萄膜炎andiritis虹膜炎.Clinicalapplications臨床應(yīng)用OphthalmologicDisorders眼科ClAntimuscarinicDrugsUsedinOphthalmology眼科使用的M型抗膽堿藥DrugDurationofEffect(days)作用持續(xù)時間UsualConcentration(%)常用濃度Atropine阿托品7–100.5–1Scopolamine東莨菪堿3–70.25Homatropine后馬托品1–32–5Tropicamide托吡卡胺0.250.5–1AntimuscarinicDrugsUsedinORespiratoryDisorders呼吸系統(tǒng)Theuseofatropine阿托品becamepartofroutinepreoperativemedication術(shù)前給藥whenanesthetics麻醉suchasether乙醚wereused,becausetheseirritant刺激性anestheticsmarkedlyincreasedairwaysecretions分泌andwereassociatedwithfrequentepisodesoflaryngospasm喉痙攣.Preanesthetic麻醉前injectionofatropine阿托品

orscopolamine東莨菪堿

couldpreventthesehazardouseffects.RespiratoryDisorders呼吸系統(tǒng)CardiovascularDisorders

心血管系統(tǒng)Markedreflexvagaldischarge迷走神經(jīng)反射性興奮

sometimesaccompaniesthepainofmyocardialinfarction心肌梗塞(eg,vasovagalattack血管迷走神經(jīng)性發(fā)作)andmayimpaircardiacoutput心輸出.Parenteral注射atropineorasimilarantimuscarinicdrugisappropriatetherapyinthissituation.Rareindividualswithoutotherdetectablecardiacdiseasehavehyperactivecarotidsinusreflexes頸動脈竇反射andmayexperiencefaintness眩暈

orevensyncope昏厥asaresultofvagaldischarge迷走興奮

inresponsetopressureontheneck,eg,fromatightcollar.Suchindividualsmaybenefitfromtheuseofatropineorarelatedantimuscarinicagent.CardiovascularDisorders心血管系GastrointestinalDisorders

消化道Antimuscarinicagentscanprovidesomereliefinthetreatmentofmildorself-limitedconditionsofhypermotility胃腸平滑肌過度興奮.UrinaryDisorders

泌尿系統(tǒng)Atropineandotherantimuscarinicdrugshavebeenusedtoprovidesymptomaticreliefinthetreatmentofurinaryurgency尿急causedbyminorinflammatorybladderdisorders膀胱炎.GastrointestinalDisorders消化CholinergicPoisoning

膽堿能中毒Severecholinergicexcessisamedicalemergency,especiallyinruralcommunitieswherecholinesteraseinhibitorinsecticides殺蟲劑arecommonlyusedandincultureswherewildmushrooms毒蘑菇arecommonlyeaten.Thepotentialuseofcholinesteraseinhibitorsaschemicalwarfare“nervegases“神經(jīng)毒氣

alsorequiresanawarenessofthemethodsfortreatingacutepoisoning.CholinergicPoisoning膽堿能中毒Overdoses過量ofatropineoritscongeners同類藥aregenerallytreatedsymptomatically對癥治療.Poisoncontrolexpertsdiscouragetheuseofphysostigmine毒扁豆堿oranothercholinesteraseinhibitor膽堿酯酶抑制藥toreversetheeffectsofatropineoverdosebecausesymptomaticmanagementismoreeffectiveandlessdangerous.Symptomatictreatmentmayrequiretemperaturecontrolwithcoolingblanketsandseizure癲癇controlwithdiazepam安定.Artificialrespiratorysupportisneededinrespiratorydepression.AntimuscarinicPoisoning抗膽堿藥中毒Overdoses過量ofatropineoritsContraindicationstotheuseofantimuscarinicdrugsarerelative相對禁忌,notabsolute.Obviousmuscarinicexcess,especiallythatcausedbycholinesteraseinhibitors膽堿酯酶抑制藥,canalwaysbetreatedwithatropine.Antimuscarinicdrugsarecontraindicatedinpatientswithglaucoma青光眼,especiallyangle-closureglaucoma急性閉角型青光眼.Inelderlymen,antimuscarinicdrugsshouldalwaysbeusedwithcautionandshouldbeavoidedinthosewithahistoryofprostatichyperplasia

前列腺肥大.Contraindications禁忌癥Contraindicationstotheuseo1Ganglionicblockingdrugs

神經(jīng)節(jié)阻斷藥2Skeletalmuscularrelaxants

骨骼肌松弛劑Nicotiniccholinoceptor

blockingdrugs煙堿型受體阻斷藥N受體阻斷藥1GanglionicblockingdrugsNicGanglionicblockingdrugs

神經(jīng)節(jié)阻斷藥GanglionPreganglionicfiberPostganglionicfiberGanglionicblockingdrugs

神經(jīng)節(jié)阻Mecamylamine美加明andtrimethaphan咪噻吩isoccasionallyusedinthetreatmentofhypertensiveemergencies高血壓危象anddissectingaorticaneurysm主動脈夾層動脈瘤;inproducinghypotension低血壓,whichcanbeofvalueinneurosurgery神經(jīng)手術(shù)toreducebleedingintheoperativefield.Clinicalapplications臨床應(yīng)用Mecamylamine美加明andtrimethaphaNeuromuscularblockingdrugsinterferewithtransmissionattheneuromuscularendplate終板.Thesecompoundsareusedprimarilyasadjuncts輔助用藥duringgeneralanesthesia全身麻醉tofacilitatetrachealintubation氣管插管andoptimizesurgicalconditionswhileensuringadequateventilation通氣.Skeletalmuscularrelaxants

骨骼肌松弛劑NeuromuscularblockingdrugsiMechanismofneuromuscularblocked作用機(jī)制Mechanismofneuromuscularblo1Nondepolarizingmuscularrelaxants(d-tubocurarine筒箭毒堿)

非除極化肌松藥2Depolarizingmuscularrelaxants(succinylcholine琥珀酰膽堿)

除極化肌松藥1Nondepolarizingmuscularrel筒箭毒堿Nondepolarizingmuscularrelaxants非除極化肌松藥筒箭毒堿Nondepolarizingmuscularr膽堿受體阻斷藥課件Duringanesthesia麻醉,administrationoftubocurarine筒箭毒堿initiallycausesmotorweakness,followedbytheskeletalmusclesbecomingflaccid松弛的andinexcitabletoelectricalstimulation.Ingeneral,largermuscles(eg,abdominal腹肌,trunk軀干,diaphragm)橫隔膜aremoreresistanttoneuromuscularblockadeandrecovermorerapidlythansmallermuscles(eg,facial面部,foot,hand).Thediaphragm膈肌

isusuallythelastmuscletobeparalyzed麻痹.