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1、中枢兴奋药CentralStimulants第一课件网CentralStimulantsDefinition:Drugsthatcanstimulatethecentralnervoussystem.Classification:Cerebralcortexstimulation:Caffeine,Theophylline…Cerebrumandbrainstemstimulation:Nikethamide,DimeflineandLobeline.Spinalcordstimulation:StrychnineCaffeine(咖啡因)【
2、MechanismofAction】Inhibitphosphodiesterase,decreasethedegradationofcAMP→cAMP↑……→physiologicaleffectCentralneuromodulatorantagonist→effectofadenosine→blocktheinhibitingeffectofadenosineoncentralnervoussystem→stimulatethecentralnervoussystem.IncreasingintracellularfreecalciumC
3、ompetitiveantagonistsofBenzodiazepinereceptor,decreasetheopenfrequencyofCl-channel→stimulatethecentralnervoussystem.Caffeine【Pharmacologicpropertiesandclinicalapplication】CNS:Insmalldoses,itcauseswakefulness,increasesmentalalertness,anddecreasesresponsetimesforsimplemotortas
4、k.Cardiovasculareffects:Smalldoses→stimulatevagusnerve→heartrate↓Largedoses→increasethesensitivityofheartrate→arrhythmiaVasoconstrictioneffects:usewithErgotamine,brainarteriectasis→treatmentofmigraine,usuallycompatiblewithantipyreticanalgesic→cold,headache,hypertensionheadac
5、he(APC、Somedon).Caffeine【Adverseeffect】Rare.Stimulation,discomfortable,insomniaOverdose→tachycardiaToxis→muscletremorLobeline(洛贝林)【Pharmacologicproperties】Stimulatecarotidbodyandaorticchemoreceptor,stimulaterespiratorycenterreflectivity.LargedosesLobelinecanstimulatemedullao
6、blongatarespiratorycenterdirectly.Stimulatesympatheticnerve→increaseintheheartrate,BP↑Takeeffectrapidly,holdtimeisshort(severalminutes).Lobelineisoftenusedtoimproverespiratorydepressionwhichinducedbyneonatalasphyxiaandpedo-infectiousdiseases,italsocanimproverespiratoryfailur
7、ewhichinducedbydrugintoxicationandCO2intoxication.Adverseeffect:increaseintheheartrate,overdose→convulsionNikethamide(尼可刹米)(Coramine可拉明)【Pharmacologicproperties】IncreasethestimulationofCNS,especiallystimulatemedullaoblongatarespiratorycenter,carotidbodyandaorticchemoreceptor
8、,andthen,stimulaterespiratorycenterreflectivity,increasetheCO2sensitivityof