抗-癫-痫-药---中国医学科学院&北京协和医学院-精品课程建设

中枢兴奋药CentralStimulants北京协和医学院基础医学院药理学系叶菜英CentralStimulants(中枢兴奋药)Definition:Drugscanstimulatethecentralnervoussystem.Classification:Cerebralcortexstimulation:Caffeine,Theophylline…Cerebrumandbrainstemstimulation:Nikethamide,DimeflineandLobeline.Spinalcordstimulation:StrychnineCaffeine(咖啡因)【MechanismofAction】Inhibitphosphodiesterase,decreasethedegradationofcAMP→cAMP↑……→physiologicaleffectCentralneuromodulatorantagonist→effectofadenosine→blocktheinhibitingeffectofadenosineoncentralnervoussystem→stimulatethecentralnervoussystem.IncreasingintracellularfreecalciumCompetitiveantagonistsofBenzodiazepinereceptor,decreasetheopenfrequencyofCl－channel→stimulatethecentralnervoussystem.Caffeine【Pharmacologicpropertiesandclinicalapplication】CNS：Insmalldoses,itcauseswakefulness,increasesmentalalertness,anddecreasesresponsetimesforsimplemotortask.Cardiovasculareffects：Smalldoses→stimulatevagusnerve→heartrate↓Largedoses→increasethesensitivityofheartrate→arrhythmiaVasoconstrictioneffects:usewithErgotamine,brainarteriectasis→treatmentofmigraine,usuallycompatiblewithantipyreticanalgesic→cold,headache,hypertensionheadache（APC、Somedon）.Caffeine【Adverseeffect】Rare.Stimulation,discomfortable,insomniaOverdose→tachycardiaToxis→muscletremorLobeline(洛贝林)Pharmacologicproperties:Stimulatecarotidbodyandaorticchemoreceptor,stimulaterespiratorycenterreflectivity.LargedosesLobelinecanstimulatemedullaoblongatarespiratorycenterdirectly.Stimulatesympatheticnerve→increaseintheheartrate,BP↑Takeeffectrapidly,holdtimeisshort(severalminutes).Lobelineisoftenusedtoimproverespiratorydepressionwhichinducedbyneonatalasphyxiaandpedo-infectiousdiseases,italsocanimproverespiratoryfailurewhichinducedbydrugintoxicationandCO2intoxication.Adverseeffect：increaseintheheartrate，overdose→convulsionNikethamide(尼可刹米)（Coramine可拉明）Pharmacologicproperties:IncreasethestimulationofCNS,especiallystimulatemedullaoblongatarespiratorycenter,carotidbodyandaorticchemoreceptor,andthen,stimulaterespiratorycenterreflectivity,increasetheCO2sensitivityofCNS,acceleratinganddeepeningbreathing,improvingrespiratoryfunction.Thestimulateeffectofcerebralcortexvasomotorcenterandspinalcordisweak.Takeeffectrapidly,holdtimeisshort，asingleintravenousboluscanmaintain5to10minutes.Nikethamide（Coramine）Clinicalapplication:variouskindsofcentralrespiratorydepression(neonatalasphyxia,CO2intoxication，drugintoxication).Adverseeffectsarerare.Overdose→BP↑，tachycardia,amyostasiaandrigor,cough,vomiting,perspiration.Toxis→convulsion.CentralStimulants[Clinicalapplication]:ApplicationconditionsofRespiratoryStimulants:tracheaissmooth,andrespiratorymuscleisnormal（noobviouslysputamentumretentionandbronchospasm）.Combinationmeasures:etiologicaltreatmentinhalingO2,artificialrespiration.Theholdingtimeofcentralstimulantsisshort,soitshouldbeusedagainandagain.Preventconvulsion（Overdose→convulsion）：severalkindsofdrugcanbeusedtakingturns,controldosesstrictly→→→Thanks!