神经系统药理魏尔清抗癫痫药课件

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PsychomotorseizuresPetitmal(absence)Grandmal(tonic-clonic)Epilepsyisnotasingleentity;itisafamilyofdifferentrecu

rrentseizuredisordersthathaveincommonthesudden,excessiveanddisorderlydischargeofcentralneurons.Thisresultsinabnormalmovementorperceptionsthatare

ofshortdurationbutthattendtorecur.Classificationofepilepsy(older)Generalizedseizures(全身发作)Grandmal(大发作):to

nic-clonicseizures(强直-阵挛)Petitmal(小发作):absenceseizures(失神发作)Partialseizures(部分性发作)Pshychomotor(精神运动性):temporallobeseizures(颞叶癫痫)Partial(部分发作):mot

or,sensory,ANS,etc.(局限性发作)ClassificationofepilepsyNormalEEGAbsenceEEGThepathwaysforseizurepropagationinpartials

eizuresandprimarygeneralizedseizuresStereotypicalcomplexpartialseizuresIneffectiveforpetitmal(absenceseizures)(3)AntiarrhythmiaNecessarytomonitorp

lasmaconcentrations(1)Grandmal/Partial:BroadspectrumofantiepilepsyIneffectiveforpetitmal(absenceseizures)Phenytoin,Carbamazepine,PhenobarbitalAdverse

effects:AntiepilepticdrugsHepatictoxicityGrandmal,statusepilepticus;Mephenytoin美芬妥英,Ethotoin乙苯妥英:analo

guesofphenytoinInductionofhepaticdrug-metabolizingenzymes(3)Antiarrhythmia(3)AntiarrhythmiaAntiepilepticdrugsPsychomotorseizuresLamotrigin

e拉莫三嗪Primidone,ValproatesodiumPrincipalsofantiepilepticdrugusesMechanismsofantiepilepticdrugsElectrophysiologicalInhibitingexcessivedischarges

InhibitingspreadofdischargesMolecularPotentiatingGABAneuronalfunctionsModulatingNa+,Ca2+,K+channelfuctions

A.AntiepilepticdrugsSpecialdrugsPhenytoinSodium苯妥英钠CONNHC6H5C6H5NaO1.PharmacologicaleffectsandthemechanismInhibitinginfluxofNa+andCa2+Inhibitingspr

eadofabnormaldischargesA.Antiepilepticdrugs2.Clinicaluses(1)AntiepilepsyGrandmal,statusepilepticus;Partialseizures(s

impleandcomplex);Ineffectiveforpetitmal(absenceseizures)(2)Trigeminalandrelatedneuralgia(3)AntiarrhythmiaA.Antiepilepticdrugs3.ADMELargerdoses:

non-linearkinetics(plasmaconcentration>10g/ml)NecessarytomonitorplasmaconcentrationsInductionofhepaticdrug-metabolizingenzymesA.Antiepil

epticdrugs3.Adverseeffects(1)LocalreactionsGIreactions;gingivalhyperplasia(2)CNSreactionsParticularlyinthecerebellumandvestibularsys

tems:nystagmus(眼球震颤),ataxia(共济失调),etc.Behavioralchanges:confusion,hallucinationA.Antiepilepticdrugs(3)HemologicalreactionsMegal

oblasticanemia(4)AllergicreactionsSkinreactions;bloodcellabnormality(includingthrombocytopenia,agranulocyt

osis);hepatictoxicity;ect.(5)SkeletalreactionsOsteomalaciabyabnormalvitaminDmetabolismandcalciumabsorptionA.Antiepilepticdrugs4.Drugin

teractions(1)Increasesplasmaconcentrationsofdrugsbydisplacementofplasmaproteinbinding(salicylates)andinhibiti

onofinactivation(isoniazid,chloramphenicol)(2)Decreasesplasmaconcentrationsofdrugs(phenobarbital,carbamazepine)byenhanci

ngmetabolism(3)PhenytoinenhancesthemetabolismofcorticosteroidsandvitaminDA.AntiepilepticdrugsEffectiveforpsychomotorseizures,andgrandmalEpileps

yisnotasingleentity;itisafamilyofdifferentrecurrentseizuredisordersthathaveincommonthesudden,excessiveanddisorderlydischargeofcen

tralneurons.(2)TrigeminalandrelatedneuralgiaPhenytoin,Carbamazepine,PhenobarbitalThisresultsinabnormalmovementorperceptionsthatareofs

hortdurationbutthattendtorecur.OtheranticovulsantdrugsParticularlyinthecerebellumandvestibularsystems:nystagmus(眼球震颤),ataxia(共济失调),etc.Adverseeffe

ctsPartial(部分发作):Primidone,ValproatesodiumDruginteractionsPartialseizures(simpleandcomplex);Phenytoin,Carbamazepine,PhenobarbitalI

nhibitingspreadofdischargesCHCOOHPrincipalsofantiepilepticdrugusesPetitmal(小发作):ClassificationofepilepsyPrincipalsofantiepilepti

cdrugusesvasodilatation,BP;(1)AntiepilepsyInhibitingbothformationandspreadofdischargesEffectiveforgrandmal,partialsimpleseizures,statusepilepticu

sPhenobarbital苯巴比妥A.AntiepilepticdrugsC2H5CONHNHCOCOCC6H5Effectiveforpsychomotorseizures,andgrandmalEffectiveformania,depression,

andneuralgiaCarbamazepine卡马西平NCONH2A.AntiepilepticdrugsBroadspectrumofantiepilepsyHepatictoxicityValproatesodium丙戊酸钠A.AntiepilepticdrugsCH3CH2C

H2CHCOOHCH3CH2CH2OtherantiepilepticdrugsPrimidone扑米酮:analoguesofphenobarbital,usedforphenobarbital-andph

enytoin-ineffectivepatientsMephenytoin美芬妥英,Ethotoin乙苯妥英:analoguesofphenytoinEthosuximide乙琥胺:peptitmalDiazepam:status

epilepticus(i.v.)Nitrozepam硝西泮,Clonazepam氯硝西泮:peptitmalLamotrigine拉莫三嗪A.AntiepilepticdrugsBoxCommontoxici

tyofantiepilepticdrugs:CNSreactionsHemologicalreactionsHepatictoxicityA.Antiepilepticdrugs(1)AntiepilepsyPrimido

ne,ValproatesodiumplasmaconcentrationmonitoringifnecessaryClassificationofepilepsy(older)CHCOOHParticularlyinthece

rebellumandvestibularsystems:nystagmus(眼球震颤),ataxia(共济失调),etc.AntiepilepticdrugsInductionofhepaticdrug-metabolizingenzymes),Phenobrbit

al(i.Effectiveforpsychomotorseizures,andgrandmalClassificationofepilepsy(older)Partialseizures(simplea

ndcomplex);Otheranticovulsantdrugs(2)Peptitmal:Ethosuximide(2)CNSreactions(3)Phenytoinenhancesthemeta

bolismofcorticosteroidsandvitaminDChoiceofdrugs(1)Increasesplasmaconcentrationsofdrugsbydisplacementofplasmaprotei

nbinding(salicylates)andinhibitionofinactivation(isoniazid,chloramphenicol)hypertensioncrisis),Pheno

brbital(i.Mechanismsofantiepilepticdrugsvasodilatation,BP;smalllargerdoses;hypertensioncrisistonic-clonicseizures(强直-阵挛)Primidon

e,ValproatesodiumClinicaluses(2)Peptitmal:EthosuximiderelaxingskeletalmusclesCHCOOHInhibitingbothformationandspreadofdischa

rgesCHCOOHStereotypicalcomplexpartialseizures(2)CNSreactionsSpecialdrugsAntiepilepticdrugsNecessaryt

omonitorplasmaconcentrationsOtheranticovulsantdrugsMechanismsofantiepilepticdrugsIneffectiveforpetitmal(absen

ceseizures)temporallobeseizures(颞叶癫痫)doseindividualization;Principalsofantiepilepticdruguses1.Choiceofdrugs(1)Grandmal/Partial:Phen

ytoin,Carbamazepine,PhenobarbitalPrimidone,Valproatesodium(2)Peptitmal:EthosuximideClonazepam,Valproat

esodium(3)Psychomotor:Carbamazepine,Phenytoin(4)Statusepilepticus:Diazepan(i.v.)Phenytoin(i.v.),Phenobrbital(i.m.)A.Antiepile

pticdrugs2.Dosage:small→largerdoses;doseindividualization;plasmaconcentrationmonitoringifnecessary3.Usage:drugcombination4.Withdrawal:gradually

andslowlyA.Antiepilepticdrugs1.Effects:centraldepression;vasodilatation,BP;relaxingskeletalmuscles2.Uses:convulsion;hypertensioncrisis

3.Adverseeffects:depressionofrespiratoryandvasomotorcenters,antagonizedbycalciumpreparations(i.v.)MagnesiumSulfate硫酸镁A.AnticonvulsantdrugsOt

heranticovulsantdrugsSedative-hypnoticdrugsA.Anticonvulsantdrugs

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