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;itisafamilyofdifferentrecurrentseizuredisord

ersthathaveincommonthesudden,excessiveanddisorderlydischargeofcentralneurons.Thisresultsinabnormalmovementorperceptionsthatareofshortdurationbut

thattendtorecur.Classificationofepilepsy(older)Generalizedseizures(全身发作)Grandmal(大发作):tonic-clonicsei

zures(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):motor,sensory,ANS

,etc.(局限性发作)ClassificationofepilepsyNormalEEGAbsenceEEGThepathwaysforseizurepropagationinpartialseizuresandprim

arygeneralizedseizuresStereotypicalcomplexpartialseizuresIneffectiveforpetitmal(absenceseizures)(3)AntiarrhythmiaNecessarytomonitorplasmaconce

ntrations(1)Grandmal/Partial:BroadspectrumofantiepilepsyIneffectiveforpetitmal(absenceseizures)Phenytoin,Car

bamazepine,PhenobarbitalAdverseeffects:AntiepilepticdrugsHepatictoxicityGrandmal,statusepilepticus;Mephenytoin美芬妥英,Ethotoin乙苯妥英:a

naloguesofphenytoinInductionofhepaticdrug-metabolizingenzymes(3)Antiarrhythmia(3)AntiarrhythmiaAntiepi

lepticdrugsPsychomotorseizuresLamotrigine拉莫三嗪Primidone,ValproatesodiumPrincipalsofantiepilepticdrugusesMe

chanismsofantiepilepticdrugsElectrophysiologicalInhibitingexcessivedischargesInhibitingspreadofdischargesMolecularPotentiatingGAB

AneuronalfunctionsModulatingNa+,Ca2+,K+channelfuctionsA.AntiepilepticdrugsSpecialdrugsPhenytoinSodium苯妥英钠CONNHC6H5C6H5NaO1.Phar

macologicaleffectsandthemechanismInhibitinginfluxofNa+andCa2+InhibitingspreadofabnormaldischargesA.Antiepilepticdrugs2.

Clinicaluses(1)AntiepilepsyGrandmal,statusepilepticus;Partialseizures(simpleandcomplex);Ineffectiveforpetitm

al(absenceseizures)(2)Trigeminalandrelatedneuralgia(3)AntiarrhythmiaA.Antiepilepticdrugs3.ADMELargerdoses:non-linearkinetics(plasmaconcentrati

on>10g/ml)NecessarytomonitorplasmaconcentrationsInductionofhepaticdrug-metabolizingenzymesA.Antiepilepticdrugs3.Adverse

effects(1)LocalreactionsGIreactions;gingivalhyperplasia(2)CNSreactionsParticularlyinthecerebellumandvestibularsystems:nyst

agmus(眼球震颤),ataxia(共济失调),etc.Behavioralchanges:confusion,hallucinationA.Antiepilepticdrugs(3)HemologicalreactionsMegaloblasticanemia(4)Allergicreac

tionsSkinreactions;bloodcellabnormality(includingthrombocytopenia,agranulocytosis);hepatictoxicity;ect.(5)SkeletalreactionsOsteomala

ciabyabnormalvitaminDmetabolismandcalciumabsorptionA.Antiepilepticdrugs4.Druginteractions(1)Increasesplasmaconcentrationsofdrugsbydisplacemento

fplasmaproteinbinding(salicylates)andinhibitionofinactivation(isoniazid,chloramphenicol)(2)Decreasesplasmaconcentrationsofdrugs(p

henobarbital,carbamazepine)byenhancingmetabolism(3)PhenytoinenhancesthemetabolismofcorticosteroidsandvitaminDA

.AntiepilepticdrugsEffectiveforpsychomotorseizures,andgrandmalEpilepsyisnotasingleentity;itisafamilyofdi

fferentrecurrentseizuredisordersthathaveincommonthesudden,excessiveanddisorderlydischargeofcentralneurons.(2)TrigeminalandrelatedneuralgiaPhe

nytoin,Carbamazepine,PhenobarbitalThisresultsinabnormalmovementorperceptionsthatareofshortdurationbutthattendtorecur.Otherant

icovulsantdrugsParticularlyinthecerebellumandvestibularsystems:nystagmus(眼球震颤),ataxia(共济失调),etc.AdverseeffectsPartial(部分发作)

:Primidone,ValproatesodiumDruginteractionsPartialseizures(simpleandcomplex);Phenytoin,Carbamazepine,PhenobarbitalInhibiting

spreadofdischargesCHCOOHPrincipalsofantiepilepticdrugusesPetitmal(小发作):ClassificationofepilepsyPrincipalsofantiepi

lepticdrugusesvasodilatation,BP;(1)AntiepilepsyInhibitingbothformationandspreadofdischargesEffectiveforgrandmal,

partialsimpleseizures,statusepilepticusPhenobarbital苯巴比妥A.AntiepilepticdrugsC2H5CONHNHCOCOCC6H5Effectivefor

psychomotorseizures,andgrandmalEffectiveformania,depression,andneuralgiaCarbamazepine卡马西平NCONH2A.Antiepilept

icdrugsBroadspectrumofantiepilepsyHepatictoxicityValproatesodium丙戊酸钠A.AntiepilepticdrugsCH3CH2CH2CHCOOHCH3CH2CH2Otherantiepile

pticdrugsPrimidone扑米酮:analoguesofphenobarbital,usedforphenobarbital-andphenytoin-ineffectivepatientsMepheny

toin美芬妥英,Ethotoin乙苯妥英:analoguesofphenytoinEthosuximide乙琥胺:peptitmalDiazepam:statusepilepticus(i.v.)Nitrozepam硝西泮,Clonazepam氯硝西泮:peptitmalLamotri

gine拉莫三嗪A.AntiepilepticdrugsBoxCommontoxicityofantiepilepticdrugs:CNSreactionsHemologicalreactionsHepatictoxicityA.

Antiepilepticdrugs(1)AntiepilepsyPrimidone,ValproatesodiumplasmaconcentrationmonitoringifnecessaryClassificationofepilepsy(older)CHCOOHParticularlyi

nthecerebellumandvestibularsystems:nystagmus(眼球震颤),ataxia(共济失调),etc.AntiepilepticdrugsInductionofhepaticdrug-metabolizingen

zymes),Phenobrbital(i.Effectiveforpsychomotorseizures,andgrandmalClassificationofepilepsy(older)Partialseizures(simpl

eandcomplex);Otheranticovulsantdrugs(2)Peptitmal:Ethosuximide(2)CNSreactions(3)Phenytoinenhancesthemetabolismofc

orticosteroidsandvitaminDChoiceofdrugs(1)Increasesplasmaconcentrationsofdrugsbydisplacementofplasmaproteinbindin

g(salicylates)andinhibitionofinactivation(isoniazid,chloramphenicol)hypertensioncrisis),Phenobrbital(i.Mechanismsofa

ntiepilepticdrugsvasodilatation,BP;smalllargerdoses;hypertensioncrisistonic-clonicseizures(强直-阵挛)Primi

done,ValproatesodiumClinicaluses(2)Peptitmal:EthosuximiderelaxingskeletalmusclesCHCOOHInhibitingbothformationandspreadofdischargesCHC

OOHStereotypicalcomplexpartialseizures(2)CNSreactionsSpecialdrugsAntiepilepticdrugsNecessarytomonitorplasmaconcentrationsO

theranticovulsantdrugsMechanismsofantiepilepticdrugsIneffectiveforpetitmal(absenceseizures)temporallobeseizures(颞叶癫痫)dosei

ndividualization;Principalsofantiepilepticdruguses1.Choiceofdrugs(1)Grandmal/Partial:Phenytoin,Carbamazepine,P

henobarbitalPrimidone,Valproatesodium(2)Peptitmal:EthosuximideClonazepam,Valproatesodium(3)Psychomotor:Car

bamazepine,Phenytoin(4)Statusepilepticus:Diazepan(i.v.)Phenytoin(i.v.),Phenobrbital(i.m.)A.Antiepilepticdrugs2.Dosage:

small→largerdoses;doseindividualization;plasmaconcentrationmonitoringifnecessary3.Usage:drugcombination4.Withdrawal:graduallyandsl

owlyA.Antiepilepticdrugs1.Effects:centraldepression;vasodilatation,BP;relaxingskeletalmuscles2.Uses:convulsion;hypertensioncrisis3.A

dverseeffects:depressionofrespiratoryandvasomotorcenters,antagonizedbycalciumpreparations(i.v.)Magnesi

umSulfate硫酸镁A.AnticonvulsantdrugsOtheranticovulsantdrugsSedative-hypnoticdrugsA.Anticonvulsantdrugs

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