神經(jīng)系統(tǒng)藥理-魏爾清-抗癲癇藥

Part9

AntiepilepticandAnticonvulsantDrugs第一頁，共三十四頁。編輯課件PsychomotorseizuresPetitmal(absence)Grandmal(tonic-clonic)Epilepsyisnotasingleentity;itisafamilyofdifferentrecurrentseizuredisordersthathaveincommonthesudden,excessiveanddisorderlydischargeofcentralneurons.Thisresultsinabnormalmovementorperceptionsthatareofshortdurationbutthattendtorecur.第二頁，共三十四頁。編輯課件Classificationofepilepsy(older)Generalizedseizures(全身發(fā)作）Grandmal（大發(fā)作）：tonic-clonicseizures（強(qiáng)直－陣攣）Petitmal（小發(fā)作）：

absenceseizures（失神發(fā)作）Partialseizures(部分性發(fā)作)Pshychomotor（精神(jīngshén)運(yùn)動(dòng)性）：

temporallobeseizures（顳葉癲癇）Partial（部分發(fā)作）：

motor,sensory,ANS,etc.（局限性發(fā)作）第三頁，共三十四頁。編輯課件Classificationofepilepsy第四頁，共三十四頁。編輯課件NormalEEGAbsenceEEG第五頁，共三十四頁。編輯課件Thepathwaysforseizurepropagationinpartialseizuresandprimarygeneralizedseizures第六頁，共三十四頁。編輯課件第七頁，共三十四頁。編輯課件Stereotypicalcomplexpartialseizures第八頁，共三十四頁。編輯課件MechanismsofantiepilepticdrugsElectrophysiologicalInhibitingexcessivedischargesInhibitingspreadofdischargesMolecularPotentiatingGABAneuronalfunctionsModulatingNa+,Ca2+,K+channelfuctions第九頁，共三十四頁。編輯課件A.

AntiepilepticdrugsSpecialdrugsPhenytoinSodium苯妥英鈉第十頁，共三十四頁。編輯課件1.Pharmacologicaleffectsandthemechanism

InhibitinginfluxofNa+andCa2+Inhibitingspreadof

abnormaldischargesA.

Antiepilepticdrugs第十一頁，共三十四頁。編輯課件第十二頁，共三十四頁。編輯課件2.Clinicaluses(1)AntiepilepsyGrandmal,statusepilepticus;Partialseizures(simpleandcomplex);Ineffectiveforpetitmal(absenceseizures)(2)Trigeminalandrelatedneuralgia(3)AntiarrhythmiaA.

Antiepilepticdrugs第十三頁，共三十四頁。編輯課件3.ADMELargerdoses:non-linearkinetics（plasmaconcentration>10

g/ml）Necessarytomonitorplasmaconcentrations

Inductionofhepaticdrug-metabolizingenzymesA.

Antiepilepticdrugs第十四頁，共三十四頁。編輯課件第十五頁，共三十四頁。編輯課件第十六頁，共三十四頁。編輯課件3.Adverseeffects(1)LocalreactionsGIreactions;gingivalhyperplasia(2)CNSreactionsParticularlyinthecerebellumandvestibularsystems:nystagmus(眼球(yǎnqiú)震顫),ataxia(共濟(jì)失調(diào)),etc.Behavioralchanges:confusion,hallucination

A.

Antiepilepticdrugs第十七頁，共三十四頁。編輯課件(3)HemologicalreactionsMegaloblasticanemia(4)AllergicreactionsSkinreactions;bloodcellabnormality(includingthrombocytopenia,agranulocytosis);hepatictoxicity;ect.(5)SkeletalreactionsOsteomalaciabyabnormalvitaminDmetabolismandcalciumabsorptionA.

Antiepilepticdrugs第十八頁，共三十四頁。編輯課件4.Druginteractions(1)Increasesplasmaconcentrationsofdrugsbydisplacementofplasmaproteinbinding(salicylates)andinhibitionofinactivation

(isoniazid,chloramphenicol)(2)Decreasesplasmaconcentrationsofdrugs

(phenobarbital,carbamazepine)

byenhancingmetabolism(3)PhenytoinenhancesthemetabolismofcorticosteroidsandvitaminDA.

Antiepilepticdrugs第十九頁，共三十四頁。編輯課件InhibitingbothformationandspreadofdischargesEffectiveforgrandmal,partialsimpleseizures,statusepilepticusPhenobarbital苯巴比妥A.

Antiepilepticdrugs第二十頁，共三十四頁。編輯課件Effectivefor

psychomotorseizures,andgrandmalEffectiveformania,depression,andneuralgiaCarbamazepine卡馬西平A.

Antiepilepticdrugs第二十一頁，共三十四頁。編輯課件第二十二頁，共三十四頁。編輯課件BroadspectrumofantiepilepsyHepatictoxicityValproatesodium丙戊酸鈉A.

AntiepilepticdrugsCH3CH2CH2CHCOOHCH3CH2CH2第二十三頁，共三十四頁。編輯課件OtherantiepilepticdrugsPrimidone撲米酮：analoguesofphenobarbital,usedforphenobarbital-andphenytoin-ineffectivepatientsMephenytoin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：peptitmalLamotrigine拉莫三嗪A.

Antiepilepticdrugs第二十四頁，共三十四頁。編輯課件第二十五頁，共三十四頁。編輯課件第二十六頁，共三十四頁。編輯課件第二十七頁，共三十四頁。編輯課件第二十八頁，共三十四頁。編輯課件Box

Commontoxicityofantiepilepticdrugs:

CNSreactionsHemologicalreactionsHepatictoxicityA.

Antiepilepticdrugs第二十九頁，共三十四頁。編輯課件Principalsofantiepilepticdruguses1.Choiceofdrugs(1)Grandmal/Partial：

Phenytoin,Carbamazepine,Phenobarbital

Primidone,Valproatesodium(2)Peptitmal:

Ethosuximide

Clonazepam,Valproatesodium(3)Psychomotor：Carbamazepine,Phenytoin(4)Statusepilepticus：Diazepan(i.v.)

Phenytoin(i.v.),Phenobrbital(i.m.)A.

Antiepilepticdrugs第三十頁，共三十四頁。編輯課件2.Dosage：

smalllargerdoses;doseindividualization;plasmaconcentrationmonitoringifnecessary3.Usage：

drugcombination4.Withdrawal：graduallyandslowlyA.

Antiepilepticdrugs第三十一頁，共三十四頁。編輯課件1.Effects：centraldepression;vasodilatation,BP;relaxingskeletalmuscles2.Uses：convulsion；hypertensioncrisis3.Adverseeffects：depressionofrespiratoryandvasomotorcenters,antagonizedbycalciumpreparations(i.v.)MagnesiumSulfate硫酸鎂A.

Anticonvulsantdrugs第三十二頁，共三十四頁。編輯課件OtheranticovulsantdrugsSedative-hypnoticdr