神经系统药理—魏尔清抗癫痫药电子教案.ppt

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1、神经系统药理魏尔清抗癫痫药Classification of epilepsy(older)Generalized seizures(Generalized seizures(全身发作全身发作全身发作全身发作）Grand malGrand mal（大发作大发作大发作大发作）：）：）：）：tonic-clonic seizures tonic-clonic seizures（强直阵挛强直阵挛强直阵挛强直阵挛）Petit mal Petit mal（小发作小发作小发作小发作）：absence seizures absence seizures（失神发作失神发作失神发作失神发作）Partial se

2、izures(Partial seizures(部分性发作部分性发作部分性发作部分性发作)PshychomotorPshychomotor（精神运动性精神运动性精神运动性精神运动性）：）：）：）：temporal lobe seizurestemporal lobe seizures（颞叶癫痫颞叶癫痫颞叶癫痫颞叶癫痫）PartialPartial（部分发作部分发作部分发作部分发作）：）：）：）：motor,sensory,ANS,motor,sensory,ANS,etc.etc.（局限性发作局限性发作局限性发作局限性发作）Classification of epilepsyNormal EE

3、GNormal EEGAbsence EEGAbsence EEGThe pathways for The pathways for seizure propagation in seizure propagation in partial seizures and partial seizures and primary generalized primary generalized seizuresseizuresStereotypical complex partial seizuresMechanisms of antiepileptic drugsElectrophysiologic

4、alElectrophysiologicalInhibiting excessive dischargesInhibiting excessive dischargesInhibiting spread of dischargesInhibiting spread of dischargesMolecularMolecularPotentiating GABA neuronal functionsPotentiating GABA neuronal functionsModulating NaModulating Na+,Ca,Ca2+2+,K,K+channel fuctionschanne

5、l fuctionsA.Antiepileptic drugsSpecial drugsPhenytoin Sodium 苯妥英钠苯妥英钠苯妥英钠苯妥英钠1.Pharmacological effects and the mechanism Inhibiting influx of Na+and Ca2+Inhibiting spread of abnormal dischargesA.Antiepileptic drugs2.Clinical uses(1)AntiepilepsyGrand mal,status epilepticus;Grand mal,status epilepticu

6、s;Partial seizures(simple and complex);Partial seizures(simple and complex);Ineffective for petit mal(absence seizures)Ineffective for petit mal(absence seizures)(2)Trigeminal and related neuralgia(3)AntiarrhythmiaA.Antiepileptic drugs3.ADME Larger doses:non-linear kinetics（plasma concentration 10 g

7、/ml）Necessary to monitor plasma concentrations Induction of hepatic drug-metabolizing enzymesA.Antiepileptic drugs3.Adverse effects(1)Local reactions GI reactions;gingival hyperplasiaGI reactions;gingival hyperplasia(2)CNS reactions Particularly in the cerebellum and vestibular systems:Particularly

8、in the cerebellum and vestibular systems:nystagmus(nystagmus(眼球震颤眼球震颤眼球震颤眼球震颤),ataxia(),ataxia(共济失调共济失调共济失调共济失调),),etc.etc.Behavioral changes:confusion,hallucinationBehavioral changes:confusion,hallucination A.Antiepileptic drugs(3)Hemological reactions Megaloblastic anemiaMegaloblastic anemia(4)All

9、ergic reactions Skin reactions;blood cell abnormality(including Skin reactions;blood cell abnormality(including thrombocytopenia,agranulocytosis);thrombocytopenia,agranulocytosis);hepatic toxicity;hepatic toxicity;ect.ect.(5)Skeletal reactions Osteomalacia by abnormal vitamin D metabolism and Osteom

10、alacia by abnormal vitamin D metabolism and calcium absorptioncalcium absorptionA.Antiepileptic drugs4.Drug interactions(1)Increases plasma concentrations of drugs by(1)Increases plasma concentrations of drugs by displacement of plasma protein binding displacement of plasma protein binding(salicylat

11、es)(salicylates)and inhibition of inactivation and inhibition of inactivation (isoniazid,chloramphenicol)(isoniazid,chloramphenicol)(2)Decreases plasma concentrations of drugs(2)Decreases plasma concentrations of drugs (phenobarbital,carbamazepine)(phenobarbital,carbamazepine)by enhancing by enhanci

12、ng metabolismmetabolism(3)Phenytoin enhances the metabolism of(3)Phenytoin enhances the metabolism of corticosteroids and vitamin Dcorticosteroids and vitamin DA.Antiepileptic drugsInhibiting both formation and spread of Inhibiting both formation and spread of dischargesdischargesEffective for grand

13、 mal,partial simple Effective for grand mal,partial simple seizures,status epilepticusseizures,status epilepticusPhenobarbital 苯巴比妥苯巴比妥苯巴比妥苯巴比妥A.Antiepileptic drugsEffective forEffective for psychomotor seizurespsychomotor seizures,and grand maland grand malEffective for mania,depression,and neuralg

14、iaEffective for mania,depression,and neuralgiaCarbamazepine 卡马西平卡马西平A.Antiepileptic drugsBroad spectrum of antiepilepsyBroad spectrum of antiepilepsyHepatic toxicityHepatic toxicityValproate sodium 丙戊酸钠丙戊酸钠丙戊酸钠丙戊酸钠A.Antiepileptic drugsCH3CH2CH2 CHCOOHCH3CH2CH2Other antiepileptic drugsPrimidone Primi

15、done 扑米酮扑米酮扑米酮扑米酮：analogues of phenobarbital,used analogues of phenobarbital,used for phenobarbital-and phenytoin-ineffective patientsfor phenobarbital-and phenytoin-ineffective patientsMephenytoin Mephenytoin 美芬妥英美芬妥英美芬妥英美芬妥英,Ethotoin,Ethotoin 乙苯妥英乙苯妥英乙苯妥英乙苯妥英：analogues of analogues of phenytoinphe

16、nytoinEthosuximide Ethosuximide 乙琥胺乙琥胺乙琥胺乙琥胺：peptit malpeptit malDiazepam:Diazepam:status epilepticus(status epilepticus(i.v.i.v.)Nitrozepam Nitrozepam 硝西泮硝西泮硝西泮硝西泮,Clonazepam,Clonazepam 氯硝西泮氯硝西泮氯硝西泮氯硝西泮：peptit malpeptit malLamotrigine Lamotrigine 拉莫三嗪拉莫三嗪拉莫三嗪拉莫三嗪A.Antiepileptic drugsBox Common toxi

17、city of antiepileptic drugs:CNS reactions Hemological reactions Hepatic toxicityA.Antiepileptic drugsPrincipals of antiepileptic drug uses1.Choice of drugs(1)Grand mal/Partial(1)Grand mal/Partial：Phenytoin,Carbamazepine,PhenobarbitalPhenytoin,Carbamazepine,Phenobarbital Primidone,Valproate sodiumPri

18、midone,Valproate sodium(2)Peptit mal:(2)Peptit mal:EthosuximideEthosuximide Clonazepam,Valproate sodiumClonazepam,Valproate sodium(3)Psychomotor(3)Psychomotor：Carbamazepine,PhenytoinCarbamazepine,Phenytoin(4)Status epilepticus(4)Status epilepticus：Diazepan(i.v.)Diazepan(i.v.)Phenytoin(i.v.),Phenobrb

19、ital(i.m.)Phenytoin(i.v.),Phenobrbital(i.m.)A.Antiepileptic drugs2.Dosage：small small larger doses;larger doses;dose individualization;dose individualization;plasma concentration monitoring if necessary plasma concentration monitoring if necessary3.Usage：drug combinationdrug combination4.Withdrawal：

20、gradually and slowlygradually and slowlyA.Antiepileptic drugs1.Effects：central depression;central depression;vasodilatation,BP vasodilatation,BP ;relaxing skeletal muscles relaxing skeletal muscles2.Uses：convulsionconvulsion；hypertension crisishypertension crisis3.Adverse effects：depression of respi

21、ratory and vasomotor centers,depression of respiratory and vasomotor centers,antagonized by calcium preparations(antagonized by calcium preparations(i.v.i.v.)Magnesium Sulfate 硫酸镁硫酸镁硫酸镁硫酸镁A.Anticonvulsant drugsOther anticovulsant drugsSedative-hypnotic drugsA.Anticonvulsant drugs此课件下载可自行编辑修改，仅供参考！此课件下载可自行编辑修改，仅供参考！感谢您的支持，我们努力做得更好！谢谢感谢您的支持，我们努力做得更好！谢谢