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第16章 抗癫痫药 和抗惊厥药

第16章 抗癫痫药 和抗惊厥药. Antiepileptics & anticonvulsive drugs. §1 antiepileptic drugs. introduction. ㈠ Epilepsy 癫痫 1、 chronic CNS disorders; 1) cerebral focus nerve cell 2) sudden 、 abnormity 、 rapid high frequency local discharge

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第16章 抗癫痫药 和抗惊厥药

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  1. 第16章 抗癫痫药和抗惊厥药 Antiepileptics & anticonvulsive drugs

  2. §1 antiepileptic drugs introduction ㈠ Epilepsy 癫痫 1、 chronic CNS disorders; 1) cerebralfocus nerve cell 2)sudden 、 abnormity 、rapid high frequencylocal discharge 3)arounddiffuse 4) cerebralfunctiondisorders 。

  3. Causes of epilepsy • Damage to the brain: 1)tumours、 2) head injury 、 3)infection、 4) cerebrovascular accident;

  4. 2、Character of paroxysm 1) abrupt onset ① staring (目瞪) ② cessation of ongoing activities ③ lasting less than 30 sec 2)transient、 3)repeat ;

  5. Classification of epileptic 1、Partial seizures: 1)、simple partial— key feature:preservation of consciousness; 2)、complex partial— impaired consciousness lasting 30sc—2min。

  6. 2、generalized seizures: 1)absence seizures(peptit-mal): 2)myoclonic seizures: a brief shock like contraction of muscle ; 3)tonic –clonic seizures: (grand-mal epilepsy)

  7. §1 antiepileptic drugs 一、manner of action : 1、 ㈠ local discharge 2、arounddiffuse. 二、mechanism of action 1 、 function of GABA 2、interfereNa+、K+、Ca2+ channel

  8. usual drugs • phenytoin sodium (苯妥英钠、大仑丁,dilantin) [ pharmacokinetics ] 1、PO.—absorption somewhat slow , F—difference obvious ; 2、stimulation,not suitable IM 3、extensively bound to serum protein ;

  9. 3、eliminationvelocitywith blood concentration correlation  10g/ml:first-order elimination kinetics ,t½ 6-24 h  10g/ml: zero-order elimination kinetics ,t½ 20-60 h

  10. [actions and uses] • epilepsy 1) Generalized tonic –clonic; partial seizure (first choice ) 2) absence seizures inefficacy ; 2.trigeminal and related neuralgias 3. arrhythmia (related to digitalis intoxication)

  11. [ adverse reactions ] 1.local stimulation (PH 2.chronic toxico ⑴ overgrown of gum collagen (in children and young) ⑵ CNS depression ; ⑶ a variety of endocrine ;

  12. 3. other 1) hypersensitivity reaction ; 2) cardiac toxicity: iv-excessive rate; 3) fatal hepatic necrosis; 4) blood system : reduce immunoglobulin neutropenial folacin

  13. carbamazepine 卡马西平(酰胺咪嗪) [characteristics ] 1、㈠Na+channel,㈠focusdischarge; 2、generalized tonic clonic and simple --- first choice neuralgia > phenytoin sodium;

  14. 3、po-- absorb slowly, induce hepaticenzyme , 4、adverse reaction 1)acute intoxication:stupor、 coma hyperirritability 、convulsion respiratory depression 2)serious intoxication: ㈠ marrow , hepatic damage 。

  15. other usual drugs 药 名character 苯巴比妥 ㈠dischargeanddiffuses , Phenobarbital use: epilepsy absence seizures efficacy 乙琥胺 Ethosuximide 丙戊酸钠widely antiepilepsy Sodium valproate ㈠Na+channel, GABA of CNS

  16. Clinicchoice drugs principles 1、types of epilepsy ; 2、 long term administration; 3、 individual of dose; 4、not suddenstop ; 3、note:adverse reaction anddrug interration

  17. §2 anticonvulsants magnesium sulfate (硫酸镁) 1、Mg2+-Ca2+competitive, 2、use:PO-catharsis im-anticonvulsion ; iv--BP 3、adverse reaction: ㈠CNS、㈠ respiratory、 administrationslowly overdose : iv.Ca2+。

  18. question • 1、 describe the choice agents of epilepsy ? • 2、which drugs prossessaction anticonvulsion ?

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