中国协和医科大学
基础医学院教案
教 研 室：
药理学
课程名称:
药理学
教师名称：
叶菜英
教师职称：
教
1
授
Teaching
topic：
Teaching
subjects：
Hours：
Antiepileptic Drugs
Teaching
aims:
Teaching
content:
Understand the classification and pathogenesis of epilepsy
Medical Students
1.5 class hours
Grasp the pharmacologic effect, mechanism of action, clinical application and
adverse effects of Sodium Phenytoin and Phenobarbital.
Grasp the pharmacologic properties and adverse effects of Ethosuximide, Sodium
Valproate, Carbamzepine and Benzodiazepines.
Key
Points:
Antiepileptic Drugs and Anticonvulsant Drugs
Difficult
Points:
Pharmacologic effect and clinical application of Sodium Phenytoin and
Phenobarbital
Evaluation
methods
Mechanism of action of Sodium Phenytoin and Phenobarbital
References
Student Assessment
1.Rang and Dale’s Pharmacology 6th edition Rang HP, Dall MM, Ritter JM,
Flower RJ , Churchill Livingstong, Elsevier, 2007
2.Golan DE， et al. Principle of Pharmacology, The pathophysiologic basis of
drug therepy 2nd ed. 2008
3.Farrell SE, Priciples of Pharmacology, Workbook 2nd ed, 2008 Lippincott.
4.Finlel R.,et al. eds, Lippincott’s Illustrated Reviews: Pharmacology 4th ed.
Lippincott 2009
5. 杨世杰主编《药理学》
（8 年制规划教材）
，人民卫生出版社，2005 年
6. 张德昌主编《医学药理学》中国协和医科大学出版社 1998 年
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Teaching
aims
Contents
Methods
Timeassignment
Antiepileptic Drugs and
Anticonvulsant
10 min
Ⅰ. Definitions in epilepsy
Comprehend
Ⅱ. Common seizure types of Epilepsy
1. grand mal
2. petit mal
3. complex partial seizures
4. simple partial seizures
Ⅲ. Pathogenesis of Epilepsy
Ⅳ. Therapeutic principle
Master
Ⅴ. Classification of
Antiepileptic Drugs
1. Hydantoins: Sodium Phenytoin
2.Barbiturates: Phenobarbital,
Primidone
3.Succinimide: Ethosuximide
4.Benzodiazepine: Diazepam,
Nitrazepam
5.Others: Sodium Valproate
Media mix,
explanation,
question-rai
sing
and
discussion
Master
Ⅵ. Physiological disposition,
Mechanism of action, clinical
application and Adverse effects
of Sodium Phenytoin
20 min
Master
Ⅶ. Pharmacologic properties and
Adverse effects of Phenobarbital,
Primidone
10 min
Ⅷ. Pharmacologic properties of
Other Antiepileptic Drugs such as
Ethosuximide, Diazepem,
Nitrazepem, Sodium Valproate and
Carbamzepine
10 min
Ⅸ.Principle of Medication
5 min
Ⅹ. Anticonvulsant Drugs
5 min
Master
Familiarity
Reflection
questions
1.
2.
Classification of Antiepileptic Drugs
Pharmacologic properties of Antiepileptic Drugs
3
Rema
rks
References
1. Rang and Dale’s Pharmacology 6th edition Rang HP, Dall MM, Ritter JM,
Flower RJ , Churchill Livingstong, Elsevier, 2007
2. Golan DE， et al. Principle of Pharmacology, The pathophysiologic basis of
drug therepy 2nd ed. 2008
3. Farrell SE, Priciples of Pharmacology, Workbook 2nd ed, 2008 Lippincott.
4. Finlel R.,et al. eds, Lippincott’s Illustrated Reviews: Pharmacology 4th ed.
Lippincott 2009
5. 杨世杰主编《药理学》
（8 年制规划教材）
，人民卫生出版社，2005 年
6. 张德昌主编《医学药理学》中国协和医科大学出版社 1998 年
Antiepileptic Drugs
I. Definitions in epilepsy
Epilepsy comprises recurrent episodes of abnormal cerebral neuronal discharge.
The resulting seizures are usually clinically obvious and vary in pattern according to
which parts of the brain are affected.
II. Common seizure types of Epilepsy


Generalised seizures.

Absence (petit mal).

Tonic/clonic (grand mal).
Partial seizures.

Simple partial seizures.

Complex partial seizures (temporal lobe epilepsy).
III. Pathogenesis of Epilepsy
The neuron in brain lesion depolarizes together suddenly, and then product
high-frequency out-break discharge. The discharge can diffuse to surrounding
normal tissue →extensive excitation →the brain function transient aberration.
IV. Therapeutic principle
 Change the permeability of Na+, Ca2+and K+ in nerve cell membrane, degrade
excitement stage, extend refractory phase.
 Directly or indirectly increase CNS levels of GABA.
V. Classification of Antiepileptic Drugs
Hydantoins：Sodium Phenytoin
Barbiturates：Phenobarbital, Primidone
Succinimide：Ethosuximide
Benzodiazepine: Diazepam, Nitrazepam
Others: Sodium Valproate
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VI. Sodium Phenytoin
Physiological disposition
Sodium Phenytoin is absorbed slowly after oral administration.→After 6-10 days,
its plasma concentration can achieve effect levels. This drug has variable interpatient
plasma concentration.
Mechanism of action
① It can block sodium channels (voltage-, frequency-, and time dependent
fashion) and inhibit the generation of action potentials.
② It can increase the function of inhibitory transmitter GABA, inhibit nerve
terminal to uptake GABA and induce the increasing of GABA receptor, thereby
enhance GABA-mediated postsynaptic inhibition.
Pharmacologic properties and Clinical application
 Anti-epileptic：It can be used for partial seizures and tonic/clonic seizures, but not for
other generalised seizure types.
 Peripheral neuralgia：cranial nerve, ischiadic nerve and cranial nerve.
 Arrhythmia : membrane-stabilizing action.
Adverse effects







Digestive system
Gingival hyperplasia
Nervous system
Hematological system
Skeletal system
Allergic response
Others
VII. Phenobarbital
Mechanism of action
a. Phenobarbital can inhibit the paradoxical discharge of epilepsy focus selectively,
enhance stimulation of surrounding tissues and block discharge diffuse to normal
tissues.
b. Phenobarbital facilitate GABA-mediated inhibition of neuronal activity.
Pharmacologic properties
 Phenobarbital can be used for all types of epilepsy. The effects by turns are:
grand mal and status epileptics＞local psychomotor seizure＞petit mal.
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 Take effect rapidly（1～2 hr), the first choice of grand mal.
 Prevent convulsive and eliminate precursory symptom.
Adverse effects
 Somnolence、depression.
 Tolerance develops after long-term treatment.
VIII. Other Antiepileptic Drugs such as Primidone, Ethosuximide, Diazepem,
Nitrazepem, Sodium Valproate and Carbamzepine
IX.
Principle of Medication
 1～2 times/year，no drugs are needed
 Grand pit (first choice): Sodium phenytoin or phenobarbital, carbamzepine,
Primidone.
 Petit mal (first choice): Ethosuximide, clonazepam and sodium valproate.
 Status epilepticus:Diazepam or sodium phenytoin (IV), phenobarbital, diazepam,
clonazepam.
 Psychomotor: Sodium phenytoin or combine with
desoxybarbital or
carbamazepine.
X. Anticonvulsant Drugs
 Convulsions are involuntary skeletal muscular contractions. Convulsions can
arise from pathological processes within or outside the brain, toxins, drug
overdose, or withdrawal from drug dependence.
 Commonly used anticonvulsant drugs are sedative and hypnotic drugs.
Magnesium Sulfate is also used on this disease.
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