Classification
of Seizure or Epilepsy—
Partial seizure—
|
§
Simplex
§
Complex
§
Partial seizure
secondarily generalized
|
Generalized seizure—
|
§
Tonic-clonic (grand
mal)
§
Absence (petit
mal)—children mostly
§
Tonic
§
Atonic
§
Clonic and myoclonic
§
Infantile spasms
|
Classification
of Anti-Epileptic drugs—
Hydantoin group—
|
§
Phenytoin
§
Mephenitoin
|
|
Iminostilbene group—
|
§
Carbamazepine
§
Oxcarbazepine
|
|
Barbiturates and
Benzodiazepines—
|
§
Phenobarbitone
§
Mephobarbitone
§
Diazepam
|
§
Clonazepam
§
Lorazepam
|
Desoxybarbiturates—
|
§
Primidone
|
|
Valproic acid group—
|
§
Sodium Valproate
|
Anti-seizure
drugs act by—
§
Blocking the Na+
channel
§
Blocking the Ca++
channel
§
Blocking the excitatory
neurotransmitters and ↑ the activity of inhibitory neurotransmitter
(GABA)
*** cognitive
function of the rain means the intelligence function of the brain
Principle
of Mechanism of Action of Anti-Epileptic drugs—
In
general, voltage dependent Na-channel enter an inactive state following each
action potential. Prolongation of this inactive state with prolongation of the
refractory period is the principle of mechanism of action of—
o
Phenytoin
o
Carbamazepine
o
Lamotrizine
o
Sodium Valproate
o
Topiramate
§
A low threshold calcium
current govern oscillatory response in thalamic neuron. Some drugs like Ethosuccimide
or Dimethadione cause low threshold of the calcium current.
§
Some drugs affect
synaptic transmission. Drugs like Benzodiazepines, Barbiturates and possibly Topiramate
enhances GABA mediated inhibition.
§
Some drugs like GABA Pentine,
Vigabatrin acts by decreasing reuptake or decreasing metabolism of GABA.
§
Some drugs act on
excitatory Glutamatergic neurotransmission, they block Glutamatergic AMPA
receptor. Drugs of this group are Phenobarbitone, Topiramate.
§
Drugs like Rimacemide
block the NMDA receptor. NMDA is N-methyl Daspertate, it is one of the subtype
of glutamate and aspartate.
Note—strong
stimulation of NMDA receptor lead to neuronal death and NMDA agonist can save
the neuron from anoxia.
Comparison between Phenytoin and Carbamazepine—
Phenytoin
|
Carbamazepine
|
1.
It is a Hydantoin
group
|
1.
It is an Iminostilbene
group
|
2.
Used in both
generalized and partial epilepsy
|
2.
Preferred drug in
partial seizure but also highly effective in generalized seizure
|
3.
After absorption about
95% is bound to plasma protein
|
3.
About 70-75% is bound
with plasma protein
|
4.
It is available in
oral and parenteral form
|
4.
It is available only
in oral form
|
5.
Does not cause
auto-induction of it’s metabolism
|
5.
Causes auto-induction
of its metabolism
|
6.
The main mode of
action of Phenytoin is to inhibit Na+ influx across neuronal cell
membrane in epileptic foci
|
6.
Mechanism of Action
appears to be same as that of Phenytoin
|
7.
Sedation occurs at
considerably higher therapeutic dose
|
7.
Usually not sedative
in its therapeutic use
|
8.
More risk of cognitive
impairment
|
8.
Least risk of
cognitive impairment
|
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