This document discusses epilepsy and antiepileptic drugs. It defines epilepsy as a neurological disorder involving periodic abnormal brain activity. There are several types of epilepsy classified by the affected brain region. Antiepileptic drugs are classified based on the type of epilepsy they treat. Several common antiepileptic drugs are discussed, including their mechanisms of action, therapeutic uses, dosages, and adverse effects. Status epilepticus, a medical emergency involving prolonged or repeated seizures, is also covered.

1. EPILEPSY AND
ANTIEPILEPTIC DRUGS
BY
PRIYA SHETE
ASSISTANT PROFESSOR
NAGPUR COLLEGE OF PHARMACY

2. Epilepsy is a neurological disorder.
Epilepsy is a periodic disarrythmia of the brain.
Depending on the area of brain involved, epilepsy is classified into the
following classes:
1) Grandmal Epilepsy (Major Epilepsy):-
A sudden loss of consciousness and major convulsion (a sudden, violent,
irregular movement of the body, caused by involuntary contraction of muscles)
consisting of tonic spasm of the whole body followed by synchronous clonic jerking
(jerking of the body) convulsion are followed by generalized CNS depression.
2) Temporal Lobe Epilepsy:-
It consist of sudden attack of altered emotional behavior and convulsions are
absent.

3. 3) Focal Cortical or Jacksonian Epilepsy:-
It consist of convulsion of single limb or a group of muscle depending on the
cortical area involved.
4) Minor Epilepsy:-
It consist of sudden loss of consciousness without convulsions.
5) Petitmal Epilepsy:-
It consist of impairment of consciousness associated with bilateral clonic, motor
activity such as eyelid blinking.
6) Myoclonic Type Epilepsy:-
It consist of isolated clonic jerk.
7) Hypsarrythmia:-
It occur in infants and consist of falling spell, head droping and myoclonic jerk.
(Myoclonus refers to a quick, involuntary muscle jerk)

4. Classification of Antiepileptic Drugs:
1) Drug used in Grandmal Epilepsy:
E.g. Phenytoin, Methoin, Phenobarbitone, Primidone, Carbamazepine.
2) Drug used in Petitmal Epilepsy:
E.g. Tridione, Paradione, Phensuximide, Ethosuximide.
3) Drug effective in Psychomotor Epilepsy:
E.g. Phenytoin, Primidone, Tridione.
4) Focal Cortical or Jacksonian Epilepsy:
E.g. Phenytoin, Methoin, Phenobarbitone,Primidone.
5) Status Epilepticus:
E.g. Paraldehyde, Thiopentone, Diazepam.

5. Phenytoin Sodium or Diphenyl Hydantoin:
Pharmacological Action:
 It inhibit the threshold of seizure (a sudden attack of illness, especially a stroke or
an epileptic fit) discharge in the brain.
 It depress neuronal sodium concentration which lead to reduction in P.T.P. (Post
Tetanic Potentiation).
 P.T.P. means enhancement of synaptic transmission (It is the biological process by
which a neuron communicates with a target cell across a synapse) which followed
the repeated tetanic high frequency stimulation of pre synaptic fibres.
 P.T.P is responsible for spread of epileptic seizure over the brain.
 Phenytoin causes exit of sodium from cerebral neuron and hence stabilize the cell
membrane for membrane stabilising action.

6. Adverse Effect:-
• Intolereance such as skin rash may occur.
• Vertigo (a sensation of whirling and loss of balance, associated
particularly with looking down from a great height)
• Ataxia (the loss of full control of bodily movements)
• Nystagmus(rapid involuntary movements of the eyes)
• Disarrythmia (abnormality in a physiological rhythm, especially in the
activity of the brain or heart)

7. Therapeutic Uses:-
It is used in treatment of
• Grandmal Epilepsy
• Temporal Lobe Epilepsy
• Focal Cortical Epilepsy
• Cardiac Arrythmia.

8. Methoin:
 It is a Phenytoin derivative.
The dose of these drug given according to the need of patients from 0.12g
twice or thrice a day to 0.4g.
 It is available in 100 mg.
 Phenytoin does not raising the convulsive threshold in normal animal
 Mesantoin is capable of raising normal or experimentally lowered electric
shock convulsive threshold in animal.
 It is more sedative than phenytoin sodium but less than phenobarbitone.

9. Toxicity:-
• Skin Rashes
• Blood dyscrasias ( it meant an imbalance of four body fluids: blood, bile,
lymph, and sputum)
• Hepatic injury
• Weakness
• Nausea
• Jaundice
• Sore Throat
• Bleeding.

10. Barbiturates:-
 It increases the seizure threshold.
 It is used for all epilepsy condition except petitmal epilepsy.
 Combination of phenytoin and phenobarbitone is used in treatment of
grandmal epilepsy and other epileptic seizure
 Phenobarbitone reduces the spread of abnormal electrical activity.
 It increases post synaptic responses to the inhibitor transmitter GABA.

11. Carbamazepine:-
 It is an anticonvulsant.
 The mechanism of action for epileptic activity is same to that of
phenytoin
 It prevent the spread of seizure discharge and elevate the seizure
threshold.
 It is also effective in prophylactic treatment of tonic-clonic seizure
 It is also used to treat pain associated with trigeminal neuralgia.

12. Primidone:-
 It is structurally related to phenobarbitone and it contain anticonvulsant activity.
 It is useful in prophylactic control of generaalised tonic-clonic,temporal lobe and
focal cortical epilepsy.
 It is used in combination with phenytoin therapy.
Tridione:-
 It is a white crystalline powder a faint balsamic odour and soluble in 5% water to
form a neutral solution.
 It is detoxicated in liver and excreted in urine
Dose:
1 to 2g daily in divided dose.
It is given orally in capsule

13. Anticonvulsant Action:-
• It is efficient to suppress the leptazol convulsions.
• The elctroconvulsive threshold in experimental animal is elevated by
troxidone.
• Troxidone and its methyl derivative are specific in petitmal which is ordinarily
difficult to control.
Untoward Effect:-
• Photophobia(day blindness)
• Nausea
• Skin rash
• Aplastic anaemia

14. Suximides:-
 Phensuximides is an anticonvulsant
 It antagonizes the leptazol convulsion in rats.
 It is specifically used in petitmal epilepsy.
Toxic Effects:-
• Nausea
• Vomitting
• Skin eruptions
• Drowsiness
• Muscular weakness

15. Ehosuximide:-
 Methsuximide are recently added drug which is used in treatment of petitmal
epilepsy.
 It can induce serious bone marrow and renal damage.
 Ethosuximide are less toxic and use in combination with phenobarbitone and
phenytoin.

16. Diazepam:-
 The muscle relaxation can be occur by diazepam because it depress
the CNS.
 It increase the seizure threshold and act as anticonvulsant.
 If diazepam given parentrally then it block the convulsion induced by
chemical and electrical stimuli in animal.
 The drug act on neuron containing GABA which is responsible for
anticonvulsant action of drug.

17. Status Epilepticus:-
 It consist of severe prolonged seizure or repeated grandma seizure without
recovery of consciousness between the attacks.
 It is a medical emergency and the patient must be hospitalized for proper
treatment.
 In treatment of controlling seizure diazepam given intravenously.
 If convulsion cannot treated with diazepam then the phenytoin is administered
intravenously.
 If convulsion still persist then paraldehyde or halothane should be used.

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