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Dr. Nadira Sultana
Pharm.d
 Epilepsy is collective term applied for
group of convulsive disorder.
 It is disorder in which the nerve cell
activity in the brain is disturbed ,
causing seizures
1. Loss or disturbance of consiousness
2. Characterised body movements
3. Autonomic hyperactivity
HYDANTOIN PHENYTOIN
BARBITURATES PHENOBARBITONE
PRIMIDONE
IMINOSTILBENES CARBAMAZEPINE
SUCCINIMIDE ETHOSUXIMIDE
ALIPHATIC CARBOXYLIC ACID SODIUM VALPROATE
BENZODIAZEPINES CLONAZEPAM
CLOBZAM
DIAZEPAM
NEWER ANTILEPTICS LAMOTRIGINE
GABAPENTINE
VIGABATRIN
 PHENYTOIN is imp derivative
 It acts by
normalizing seizures
reducing sodium conc in brain cell which leads to
decrease in post tetanus potentiation
 Absorbtion :well on oral
 Onset of action slow , duration of action long
 Metabolism through enterohepatic circulation
 Excretion :urine within 48hours
 CNS: giddiness,tremors,headache,insomnia, drowsiness
 GIT: nausea ,vomiting, anorexia
 RASHES: urticaria(hives), scarlantiform, measles like rashes
 GUMS: swelling, bleeding and gingivitis
 FOETAL HYDANTOIN SYNDROME: cleft palate , hair lip
and microcephaly in the foetus
 OTHERS : hepatitis, jaundice, megaloblastic anemia ,
lymphadenopathy
 Dose : 100mg TID by oral and gradually
increase to 500mg
 Use
grand mal, psychomotor epilepsy and
cardiac arrhythmias
 PHENOBARBITONE
 Use
grand mal, focal cortical and psychomotor epilepsy
 not use in petitmal epilepsy
 Sudden withdrawal increases the frequency of
convulsions..gradually substituted by phenytoin
 DOSE : 60-80mg divided doses
 ADR: drowsiness, depression , lethargy
 Tricyclic compound
 Structural similar imipramine(anti depressant drug)
 More effective in temporal epilepsy and grand mal
epilepsy
 Remarkably effective in trigeminal neuralgia and
glossopharyngeal neuralgia
 Absorbtion : slow
 Bioavailibility : 90%
 Dose :100mg BD tablet ..gradually increase upto
600-1200mg per day for temporal epilepsy
 Anorexia, nausea, vomiting, giddiness, skin
rashes, diplopia , blurred vision,
agranulocytosis , peripheral neuritis , aplastic
anemia
 Ethosuximide
 Use: petitmal epilepsy
 Orally effective
 ADR :anorexia, nausea , vomiting , drowziness
 Dose: initial 250mg per day gradually increase by
250mg each week to 750-1000mg
 Highly effective in petitmal
 Ineffective in focal cortical and temporal epilepsy
 Mechanism
inhibition of gamma aminobutyrate transaminase
potentiation of post synaptic GABA activity
 Absorbtion: complete after oral
 Metabolised : liver 90%
 ADR: nausea , vomit, hepatic damage, sedation, ataxia,
spina bifida
 Dose ;600mg to 1600mg per day orally
 It is benzodiazepine compound
 Effective in petitmal and myoclonic seizures
 It acts by increasing effect of GABA in CNS
 Treating grandmal –can be used with
phenytoin or phenobarbitone.
 ADR: drowsiness, ataxia, personality changes,
tremor, vertigo ,confusion
 Emergency drug for status epilepticus and
tetanus
 Used i.v
LAMOTRIGINE
 It is phenyltriazine compound
 It acts by blocking Na+ and preventing
release of glutamate
 Used in add on drug in resistant patient
 ADR : sleepiness, dizziness, diplopia, ataxia
and vomit
 It is an GABA agonist
 Highly lipid soluble
 Does not act on GABA receptors but acts on releasing GABA
 Well absorb orally
 Excret unchanged in urine
 Adr : mid sedation, tiredness , dizziness
 Use: partial seizure resistant to other drugs
 It is GABA transaminase inhibitor which acts
by increasing synaptic GABA concentration
 Well absorb orally , excrete unchanged in
urine
 Use : refractory epilepsy
 Adr : weight gain, drowsiness , depression ,
diplopia

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Drugs used in epilepsy.pptx by dr. nadira sultana

  • 2.  Epilepsy is collective term applied for group of convulsive disorder.  It is disorder in which the nerve cell activity in the brain is disturbed , causing seizures
  • 3. 1. Loss or disturbance of consiousness 2. Characterised body movements 3. Autonomic hyperactivity
  • 4. HYDANTOIN PHENYTOIN BARBITURATES PHENOBARBITONE PRIMIDONE IMINOSTILBENES CARBAMAZEPINE SUCCINIMIDE ETHOSUXIMIDE ALIPHATIC CARBOXYLIC ACID SODIUM VALPROATE BENZODIAZEPINES CLONAZEPAM CLOBZAM DIAZEPAM NEWER ANTILEPTICS LAMOTRIGINE GABAPENTINE VIGABATRIN
  • 5.  PHENYTOIN is imp derivative  It acts by normalizing seizures reducing sodium conc in brain cell which leads to decrease in post tetanus potentiation  Absorbtion :well on oral  Onset of action slow , duration of action long  Metabolism through enterohepatic circulation  Excretion :urine within 48hours
  • 6.  CNS: giddiness,tremors,headache,insomnia, drowsiness  GIT: nausea ,vomiting, anorexia  RASHES: urticaria(hives), scarlantiform, measles like rashes  GUMS: swelling, bleeding and gingivitis  FOETAL HYDANTOIN SYNDROME: cleft palate , hair lip and microcephaly in the foetus  OTHERS : hepatitis, jaundice, megaloblastic anemia , lymphadenopathy
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  • 11.  Dose : 100mg TID by oral and gradually increase to 500mg  Use grand mal, psychomotor epilepsy and cardiac arrhythmias
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  • 13.  PHENOBARBITONE  Use grand mal, focal cortical and psychomotor epilepsy  not use in petitmal epilepsy  Sudden withdrawal increases the frequency of convulsions..gradually substituted by phenytoin  DOSE : 60-80mg divided doses  ADR: drowsiness, depression , lethargy
  • 14.  Tricyclic compound  Structural similar imipramine(anti depressant drug)  More effective in temporal epilepsy and grand mal epilepsy  Remarkably effective in trigeminal neuralgia and glossopharyngeal neuralgia  Absorbtion : slow  Bioavailibility : 90%  Dose :100mg BD tablet ..gradually increase upto 600-1200mg per day for temporal epilepsy
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  • 17.  Anorexia, nausea, vomiting, giddiness, skin rashes, diplopia , blurred vision, agranulocytosis , peripheral neuritis , aplastic anemia
  • 18.  Ethosuximide  Use: petitmal epilepsy  Orally effective  ADR :anorexia, nausea , vomiting , drowziness  Dose: initial 250mg per day gradually increase by 250mg each week to 750-1000mg
  • 19.  Highly effective in petitmal  Ineffective in focal cortical and temporal epilepsy  Mechanism inhibition of gamma aminobutyrate transaminase potentiation of post synaptic GABA activity  Absorbtion: complete after oral  Metabolised : liver 90%  ADR: nausea , vomit, hepatic damage, sedation, ataxia, spina bifida  Dose ;600mg to 1600mg per day orally
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  • 21.  It is benzodiazepine compound  Effective in petitmal and myoclonic seizures  It acts by increasing effect of GABA in CNS  Treating grandmal –can be used with phenytoin or phenobarbitone.  ADR: drowsiness, ataxia, personality changes, tremor, vertigo ,confusion
  • 22.  Emergency drug for status epilepticus and tetanus  Used i.v LAMOTRIGINE  It is phenyltriazine compound  It acts by blocking Na+ and preventing release of glutamate  Used in add on drug in resistant patient  ADR : sleepiness, dizziness, diplopia, ataxia and vomit
  • 23.  It is an GABA agonist  Highly lipid soluble  Does not act on GABA receptors but acts on releasing GABA  Well absorb orally  Excret unchanged in urine  Adr : mid sedation, tiredness , dizziness  Use: partial seizure resistant to other drugs
  • 24.  It is GABA transaminase inhibitor which acts by increasing synaptic GABA concentration  Well absorb orally , excrete unchanged in urine  Use : refractory epilepsy  Adr : weight gain, drowsiness , depression , diplopia