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ANTI-EPILEPTIC DRUG
SAWAN….???   EPILEPSY…????
                                   SEIZURE…????




                         FIT…???
Objectives
• To know types of drugs used in treating
  seizure/epilepsy
• To know the pharmacological actions of the
  drugs
• To know the effects of drugs on the specific
  functions of the system
Seizure
• 2nd neurologic disorder after stroke in US
• brief episodes of brain dysfunction resulting from
  abnormal electrical activity of cerebral neurons
  causing involuntary movement, sensations or
  thoughts
• Causes: diseases, infection, head injury, heredity etc
• Epilepsy- chronic seizure (abnormal & excessive
  electrical discharges of nerve cells)
Seizure
• A seizure occurs when the brain's nerve cells
  misfire and generate a sudden, uncontrolled surge
  of electrical activity in the brain
• During a seizure, each cell may fire as many as 500
  times a second, much faster than the normal rate
  of about 80 times a second in the brain and spinal
  cord.
CLASSIFICATION OF
                                  SEIZURES




Generalized seizures                    Partial seizures

Begin in one area of the brain &            Begin in a specific area of the
rapidly spread throughout both              brain & often indicate a localized
hemispheres of the brain                    brain lesion such as birth injury,
                                            trauma, stroke or tumor
PARTIAL SEIZURES                       GENERALIZED
                                         SEIZURES

                              - Tonic-clonic / major motor seizure
                                              (common)
                            • Tonic – involves contraction of skeletal
- Simple partial seizures                      muscles
   (consciousness is not     • Clonic – rapid rhythmic & symmetric
                                  jerking movements of the body
         affected)
                            - Absence seizure (abrupt alterations in
   - Complex partial
                                consciousness, lasts few seconds; etc
     seizures (level of               blank, staring expression
     consciousness is            with/without blinks of the eyelids)
        decreased)             - Myoclonic type ( contraction of a
                                    muscle or group of muscles)
                            - Akinetic type (absence of movement )
                                        - Mixed seizures
CAUSES OF SEIZURES




  CHILDREN           MIDDLE YEARS          ELDERLY




• Birth traumas
                  • Head injuries      • Brain tumors
• Infections
                  • Infections         • Strokes
• Congenital
                  • Alcohol
  abnormalities
                    stimulant drugs
• High fevers
                  • Medication side
                    effects
Antiepileptic / Antiseizure Drugs

Tonic-clonic &                        Myoclonic
                   Absence seizures                     Others
partial seizures                       seizures




Carbamazepine         Ethosuximide                  Levetiracetam
                        (Zarontin)    Clonazepam
   (Tegrefol)                                          (Keppra)
                      Valproic acid    (Klonopin)
  Phenytoin                                          Gabapentin
   (Dilantin)          (Depakene)                    (Neurontin)
Pharmacokinetic
• Slightly soluble; good absorption; 80-100%
  dose reaching circulation
• Not highly bound to protein plasma
• Cleared by hepatic mechanism; active
  metabolites cleared by liver
• Medium-to long acting
Carbamazepine (Tegrefol)

• Strong inducing agent; therefore many drug
  interactions
• It is given orally
• It is metabolized in the liver
• Contraindicated in patients with previous bone
  marrow depression
Phenytoin (Dilantin)
• Use for patients with tonic-clonic seizures and
  some partial seizures
• Acts to promote intracellular removal of
  sodium during the refractory period
• Antagonism (blocking) of Na+ channels to
  reduce excitability
• Antagonism of Ca++ channels
• Adverse effects: CNS (ataxia, drowsiness) &
  GIT (nausea, vomiting)
Ethosuximide (Zarontin)
• The main drug used to treat absence seizures,
  may be uses with other AEDs for treatment of
  mixed seizures
• Adverse effects: nausea and anorexia. (mental
  disturbances)
Clonazepam (Klonopin)
• Act by potentiating the actions of GABA causing
  neurotransmission inhibition (primarily in the
  CNS)
• Can be used to induce sleep (high dose),
  anticonvulsant therapy and reduction in muscle
  tone.
• Adverse effects: drowsiness, fatigue, dizziness,
  muscle hypotonia, co-ordination disturbances;
  also poor concentration, restlessness, confusion,
  amnesia
Valproic acid (Depakene)
• Thought to enhance the effects of GABA in the
  brain
• Used to treat manic reactions in bipolar
  disorder & to prevent migraine headaches
• Extensively metabolised in the liver
• Rapidly transported across the blood brain
  barrier
• Adverse effects: Nausea, vomiting, anorexia,
  abdominal pain, diarrhoea & weight gain
Gabapentin (Neurontin)
• Incompletely absorbed in the gut
• Acts via:
   – Increased synthesis and release of GABA
   – Decrease degradation of GABA
   – Inhibition of Ca++ channels

• Adverse effects:
   – CNS effects (dizzy, drowsy, fatigue, headache, double
     visions)
   – Nausea and vomiting
• Contraindication: be careful with sudden withdrawal in
  the elderly due to kidney effects and alterations in acid-
  base balance.
Side Effects
• Antiepileptic drugs frequently produce CNS and
  gastrointestinal side effects

• Some antiepileptic drugs infrequently cause severe
  hematologic or hepatic toxicity

• Valproate and phenytoin cause birth defects

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Drugs in epilepsy

  • 2. SAWAN….??? EPILEPSY…???? SEIZURE…???? FIT…???
  • 3. Objectives • To know types of drugs used in treating seizure/epilepsy • To know the pharmacological actions of the drugs • To know the effects of drugs on the specific functions of the system
  • 4. Seizure • 2nd neurologic disorder after stroke in US • brief episodes of brain dysfunction resulting from abnormal electrical activity of cerebral neurons causing involuntary movement, sensations or thoughts • Causes: diseases, infection, head injury, heredity etc • Epilepsy- chronic seizure (abnormal & excessive electrical discharges of nerve cells)
  • 5. Seizure • A seizure occurs when the brain's nerve cells misfire and generate a sudden, uncontrolled surge of electrical activity in the brain • During a seizure, each cell may fire as many as 500 times a second, much faster than the normal rate of about 80 times a second in the brain and spinal cord.
  • 6. CLASSIFICATION OF SEIZURES Generalized seizures Partial seizures Begin in one area of the brain & Begin in a specific area of the rapidly spread throughout both brain & often indicate a localized hemispheres of the brain brain lesion such as birth injury, trauma, stroke or tumor
  • 7. PARTIAL SEIZURES GENERALIZED SEIZURES - Tonic-clonic / major motor seizure (common) • Tonic – involves contraction of skeletal - Simple partial seizures muscles (consciousness is not • Clonic – rapid rhythmic & symmetric jerking movements of the body affected) - Absence seizure (abrupt alterations in - Complex partial consciousness, lasts few seconds; etc seizures (level of blank, staring expression consciousness is with/without blinks of the eyelids) decreased) - Myoclonic type ( contraction of a muscle or group of muscles) - Akinetic type (absence of movement ) - Mixed seizures
  • 8.
  • 9. CAUSES OF SEIZURES CHILDREN MIDDLE YEARS ELDERLY • Birth traumas • Head injuries • Brain tumors • Infections • Infections • Strokes • Congenital • Alcohol abnormalities stimulant drugs • High fevers • Medication side effects
  • 10. Antiepileptic / Antiseizure Drugs Tonic-clonic & Myoclonic Absence seizures Others partial seizures seizures Carbamazepine Ethosuximide Levetiracetam (Zarontin) Clonazepam (Tegrefol) (Keppra) Valproic acid (Klonopin) Phenytoin Gabapentin (Dilantin) (Depakene) (Neurontin)
  • 11. Pharmacokinetic • Slightly soluble; good absorption; 80-100% dose reaching circulation • Not highly bound to protein plasma • Cleared by hepatic mechanism; active metabolites cleared by liver • Medium-to long acting
  • 12. Carbamazepine (Tegrefol) • Strong inducing agent; therefore many drug interactions • It is given orally • It is metabolized in the liver • Contraindicated in patients with previous bone marrow depression
  • 13. Phenytoin (Dilantin) • Use for patients with tonic-clonic seizures and some partial seizures • Acts to promote intracellular removal of sodium during the refractory period • Antagonism (blocking) of Na+ channels to reduce excitability • Antagonism of Ca++ channels • Adverse effects: CNS (ataxia, drowsiness) & GIT (nausea, vomiting)
  • 14. Ethosuximide (Zarontin) • The main drug used to treat absence seizures, may be uses with other AEDs for treatment of mixed seizures • Adverse effects: nausea and anorexia. (mental disturbances)
  • 15. Clonazepam (Klonopin) • Act by potentiating the actions of GABA causing neurotransmission inhibition (primarily in the CNS) • Can be used to induce sleep (high dose), anticonvulsant therapy and reduction in muscle tone. • Adverse effects: drowsiness, fatigue, dizziness, muscle hypotonia, co-ordination disturbances; also poor concentration, restlessness, confusion, amnesia
  • 16. Valproic acid (Depakene) • Thought to enhance the effects of GABA in the brain • Used to treat manic reactions in bipolar disorder & to prevent migraine headaches • Extensively metabolised in the liver • Rapidly transported across the blood brain barrier • Adverse effects: Nausea, vomiting, anorexia, abdominal pain, diarrhoea & weight gain
  • 17. Gabapentin (Neurontin) • Incompletely absorbed in the gut • Acts via: – Increased synthesis and release of GABA – Decrease degradation of GABA – Inhibition of Ca++ channels • Adverse effects: – CNS effects (dizzy, drowsy, fatigue, headache, double visions) – Nausea and vomiting • Contraindication: be careful with sudden withdrawal in the elderly due to kidney effects and alterations in acid- base balance.
  • 18.
  • 19. Side Effects • Antiepileptic drugs frequently produce CNS and gastrointestinal side effects • Some antiepileptic drugs infrequently cause severe hematologic or hepatic toxicity • Valproate and phenytoin cause birth defects