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PHPY 305 > 6. Antiepileptic Drugs > Flashcards

6. Antiepileptic Drugs Flashcards

1
Q

What are seizures?

Symptoms?

A

Seizures are sudden, excessive, and synchronous discharges of neurons
10% of pop will have 1 seizure in life
Epilepsy has a bimodal distribution: more common in early childhood and in elderly
GABA receptor major in these ones
Can create a recurring circuit if you get one seizure

The abnormal electrical activity may result in:
Transient loss of consciousness, abnormal movements (overstim of area of brain involved with movements), atypical or odd behaviour, distorted perception

Slide 5

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2
Q

What is the first (1 of 2) type of seizures: partial/focal (onset)?

A

Happening in a distinct area of brain

  • simple partial, partial sensory seizure
  • aura (can sense something)
  • complex partial, temporal lobe seizure
  • secondarily generalized

All AEDs are effective except ethosuximide

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3
Q

What is the second (2 of 2) type of seizures: generalized (onset)?

A 
No aura (can’t sense somethings up)
Incorporate much of brain if not all of it
- generalized tonic clonic (GTC)
- tonic/atonic 
- absence (go blank)
- myoclonic

AED options are more limited (want to be more selective, if you suppress some areas too much you can kill the patient)

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4
Q

What are the 11 drugs used for partial seizures (simple, complex, secondarily generalized)(has

A 
Carbamazepine
Lacosamide
Oxcarbazepine
Phenytoin 
Phenobarbital
Primidone
Tiagabine
Vigabatrin 
Gabapentin
Pregabalin 
Ezogabine
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5
Q

What are the 6 drugs used for generalized and partial onset seizures?

A 
Felbamate
Lamotrigine
Levetiracetam
Topiramate
Valproate
Zonisamide
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6
Q

What is the one drug used for absence seizures?

A

Ethosuzimide

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7
Q

What are the 6 mechanisms of actions of all the antiepileptics?

A
  1. Voltage gated sodium channels- blockade of fast inactivated channels (slow inactivation phase)
  2. Potentiation of GABAergic mechanisms- reduce likelihood you reach AP
  3. Blockade of calcium channels- block Ca channels, block neurotransmitter release, lower seizure activity
  4. Blockade of glutamate receptor channels (NMDA, AMPA)- NMDA are ones that can drive cell death, AMPA does not (they recruit NMDA)
  5. Opening of voltage gated potassium channels- potassium rushes out and quickly repolarizes membrane potential
  6. Antagonism of exocytosis

Slide 7-21

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8
Q

Which drugs use the first (1) mechanism: voltage gated sodium channels?

A 
Partial seizures:
Carbamazepine (1)
Lacosamide (1)
Oxcarbazepine (1)
Phenytoin (1)
Phenobarbital (1, 2)

Generalized and partial onset seizures:
Lamotrigine (1)
Valproate (1, 2, 3, 5)
Zonisamide (1, 3)

Absence seizures:
None

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9
Q

Which drugs use the second (2) mechanism: potentiation of GABAergic mechanisms?

A 
Partial seizures:
Phenobarbital (1, 2) - barbiturate
Primidone (2) - barbiturate
Tiagabine (2) 
Vigabatrin (2)

Generalized and partial onset seizures:
Felbamate (2, 4)
Topiramate (2, 4)
Valproate (1, 2, 3, 5)

Absence seizures:
None

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10
Q

Which drugs use the third (3) mechanism: blockade of calcium channels?

A

Partial seizures:
Gabapentin (3)
Pregabalin (3)

Generalized and partial onset seizures:
Valproate (1, 2, 3, 5)
Zonisamide (1, 3)

Absence seizures:
Ethosuzimide (3)

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11
Q

Which drugs use the fourth (4) mechanism: blockade of glutamate receptor channels (NMDA, AMPA)?

A

Partial seizures:
None

Generalized and partial onset seizures:
Felbamate (2, 4)
Topiramate (2, 4)

Absence seizures:
None

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12
Q

Which drugs use the fifth (5) mechanism: opening of voltage gated potassium channels?

A

Partial seizures:
Ezogabine (5)

Generalized and partial onset seizures:
Valproate (1, 2, 3, 5)

Absence seizures:
None

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13
Q

Which drugs use the sixth (6) mechanism: antagonism of exocytosis?

A

Partial seizures:
None

Generalized and partial onset seizures:
Levetiracetam (6)

Absence seizures:
None

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14
Q

What are the 4 antiepileptics not metabolized by hepatic enzymes?

A

Gabapentin
Pregabalin
Vigabatrin
Levetiracetam

These are excreted by kidney

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15
Q

How are drug interactions possible with these drugs?

A

By blocking antiseizure drug metabolism
By displacing the drugs from plasma proteins binding sites (increase potency)
Induction of antiseizure drug metabolism (by rifamipin or other antiseizure meds) (decreases potency)

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16
Q

What are the 3 liver P450 enzyme inducers?

A

Phenytoin
Phenobarbital
Carbamazepine

Slide 25

17
Q

What is the ideal treatment of epilepsy?

A 
Effective (in all seizure types)
No adverse effects 
No long term risks 
No interactions with other drugs
Long lasting action
Safe in pregnancy 
Inexpensive 
Start 1 AED, low, go slow
Taper slowly
If adding 2nd AED, add one with second mechanism of action
Always add folate in pregnancy

PHPY 305 (24 decks)

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