L11- Anti-epileptics (MOA, AEs) Flashcards

1
Q

what are the general MOAs of Anti-epileptic drugs, include subtypes

A

1) Blockade of V-gated ion channels
- Na+ V-gated channels
- T-type Ca++ channels

2) Modulation of synaptic transmission
- enhance GABA neurotransmission
- reduce Glutamate neurotransmission

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2
Q

list the anti-eplileptics that block Na V-gated channels

A
  • phenytoin
  • carbamazepine, oxcarbazepine
  • lamotrigine
  • zonisamide
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3
Q

list the anti-epileptics that block T-type Ca channels

A

-phenobarbital
-valproate
-topiramate
(ethosuximide)

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4
Q

Absence Seizures:

  • (1) is the main neuronal activity involved
  • (2) is the necessary mechanism for prevention and treatment, and (3) are the drugs with (2)
A

1- oscillatory neuronal activity between thalamus and cortex

2- blockade of T-type Ca channels; they’re responsible for oscillatory responses in thalamic neurons

3- valproate, ethosuximide

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5
Q

agents affecting GABA neurotransmission:

  • (1) have direct GABA receptor actions
  • (2) inhibits GABA degradation (include enzyme)
  • (3) inhibits GABA reuptake
A

1- benzodiazepines, barbiturates, topiramate

2- Vigabatrin inhibits GABA aminotransferase

3- Tiagabine

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6
Q

describe the subtle difference in action of benzodiazepines and barbituates

A

Benzodiazepines: inc frequency of GABA channel opening (Ben likes it more often)

Barbituates: inc time GABA channels are open (Barb likes it longer)

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7
Q

agents affecting GABA neurotranmission:

  • (1) block glutamate receptors
  • (2) dec glutamate release from neurons by blocking (3)
  • (4) binds to synaptic vesicle unit, (5), to prevent release of glutamate- exact mechanism is unknown
A

1- phenobarbital, topiramate

2- gabapentin, pregablin
3- blocking V-gated Ca channels (prevents Ca influx and vesicle release)

4- levetiracetam
5- SV2A- synpatic vesicle glycoprotein 2A

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8
Q

______ are the cytochrome P450 inducers

A
  • carbamazepine (oxcarbazepine is weak inducer)
  • phenobarbital
  • phenytoin
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9
Q

list the AEs for valproate

A

(all liver effects)

  • hepatotoxicity
  • inhibits cytochrome P450 –> inhibits metabolism of itself and other drugs
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10
Q

list the AEs for phenytoin

A
  • diplpia, ataxia
  • gingival hyperplasia
  • hirsuitism
  • rash + Steven-Johnson syndrome

-coarsening of facial features in children

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11
Q

list the drugs with zero order kinetics

A

phenytoin, aspirin, ethanol

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12
Q

list the AEs for carbamazepine

A
  • aplastic anemia
  • agranulocytosis

-rash + Steven-Johnson

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13
Q

define Steven-Johnson syndrome

A

life-threatening disease consisting of mucosal changes w/ sloughing (reaction to disease or drug)

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14
Q

list the anti-epileptics with high risk for Steven-Johnson syndrome

A
  • phenytoin
  • lamotrigine
  • carbamazepine
  • phenobarbital
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15
Q

list the AEs for lamotrigine

A

rash + Steven-Johnson syndrome (black-box warning)

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16
Q

list the AEs for phenobarbital, which is a metabolite of ______

A

Primidone –> metabolizes into phenobarbital

  • sedation, drowsiness
  • cognitive impairment, hyperactivity
  • rash + Steven-Johnson syndrome
  • tolerance, dependence
  • P450 inducer
17
Q

list AEs for vigabatrin

A

visual field loss

18
Q

list AEs for felbamate

A
  • aplastic anemia
  • hepatotoxicity

2nd line for refractory epilepsy

19
Q

______ is the biggest risk with anti-epileptic overdoses

A

(rarely lethal)

respiratory depression –> requires supportive Tx

20
Q

______ is a teratogen with anti-folate effects

A

Valproate- effects are null with folic acid supplementation

21
Q

______ is a key effect of anti-epileptic needed to be monitored during pregnancy / child-birth

A

anti-epileptics –> inc vitK degradation in fetus –> bleeding in newborn – fixed with IM vitK at birth

22
Q

list the anti-epileptics effective at treating neuropathic pain

A

carbamazepine
gabapentin
pregablin

23
Q

list the anti-epileptics effective at treating bipolar disorder

A

carbamazepine
lamotrigine
valproate

24
Q

list the anti-epileptics effective at treating migraines

A

topiramate

valproate

25
Q

______ is 1st line treatment for essential tremor

A

primidone (+ propanolol)