Epilepsy Drugs (Segars) Flashcards

1
Q

AEDs

A

Antiepileptic Drugs; either decrease excitability neurotransmitters (glutamate) or increase inhibitory neurotransmitters (GABA)

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2
Q

What are the 4 classes of drugs that act on the presynaptic neuron to decrease the release of glutamate?

A
  1. Na+ VG channel blockers
  2. T-type Ca2+ channel blockers
  3. Synaptic Vesicle 2A (SV2A) protein inhibitors
  4. alpha-2-delta Ca2+ channel inhibitors
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3
Q

What “state” does the Na+ VG channel blockers work?

A

open state (inactivation gate and pore are both open)

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4
Q

What are the Na+ VG channel blockers?

A

Carbamazepine (Oxcarbaxepine/Eslicarbazepine)
Lamotrigine (LMT)
Phenytoin (Fosphenytoin; IV form)
Valproic acid (Divalproex/Valproate; IV form)
Lacosamide (Zonisoamide/Rufinamide)

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5
Q

Carbamazepine

A

AED; Na+ VG channel blocker that acts on the presynaptic neuron to decrease the release of glutamate; “state” and “use-dependent”

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6
Q

Lacosamide

A

AED; Na+ VG channel blocker that acts on the presynaptic neuron to decrease the release of glutamate; less “state” dependent than any of the other Na+ VG blockers

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7
Q

Phenytoin

A

AED; Na+ VG channel blocker that acts on the presynaptic neuron to decrease the release of glutamate; “state” and “use-dependent”; (Fosphenytoin; IV form)

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8
Q

Lamotrigine (LMT)

A

AED; Na+ VG channel blocker that acts on the presynaptic neuron to decrease the release of glutamate; “state” and “use-dependent”

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9
Q

What is the drug of choice for absence (petit Mal) seizures?

A

Ethosuximide; T-type Ca2+ channel blocker

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10
Q

What are the 2 T-type Ca2+ channel blockers?

A

Ethosuximide** (first choice) and Zonisamide

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11
Q

What agent would you use to treat a patient who presents with a seizure showing target cortex-thalamus oscillations with 3-Hz spikes and what is it’s MOA?

A

Ethosuximide** (first choice); t-type Ca2+ channel blockers on the presynaptic neuron

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12
Q

Ethosuximide

A

drug of choice for absence (petit Mal) seizures; t-type Ca2+ channel blockers on the presynaptic neuron

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13
Q

What are the two Synaptic Vesicle 2A (SV2A) protein inhibitors?

A

“acetame’s”
Levetiracetam and Brivaracetam

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14
Q

What are the two alpha-2-delta Ca2+ channel inhibitors?

A

Gabapentin and pregabalin

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15
Q

What are the 2 classes of drugs that act on the postsynaptic neuron to decrease the release of glutamate?

A
  1. AMPA receptor blockers
  2. NMDA receptor blockers
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16
Q

What are the two AMPA receptor blockers?

A

Perampanel (PerAMPAnel) and Topiramate

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17
Q

Perampanel

A

AMPA receptor blocker that acts on the postsynaptic neuron to decrease the effects of glutamate

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18
Q

What is the one NMDA receptor blocker?

A

Felbamate

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19
Q

A patient has been observed staring into space periodically and is thought to be suffering from a type of motor seizure. What is the suspected diagnosis and treatment?

A

absence (petit Mal) seizures; Ethosuximide** (first choice); t-type Ca2+ channel blockers on the presynaptic neuron

20
Q

What class of AED(s) acts on both pre and postsynaptic neurons to decrease glutamate release?

A

OPEN K+ channels - Ezogabine

21
Q

Ezogabine

A

AED that OPENs K+ channels on both pre and postsynaptic neurons to decrease glutamate release

22
Q

What are the 3 classes of drugs that block GABA re-uptake or metabolism?

A
  1. Stimulate GAD - Valproic acid, Gabapentin and Pregabalin
  2. Inhibit GABA-T - Vigabatrin and Valproic acid
  3. Inhibit GAT-1 - Tiagabine
23
Q

What are the two ways AEDs enhance inhibitory (GABA) actions?

A
  1. Block GABA re-uptake or metabolism
  2. Potentiate GABA receptor Cl- currents
24
Q

What 3 drugs Stimulate GAD to enhance inhibitory (GABA) actions?

A

Valproic acid, Gabapentin and Pregabalin

25
Q

What drug is used to inhibit GABA-T to enhance inhibitory (GABA) actions?

A

Vigabatrin and Valproic acid

26
Q

Tiagabine

A

AED used to inhibit GABA-T from transferring GABA back into the presynaptic neuron

27
Q

Which drugs are used to inhibit GAT-1 to enhance inhibitory (GABA) actions?

A

Vigabatrin and Valproic acid

28
Q

Vigabatrin

A

AED used to inhibit GAT-1 to enhance inhibitory (GABA) actions in the presynaptic neuron; toxicity of permanent vision loss; prescribed only through the REMS program and d/c if no improvement after 3 months

29
Q

What are the 3 classes of drugs that are used to potentiate GABA receptor Cl- currents on the post-synaptic neuron?

A
  1. Barbiturates (PB)
  2. Benzodiazepines (BZD)
  3. Topiramate/Cenobamate
30
Q

Benzodiazepines

A

Lorazepam, Diazepam, Clonazepam, and Clobazam; AEDS used potentiate GABA receptor Cl- currents on the post-synaptic neuron; GABA needs to be present (GABA-dependent)

31
Q

GABA-dependent post-synaptic GABAnergic enhancers

A

Benzodiazepines (Lorazepam, Diazepam, Clonazepam, and Clobazam) and Topiramate/Cenobamate

32
Q

Phenobarbital and Primidone

A

Barbiturates; AEDS used potentiate GABA receptor Cl- currents on the post-synaptic neuron; does NOT need GABA to be present (GABA-independent)

33
Q

Barbiturates (PB)

A

Phenobarbital and Primidone; AEDS used potentiate GABA receptor Cl- currents on the post-synaptic neuron; does NOT need GABA to be present (GABA-independent); high doses are lethal!

34
Q

Lorazepam, Diazepam, Clonazepam, and Clobazam

A

Benzodiazepines; AEDS used potentiate GABA receptor Cl- currents on the post-synaptic neuron; GABA needs to be present (GABA-dependent)

35
Q

High doses of which GABAnergic enhancing drug is known to be lethal?

A

Barbiturates (PB); Phenobarbital and Primidone; lethal respiratory depression

36
Q

What are the 3 MOAs of topiramate?

A
  1. VG Na+ channel blocker (presynaptic)
  2. AMPA receptor blocker (postsynaptic)
  3. GABA promoting agent (postsynaptic)
37
Q

What are the 3 MOAs of valproic acid?

A
  1. VG Na+ channel blocker (presynaptic)
  2. GAD stimulator (presynaptic)
  3. GABA-T inhibitor (presynaptic)
38
Q

What are the dual MOAs of gabapentin and pregabalin?

A
  1. alpha-2-delta Ca2+ channel blockers (presynaptic)
  2. GAD stimulation (presynaptic)
39
Q

What are the 3 indications to add Cannabidiol (Epidiolex) to the drug regimen?

A
  1. Dravet syndrome
  2. Lennox-Gastaut syndrome
  3. Tuberous Sclerosis Complex
40
Q

What bloodwork should you monitor if you are considering to add Cannabidiol (Epidiolex) as a therapeutic agent?

A

liver enzymes; AST/ALT and albumin

41
Q

What is a major side effect of Cannabidiol (Epidiolex)?

A

hepatocellular injury; monitor liver enzymes; AST/ALT and albumin

42
Q

What are two major risks for ALL AED agents?

A
  1. abrupt withdrawal may precipitate status epilepticus
  2. suicidal behavior and ideation
43
Q

Status epilepticus

A

a seizure that persists for sufficient length of time or is repeated frequently enough that recovery between attacks do not occur

44
Q

What is first line treatment for a patient in status epilepticus?

A

IV Benzodiazepines (BZDs) - Lorazepam, Diazepam, Clonazepam, and Clobazam or/and Levetiracetam

45
Q

Which 3 AEDs are strong cyp450 inducers?

A
  1. Carbamazepine
  2. Phenytoin
  3. Barbiturates (PB) - Phenobarbital and Primidone
46
Q

Which 3 scenerios do you need to consider when adding AED inducers to the therapeutic regimen?

A
  1. Contraceptives
  2. Anticoagulants
  3. Antivirals (HIV medications)
47
Q

Which AED agent is cautioned against due to the adverse effect of causing permanent vision loss?

A

Vigabatrin; AED used to inhibit GAT-1 to enhance inhibitory (GABA) actions in the presynaptic neuron