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IDT Fall > Lec 3: Antiepileptic Agents > Flashcards

Lec 3: Antiepileptic Agents Flashcards

1
Q

what are the two different cellular mechanisms associated with seizures?

A

too much excitation (ions flowing inward like Na2+ and Ca2+) via the glutamate NT
too little inhibition (ions flowing outward like Cl- and K+) via the GABA NT

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2
Q

“anti-seizure drugs” can be prescribed for other reasons such as?

A

migraines (prophylactic) and some pain conditions

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3
Q

define what Epilepsy is

A

A CHRONIC disorder characterized by recurrent seizures

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4
Q

what is Dravet Syndrome?

A

a mutation in a Na+ channel subunit SCN1A

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5
Q

T/F the majority of people with epilepsy are resistant to treatments and usually try various treatments before finding one that is beneficial

A

False, only 30% of people are refractory to treatment

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6
Q

what does SUDEP stand for?

A

sudden unexplained death in epilepsy

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7
Q

list the first generation antiseizure medications

A

potassium bromide, phenobarbital, phenytoin, primidone, and ethosuximide

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8
Q

what is phenytoin specifically classified as?

A

an Na2+ channel blocker

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9
Q

what is primidone specifically classified as?

A

an Na2+ channel and GABA blocker

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10
Q

what is ethosuximide specifically classified as?

A

T-type Ca2+ channel blocker

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11
Q

list the second generation antiseizure medications

A

Benzos:
diazepam, carbamazepine, valproate, clonazepam, and clobazam

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12
Q

T/F benzos have broad anti-seizure activity

A

True

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13
Q

what is carbamazepine specifically classified as?

A

Na+ channel blocker

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14
Q

what is valproate specifically classified as?

A

Na+ channel blocker

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14
Q

what is clonazepam specifically classified as?

A

GABA potentiation

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15
Q

what is clobazam specifically classified as?

A

GABA potentiation

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16
Q

Vigabatrin:
drug class?
what does it do?

A

third generation antiseizure agent
irreversible GABA-T inhibitor

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17
Q

Lamotrigine
drug class?
what does it do?

A

third generation antiseizure agent
Na+ channel blocker

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18
Q

Oxcarbazepine
drug class?
what does it do?

A

third generation antiseizure agent
Na+ channel blocker

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19
Q

Felbamate
drug class?
what does it do?

A

third generation antiseizure agent
multiple functions

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20
Q

Gabapentin
drug class?
what does it do?

A

third generation antiseizure agent
binds presynaptic calcium channel α2δ subunit to modulate NT (Glutamate) release

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21
Q

Topiramate
drug class?
what does it do?

A

third generation antiseizure agent
multiple functions

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22
Q

Tiagabine
drug class?
what does it do?

A

third generation antiseizure agent
GABA potentiation; inhibits GABA reuptake

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23
Q

Levetiracetam (Keppra)
drug class?
what does it do?

A

third generation antiseizure agent
Synaptic Vesicle Glycoprotein 2A (SV2A) modulation

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24
Q

Zonisamide
drug class?
what does it do?

A

third generation antiseizure agent
Na+ channel blocker

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25
Q

Pregablin
drug class?
what does it do?

A

third generation antiseizure agent
presynaptic calcium channel α2δ subunit

26
Q

Rufinamide
drug class?
what does it do?

A

third generation antiseizure agent
Na+ channel blocker

27
Q

Lacosamide (Vimpat)
drug class?
what does it do?

A

third generation antiseizure agent
enhanced slow activation of sodium channels

28
Q

Eslicarbazepine acetate
drug class?
what does it do?

A

third generation antiseizure agent
a prodrug to Eslicarbazepine - Na+channel blocker

29
Q

Retigabine
drug class?
what does it do?

A

third generation antiseizure agent
K+ channel activator

30
Q

Perampanel
drug class?
what does it do?

A

third generation antiseizure agent
Glutamate (AMPA) antagonist

31
Q

Brivaracetam
drug class?
what does it do?

A

third generation antiseizure agent
SV2A modulation

32
Q

Cannabidiol (CBD)
drug class?
what does it do?

A

third generation antiseizure agent
CB1 negative allosteric modulator

33
Q

Cenobamate
drug class?
what does it do?

A

third generation antiseizure agent
Na+channel enhances inactivation and slows recovery; possible GABA receptor upregulation

34
Q

Define a class I seizure

A

partial, focal, local seizures: seizure is confined to a local area

35
Q

Define a class II seizure

A

generalized seizures: bilaterally symmetrical and without local onset

36
Q

Define a class III seizure

A

unclassified seizures

37
Q

Define a class IV seizure

A

special syndromes: syndromes characterized by the presence of seizures

38
Q

Define a class I “simple partial” seizure

A

Consciousness is not impaired

39
Q

Define a class I “complex partial” seizure

A

Impaired consciousness: begins as a simple partial seizure that progresses and is preceded by an aura. impaired memory occurs during seizure

40
Q

Define a class I “Partial seizure evolving into secondarily generalized
tonic-clonic seizure”

A

alternating contractions with relaxation causing loss of consciousness preceded by an aura

41
Q

Define a class II “absence (petit mal)” seizure

A

sudden interruption of consciousness, blank stare, no aura

42
Q

Define a class II “myoclonic” seizure (random discharges in motor cortex)

A

brief and sudden contractions of muscles

43
Q

Define a class II “tonic-clonic (grand mal)” seizure

A

abrupt onset usually with no aura with contractions and relaxation/shaking followed by unconsciousness

44
Q

define what status epilepticus is

A

either:
-seizures occurring acutely in greater intensity, number, or length than usual
-prolonged seizure lasting longer than 10 minutes or repeated seizures over the course of 30 minutes

45
Q

is status epilepticus occurrence a major concern?

A

yes, it is life threatening and emergency care should begin immediately

46
Q

how can we treat status epilepticus?

A

initially with benzos such as:
IV diazepam
IV lorazepam
IM midazolam

47
Q

**know the appearance of interictal EEG paroxysm, silent period, tonic seizure, clonic seizure, and prostictal depression

A

Slide 13

48
Q

name the drugs that block voltage-dependent Na+ channels used for seizures. what specifically do they inhibit the channels from doing?

A

Phenytoin
Carbamazepine
Lamotrigine
Valproate
Topiramate
Oxcarbazepine
Primidone
– they inhibit high frequency repetitive firing and fast inactivation

49
Q

what is Lacosamide’s mechanism at voltage-dependent Na+ channels?

A

likely inhibits slow inactivation

50
Q

what is Rufinamide’s mechanism? what syndrome is it approved to treat?

A

may inhibit slow inactivation of voltage-dependent Na+ channels
it is approved to treat Lennox-Gastaut syndrome (a childhood-
onset epilepsy syndrome)

51
Q

name the drugs that target GABAergic synapses and what specifically they each do

A

Valproate: modifies amino acid metabolism
Vigabatrin: irreversible GABA-T inhibitor
Tiagabine: preferentially binds GAT-1 (not GAT-2 or GAT-3)
Benzodiazepenes: allosteric modulators of GABA A (enhance affinity/ increase frequency of channel opening)
Barbiturates: allosteric modulators of GABA A (increase efficacy/ duration of opening)
Topiramate: distinct modulator of GABA A

52
Q

describe the mechanism of gabapentin and pregabalin and an additional thing they are used to treat

A

Bind a2dsubunit of voltage-operated Ca2+ channels and blocks (Anti seizure activity is most likely to decrease presynaptic release of glutamate)
they are analgesics approved for nerve pain

53
Q

describe the mechanism of Levetiracetam and Brivaracetam

A

bind synaptic vesicle protein SV2A and modify release of neurotransmitter (has clear anti-seizure efficacy)

54
Q

Perampanel:
monotherapy for what category of seizures?
add on therapy for what category of seizures?
drug class?

A

-Monotherapy for partial seizures
-Add on therapy for generalized seizures
-noncompetitive AMPA receptor antagonist

55
Q

Felbamate:
used for what category of seizures?
what are the issues with this drug?
when is it used for seizures?

A

partial seizures
Causes high rate of aplastic anemia and severe hepatitis
as a third-line drug for refractory cases

56
Q

CBD:
used for what category of seizures?

A

first in class for rare pediatric epilepsy syndromes

57
Q

which 2 drugs block T-type Ca2+channels? what does the “T” mean?

A

Ethosuximide
Valproate
T = Low Voltage Activated Channel

58
Q

what are the typical Anti-epileptic drug (AED) side effects?

A

drowsiness, fatigue/mental slowing, dizziness, blurred vision, mood changes, and Many idiosyncratic (individualistic) reactions (rash, gingival
hyperplasia (oral condition that causes your gums to overgrow), bone density loss, hepatotoxicity

59
Q

Vigabatrin has an FDA black box warning for what reason?

A

can cause permanent vision loss

60
Q

what is a specific side effect lamotrigine may cause?

A

life-threatening skin rash

61
Q

T/F AED may increase the risk of suicidal thoughts and changes in behavior

A

true

62
Q

how do AED effect contraception?

A

increased oral contraception failure rate

63
Q

what are the warnings of using AED during pregnancy?

A

Greater incidence of congenital defects

IDT Fall (29 decks)

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