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PDA2 > Pharmacology of Antiseizure Drugs > Flashcards

Pharmacology of Antiseizure Drugs Flashcards

1
Q

What drugs are GABA receptor agonists?

A

benzodiazepines

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2
Q

What drugs inhibit GABA reuptake?

A

tiagabine

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3
Q

What drugs target GABA metabolism?

A

valproic acid and vigabatrin

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4
Q

Describe the GABA channel/receptor

A

Cl- permeable inotropic receptor, inhibitory= influx of Cl- to increase membrane polarization

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5
Q

What is the MOA of Phenobarbital?

A

prolongs Cl- channel opening in presence of GABA by binding to an allosteric site

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6
Q

What is the MOA of benzodiazepines?

A

requires initial activity of GABA for their activity then increases the frequency of channel opening

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7
Q

What drugs are benzodiazepines?

A

-diazepam
-clobazam
-clonazepam
-clorazepate
-lorazepam

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8
Q

What is the MOA of Tiagabine?

A

inhibits GABA transporter to decrease glial and presynaptic neuronal uptake of the inhibitory GABA

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9
Q

What is the MOA of Valproic Acid?

A

-potentiates effects of GABA by enhancing the activity of glutamic acid decarboxylase which converts glutamate to GABA
-inhibits metabolism of GABA
-mimics actions of GABA at postsynaptic receptor sites

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10
Q

What are the adverse effects of Valproic Acid?

A

alopecia and weight gain with chronic use

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11
Q

What is the MOA of Vigabatrin?

A

structural analog of GABA, irreversible inhibition of GABA transaminase “suicide inhibitor”, duration of action is based on synthesis of GABA-T (~5 days)

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12
Q

What is the MOA of Carbamazepine (Tegretol)?

A

inhibits voltage gated Na+ channels (binds alpha subunit)= maintains Na+ channels in activated state= inhibits generation of action potential

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13
Q

What are the indications of Carbamazepine (Tegretol)?

A

-partial seizures
-generalized tonic seizures
-mixed seizure patterns

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14
Q

What are the adverse effects of Carbamazepine (Tegretol)?

A

Stevens-Johnson Syndrome (SJS)/toxic epidermal necrolysis (TEN) increased risk for HLA-B 1502 allele

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15
Q

What is the MOA of Phenytoin sodium (Dilantin)?

A

block voltage gated Na+ channels in the inactive state (slow rate of recovery)

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16
Q

What are the adverse effects of Phenytoin (Dilantin)?

A

-SJS/TEN *increased risk for HLA-B 1502 allele
-gingival hyperplasia
-hirsutism

17
Q

What is the MOA of Lacosamide?

A

Na+ channel inhibitor, selectively binds to fast inactivated Na+ channels

18
Q

What is the MOA of Lamotrigine?

A

Na+ channel inhibitor, neuronal voltage-gated Na+ channels and blocks the release of glutamate through the stabilization of the presynaptic membrane

19
Q

What is the MOA of Zonisamide?

A

multiple MOA but primary MOA is inhibition of neuronal voltage-gated Na+ channels= prolongs Na+ channel inactivation and stabilizes the cell membrane

20
Q

What is the MOA of Cenobamate?

A

-reduces repetitive neuronal firing by inhibiting voltage-gated Na+ channels
-positive allosteric modulator of GABA ion channel

21
Q

What are the indications of Cenobamate?

A

partial onset seizures in adults

22
Q

What is the MOA of Gabapentin?

A

bind to alpha2omega subunit of P/Q type voltage gated Ca2+ channels in the neuronal synapse and reduce Ca2+ entry into neurons, which may inhibit synaptic release of excitatory neurotransmitters such as glutamate

23
Q

What is the MOA of Ethosuximide?

A

inhibit low voltage activated T-type Ca2+ channels in the thalamocortical neurons

24
Q

What is the indication of Ethosuximide?

A

1st line for generalized absence seizures

25
Q

What is the MOA of Levetiracetam?

A

binds SV2A (important for normal synaptic function), reducing synaptic vesicle cycling which decreases synaptic transmission which may modulate neurotransmitter release

26
Q

What is the MOA of Topiramate?

A

multiple MOA but primarily antagonist at the AMPA/kainite subtype of glutamate receptor

27
Q

What is the MOA of Perampanel?

A

noncompetitive antagonist of the AMPA glutamate receptor

28
Q

What is the MOA of Felbamate?

A

antagonist at the strychine-insensitive glycine recognition site of the NMDA receptor-ionophore complex= raises the seizure threshold

PDA2 (13 decks)

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