Antiepileptic agents Flashcards

1
Q

Na channel blockers

A
carbamazepine
oxcarbamazepine
eslicarbazepine
lamotrigine
phenytoin
rufinamide
topiramate
valproic acid
lacosamide
zonisamide
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2
Q

AMPA receptor blockers

A

Topiramate

PerAMPAnel

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3
Q

NMDA receptor blocker

A

Felbamate

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4
Q

Low threshold Ca T-type channel blockers

A

ethosuximide

zonisamide

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5
Q

Synaptic vesicle 2A protein blockers

A

levetiracetam

brivaracetam

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6
Q

a2d Ca channel blockers

A

gabapentin

pregabalin

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7
Q

K channel opener

A

Ezogabine

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8
Q

Pre-synaptic GABA promoting agents

GAD stimulation

A

valproic acid
Gabapentin
pregabalin

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9
Q

Pre-synaptic GABA promoting agents

GAT-1 inhibition

A

Tiagabine

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10
Q

Pre-synaptic GABA promoting agents

GABA-T inhibition

A

Vigabatrin

valproic acid

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11
Q

Post-synaptic GABA promoting agents

A

1) Barbiturates
phenobarbital
primidone

2) Benzodiazapines
clonazepam
clobazam
lorazepam
diazepam

3) topiramate

ezogabine
(high doses)

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12
Q

What are Topiramate’s 3 MOAs

A

Na channel blocker
AMPA receptor blocker
Post-synaptic GABA promoting agent

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13
Q

What are valproic acid’s 3 MOAs

A

Na channel blocker
presynaptic GAD stimulation
presynaptic GABA-t inhibition

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14
Q

What is the general treatment of convulsive status epilepticus

A

Lorazepam then Levetiracetam

The two L’s

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15
Q

Which Na channel blockers prolong fast inactivation state of Na ion channels?

A
Carbamazapine
lamotrigine
phenytoin
topiramate
valproic acid
Lacosamide
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16
Q

Which Na channel blockers enhance slow inactivation of Na channels

A

Lacosamide

17
Q

What is ethosuximide used to treat

A

Absence seizures

Only limits excitation of T type Ca channels

18
Q

What are the two ways antiepileptic drugs target epileptic-transmitter systems?

A
Suppress excitatory (glutamate) actions
Enhance inhibitory (GABA) actions
19
Q

What is the MOA of benzodiazepines?

A

BZD binds to a distinct site –> allosteric change that potentiates GABA binding –>

Cl channels open with GREATER FREQUENCY

20
Q

What is the MOA of barbiturates

A

PB bind to a distinct site and increases the DURATION of Cl channel opening

21
Q

Which is more lethal: PB of BZD?

Why?

A

PB>BZD

high doses of barbiturates are GABA independent while BZD is GABA dependent

22
Q

What are the broad warnings of all AEDs?

A

1) abrupt withdrawal of antiepileptic meds may precipitate status epilepticus
2) Suicidal behavior and ideation

23
Q

What are toxicities of phenytoin?

A

GINGIVAL HYPERPLASIA
hypocalcemia/vit. D deficit/osteoporosis
hypothyroidism
CV risk

24
Q

Chronic administration of carbamazepine, phenytoin, phenobarbital and valproic acid are associated with what condition?

Why?

A

Osteopenia/osteoporosis

These drugs induce CYP450-dependent vitamin D catabolism. Lack of vit. d —> decreased absorption of intestinal calcium –> compensatory PTH-mediated bone demineralization for Ca homeostasis

25
Q

Toxicities of Carbamazepine

A

leukopenia/neutropenia/thrombocytopenia
-need baseline CBC (WBC)

hypocalcemia/vit. D deficit/osteoporosis

26
Q

What analog of carbamazepine is a less potent CYP450 inducer?

A

oxcarbazepine

27
Q

Carbamazapine is an inducer of CYP450 enzymes and what

A

CBZ induces self-metabolism

28
Q

Toxicities of phenobarbital

A

CNS depressant with fatality risk

Hypocalcemia/ etc.

29
Q

Toxicities of Vigabatrin

How is it prescribed?

A

Permanent, progressive, bilateral, concentric, vision loss
discontinue after max of 3 months if no effective response

Prescribeable only via REMS program

30
Q

The AED CYP inducers can increase clearance of what?

A

oral hormonal contraceptives
warfarin
HIV medications