Antiepileptic Drugs Flashcards

1
Q

general goal of antiepilpetics

A

*reduce the ability of neurons to fire action potentials at a high rate and reduce neuronal synchronization

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2
Q

4 main mechanisms of action of antiepilpetics

A
  1. modulate voltage-gated sodium, calcium, or potassium channels
  2. enhance fast GABA-mediated synaptic inhibition (MORE inhibition)
  3. reduce fast glutamate-mediated excitation (LESS excitation)
  4. modify synaptic release process
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3
Q

antiepileptics that target voltage-gated SODIUM channels

A

-carbamezepine
-phenytoin
-lamotrigine
-lacosamide

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4
Q

antiepileptics that target voltage-gated CALCIUM channels

A

ethosuximide

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5
Q

antiepileptics that enhance GABA inhibition by targeting GABA receptors

A

-phenobarbital
-benzodiazepines

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6
Q

antiepileptics that enhance GABA inhibition by targeting GAT-1 GABA transporter

A

tiagabine

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7
Q

antiepileptics that enhance GABA inhibition by targeting GABA transaminase

A

vigabatrin

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8
Q

antiepileptics that target SV2A to inhibit glutamate release

A

levetiracetam

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9
Q

antiepileptics that target alpha-2-delta to inhibit glutamate release

A

-gabapentin
-pregabalin

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10
Q

narrow-spectrum antiepileptic agents

A

*specific for a given seizure type (usually focal)
*these can exacerbate certain generalized onset seizures

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11
Q

broad-spectrum antiepileptics

A

effective in focal and generalized seizures

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12
Q

carbamazepine - target & seizure type

A

*target: blocks voltage-gated sodium channels
*SZ type: narrow (focal)

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13
Q

phenytoin - target & seizure type

A

*target: blocks voltage-gated sodium channels
*SZ type: narrow (focal; gen. tonic-clonic)

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14
Q

lamotrigine - target & seizure type

A

*target: blocks voltage-gated sodium channels
*SZ type: broad

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15
Q

lacosamide - target & seizure type

A

*target: blocks voltage-gated sodium channels
*SZ type: narrow (focal)

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16
Q

ethosuximide - target & seizure type

A

*target: blocks voltage-gated CALCIUM channels (T-type calcium channels)
*SZ type: narrow (ABSENCE)

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17
Q

phenobarbital - target & seizure type

A

*target: GABA receptors (enhancing GABA inhibition)
*SZ type: narrow (focal)

18
Q

benzodiazepines - target & seizure type

A

*target: GABA receptors (enhancing GABA inhibition)
*SZ type: broad (for status epilepticus)

19
Q

tiagabine - target & seizure type

A

*target: GAT-1 GABA transporter (enhancing GABA inhibition)
*SZ type: narrow (focal)

20
Q

levetiracetam - target & seizure type

A

*target: SV2A (inhibits glutamate release)
*SZ type: broad

21
Q

gabapentin & pregabalin - target & seizure type

A

*target: alpha-2-delta (inhibits glutamate release)
*SZ type: narrow; used more for other things (neuropathic pain, restless leg syndrome, anxiety)

22
Q

valproate - uses

A

*SZ type: broad (generalized tonic-clonic)
*used for many other things, like mood stabilization in bipolar disease and to prevent migraines

23
Q

topiramate - seizure type

A

*SZ type: broad

24
Q

phenytoin - testable pearls

A

*zero-order metabolism
*highly bound to albumin
*ADEs: hirsutism, nystagmus, gingival hyperplasia
*tons of drug interactions

25
Q

carbamazepine - testable pearls

A

*induces its own metabolism
*ADEs: agranulocytosis (leukopenia), teratogenic, SIADH
*tons of drug interactions

26
Q

lacosamide - testable pearls

A

*minimal drug interactions

27
Q

gabapentin and pregabalin - testable pearls

A

*do NOT act via GABA
*instead, act via alpha-2-delta to inhibit glutamate release

28
Q

levetiracetam - testable pearls

A

*NO LIVER METABOLISM
*few drug interactions

29
Q

valproate - testable pearls

A

*teratogenic
*causes hepatotoxicity

30
Q

topiramate & zonisamide - testable pearls

A

*cause cognitive impairment & weight loss
*metabolic acidosis via CA inhibition

31
Q

antiepileptic drugs associated with Stephens-Johnson Syndrome

A

*lamotrigine
*carbamazepine

32
Q

which antiepileptics INDUCE CYP450 enzymes

A

*carbamazepine
*phenytoin
*phenobarbital

33
Q

which antiepileptics INHIBIT CYP450 enzymes

A

*valproate

34
Q

which 2 antiepileptics have minimal drug interactions

A

*levetiracetam
*lacosamide

35
Q

treatment of status epilepticus

A
  1. give benzodiazepine (usually IV lorazepam)
  2. follow immediately with IV loading dose of either:
    -fosphenytoin
    -valproate
    -levetiracetam
36
Q

what symptoms do all antiepileptic drugs cause

A

*dizziness
*fatigue
*ataxia
*diplopia

37
Q

phenytoin - adverse drug effects

A

*hirsutism (excess hair, often around mouth and chin)
*nystagmus
*gingival hyperplasia

38
Q

carbamazepine - adverse drug effects

A

*agranulocytosis (leukopenia)
*Stephens-Johnson syndrome
*teratogenic in first trimester
*SIADH (too much ADH secretion)

39
Q

which antiepileptic med is used for absence seizures

A

ethosuximide

40
Q

elimination of levetiracetam (Keppra)

A

NO liver metabolism:
*two-thirds excreted unchanged in urine
*one-third metabolized in the blood

41
Q

phenobarbital - adverse drug effects

A

*severe sedation
*cardiac depression and hypotension in high doses
*drug interactions