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AEDs Flashcards

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1
Q

Pregabalin:
- Mechanism of action
- Bioavailability
- Hepatic metabolism?
- Excretion

A

Pregabalin
- Mechanism of action: structural analog of Gaba, binds to alpha-2-deta subunit of voltage-gated calcium channel
- Bioavailability drops from 60%-33% when total daily dose increased form 900 to 3500 mg
- Not hepatically metabolized
>90% excreted unchanged in urine

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2
Q

Drugs to avoid in:
- Dravet Syndrome

A

Sodium channel agents (may worsen)

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3
Q

Primary side effects to consider: Phenobarbital (6)

A
  • sedation
  • rash
  • hepatotoxicity
  • aplastic anemia
  • osteopenia
  • CT d/o
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4
Q

Primary side effects to consider:
Phenytoin
General (6)
Dose dependent (5)

A
  • SJS
  • Blood dyscrasia
  • hepatotoxicity
  • gingival hyperplasia
  • hirsutism
  • osteopenia
    Dose-dependent
  • Nystagmus
  • Diplopia
  • ataxia / incoordination
  • dysarthria
  • Drowsiness
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5
Q

Primary side effects to consider:
Primidone

A

Same as phenobarbital (metabolized into phenobarbital)

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6
Q

Primary side effects to consider:
Ethosuximide

A

stomach upset
abdominal pain/cramps

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7
Q

Primary side effects to consider: clonazepam (4)

A
  • somnolence
  • lethargy
  • sexual dysfunction
  • tolerance (long term)
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8
Q

Primary side effects to consider:
Clorazepate (tranxene)

A
  • Somnolence
  • Lethargy
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9
Q

Primary side effects to consider:
Carbamazepine (8)

A
  • Sedation
  • Neutropenia
  • hyponatremia
  • bradycardia
  • SJS
  • Agranulocytosis
  • Hepatotoxicity
  • pancreatitis
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10
Q

Primary side effects to consider:
Valproate (7)

A
  • Weight gain
  • tremor
  • thrombocytopenia
  • pancreatitis
  • hepatotoxicity
  • hyperammonemia
  • Hair loss
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11
Q

Primary side effects to consider:
VIgabatrin (3)

A
  • permanent visual field deficit (older studies say 30-40%, likely less)
  • reversible subcortical edema
  • somnolence
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12
Q

Primary side effects to consider:
Zonisamide (5)

A
  • Cross-reacts with sulfa
  • hypohydrosis
  • nephrolithiasis
  • metabolic acidosis
  • weight loss
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13
Q

Primary side effects to consider:
Lamotrigine (4)

A
  • NON-sedating
  • insomnia
  • SJS
  • myoclonus
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14
Q

Primary side effects to consider: Felbamate (3 + 4)

A
  • aplastic anemia
  • liver failure
  • weight loss
  • Increases levels of phenytoin, valproate, phenobarbital, clobazam
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15
Q

Primary side effects to consider:
Gabapentin (3)

A
  • sedation
  • weight gain
  • myoclonus
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16
Q

Primary side effects to consider:
Topiramate (5)

A
  • weight loss
  • cognitive slowing
  • dysesthesia
  • Glaucoma
  • nephrolithiasis
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17
Q

Primary side effects to consider:
Tiagabine (3)

A
  • Sedation
  • cognitive slowing
  • worsens some generalized seizures (myoclonic, absence)
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18
Q

Primary side effects to consider:
Oxcarbazepine (4)

A
  • hyponatremia (per book only in elderly)
  • Decreases OCP levels
  • Sedation
  • Rash
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19
Q

Primary side effects to consider:
Levetiracetam (2)

A
  • Irritability
  • Depression
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20
Q

Primary side effects to consider: pregabalin (3)

A
  • Sedation
  • swelling in lower extremities
  • blurred vision
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21
Q

Primary side effects to consider:
Rufinamide (3)

A
  • Loss of apetite
  • aggravated seizures
  • Status epilepticus
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22
Q

Primary side effects to consider:
Lacosamide (7)

A
  • Dizziness / vertigo > vomiting
  • Ataxia
  • diplopia
  • Blurred vision
  • Fatigue
  • Rash
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23
Q

Primary side effects to consider:
Esclicarbazepine (aptiom) (4)

A
  • Nausea
  • Dizziness
  • Diplopia
  • hyponatremia (1-2%)
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24
Q

Primary side effects to consider:
Clobazam (3)

A
  • somnolence
  • lethargy
  • note less addictive potential than other benzo
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25
Primary side effects to consider: Ezogabine (potiga) (3)
- Urinary Retention - Tremor - bluish skin discoloration
26
Primary side effects to consider: Perampanel (fycompa)
- Ataxia - Severe mood issues (hostility, homicidal ideation, aggression)
27
ASM's to Consider: Focal onset, +/- secondary generalization - Main (5) - Less preferred (4)
Main: - Lamotrigine - levetiracetam - oxcarbazepine - lacosamide - topiramate Less likely as 1st agent: - Carbamazepine - Valproate - Esclicarobazapine - phenytoin
28
ASM's to Consider: Primary GTC (5)
- Valproate - Levetiracetam - Lamotrigine - Topiramate - zonisamide
29
ASM's to Consider: Absence (3) Drugs to avoid: (5)
Consider - Ethosuximide - Valproate - (less preferred) lamotrigine AVOID - phenytoin - carbamazepine - gabapentin - tiagabine - vigabatrin
30
ASM's to Consider: Generalized myoclonic (3) Drugs to avoid (6)
Consider - levetiracetam - valproate - clonazepam Avoid - phenytoin - carbamazepine - gabapentin - tiagabine - vigabatrin - pregabalin
31
ASM's to Consider SeLECTS (2)
- LEV - OXC
32
ASM's to Consider: young women (3) Avoid (1 + 2 others)
Consider - levetiracetam - lamotrigine - lacosamide Avoid - Valproate (teratogen) - Carbamazepine - Phenytoin
33
ASM's to Consider: Depressed patient (1) Avoid (3)
Consider - Lamotrigine Avoid - pheyntoin - phenonbarbital - primidone
34
ASM's to consider: Emotionally labile person (5) Avoid (1)
Consider (due to mood stabilizing effect) - Valproate - carbamazepine - lamotrigine - oxcarbazepine - topiramate Avoid - Levetiracetam
35
ASM's to Consider: Hepatic disease (3) Avoid (3)
Consider: - Levetiracetam - lamotrigine - pregabalin Avoid - valproate - phenytoin - carbamazepine
36
ASM's to Consider: obesity (2) avoid (3)
Consider (due to weight loss) - Topiramate - Zonisamide Avoid - Valproate - Gabapentin - Pregabalin
37
ASM's to Consider: Chronic pain (4)
- Gabapentin - pregabalin - carbamazepine - pregabalin
38
ASM's to Consider: on many other meds (3) Avoid (1)
Consider - Levetiracetam - pregabalin - gabapentin Avoid Enzyme inducers
39
ASM's to Consider: Han Chinese or Taiwanese
Carbamazepine oxcarbazepine Note: can use if you check HLA-B 1502)
40
Patient on ASM develops rash, what cross-reactivities do you need to consider (4)
Carbamazepine <>Oxcarbazepine Carbamazepine <>Phenytoin Carbamazepine <>Phenobarbital Phenytoin <>Zonisamide
41
Enzyme Inducing ASMs: strong (5) Weak (1)
Strong - Phenobarbital - primidone - phenytoin - carbamazepine - Oxcarbazepine (doses >900 mg) Weak - Lamotrigine (weak)
42
Enzyme inhibiting ASM Strong (1) Weak (1)
Strong: Valproate Weak: Topiramate
43
44
Phenobarbital lowers concentrations of which ASM (3 main + 1), and what 3 other non-asm drugs
- valproate - ethosuximide - lamotrigine - may reduce carbamazepine, but increase carbamazepine epoxide Also reduces effectiveness of - warfarin - steroids - OCP
45
Patient with epilepsy and Dupuytren's Contracture. - What medicine could they be on that could cause this? - What other connective tissue conditions is this med also associated with?
Phenobarbital Also associated with - platar fibromatosis - frozen shoulder
46
Pregnancy risk: Phenobarbital Category Risks (2)
Category: - D Risks: - cardiac malformations - reduced cognitive abilities (in male offspring)
47
Pharmacokinetics: phenytoin oral bioavailability: adults oral bioavailability: Neonates Factors that reduce oral bioavailability (3)
Oral Bioavailability: adults - 90% oral bioavailability: neonates - much lower Also reduced with - Nasogastric feedings - calcium - antacids
48
Patient in ICU for breakthrough seizures treated with fosphenytoin has toxicity at an unexpectedly low dose. What medication could they be on and why did this happen?
Valproate - competes for protein binding sites, which leads to higher Free levels of phenytoin
49
ASM metabolization,Carbamazepine: - Non-ASMs that can affect concentrations (4) - Metabolite affected by what 4 ASM
Affects concentration d/t CYP3A4 - Macrolide antibiotics (other than azithromycin) - Fluoxetine - Propoxyphene - Grapefruit juice Metabolite (epoxide) affected by - valproate - felbamate - oxcarbazepine - zonisamide
50
ASM metabolization, Carbamazepine: - Important factor about dosing -What 4 drugs do you need to be especially notable for and why?
Dosing: - Auto-inducer (takes 2-4 weeks to reach steady state) Strong inducer of cytochrome P450, increases clearance of: - OCPs - Warfarin - Valproate - lamotrigine
51
Oxcarbazpine: - Bioavailability - half-life (main drug) - half-life (active metabolite) - Big reasons why it replaced carbamazepine (2)
- bioavaibility- 90% - half-life (main drug) 1-3.7h - half-life (metabolite) 8-10 h Replaced carbamazepine due to - Not affected by 3A4 inhibitors (fluoxetine, erythromycin, grapefruit juice) - No auto-induction
52
What condition is Felbamate approved by the FDA to treat specifically?
Lennox-Gastaut Syndrome
53
Patient with Absence seizures presents with fever, arthralgia, malar rash? - What two should you get? - What two organs can also be involved - What other two ASMs can cause this
Lupus-like syndrome (Ethosuximide, Phenytoin, Carbamazepine) Labs: - Elevated ANA - Elevated anti DS DNA antibodies Other organ systems - Pleural effusion - Myocarditis
54
Why does topirimate cause kidney stones?
inhibits carbonic anydrase - Increased urinary citrate - Alkalinized urine
55
risk factors for aplastic anemia when starting felbamate (6)
- female sex - caucasian race - Adult age - history of cyotopenia - allergy / toxiticy to other ASM - diagnosis / serological evidence of an autoimmune disorder
56
Mechanism of action: felbamate
binds to NR2B subunit of NMDA receptor (selective inhibition)
57
factors that increase risk of VPA-induced hyperammonemia (6)
- urea cycle defects - carnitine deficiency - protein rich diets - hypercatabolic states - phenobarbital - topiramate
58
Why does levocarnitine help with VPA-induced hyperammonemia?
- Carnitine required for beta-oxidation - VPA depletes carnitine - this shifts to OMEGA-oxidation > toxic metabolites > ammonia
59
Which other AED, when taken with VPA, can increase risk of valproate-induced encephalopathy? Why?
- Topiramate - synergistic action on Ornithine metabolism > hyperammonemia
60
medication known to case spike-wave-stupor
Tiagabine (either for seizures or insomnia)
61
Side effects of AcTH - Leading causes of death (2) - Other symptoms (4) - MRI findings (onset, peak, resolution)
Leading causes of death: - cardiomyopathy - infection others: - hypertension - proteinuria - bleeding - neuropsych (agitation, apathy, insomnia) MRI: - onset: within first week -maximum 4 weeks - resolves 1-4 weeks following completion of treatment
62
mechanism of action: Esogabine
potassium channel opener
63
Name two differences between visual changes that happen with Vigabatrin versus Esogabine
1: cause - Ezogabine: due to pigmentary abnormalities - Vigabatrin: damage to the nerve 2: Reversibility - Ezogabine: reversible - Vigabatrin: Irreversible
64
HLA alleles and what they're associated with: HLA-B*1502 (2) HLA-A*3101 (2)
HLA-B*1502: CBZ-induced Stevens-Johnson syndrome (SJS) and Toxic Epidermal Necrolysis (TEN) HLA-A*3101: CBZ_induced Hypersensitivity syndrome (HSS) and Maculopapular exanthema (MPE)
65
Felbamate drug interaction: What enzyme? What ASMs can increase (2) What ASMs can decrease (1)
Enzyme: CYP2C19 Increases: - phenytoin - valproate (but due to metabolism by beta-oxidation) Decreases: - carbamazepine (and epoxide)
66

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