AEDs Flashcards

1
Q

Carbamazepine: mechanism

A

Binds to neuronal sodium channels to reduce sustained high-frequency repetitive firing of action potentials

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2
Q

Carbamazepine: indication

A

Partial and secondarily generalized seizures

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3
Q

Carbamazepine: dose

A

Start 400 mg/day in 2 divided doses
Maximum 1,600 mg/day
Several long-acting forms available

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4
Q

Carbamazepine: side effects

A
  • Dose-related
  • Drowsiness, dizziness, ataxia, dyskinesias, and visual disturbance
  • Rare: Severe idiosyncratic hematologic reactions of agranulocytosis and aplastic anemia
  • Induces CYP-450 isoenzyme
  • Consider screening for HLA-B*1502 allele in Asians as this is associated wtih marked increase in skin rash.
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5
Q

Ethosuximide: mechanism

A

Decreases the bursting of thalamocortical neurons responsible for generation of 3 Hz spike-and-wave discharges via reduction of low threshold (T-type) calcium channel currents

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6
Q

Ethosuximide: indications

A

Absence seizures

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7
Q

Ethosuximide: dose

A

500 mg in 2 divided doses

May increase to 1,500 mg/day

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8
Q

Ethosuximide: side effects

A
  • Common: nausea, vomiting, weight loss, diarrhea, abdominal pain, constipation
  • Serious: blood dyscrasias
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9
Q

Fosphenytoin: dose

A

Loading dose of 15-20 mg phenytoin equivalents/kg

Can be administered in 100-150 mg PE/min

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10
Q

Fosphenytoin: side effects

A

Risk of hypotension and cardiac dysfunction lower than for phenytoin

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11
Q

Phenobarbital: mechanism

A
  • Enhancement of GABA-mediated inhibitory synaptic transmission
  • Voltage-regulated calcium ion channels
  • Reduces glutamate-mediated excitation
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12
Q

Phenobarbital: indication

A

All seizures except absences

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13
Q

Phenobarbital: dose

A

1.5-4 mg/kg/day in daily doses

IV available

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14
Q

Phenobarbital: side effects

A
  • Common: sedation, drowsiness, hyperactivity, irritability, and insomnia
  • Rare: cognitive impairment, depression, movement disorders, megaloblastic anemia, osteoporosis, connective tissue disorders, teratogenicity, and exacerbation of porphyria
  • Induces CP-450 isoenzyme, resulting in drug-drug interactions
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15
Q

Phenytoin: mechanism

A
  • Rate-dependent inhibition of sodium channels
  • Calmodulin and cyclic nucleotide 2nd messenger systems
  • Inhibition of voltage-dependent neurotransmitter release at the synapse
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16
Q

Phenytoin: indications

A
  • Partial-onset seizures and generalized tonic-clonic seizures
  • Limited efficacy in absence, myoclonic, or atonic seizures
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17
Q

Phenytoin: dose

A

Start 200-300 mg in 3 divided doses
Increase until maintenance dose reached (300-400 mg daily)
Loading dose of 1,000 mg may be given in 3 divided dose in 2 hour intervals or by IV

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18
Q

Phenytoin: side effects

A
  • Common: nystagmus, blurred vision, ataxia, slurred speech, gingival hypertrophy, hirsutism
  • Long-term use: osteoporosis, peripheral neuropathy, cerebellar atrophy, gum hypertrophy
  • Serious: purple glove syndrome
19
Q

Phenytoin: metabolism

A

Metabolized by CYP-450 system
Excretion by urine and feces
Conversion from 1st-order to Zero-order kinetics at levels in middle of average therapeutic range
Induces CYP-450, resulting in multiple interactions with other medications

20
Q

Valproate: mechanism

A
  • Increased rate of GABA turnover
  • Reduction of NMDA glutamate receptor-mediated excitation
  • Inhibit sustained repetitive firing of neurons with blockage of voltage-dependent sodium channels
21
Q

Valproate: indications

A

Complex partial seizures, generalized, absence seizures

Also effective for headache and mood stabilization

22
Q

Valproate: dose

A

15 mg/kg a day in divided doses with weekly dose increases of 5-10 mg/kg
IV available
Long-acting form available

23
Q

Valproate: side effects

A
  • Common: drowsiness, tremor, nausea, vomiting, hair loss, weigh gain, tremor
  • Serious: hepatotoxicity, hemorrhagic pancreatitis
24
Q

Felbamate: mechanism

A

Interaction with NMDA receptors, resulting in decreased excitatory amino acid neurotransmission

25
Q

Felbamate: indications

A

Partial seizures with or without secondary generalization
Originally developed for Lennox-Gastaut syndrome
Use in severely refractory patients only

26
Q

Felbamate: dose

A

1,200 mg/day in divided doses every 8 hours

Slowly increased to target range of 2,400-3,600 mg/day

27
Q

Felbamate: side effects

A
  • Common: nausea, headache, insomnia. Significant weight loss in long-term use
  • Serious: aplastic anemia, hepatic failure. Most serious teratogenic AED, should be avoided in all women of childbearing age.
  • CBC and LFT every 2 weeks for 1st 6 months
28
Q

Gabapentin: mechanism

A
  • Reduction of glutamate release at cortical synapses

- Reduction of activity-dependent release via interaction with P/Q-type voltage-gated calcium channels

29
Q

Gabapentin: indications

A

Partial seizures

30
Q

Gabapentin: dose

A

300 mg/day with rapid escalation to initial target dose of 1,800 mg/day in 3 divided doses. Can be as high as 3,600 mg/day

31
Q

Gabapentin: side effects

A
  • Common: somnolence, dizziness, ataxia, weight gain, and fatigue
  • Not metabolized in liver, few drug interactions
32
Q

Lacosamide: mechanism

A
  • Modifies sodium channels

- Inactivates high-frequency neuronal firing

33
Q

Lacosamide: indication

A

Partial seizures

34
Q

Lacosamide: dose

A

100 mg in 2 divided doses. Increase to 100-40 mg/day

IV available

35
Q

Lacosamide: side effects

A
  • Common: dizziness (esp in combo with other Na channel modulators), nausea, headache, diplopia
  • May cause PR interval prolongation
  • Little drug-drug interaction
36
Q

Lamotrigine: mechanism

A

Blocks excitatory sodium ion channels in a voltage-dependent and use-dependent manner

37
Q

Lamotrigine: indication

A

Partial and generalized seizures, including primary generalized seizures
Mood stabilizing

38
Q

Lamotrigine dose

A

25 mg every day to be titrated up by 25 mg every 2 weeks until 100 mg/day
Maintenance 200-400 mg/day
If on enzyme-inducing: start at 50mg/day. Titrate up to 300-500 mg/day.
If taking valproate: start 25 mg every other day, titrate up to 100-200 mg/day
Long-acting form available

39
Q

Lamotrigine: side effects

A
  • Common: dizziness, ataxia, somnolence, headache, blurred vision, nausea, vomiting. Insomnia
  • Serious: Rash with rapid escalation or valproic acid coadministration. Can be life threatening
40
Q

Levetiracetam: mechanism

A

Modifies synaptic protein SV2A

41
Q

Levetiracetam: indications

A

Partial and generalized epilepsy

42
Q

Levetiracetam: dose

A

1,000 mg/day divided in 2 doses
Increase to reach target of 1,000-3,000mg/day
IV form available
Long-acting form available

43
Q

Levetiracetam: side effects

A

Common: somnolence, irritability, ataxia