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PR3153 CA > Antiseizure medications > Flashcards

Antiseizure medications Flashcards

1
Q

MOA of phenytoin

A
  • Blockade of voltage gated Na+ channels
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2
Q

indication for phenytoin

A
  • All except absence seizures
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3
Q

TDM of phenytoin

A
  • Narrow therapeutic range (40-100uM)
  • Saturation kinetics
  • Non-linear relationship between dose and steady state plasma concentration
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4
Q

MOA of carbamazepine

A
  • Blockade of voltage gated Na+ channels
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5
Q

indication for carbamazepine

A
  • All except absence seizures
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6
Q

PK of carbamazepine

A
  • CYP450 inducer
  • Half-life of carbamazepine shortens with repeated dose
  • Accelerates elimination of other drugs
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7
Q

Pharmacogenomics of carbamazepine

A
  • In Asians: test for HLAB*1502 allele before commencing carbamazepine due to increased risk of SJS/TEN
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8
Q

MOA of sodium valproate

A
  • Blockade of voltage gated Na+ and Ca2+ channels
  • Inhibits GABA transaminase (an enzyme which breaks down GABA)  increases GABA  increased inhibition of neuron
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9
Q

indication of sodium valproate

A

all seizures

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10
Q

PK of sodium valproate

A
  • Strongly bound to plasma protein
  • Can displace other antiepileptics
  • In combination therapy, since valproate can displace other antiepileptics, apparent free drug concentration will be higher than expected, dose adjust accordingly
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11
Q

ADR of ASM: dose related

A

Drowsiness, confusion, nystagmus, ataxia (movement coordination disorder),
slurred speech, nausea, unusual behaviour, mental changes, coma

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12
Q

ADR of ASM: Non dose related

A

Hirsutism, acne, gingival hyperplasia (gums become swollen and overgrown), folate deficiency, osteomalacia (bones getting softer), hypersensitivity reactions (including Stevens-Johnson syndrome)

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13
Q

MOA of diazepam

A
  • Diazepam binds to regulatory site, not site where GABA binds at
  • Enhances binding of GABA to GABA binding site
  • Needs GABA to work
  • Results in potentiating the influx of Cl- ions leading to hyperpolarisation of cell
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14
Q

Overdose of diazepam

A
  • Severe respiratory depression, esp with alcohol
  • Reversal: Flumazenil, a benzodiazepine antagonist
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15
Q

indication for levetiracetam

A
  • 2nd line adjunctive therapy
  • For partial onset seizures, myoclonic and primary generalised tonic clonic seizures
  • Can be used as monotherapy for partial onset seizures in newly diagnosed epilepsy
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16
Q

PK for levetiracetam

A
  • Highly soluble and permeable
  • Low intra and inter subject variability
  • Linear kinetics
  • Route: Oral or IV
17
Q

ADR for levetiracetam

A

Common
- Headache, vertigo, cough, depression, insomnia

Rare
- Agranulocytosis (decreased neutrophil count), suicide, delirium, dyskenisia (involuntary, erratic writhing of body)

18
Q

MOA of lamotrigine

A
  • Blocks voltage-gated sodium channels
  • Inhibits release of glutamate
  • Impedes sustained repetitive neuronal depolarization
19
Q

Indication of lamotrigine

A
  • 2nd line adjunctive therapy
  • Can be used as monotherapy for generalised/partial onset seizures, including tonic clonic seizures
  • Monotherapy of typical absence seizures
20
Q

PK of lamotrigine

A
  • Half life shorter in: induction of metabolism enzyme
    o Children
    o Co-administration with carbamazepine and phenytoin
  • Half life increased in: inhibition of metabolism enzyme
    o Co-administration with valproate
21
Q

ADR of lamotrigine

A

Common
- Headache, irritability, aggression, tiredness

Rare
- Agranulocytosis (decreased neutrophil count), hallucination, movement disorders, SJS/TEN, hepatic failure

22
Q

Indication of topiramate

A
  • Monotherapy for generalised/partial onset seizures, including tonic clonic seizures
  • Prophylaxis of migraine (not treatment)
23
Q

PK of topiramate

A
  • Linear PK
  • Route: Oral
  • Long half life
  • Renal CL
  • Not a potent inducer of drug metabolising enzymes
24
Q

ADR of topiramate

A

Common
- Depression, somnolence, fatigue, nausea, weight change

Rare
- Neutropenia, mania, tremor, transient blindness, SJS/TEN, hepatic failure

PR3153 CA (3 decks)

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