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Perampanel

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Perampanel, Fycompa

  • Indications
  1. Refractory partial-onset Seizures
  2. Generalized Tonic Clonic Seizures (adjunct)
  • Contraindications
  1. Severe renal disease
  2. Severe liver disease
  3. Combination with strong CYP3A4 Inducers
  • Mechanism
  1. Antiepileptic
  2. Glutamate receptor Antagonist (first in the class)
    1. Selective for AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) subunit of Glutamate receptors
    2. Prevents Glutamate triggered Neuronal activation and excitation, as well as repetitive firing
    3. Stabilizes hyper-excited Neuronal membranes
  • Precautions
  1. FDA Schedule III
    1. Abuse potential due to associated euphoria
  • Adverse Effects
  1. Mood changes
    1. Euphoria
    2. Anger, irritability or hostility
  2. Dizziness, Vertigo or Ataxia
  3. Headache
  4. Weight gain
  5. Sedation
    1. Caution when combined with other CNS Depressants
  • Dosing
  • Adults and Children over Age 12 years
  1. FDA approved for age over 12 years
  2. Initial: 2 mg orally at bedtime
  3. Titrate To: 4-8 mg orally at bedtime (increase by 2 mg/day on a weekly basis)
    1. Slow dose titration to every 2 weeks or less in the elderly
    2. Slow dose titration in moderate renal Impairment (avoid in severe renal Impairment)
  4. Maximum: 12 mg/day
    1. Hepatic Impairment: 6 mg/day max in mild disease, 4 mg max in moderate disease (avoid in severe liver disease)
  • Drug Interactions
  1. Levonorgestrel containing contraceptives
    1. Perampanel at maximum dose (12 mg/day) decreases the contraceptive efficacy
    2. Use alternative Contraception
  2. CYP3A4 Inducers
    1. Increase starting dose to 4 mg in moderate enzyme inducers
    2. Avoid with strong enzyme inducers
  • Safety
  1. Unknown Safety in Pregnancy
    1. Developmental toxicity in animals
  2. Unknown Safety in Lactation
  • Resources
  1. Perampanel (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=71cf3309-e182-473c-8b0b-280cabd0e122
  2. Medscape
    1. http://reference.medscape.com/drug/fycompa-perampanel-999784
  • References
  1. (2014) Presc Lett 21(11): 65
  2. (2022) Presc Lett, Resource #361206, Antiseizure Medications
  3. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 56-7
  4. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  5. French (2012) Neurology 79(6):589-96 [PubMed]