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105 - Perampanel

Published online by Cambridge University Press:  06 October 2020

Stephen D. Silberstein
Affiliation:
Thomas Jefferson University, Philadelphia
Michael J. Marmura
Affiliation:
Thomas Jefferson University, Philadelphia
Hsiangkuo Yuan
Affiliation:
Thomas Jefferson University, Philadelphia
Stephen M. Stahl
Affiliation:
University of California, San Diego
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Summary

THERAPEUTICS

Brands

• Fycompa

Generic?

• No

Class

• Antiepileptic drug (AED)

Commonly Prescribed for

(FDA approved in bold)

Adjunctive therapy for the treatment of partial-onset seizures with or without secondarily generalized seizures in patients with epilepsy aged 12 years and older

• Primary generalized tonic-clonic seizures in patients with epilepsy aged 12 years and older. Lennox-Gastaut syndrome

How the Drug Works

• Perampanel is a non-competitive selective antagonist of the ionotropic α-amino-3-hydroxy-5-methyl-4 isoxazolepropionic acid (AMPA) glutamate receptor on postsynaptic neurons. Its binding stabilizes the resting state of the channel and disrupts channel opening in response to agonist (e.g., glutamate) binding

• The precise mechanism by which perampanel exerts its antiepileptic effects in humans has not been fully elucidated

How Long Until It Works

• Drug steady state is reached in weeks

If It Works

• The goal is seizure remission. Continue as long as effective and well tolerated. Consider tapering and slowly stopping after 2 years without seizures, depending on the type of epilepsy

If It Doesn't Work

• Increase to highest tolerated dose

• Consider changing to another agent, adding a second agent, using a medical device, or a referral for epilepsy surgery evaluation. When adding a second agent, keep drug interactions in mind

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Drug interactions can complicate multi-drug therapy

Tests

• Not available

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• CNS AEs are probably caused by glutamate blockade effects

Notable AEs

• Dizziness, gait disturbance, somnolence, fatigue, falls, nausea, vertigo

• Hostility and aggressive behavior in 10–20% of patients under maximum dosage. They usually appear within the first 6 weeks of treatment

Life-Threatening or Dangerous AEs

• Suicidal behavior and ideation

• Withdrawal epilepsy, although rare due to its long half-life

Weight Gain

• Not unusual

Type
Chapter
Information
Essential Neuropharmacology
The Prescriber's Guide
, pp. 385 - 387
Publisher: Cambridge University Press
Print publication year: 2015

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  • Perampanel
  • Stephen D. Silberstein, Thomas Jefferson University, Philadelphia, Michael J. Marmura, Thomas Jefferson University, Philadelphia, Hsiangkuo Yuan, Thomas Jefferson University, Philadelphia
  • Edited in consultation with Stephen M. Stahl, University of California, San Diego
  • Book: Essential Neuropharmacology
  • Online publication: 06 October 2020
  • Chapter DOI: https://doi.org/10.1017/9781316161753.106
Available formats
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  • Perampanel
  • Stephen D. Silberstein, Thomas Jefferson University, Philadelphia, Michael J. Marmura, Thomas Jefferson University, Philadelphia, Hsiangkuo Yuan, Thomas Jefferson University, Philadelphia
  • Edited in consultation with Stephen M. Stahl, University of California, San Diego
  • Book: Essential Neuropharmacology
  • Online publication: 06 October 2020
  • Chapter DOI: https://doi.org/10.1017/9781316161753.106
Available formats
×

Save book to Google Drive

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Google Drive.

  • Perampanel
  • Stephen D. Silberstein, Thomas Jefferson University, Philadelphia, Michael J. Marmura, Thomas Jefferson University, Philadelphia, Hsiangkuo Yuan, Thomas Jefferson University, Philadelphia
  • Edited in consultation with Stephen M. Stahl, University of California, San Diego
  • Book: Essential Neuropharmacology
  • Online publication: 06 October 2020
  • Chapter DOI: https://doi.org/10.1017/9781316161753.106
Available formats
×