Perampanel
Antiseizure medicines
Antiseizure medicines
The first AMPA glutamate receptor blocker for epilepsy, taken once a day at bedtime. It can cause hostility and aggression.
Quick facts
- Group
- Antiseizure medicines
- Target
- AMPA-type ionotropic glutamate receptor (GluA2)
- Used for
- Partial-onset
- Key effects
- Dizziness · Poor coordination and falls · Irritability
- Monitor
- Mood · Falls and balance · Weight
- ATC
- N03AX22
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows perampanel bound to the AMPA receptor GluA2 of the rat, whose binding site matches the human receptor's.
Perampanel is a first-in-class, selective, noncompetitive antagonist of the AMPA-type glutamate receptor. By damping fast excitatory transmission it prevents repetitive neuronal firing, and it appears to act more on the spread of seizures than on their start.
- Perampanel binds the AMPA receptor outside the glutamate site
- Fast excitatory currents shrink
- Seizure spread is limited
- Fewer focal and tonic-clonic seizures
Indications
- Partial-onset (focal) seizures Epilepsy and seizures →
- Primary generalized tonic-clonic seizures, as add-on treatment Epilepsy and seizures →
Adverse effects
Common
- Dizziness, a spinning sensation and drowsiness
- Poor coordination and falls, especially in older adults
- Irritability
- Weight gain
- Nausea, headache and tiredness
Contraindications
- Allergy to perampanel or any component of the product
Key interactions
- Carbamazepine, oxcarbazepine and topiramate
- Lower perampanel levels
- Contraceptives with levonorgestrel or other progestins
- May work less well; another method is used during treatment and for 1 month after
- St John's wort
- May lower perampanel levels
- Alcohol
- Worse dizziness, sedation and behavioural effects
What is monitored
- Mood, behaviour and aggression, during treatment and for a month after stopping
- Falls and balance
- Weight
- Seizure diary
Administration and safety
- Oral tablet or suspension at bedtime; the suspension is measured with the syringe supplied
- Raised gradually, not more often than once a week
- It can be habit-forming
Pregnancy and breastfeeding
Its safety in pregnancy is not established; contraception is discussed because perampanel can reduce progestin effectiveness.
Nursing care
- Ask about psychiatric history and aggressive behaviour before starting
- Tell the family to report any change in mood or behaviour at once
- Assess fall risk in older adults
- Advise a contraceptive method other than progestin-based ones
Pharmacokinetics
- Absorption
- Well absorbed by mouth
- Distribution
- Highly bound to plasma albumin
- Metabolism
- In the liver by CYP3A and glucuronidation
- Half-life
- Very long, which allows once-daily use
Test yourself
Think of the answer, then tap the question to see it.
What is the mechanism of perampanel?
Selective noncompetitive antagonism of AMPA-type glutamate receptors.
Which boxed warning applies to perampanel?
Serious psychiatric and behavioural reactions, including hostility and aggression.
Why can perampanel be given once a day?
Its half-life is very long.
Connections
← Back to the class: Antiseizure medicines
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Perampanel: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); RCSB PDB - 5L1F: AMPA subtype ionotropic glutamate receptor GluA2 in complex with noncompetitive inhibitor Perampanel (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.