Fycompa Perampanel Tablets

1. Indications and Usage
Partial-Onset Seizures:
Treatment of patients 4 years of age and older with partial-onset seizures with or without secondary generalization as adjunctive therapy.
Primary Generalized Tonic-Clonic Seizures:
Treatment of patients 12 years of age and older with primary generalized tonic-clonic seizures as adjunctive therapy.
2. Dosage and Administration
Route of Administration:
For Oral Use ONLY.
Recommended Dosage:
Starting Dose: 2 mg once daily at bedtime.
Titration: Dose can be increased in 2 mg increments at intervals of no less than 1 week (or 2 weeks depending on co-administered drugs).
Maintenance: Recommended dose is 4 mg to 12 mg once daily.
Maximum Dose: 12 mg once daily.
Administration:
Swallow tablets whole; do not chew, crush, or split.
Take once daily at bedtime (to minimize CNS side effects).
3. Mechanism of Action
AMPA Receptor Antagonism:
Perampanel is a selective, non-competitive antagonist of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor.
Blocking Excitation:
Glutamate is the major excitatory neurotransmitter in the brain. By blocking AMPA receptors on the postsynaptic membrane, perampanel inhibits glutamate-mediated neuronal excitation.
Seizure Control:
This inhibition reduces the excessive neuronal firing associated with seizure propagation.
4. Safety and Warnings
Serious Psychiatric and Behavioral Reactions (Boxed Warning):
Severe psychiatric and behavioral adverse reactions (e.g., aggression, hostility, irritability, and homicidal ideation) have occurred.
Action: Monitor patients for emergence or worsening of these symptoms. Discontinue immediately if severe reactions occur.
Dizziness and Coordination Problems:
May cause dizziness, ataxia, and somnolence. Caution patients regarding driving or operating machinery.
Suicidal Behavior:
Monitor for emergence of suicidal thoughts or behavior.
Drug Interactions:
CYP3A4 Inducers: Drugs like carbamazepine, phenytoin, or oxcarbazepine significantly decrease perampanel exposure (approx. 50–67%), requiring dose adjustments (up to 12 mg max).
Oral Contraceptives: At doses ≥12 mg/day, it may reduce the efficacy of hormonal contraceptives (e.g., levonorgestrel).
5.Adverse Reactions
Most Common:
Dizziness, somnolence, headache, fatigue, irritability, nausea, vomiting, weight gain, diarrhea, and fall.
6.Drug Interactions
Metabolism:
Primarily metabolized by CYP3A4/5.
Contraindications/Precautions:
Avoid strong CYP3A4 inducers (e.g., rifampin).
Caution with CNS depressants (e.g., alcohol, opioids) due to additive effects.
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Perampanel.
Available Strength: 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg tablets.
Appearance: Film-coated tablets (color varies by strength).
Storage: Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F).