Perampanel


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Adjunctive therapy in partial seizures and generalised tonic-clonic seizures Initial: 2 mg once daily at bedtime, adjust in increments of 2 mg at intervals of at least 2 wk, according to response. Maintenance: 4-8 mg/day. Max: 12 mg/day.
Dosage Details
Oral
Generalised tonic-clonic seizures, Partial seizures
Adult: As adjunctive therapy: Initially, 2 mg once daily at bedtime, adjusted in increments of 2 mg at intervals of at least 2 wk, according to response. Maintenance: 4-8 mg daily. Max: 12 mg daily.
Child: ≥12 yr Same as adult dose. 
Special Patient Group
Patients taking concomitant CYP3A inducing antiepileptics: Titrate at intervals of at least 1 wk.
Renal Impairment
Moderate to severe: Contraindicated.
Hepatic Impairment
Mild to moderate: Max: 8 mg daily. Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Severe hepatic and moderate to severe renal impairment.
Special Precautions
Patient w/ history of psychiatric or behavioural problems and substance abuse, and those at risk of falls. Patients taking concomitant CYP3A inducing antiepileptics. Mild to moderate hepatic impairment. Childn. Pregnancy and lactation.
Adverse Reactions
Significant: Dizziness, somnolence, fatigue, gait disturbance (e.g. balance disorder, ataxia, abnormal coordination).
Nervous: Drowsiness, dysarthria, vertigo, anxiety, confusion, paraesthesia, fall.
GI: Increased/decreased appetite, nausea, vomiting.
Endocrine: Wt gain.
Musculoskeletal: Back pain.
Ophthalmologic: Diplopia, blurred vision.
Dermatologic: Rash.
Potentially Fatal: Serious neuropsychiatric events (e.g. aggression, irritability, anger, hostility, homicidal and suicidal ideation).
Patient Counseling Information
This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery. Avoid abrupt withdrawal.
MonitoringParameters
Monitor seizure frequency and duration, suicidality (during therapy and for at least 1 mth after discontinuation), wt.
Drug Interactions
Increased metabolism w/ other antiepileptics that are CYP3A inducers (e.g. carbamazepine, oxcarbazepine, phenytoin). May decrease the efficacy of OCs. Decreased concentrations w/ strong CYP enzyme inducers (e.g. rifampicin). Increased risk of CNS-related adverse effect of other CNS depressants (e.g. benzodiazepines, opiate analgesics, barbiturates, sedating antihistamines).
Food Interaction
Increased sedative and cognitive effects w/ alcohol. Decreased concentrations w/ St. John’s wort.
Action
Description: Perampanel is a selective, non-competitive antagonist of the ionotropic α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor on post-synaptic neurons. Its exact mechanism of action is not yet determined, however, it is known to reduce neuronal excitation by blocking the activity of glutamate, the primary excitatory neurotransmitter in the CNS.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed. Time to peak plasma concentration: 0.5-2.5 hr.
Distribution: Plasma protein binding: Approx 95%, mainly to albumin and α1-acid glycoprotein.
Metabolism: Extensively metabolised via oxidation, mainly by CYP3A4/5 enzymes (and to a lesser extent by CYP1A2 and CYP2B6 enzymes), w/ sequential glucuronidation.
Excretion: Via urine and faeces, as oxidative and conjugated metabolites. Elimination half-life: Approx 105 hr.
Chemical Structure

Chemical Structure Image
Perampanel

Source: National Center for Biotechnology Information. PubChem Database. Perampanel, CID=9924495, https://pubchem.ncbi.nlm.nih.gov/compound/Perampanel (accessed on Jan. 22, 2020)

Storage
Store between 15-30°C.
MIMS Class
ATC Classification
N03AX22 - perampanel ; Belongs to the class of other antiepileptics.
References
Anon. Perampanel. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/04/2017.

Anon. Perampanel. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/04/2017.

Buckingham R (ed). Perampanel. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2017.

Fycompa Tablet and Suspension (Eisai Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/04/2017.

Joint Formulary Committee. Perampanel. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2017.

Disclaimer: This information is independently developed by MIMS based on Perampanel from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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