Perampanel

Oral
Generalised tonic-clonic seizures, Partial seizures

Patients taking concomitant CYP3A inducing antiepileptics: Titrate at intervals of at least 1 wk.

Moderate to severe: Contraindicated.

Mild to moderate: Max: 8 mg daily. Severe: Contraindicated.

May be taken with or without food.

Severe hepatic and moderate to severe renal impairment.

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.

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).

This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery. Avoid abrupt withdrawal.

Monitor seizure frequency and duration, suicidality (during therapy and for at least 1 mth after discontinuation), wt.

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).

Increased sedative and cognitive effects w/ alcohol. Decreased concentrations w/ St. John’s wort.

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.

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

Store between 15-30°C.

Anticonvulsants

N03AX22 - perampanel ; Belongs to the class of other antiepileptics.

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.