Company: Eisai Ltd.
Legal category: Prescription. GMS. Sport permitted.
Active ingredient: Perampanel 2mg, 4mg, 6mg, 8mg, 10mg, 12mg.
Description: Round, biconvex film-coated tablets. Orange, red, pink, purple, green or blue, marked E275, E277, E294, E295, E296 or E297 on one side, and 2, 4, 6, 8, 10 or 12 on reverse, respectively.
Presentation: 2mg-7, €40.95; all other strengths-28, €163.80.
Indication: Adjunctive treatment of partial-onset seizures with or without secondarily generalised seizures in patients with epilepsy aged 12 years and older.
Pharmacology: Perampanel is a first-in-class selective, non-competitive antagonist of the ionotropic α-amino-3- hydroxy-5-methyl-4-isoxazoleproprionic acid (AMPA) glutamate receptor on post-synaptic neurons. Glutamate is the primary excitatory neurotransmitter in the central nervous system and is implicated in a number of neurological disorders caused by neuronal overexcitation. Activation of AMPA receptors by glutamate is thought to be responsible for most fast excitatory synaptic transmission in the brain. The precise mechanism by which perampanel exerts its anti-epileptic effects remains to be fully elucidated.
Dosage: Adult: 12 years and over, initially 2mg/day swallowed whole at bedtime. Titrate according to patient response. May be increased by 2mg/day increments to maintenance of 4mg/day to 8mg/day. Based on patient response at 8mg/day, may be increased by 2mg/day increments to 12mg/day. Titrate after at least 2 week intervals if taking drugs that do not shorten the half-life of perampanel. Titrate after at least 1 week intervals if taking drugs that shorten the half-life of perampanel. Mild to moderate hepatic impairment: Up-titrate using 2mg doses after at least 2 week intervals based on patient response. Maximum 8mg/day. Elderly: Caution in polymedicated patients. Children: Under 12 years, safety and efficacy not established.
Contraindications: Hypersensitivity to the active substance or to any of the excipients. Pregnancy, lactation.
Special precautions: Not recommended: Moderate/severe renal impairment, haemodialysis, severe hepatic impairment. Monitor for signs of suicidal ideation and behaviours. Withdraw gradually; rebound seizures may occur. Increased risk of falls (especially in elderly). Consider dose reduction in cases of persistent aggressive symptoms. History of substance abuse (caution). Women of childbearing potential must use additional non-hormonal forms of contraception. Driving/using machines (dizziness and somnolence may occur). Contains lactose.
Drug interactions: Oral contraceptives, CYP 3A inducing anti-epileptics (carbamazepine, phenytoin, oxcarbazepine), other anti-epileptics (see SPC), cytochrome P450 inducers/inhibitors, CYP3A4 substrates, alcohol.
Adverse drug reactions: Dizziness, somnolence, decreased or increased appetite, aggression, anger, anxiety, confusional state, ataxia, dysarthria, balance disorder, irritability, diplopia, blurred vision, vertigo, nausea, back pain, gait disturbance, fatigue, increased weight, falls.
Full prescribing information and references available from Eisai Ltd. Telephone: 0044 (0) 208 600 1400. Email: EUmedinfo@eisai.net