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