Perampanelum

Uses

Perampanelum is a non-competitive AMPA glutamate receptor antagonist used to treat partial-onset seizures with or without secondarily generalized seizures, and as adjunctive treatment of primary generalized tonic-clonic seizures in patients with epilepsy.

Used in patients over 12 years old for the treatment of partial-onset seizures that may or may not occur with generalized seizures.

Perampanelum is also used to associated treatment for these conditions: Grand mal Generalized tonic-clonic seizure, Partial-Onset Seizures

How Perampanelum works

The exact mechanism of action of perampanel in seizures is not yet determined, but it is known that perampanel decreases neuronal excitation by non-competitive ihibition of the AMPA receptor.

Toxicity

The FDA label includes an important warning of serious or life-threatening behavioral and psychiatric adverse reactions including aggression, hostility, irritability, anger, and homicidal thoughts in patients taking perampanel.

Food Interaction

• Take with or without food. Food slows the rate of absorption but not the extent.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Perampanelum Cholesterol interaction

[Moderate] Increased levels of triglycerides have occurred in patients using perampanel.

Care should be taken when prescribing this agent to patients with high triglycerides levels, and close monitoring of lipid profile is recommended during therapy.

Perampanelum Drug Interaction

Moderate: aripiprazole, lorazepam, diphenhydramine, brivaracetam, divalproex sodium, levetiracetam, lamotrigine, escitalopram, pregabalin, clobazam, quetiapine, topiramate, sertraline, cetirizineUnknown: fluticasone nasal, esomeprazole, montelukast, lacosamide, cyanocobalamin, cholecalciferol

Perampanelum Disease Interaction

Major: renal impairmentModerate: suicidal tendency, elevated triglycerides, weight gain, Perampanel – hepatic impairment

Volume of Distribution

The volume of distribution of perampanel was not quantified.

Elimination Route

After oral adminitration, perampanel is absorbed rapidly and completely.

Half Life

Perampanelum has a long elmination half-life of about 105 hours.

Clearance

In healthy patients, perampanel has a clearance of about 12 mL/min.

Elimination Route

Perampanelum is eliminated mostely in the feces (48%) and to a lesser exten in the urine (22%).

Innovators Monograph

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