THERAPEUTICS

Brands

• Aptiom

Generic?

• No

Class

• Antiepileptic drug (AED)

Commonly Prescribed for

(FDA approved in bold)

• Adjunctive treatment of partial-onset seizures

• Generalized tonic-clonic seizures

How the Drug Works

• Eslicarbazepine acetate is a prodrug that is metabolized to its major active metabolite eslicarbazepine (S-licarbazepine), and to the minor active metabolites R-licarbazepine and oxcarbazepine

• Eslicarbazepine binds to the inactivated form of the voltage-gated sodium channel (VGSC) and prevents its reversion to the receptive resting or deactivated form. The mechanism is shared by carbamazepine and oxcarbazepine

• The affinity of S-licarbazepine for VGSC in the resting state was 5- to 15-fold lower than that of R-licarbazepine, oxcarbazepine, and carbamazepine. Thus, eslicarbazepine had enhanced inhibitory selectivity for rapidly firing neurons versus those displaying normal activity; i.e., eslicarbazepine binds preferentially to active neurons

How Long Until It Works

• Seizures: 2 weeks or less

If It Works

• The goal is seizure remission. Continue as long as effective and well tolerated. Consider tapering and slowly stopping after 2 years without seizures, depending on the type of epilepsy

If It Doesn't Work

• Increase to highest tolerated dose

• Consider changing to another agent, adding a second agent, using a medical device, or a referral for epilepsy surgery evaluation. When adding a second agent, keep drug interactions in mind

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Drug interactions can complicate multi-drug therapy

Tests

• Check sodium levels for symptoms of hyponatremia or in patients susceptible to hyponatremia

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• CNS AEs are probably caused by sodium channel blockade effects

Notable AEs

• Sedation, dizziness, ataxia, headache, tremor, blurred vision, vertigo, cognitive dysfunction

• Nausea, vomiting, anorexia, dyspepsia

Life-Threatening or Dangerous AEs

• Suicidal behavior and ideation

• Dermatological reactions uncommon and rarely severe but include erythema multiforme, toxic epidermal necrolysis, and Stevens-Johnson syndrome. Drug reaction with eosinophilia and systemic symptoms (DRESS)/multi-organ hypersensitivity