eslicarbazepine

eslicarbazepine

(es-lye-kar-bay-ze-peen) ,

Aptiom

(trade name)

Classification

Therapeutic: anticonvulsants
Pharmacologic: carbamazepine analogues
Pregnancy Category: C

Indications

Adjunctive treatment of partial-onset seizures.

Action

Inhibits voltage-gated sodium channels.

Therapeutic effects

Decreased incidence and severity of partial-onset seizures.

Pharmacokinetics

Absorption: Eslicarbazepine acetate (the oral dose form) is rapidly converted to eslicarbazepine, its active form which is 90% bioavailable.
Distribution: Enters breast milk, remainder of distribution unknown.
Metabolism and Excretion: Rapidly and extensively metabolized via first-pass hepatic metabolism to its active form (eslicarbazepine); other minor metabolites have anticonvulsant activity. Excreted in urine as unchanged eslicarbazepine and metabolites.
Half-life: 13–20 hr.

Time/action profile (blood levels†)

ROUTEONSETPEAKDURATION
POunknown1–4 hr 24 hr
†Anticonvulsant effect is evident within 28 days of treatment.

Contraindications/Precautions

Contraindicated in: Hypersensitivity to eslicarbazepine or oxcarbazepine; Severe hepatic impairment; Obstetric: May cause fetal harm; Lactation: Enters breast milk, avoid breast feeding;.
Use Cautiously in: Concurrent use with carbamazepine (↑ risk of adverse reactions);Renal impairment (dose adjustment required for CCr < 50 mL/min); Geriatric: Consider age-related decrease in renal, hepatic and cardiovascular function, concurrent disease states and drug therapies; Pediatric: Safe and effective use in children < 18 yr has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • suicidal behavior/ideation (life-threatening)
  • dizziness (most frequent)
  • drowsiness (most frequent)
  • fatigue (most frequent)
  • cognitive dysfunction
  • depression
  • headache
  • insomnia
  • vertigo

Ear, Eye, Nose, Throat

  • visual changes

Gastrointestinal

  • nausea (most frequent)
  • drug-induced liver injury
  • vomiting

Dermatologic

  • serious dermatologic reactions including Stevens-Johnson Syndrome (life-threatening)

Endocrinologic

  • abnormal thyroid function

Fluid and Electrolyte

  • hyponatremia

Neurologic

  • gait disturbance
  • tremor

Miscellaneous

  • hypersensitivity reactions including anaphylaxis, angioedema, drug reaction with eosinophilia and systemic symptoms (DRESS)/multiorgan hypersensitivity (life-threatening)

Interactions

Drug-Drug interaction

When used with carbamazepine dose adjustments of both medications may be needed.When used with phenytoin, dose of eslicarbazepine may need to be ↑ and phenytoin dose adjusted.Dose may need to be ↑ when used concurrently with phenobarbital or primidone.May ↓ effectiveness of hormonal contraceptives (additional/alternative contraception required).May ↑ blood levels of clobazam, phenytoin or omeprazole.May induce CYP3A4 enzyme system resulting in ↓ levels of other drugs metabolized by CYP3A4 including simvastatin or rosuvastatin.May alter the response to warfarin.

Route/Dosage

Oral (Adults) 400 mg once daily initially, after 1 wk increase to 800 mg daily, can be increased after 1 wk to maximum of 1200 mg daily (usual maintenance dose is 800 mg daily). Do not discontinue abruptly.

Renal Impairment

Oral (Adults) CCr < 50 mL/min—200 mg once daily initially, after 2 wk increase to 400 mg once daily, may be increases to a maximum maintenance dose of 600 mg once daily. Do not discontinue abruptly.

Availability

Tablets: 200 mg, 400 mg, 600 mg, 800 mg

Nursing implications

Nursing assessment

  • Monitor closely for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts or behavior or depression.
  • Assess for signs and symptoms of anaphylaxis (rash, dyspnea, laryngeal edema). Discontinue eslicarbazepine and treat symptomatically.
  • Monitor for signs and symptoms of hyponatremia (nausea, tiredness, lack of energy, irritability, confusion, muscle weakness or muscle spasms, more frequent or severe seizures.
  • Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis and/or eosinophilia.
  • Lab Test Considerations: Monitor hepatic function (AST, ALT, bilirubin) prior to starting and periodically during therapy. Discontinue eslicarbazepine if jaundice or significant liver injury occurs.
    • May cause ↓ T3 and T4 (free and total) levels; may not be associated with other abnormal thyroid function tests. Evaluate abnormal thyroid tests clinically.
    • Monitor serum sodium periodically during therapy. May cause hyponatremia.

Potential Nursing Diagnoses

Risk for injury (Adverse Reactions)

Implementation

  • Oral: Administer with or without food. Tablets may be swallowed whole or crushed.

Patient/Family Teaching

  • Instruct patient to take eslicarbazepine as directed. Do not stop taking without consulting health care professional; dose should be decreased gradually upon discontinuation.
  • Instruct patients that behavioral changes; swelling of face, eyes, lips or tongue; trouble swallowing or breathing; skin rash; hives; fever; swollen glands; sore throat; painful sores in mouth or around eyes; yellowing of skin or eyes; unusual bleeding or bruising; severe fatigue or weakness; severe muscle pain; frequent infections or infections that don't go away should be reported to health care professional immediately. Advise patient and family to notify health care professional if thoughts about suicide or dying, attempts to commit suicide; new or worse depression; new or worse anxiety; feeling very agitated or restless; panic attacks; trouble sleeping; new or worse irritability; acting aggressive; being angry or violent; acting on dangerous impulses; an extreme increase in activity and talking, other unusual changes in behavior or mood occur.
  • May cause nervous system problems or cognitive dysfunction (dizziness, trouble walking or coordination, feeling sleepy or tired, trouble concentrating, vision problems, memory impairment, amnesia, speech disorder, slowness of thought). Advise patients to avoid driving or other activities requiring alertness until response to medication is known. May require discontinuation of therapy.
  • Inform patient that fever associated with signs or other organ system involvement (rash, lymphadenopathy, hepatic dysfunction) may be related to eslicarbazepine; notify health care professional immediately.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Advise patients to carry identification describing disease and medication regimen at all times.
  • Advise female patients to use a nonhormonal form of contraception while taking eslicarbamazepine, to avoid breastfeeding, and to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Encourage patients who become pregnant to enroll in the North American Antiepileptic Drug Pregnancy Registry. Must be done by patients themselves by calling 1-888-233-2334 or on the website http://www.aedpregnancyregistry.org.
  • Emphasize the importance of follow-up lab tests and eye exams to monitor for side effects.

Evaluation/Desired Outcomes

  • Decreased incidence and severity of partial-onset seizures.
References in periodicals archive ?
Impact on quality of life and clinician-related global improvement with eslicarbazepine acetate as add-on treatment to antiepileptic monotherapy in adults with partial-onset seizures.
Reddy's Laboratories Introduces Geodon II-99 Sun Pharmaceutical Unveils Zyprexa Zydis II-99 H Lundbeck Introduces Onfi Anti-Epileptic Drug in US II-99 Eisai and Nobelpharma to Introduce Fostoin Anticonvulsant Agent II-99 Eisai Europe Launches Zebinix Eslicarbazepine Acetate II-99 Eisai Launches Fycompa II-99 H.
Eslicarbazepine (Aptiom) is indicated as adjunctive treatment of partial-onset seizures.
The AEDs in this category are: valproate, lamotrigine, perampanel, retigabine, rufinamide, clobazam, clonazepam, oxcarbazepine, eslicarbazepine, zonisamide, topiramate.
The FDA reported that three studies of patients with partial epilepsy showed the drug, also known by its chemical name eslicarbazepine acetate, effectively reduced the frequency of seizures.
Dainippon Sumitomo gained the drug, also known by its chemical name eslicarbazepine acetate, in its October purchase of Sepracor Inc.
The expanding number and growing uptake of third-generation antiepileptic drugs (AEDs), led by lacosamide (UCB's Vimpat) and including other agents such as perampanel (Eisai's Fycompa), eslicarbazepine acetate (Sunovion/Bial/Eisai's Zebinix/Stedesa*) and ezogabine/retigabine (GlaxoSmithKline/Valeant's Potiga/Trobalt), will be a major contributor to such growth.
AES represents a significant milestone for eslicarbazepine acetate, with 19 abstracts to present over four days with two important sub analyses from a European real-world study.
s Canadian subsidiary is seeking regulatory approval to sell Stedesa, or eslicarbazepine acetate, in Canada as an adjunctive therapy for partial-onset seizures in adults with epilepsy, the company reported in a news release.
Bial) is pleased to announce positive results for a pivotal phase 3 non-inferiority study comparing the efficacy and safety of eslicarbazepine acetate (ESL) to controlled release carbamazepine (CBZ-CR) as monotherapy in newly diagnosed adult patients with partial-onset seizures (POS).
has filed an application with regulators to sell eslicarbazepine acetate under the name Stedesa as a treatment for partial-onset seizures in adults with epilepsy.