es-lye-kar-BAY-ze-peen

Therapeutic Classification: anticonvulsants

Pharmacologic Classification: carbamazepine analogues

• Partial-onset seizures (as monotherapy or adjunctive therapy).

• Inhibits voltage-gated sodium channels.

• Decreased incidence and severity of partial-onset seizures.

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/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.

(blood levels†)

†Anticonvulsant effect is evident within 28 days of treatment.

Contraindicated in:

• Hypersensitivity to eslicarbazepine or oxcarbazepine
• Severe hepatic impairment
• Concomitant use with oxcarbazepine
• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• Concurrent use with carbamazepine (↑ risk of adverse reactions)
• Renal impairment (dose adjustment required for CCr <50 mL/min)
• Pedi: Children <4 yr (safety and effectiveness not established).
• Geri: Consider age-related ↓ in renal, hepatic and cardiovascular function, concurrent disease states and drug therapies in older adults

Derm: STEVENS-JOHNSON SYNDROME, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), TOXIC EPIDERMAL NECROLYSIS.

EENT: visual changes.

Endo: abnormal thyroid function.

F and E: hyponatremia.

GI: nausea, drug-induced liver injury, vomiting.

Hemat: agranulocytosis, leukopenia, pancytopenia.

Neuro: dizziness, drowsiness, fatigue, cognitive dysfunction, depression, gait disturbance, headache, insomnia, SUICIDAL BEHAVIOR/IDEATION, tremor, vertigo.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA).

Drug-Drug:

• Carbamazepine may ↓ levels; when used concomitantly, dosage adjustments of both medications may be needed.
• Phenytoin, phenobarbital, and primidone may ↓ levels; may need to ↑ eslicarbazepine dose when used concomitantly.
• May ↓ effectiveness of hormonal contraceptives (additional/alternative contraception required).
• May ↑ blood levels of clobazam, phenytoin or omeprazole.
• May ↓ levels and effectiveness of CYP3A4 substrates, including simvastatin or rosuvastatin.
• May alter the response to warfarin.

• PO (Adults): 400 mg once daily initially; may ↑ by 400–600 mg/day on weekly basis to maintenance dosage of 800–1600 mg once daily.
• PO (Children ≥4 yr and >38 kg): 400 mg once daily initially; may ↑ by 400 mg/day on weekly basis to maintenance dosage of 800–1200 mg once daily.
• PO (Children ≥4 yr and 32–38 kg): 300 mg once daily initially; may ↑ by 300 mg/day on weekly basis to maintenance dosage of 600–900 mg once daily.
• PO (Children ≥4 yr and 22–31 kg): 300 mg once daily initially; may ↑ by 300 mg/day on weekly basis to maintenance dosage of 500–800 mg once daily.
• PO (Children ≥4 yr and 11–21 kg): 200 mg once daily initially; may ↑ by 200 mg/day on weekly basis to maintenance dosage of 400–600 mg once daily.

(Generic available)

• Tablets: 200 mg; 400 mg; 600 mg; 800 mg;

• Monitor seizure activity during therapy.
• 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.
• Monitor for signs and symptoms of DRESS (fever, rash, lymphadenopathy, and/or facial swelling, associated with involvement of other organ systems (hepatitis, nephritis, hematologic abnormalities, myocarditis, myositis) during therapy. May resemble an acute viral infection. Eosinophilia is often present. Discontinue therapy if signs occur.

• 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 and chloride levels periodically during therapy. May cause hyponatremia.
  • May cause pancytopenia, agranulocytosis, and leukopenia. Discontinue therapy if hematologic adverse reactions occur.

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

• Instruct patient to take eslicarbazepine as directed. Do not stop taking without consulting health care professional; dose should be decreased gradually upon discontinuation.
• 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.
• 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; signs and symptoms of DRESS; frequent infections or infections that don't go away should be reported to health care professional immediately.
• 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.
• Rep: Advise female patients to use a nonhormonal form of contraception while taking eslicarbazepine, 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 www.aedpregnancyregistry.org. May impair female fertility.
• Emphasize the importance of follow-up lab tests and eye exams to monitor for side effects.

• Decreased incidence and severity of partial-onset seizures.

Aptiom

NDC Code^*

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-202- Aptiom
    • 63402-202-28- 4 BLISTER PACK in 1 CARTON (63402-202-28) > 7 TABLET in 1 BLISTER PACK (63402-202-07)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-202- Aptiom
    • 63402-202-30- 30 TABLET in 1 BOTTLE (63402-202-30)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-204- Aptiom
    • 63402-204-28- 4 BLISTER PACK in 1 CARTON (63402-204-28) > 7 TABLET in 1 BLISTER PACK (63402-204-07)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-204- Aptiom
    • 63402-204-30- 30 TABLET in 1 BOTTLE (63402-204-30)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-206- Aptiom
    • 63402-206-28- 4 BLISTER PACK in 1 CARTON (63402-206-28) > 7 TABLET in 1 BLISTER PACK (63402-206-07)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-206- Aptiom
    • 63402-206-60- 60 TABLET in 1 BOTTLE (63402-206-60)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-208- Aptiom
    • 63402-208-28- 4 BLISTER PACK in 1 CARTON (63402-208-28) > 7 TABLET in 1 BLISTER PACK (63402-208-07)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-208- Aptiom
    • 63402-208-30- 30 TABLET in 1 BOTTLE (63402-208-30)

• 63402- Sunovion Pharmaceuticals Inc.
  • 63402-248- Aptiom
    • 63402-248-56- 4 BLISTER PACK in 1 CARTON (63402-248-56) > 1 KIT in 1 BLISTER PACK (63402-248-14) * 7 TABLET in 1 BLISTER PACK (63402-208-17) * 7 TABLET in 1 BLISTER PACK (63402-204-17)