Eslicarbazepine Acetate

Eslicarbazepine acetate is used for partial-onset seizures as monotherapy or adjunctive therapy. Eslicarbazepine acetate is available under the following different brand names: Aptiom.

Dosages of Eslicarbazepine Acetate:

Adult and Pediatric Dosage Forms and Strengths

Tablet

• 200mg
• 400mg
• 600mg
• 800mg

Dosage Considerations – Should be Given as Follows:

Partial-Onset Seizures

Indicated for partial-onset seizures as monotherapy or adjunctive therapy

• Initial
  • 400 mg orally once daily
  • For some patients, treatment may be initiated at 800 mg once daily if the need for additional seizure reduction outweighs an increased risk of adverse reactions during initiation
• Titration and maintenance
  • Increase dose by weekly increments of 400-600 mg, based on clinical response and tolerability
  • The recommended maintenance dose is 800-1600 mg once daily
  • Monotherapy: Consider 800 mg/day maintenance dose in patients unable to tolerate 1200 mg/day
  • Adjunctive therapy: 1600 mg/day should be considered in patients who did not achieve a satisfactory response with 1200 mg/day

• Recommended initial weight-based dosage
  • 11-21 kg: 200 mg orally once daily initially; titration increment not to exceed 200 mg/day
  • 22-38 kg: 300 mg orally once daily; titration increment not to exceed 300 mg/day
  • Greater than 38kg: 400 mg orally once daily; titration increment not to exceed 400 mg/day
  • Dosage should be increased based on clinical response and tolerability, no more frequently than once per week

• Maintenance dosage
  • 11-21 kg: Not to exceed 400-600 mg/day
  • 22-31 kg: Not to exceed 500-800 mg/day
  • 32-38 kg: Not to exceed 600-900 mg/day
  • Greater than 38kg: Not to exceed 800-1200 mg/day

Children under 4 years: Safety and efficacy not established

Dosage Modifications

Do not take adjunctively with oxcarbazepine

Coadministration with enzyme-inducing AEDs (e.g., carbamazepine, phenytoin, phenobarbital, primidone): May need to increase eslicarbazepine dose

Renal impairment

• Mild (CrCl 50 mL/minute or greater): No dosage adjustment is necessary
• Moderate-to-severe (CrCl less than 50 mL/minute): Reduce the initial, titration, and maintenance doses by 50%; may adjust titration and maintenance doses according to clinical response

Hepatic impairment

• Mild-to-moderate: No dosage adjustment is required
• Severe: Not recommended (not studied)

Dosing Considerations

When discontinuing eslicarbazepine acetate, gradually reduce the dose and avoid abrupt discontinuation to minimize the risk of increased seizure frequency and status epilepticus

Common side effects of eslicarbazepine acetate include:

• Dizziness
• Headache
• Drowsiness
• Nausea
• Double vision
• Blurred vision
• Vomiting
• Diarrhea
• Fatigue
• Loss of coordination
• Balance disorder
• Falls
• Tremors
• Low blood sodium (hyponatremia)
• Weakness/lethargy
• Gait disturbance
• Swelling of extremities
• Urinary tract infections (UTIs)
• Depression
• Rash
• Insomnia
• Slurred speech
• Memory disturbance
• Nystagmus
• Constipation
• Abdominal pain

Postmarketing side effects of eslicarbazepine acetate reported include:

• Hematologic and Lymphatic Systems: Leukopenia, agranulocytosis, thrombocytopenia, megaloblastic anemia, and pancytopenia
• Metabolism and Nutrition Disorders: Syndrome of inappropriate antidiuretic hormone secretion (SIADH)

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

• Severe interactions of eslicarbazepine acetate include:
  • artemether/lumefantrine
  • cariprazine
  • cobimetinib
  • daclatasvir
  • dienogest/estradiol valerate
  • doravirine
  • elbasvir/grazoprevir
  • elvitegravir/cobicistat/emtricitabine/tenofovir DF
  • lumacaftor/ivacaftor
  • lumefantrine
  • lurasidone
  • naloxegol
  • ombitasvir/paritaprevir/ritonavir
  • ombitasvir/paritaprevir/ritonavir & dasabuvir
  • oxcarbazepine
  • panobinostat
  • praziquantel
  • regorafenib
  • rilpivirine
  • roflumilast
  • vandetanib
• Eslicarbazepine acetate has serious interactions with at least 79 different drugs.
• Eslicarbazepine acetate has moderate interactions with at least 165 different drugs.
• Eslicarbazepine acetate has mild interactions with at least 82 different drugs.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

• This medication contains eslicarbazepine acetate. Do not take Aptiom if you are allergic to eslicarbazepine acetate or any ingredients contained in this drug.
• Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity to eslicarbazepine or oxcarbazepine

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Eslicarbazepine Acetate?”

Long-Term Effects

• See "What Are Side Effects Associated with Using Eslicarbazepine Acetate?”

Cautions

• See FDA warning on potential suicidal behavior; monitor patients for notable changes in behavior that might be associated with suicidal thoughts or depression (notify healthcare provider immediately if symptoms occur)
• Antiepileptic drugs (AEDs), including eslicarbazepine, increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication; monitor patients for notable changes in behavior that might be associated with suicidal thoughts or depression (notify healthcare provider immediately if symptoms occur)
• Serious dermatologic reactions reported, including Stevens-Johnson syndrome (SJS); serious and sometimes fatal dermatologic reactions, including toxic epidermal necrolysis (TEN) and SJS, have been reported in patients using oxcarbazepine or carbamazepine which are chemically related
• Drug reaction with eosinophilia and systemic symptoms (DRESS) reported; DRESS may be fatal or life-threatening, and although not exclusively, presents with fever, rash, and/or lymphadenopathy, in association with other organ system involvement, such as hepatitis, nephritis, hematological abnormalities, myocarditis, or myositis sometimes resembling an acute viral infection
• Clinically significant hyponatremia (sodium less than 125 mEq/L); consider monitoring serum sodium and chloride levels during maintenance treatment, particularly in patients receiving other medications known to decrease serum sodium levels, and perform in patients exhibiting symptoms of hyponatremia develop (e.g., nausea/vomiting, malaise, headache, lethargy, confusion, irritability, muscle weakness/spasms, obtundation, or increase in seizure frequency or severity)
• Anaphylactic reactions and angioedema: Monitor for breathing difficulties or swelling; discontinue if another cause cannot be established
• Hyponatremia: Monitor sodium levels in patients at risk or patients experiencing hyponatremia symptoms
• Neurological adverse reactions: Monitor for dizziness, disturbance in gait and coordination, somnolence, fatigue, cognitive dysfunction, and visual changes; caution when driving or operating machinery
• Discontinuing: Withdraw gradually to minimize the risk of increased seizure frequency and status epilepticus
• Drug-induced liver injury: Discontinue jaundice or evidence of significant liver injury
• Dose-dependent decreases in serum T3 and T4 (free and total) values reported
• Rare cases of pancytopenia, agranulocytosis and leukopenia have been reported during postmarketing use of eslicarbazepine; consider discontinuation of treatment in patients who develop pancytopenia, agranulocytosis, or leukopenia

Pregnancy and Lactation

• The limited available data with eslicarbazepine acetate use in pregnant women are insufficient to inform a drug-associated risk of adverse developmental outcomes. Women who are taking eslicarbazepine acetate during pregnancy are encouraged to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling 1-888-233-2334 or visiting http://www.aedpregnancyregistry.org.
• Women of reproductive potential taking eslicarbazepine acetate who are using a contraceptive containing ethinylestradiol or levonorgestrel are advised to use additional or alternative non-hormonal birth control.
• Eslicarbazepine is present in human milk. The effects of eslicarbazepine acetate on breastfed infants or milk production are unknown. Consult your doctor before breastfeeding.