Pharm

Eslicarbazepine

search

Eslicarbazepine, Aptiom

  • Indications
  1. Adjunctive agent in Refractory Partial-Onset Seizures
  2. Bipolar Disorder
  3. Trigeminal Neuralgia
  • Contraindications
  1. MAO Inhibitor use within last 14 days
  2. Bone Marrow suppression
  3. Pregnancy
  4. Tricyclic compound sensitivity
  • Mechanism
  1. Dibenzazepine Anticonvulsant with chemical structure similar to Tricyclic Antidepressants
  2. Primary anticonvulsant effects
    1. Inhibits Neuron depolarization and Glutamate release
    2. Sodium Channel Blocker (similar to Carbamazepine and Oxcarbazepine)
      1. Binds Sodium channels that are in an inactive state
      2. Decreases Sodium, Calcium and Potassium currents across Neuronal membranes
  3. Other effects
    1. Diuretic
  • Dosing
  • Adults
  1. Normal Renal Function
    1. Initial: 400 mg orally once daily for 1 week
    2. Increase dose by 400 mg to 600 mg per week as needed
    3. Maintenance: 800 mg orally once daily
    4. Maximum dose: 1200 mg/day (doses up to 1600 mg may be used if 1200 mg is not sufficient)
  2. Decreased Renal Function (Creatinine Clearance <50 ml/min)
    1. Initial: 200 mg orally once daily for 2 weeks
    2. Maintenance: 400 mg orally once daily (50% of standard dose)
    3. Maximum dose: 600 mg/day
  • Dosing
  • Children (ages 4 to 17 years old)
  1. Weight 11 to 21 kg
    1. Start 200 mg orally daily
    2. Increase dose by 200 mg/day per week as needed
    3. Maintenance: 400-600 mg orally once daily
  2. Weight 22 to 31 kg
    1. Start 300 mg orally daily
    2. Increase dose by 300 mg/day per week as needed
    3. Maintenance: 500-800 mg orally once daily
  3. Weight 32 to 38 kg
    1. Start 300 mg orally daily
    2. Increase dose by 300 mg/day per week as needed
    3. Maintenance: 600-900 mg orally once daily
  4. Weight >38 kg
    1. See Adult Dosing
  5. Decreased Renal Function (Creatinine Clearance <50 ml/min)
    1. Decrease dose by 50%
  • Safety
  1. Avoid in Pregnancy
    1. Risk of Spina bifida, Developmental Delay
  2. Unknown Safety in Lactation
    1. Enters Breast Milk
  • Adverse Effects
  1. Common
    1. Dizziness
    2. Somnolence
    3. Headache
    4. Nausea
    5. Double Vision
  2. Serious
    1. Hyponatremia
    2. Cardiac conduction abnormality (increases A-V delay)
    3. Hyponatremia (SIADH)
      1. Occurs in up to 40% of patients
      2. Risk factors include older age, Diuretic use and concurrent Selective Serotonin Reuptake Inhibitor (SSRI) use
    4. Hepatotoxicity or Liver failure (very rare)
    5. Life-Threatening Drug-Induced Rashes
      1. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS Syndrome)
      2. Stevens-Johnson Syndrome or Toxic Epidermal Necrolysis (TEN)
        1. Most common with asian descent and HLA-B 1502 Mutation (and possibly HLA-B3101)
  • Drug Interactions
  1. Do not use with other similar Sodium Channel Blocker agents such as Carbamazepine and Oxcarbazepine
  2. Fewer Drug Interactions than with Carbamazepine
  3. MAO Inhibitors (potentially lethal Drug Interactions)
  4. Hormonal contraceptives
    1. Eslicarbazepine decreases the contraceptive efficacy
    2. Use alternative, non-hormonal agents or backup Contraception
  • Resources
  1. Eslicarbazepine (Medscape)
    1. http://reference.medscape.com/drug/aptiom-eslicarbazepine-acetate-999902
  2. Eslicarbazepine Tablet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3d0c9554-eaeb-4694-8089-00133fcadce3
  • References
  1. (2014) Presc Lett 21(11): 65
  2. Ben-Menachem (2010) Epilepsy Curr 10(1): 7–8 [PubMed]
  3. (2022) Presc Lett, Resource #361206, Antiseizure Medications
  4. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 56-7
  5. Hamilton (2020) Tarascon Pocket Pharmacopoeia