Absorption: Rapidly absorbed after oral administration and rapidly converted to the active 10-hydroxy metabolite (MHD).
Distribution: Enters breast milk in significant amounts.
Metabolism/Excretion: Extensively converted to MHD, which is then primarily excreted by the kidneys.
Half-life: Oxcarbazepine — 2 hr; MHD — 9 hr.
Contraindicated in:
- Hypersensitivity to oxcarbazepine, carbamazepine, or eslicarbazepine.
Use Cautiously in:
- All patients (may ↑ risk of suicidal thoughts/behaviors)
- Renal impairment (dose ↓ recommended if CCr <30 mL/min)
- Severe hepatic impairment
- OB: May be teratogenic (associated with oral clefts and cardiac abnormalities); levels of active metabolites may gradually ↓ during pregnancy which may ↑ seizure risk; use during pregnancy only if maternal benefit outweighs potential risk to fetus
- Lactation: Use while breast feeding only if maternal benefit outweighs potential risk to infant
- Rep: Women of reproductive potential
- Pedi: Children <2 yr (immediate-release) and <6 yr (extended-release) (safety not established).
Exercise Extreme Caution in:
- Patients positive for HLA-B*1502 alleles (unless benefits clearly outweigh the risks) (↑ risk of serious skin reactions).
Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, acne, rash, urticaria.
EENT: abnormal vision, diplopia, nystagmus.
Endo: hypothyroidism.
F and E: hyponatremia.
GI: abdominal pain, dyspepsia, nausea, vomiting, thirst.
Neuro: ataxia, gait disturbances, tremor , SEIZURES, SUICIDAL THOUGHTS, dizziness/vertigo, drowsiness/fatigue, headache, cognitive symptoms.
Misc: hypersensitivity reactions, lymphadenopathy.
(Immediate-release tablets and oral suspension can be interchanged at equal doses.)
- PO (Adults): Adjunctive therapy (immediate–release) — 300 mg twice daily, may ↑ by up to 600 mg/day at weekly intervals up to 1200 mg/day (up to 2400 mg/day may be needed); Conversion to monotherapy (immediate–release) — 300 mg twice daily; may ↑ by 600 mg/day at weekly intervals, while other antiepileptic drugs are tapered over 3–6 wk; dose of oxcarbazepine should be ↑ up to 2400 mg/day over a period of 2–4 wk; Initiation of monotherapy (immediate–release) — 300 mg twice daily, ↑ by 300 mg/day every 3rd day, up to 1200 mg/day. Maximum maintenance dose should be achieved over 2–4 wk; Adjunctive therapy or monotherapy (extended–release) — 600 mg once daily for 1 wk; may ↑ by 600 mg/day at weekly intervals up to 1200–2400 mg once daily; Concurrent use of strong CYP3A4 inducer (carbamazepine, phenobarbital, phenytoin, rifampin) (extended–release) — consider initiating therapy with 900 mg once daily.
- PO (Children 2–16 yr): Adjunctive therapy (immediate release) — 4–5 mg/kg twice daily (up to 600 mg/day), ↑ over 2 wk to achieve 900 mg/day in patients 20–29 kg, 1200 mg/day in patients 29.1–39 kg and 1800 mg/day in patients >39 kg (range 6–51 mg/kg/day). In patients <20 kg, initial dose of 16–20 mg/kg/day may be used not to exceed 60 mg/kg/day. Conversion to monotherapy (immediate release) — 8–10 mg/kg/day given twice daily; may ↑ by 10 mg/kg/day at weekly intervals, whereas other antiepileptic drugs are tapered over 3–6 wk; dose of oxcarbazepine should be ↑ up to 600–900 mg/day in patients
20 kg, 900–1200 mg/day in patients 25–30 kg, 900–1500 mg/day in patients 35–40 kg. 1200–1500 mg/day in patients 45 kg, 1200–1800 mg/day in patients 50–55 kg, 1200–2100 mg/day in patients 60–65 kg, and 1500–2100 mg/day in patients 70 kg. Maximum maintenance dose should be achieved over 2–4 wk. - PO (Children 6–17 yr): Adjunctive therapy or monotherapy (extended-release) — 8–10 mg/kg once daily (up to 600 mg/day) for 1 wk; may ↑ by 8–10 mg/kg/day at weekly intervals over 2–3 wk to achieve 900 mg/day in patients 20–29 kg, 1200 mg/day in patients 29.1–39 kg and 1800 mg/day in patients >39 kg; Concurrent use of strong CYP3A4 inducer (carbamazepine, phenobarbital, phenytoin, rifampin) (extended–release) — consider initiating therapy with 12–15 mg/kg (max dose = 900 mg) once daily.
Renal Impairment
- PO (Adults): CCr<30 mL/min (immediate and extended–release). Initiate therapy at 300 mg/day and ↑ slowly to achieve desired response.
Therapeutic Classification: anticonvulsants
Pharmacologic Classification: carbamazepine analogues
(blood levels)
†Steady-state levels of MHD are reached after 2–3 days during twice-daily dosing.
