Dosing & Uses
Dosage Forms & Strengths
tablet, film-coated (Trileptal, generic)
- 150mg
- 300mg
- 600mg
tablet, extended-release (Oxtellar XR)
- 150mg
- 300mg
- 600mg
oral suspension (Trileptal, generic)
- 300mg/5mL
Partial Seizures
Adjunctive treatment
- Trileptal: 300 mg PO q12hr initially; may increase at weekly intervals by 600 mg/day up to 1200 mg/day
- Oxtellar XR: 600 mg PO qDay initially; may increase at weekly intervals by 600 mg/day increments to target dosage range of 1200-2400 mg qDay
Monotherapy (if converting from other AED)
- Initial: 300 mg PO q12hr; increase by 600 mg/day qWeek up to 2400 mg/day
- Reduce and withdraw concomitant antiepileptic drugs (AEDs) over 3-6 weeks while reaching maximum oxcarbazepine dose in 2-4 weeks
Monotherapy (if AED naive)
- Initial: 300 mg PO q12hr; increase by 300 mg/day q3Day to 1200 mg/day divided q12hr
Bipolar Disorder (Off-label)
300 mg/day PO initially; may titrate to 1800-2400 mg/day maximum
Diabetic Neuropathy (Off-label)
150-300 mg/day PO initially; may increase to 900-1200 mg/day (general recommendation)
Doses up to 1800 mg/day studied, with positive results
Neuralgia/Neuropathy (Off-label)
300 mg PO q8-12hr initially; may adjust dose to 400-2000 mg divided q8-12hr (maximum tolerated or effective dose)
Dosage Modifications
Strong CYP3A4 inducers or UGT inducers
- Strong CYP3A4 inducers and/or UGT inducers decrease systemic exposure to 10-monohydroxy derivative (MHD), the active metabolite
- Dosage adjustment of oxcarbazepine may be required after initiation, dosage modification, or discontinuation of such induce
- Oxtellar XR: Initiate at 900 mg qDay
Renal impairment
- There is a linear correlation between creatinine clearance (CrCl) and the renal clearance of MHD
- Severe (CrCl <30 mL/min)
- Oxtellar XR: Administer lower starting dosage and increase, if necessary, at a slower than usual rate until the desired clinical response is achieved
- Trileptal: Decrease usual starting dose by 50% and increase slowly to achieve desired clinical response
- ESRD: Use immediate-release oxcarbazepine instead of long-acting
Hepatic impairment
- Mild-to-moderate: No dose adjustment required
- Severe: Not evaluated, and therefore is not recommended
Dosing Considerations
Conversion from immediate release to Oxtellar XR: Higher doses of Oxtellar XR may be required
Dosage Forms & Strengths
tablet, film-coated (Trileptal, generic)
- 150mg
- 300mg
- 600mg
tablet, extended-release (Oxtellar XR)
- 150mg
- 300mg
- 600mg
oral suspension (Trileptal, generic)
- 300mg/5mL
Partial Seizures (Adjunctive Treatment)
Trileptal (age 2-4 years)
Trileptal (age 4-16 years)
Oxtellar XR (age 6-17 years)
- Initial: 8-10 mg/kg PO qDay; not to exceed 600 mg/day in the first week
- Target maintenance dose
- May titrate to higher dose at weekly intervals in 8-10 mg/kg/day increments (not to exceed 600 mg) to reach the following target maintenance dosage ranges over 2-3 weeks
- 20-29 kg: 900 mg PO qDay
- >29-39 kg: 1200 mg PO qDay
- >39 kg: 1800 mg PO qDay
Partial Seizures (Monotherapy)
Trileptal (age 4-16 years)
- Conversion to monotherapy in patients receiving concomitant AEDs: 8-10 mg/kg/day PO divided q12hr intially, while simultaneously reducing concomitant AEDs dose(s) over 3-6 weeks; may increase Triletpa dose qWeek by maximum increment of 10 mg/kg/day
- AED-naive: Initial 8-10 mg/kg/day PO divided q12hr; may increase q3Days by 5 mg/kg/day
- Target maintenance dose
- 20-24.99 kg: 600-900 mg/day
- 25-34.99 kg: 900-1200 mg/day
- 35-44.99 kg: 900-1500 mg/day
- 45-49.99 kg: 1200-1500 mg/day
- 50-59.99 kg: 1200-1800 mg/day
- 60-69.99 kg: 1200-2100 mg/day
- 70 kg: 1500-2100 mg/day
Oxtellar XR (age 6-17 years)
- Initial: 8-10 mg/kg PO qDay; not to exceed 600 mg/day in the first week
- Target maintenance dose
- May titrate to higher dose at weekly intervals in 8-10 mg/kg/day increments (not to exceed 600 mg) to reach the following target maintenance dosage ranges over 2-3 weeks
- 20-29 kg: 900 mg PO qDay
- >29-39 kg: 1200 mg PO qDay
- >39 kg: 1800 mg PO qDay
Dosage Modifications
Strong CYP3A4 inducers or UGT inducers
- Strong CYP3A4 inducers and/or UGT inducers decrease systemic exposure to 10-monohydroxy derivative (MHD), the active metabolite
- Dosage adjustment of oxcarbazepine may be required after initiation, dosage modification, or discontinuation of such induce
- Oxtellar XR: Initiate at 12-15 mg/kg qDay (not to exceed 900 mg/day in first week)
Renal impairment
- There is a linear correlation between creatinine clearance and the renal clearance of MHD (active metabolite)
- Recommendations for children with renal impairment are not available
Hepatic impairment
- Mild to moderate: No dose adjustment required
- Severe: Unknown if dosage adjustment necessary for immediate release dosage form; extended release, not recommended
Dosing Considerations
Conversion from immediate-release to Oxtellar XR: Higher doses of Oxtellar XR may be required
For extended-release dosage administration consider initial dose of 300-450 mg/day
May increase at weekly intervals to desired effect; not to exceed 2400 mg/day
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Dizziness (30-50%)
Diplopia (30-50%)
Headache (26-30%)
Nausea/vomiting (26-30%)
Nystagmus (26-30%)
Somnolence (26-30%)
Ataxia (10-30%)
Abnormal gait (16-20%)
Tremor (16-20%)
Abdominal pain (11-15%)
Fatigue (11-15%)
Vertigo (11-15%)
Vision abnormalities (11-15%)
1-10%
Dyspepsia (5-6%)
Rash (4%)
Insomnia (2-4%)
Abnormal thinking (<4%)
Hyponatremia (1-3%)
Muscle weakness (1-2%)
Hypotension (<2%)
Speech disorder (1%)
Asthenia
Postmarketing Reports
Angioedema
Anaphylaxis
Multiorgan immune hypersensitivity reaction
Hematic and lymphatic systems: Bone marrow depression, agranulocytosis, aplastic anemia, pancytopenia, neutropenia
Digestive system: Pancreatitis and/or lipase and/or amylase increased
Metabolism and nutrition disorders: Folic acid deficiency, hypothyroidism
Skin and appendages: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis
Skeletal: Fractures, decreased bone mineral, osteoporosis
Body as a whole: Multiorgan hypersensitivity disorders characterized by features such as rash, fever, lymphadenopathy, abnormal liver function tests, eosinophilia, and arthralgia
Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)/Multi-Organ Hypersensitivity
Warnings
Contraindications
Known hypersensitivity to oxcarbazepine or any of its components, or to eslicarbazepine acetate
Cautions
Hypersensitivity reactions may occur; if signs or symptoms of hypersensitivity develop, discontinue treatment immediately
Antiepileptic drugs (AEDs) increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication; monitor for the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior
Caution performing tasks that require mental alertness
Potentially fatal skin reactions may occur (eg, Stevens-Johnson syndrome)
Discontinue if dermatological reactions occur
Significant hyponatremia and syndrome of inappropriate antidiuretic hormone secretion (SIADH) may develop (monitor especially in patients at risk of hyponatremia)
Pancytopenia, agranulocytosis, and leukopenia reported rarely
Long term use has been associated with decreased mineral density, osteopenia, osteoporosis, and fractures, CNS-related adverse effects including difficulty with concentration, psychomotor slowing, speech or language problems, somonolence or fatigue, coordination of abnormalities, including ataxia and gait disturbances
Hypothyroidism reported; monitor thyroid function, especially in children; discontinuation of therapy associated with return of normal thyroxine levels
Patients carrying the HLA-B*1502 allele may be at increased risk for Stevens-Johnson syndrome and epidermal necrolysis
Half-life of primary active metabolite is prolonged 3- to 4-fold and AUC is doubled in patients with CrCl <30 mL/min; adjust dose in these patients
Exacerbation of or new onset of primary generalized seizures reported; risk of aggravation of primary generalized seizures is seen especially in children but may also occur in adults; discontinue therapy if it occurs
Do not discontinue anticonvulsants abruptly; withdraw gradually because of risk of increased seizure frequency and status epilepticus; if withdrawal is needed because of serious adverse event, rapid discontinuation can be considered
Plasma levels of the active metabolite of oxcarbazepine, the 10¬ monohydroxy derivative (MHD), may gradually decrease throughout pregnancy; recommend patients be monitored carefully during pregnancy; close monitoring should continue through the postpartum period because MHD levels may return after delivery (see Pregnancy)
DRESS
- Drug reaction with eosinophilia and systemic symptoms (DRESS), also known as multi-organ hypersensitivity, reported
- Some of these events have been fatal or life-threatening
- DRESS typically, although not exclusively, presents with fever, rash, and/or lymphadenopathy, in association with other organ system involvement (eg, hepatitis, nephritis, hematologic abnormalities, myocarditis, or myositis), sometimes resembling an acute viral infection
Drug interactions overview
- Phenytoin levels have been shown to increase with concomitant use of oxcarbazepine at doses >1200 mg/day; therefore, it is recommended that the plasma levels of phenytoin be monitored during oxcarbazepine titration and dosage modification; a dose reduction of phenytoin may be required
- Strong CYP450 enzymes and/or UGT inducers (eg, rifampin, carbamazepine, phenytoin and phenobarbital) have been shown to decrease the plasma/serum levels of MHD, the active metabolite of oxcarbazepine (25% to 49%) (see Dosage Considerations)
- Concurrent use of oxcarbazepine with hormonal contraceptives may render these contraceptives less effective
Pregnancy & Lactation
Pregnancy
There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to AEDs, such as TRILEPTAL, during pregnancy. Encourage women who are taking TRILEPTAL during pregnancy to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling 1-888-233-2334 or visiting http://www.aedpregnancyregistry.org/
No adequate and well-controlled clinical studies of oxcarbazepine in pregnant women; however, oxcarbazepine is closely related structurally to carbamazepine, which is considered to be teratogenic in humans
Data on a limited number of pregnancies from pregnancy registries suggest congenital malformations associated with oxcarbazepine monotherapy use (eg, craniofacial defects such as oral clefts and cardiac malformations such as ventricular septal defects)
Use of drug with hormonal contraceptives containing ethinylestradiol or levonorgestrel associated with decreased plasma concentrations of these hormones and may result in a failure of therapeutic effect of oral contraceptive drug; advise women of reproductive potential taking drug who are using a contraceptive containing ethinylestradiol or levonorgestrel to use additional or alternative non-hormonal birth control
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus
Oxcarbazepine levels may decrease during pregnancy
Lactation
Oxcarbazepine and its active metabolite (MHD) are excreted in human milk
A milk-to-plasma concentration ratio of 0.5 was found for oxcarbazepine and MHD
Owing to potential serious adverse reactions to oxcarbazepine in nursing infants, developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed infant from drug or from underlying maternal
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
MHD stabilizes neuronal membranes by blocking Na+ channels; this may inhibit repetitive firing and may decrease the propagation of synaptic impulses; may also increase potassium conductance and modulate the activity of high-voltage activated calcium channels
Absorption
Bioavailability: Complete
Peak serum time: 4-6 hr
Distribution
Protein bound: 40% (MHD); primarily bound to albumin
Vd: 49 L
Metabolism
Rapidly reduces by cytosolic enzymes in the liver to active metabolite
Metabolites (active): MHD
Enzymes induced: CYP3A4
Enzymes inhibited: CYP2C19
Elimination
Half-life: 2 hr (immediate-release parent drug); 9 hr (immediate-release derivative MHD); 7-11 hr (extended-release parent drug); 9-11 hr (extended-release derivative MHD)
Excretion: Urine (>95%)
Administration
Oral Suspension Preparation
Shake bottle well and prepare dose immediately afterwards
Withdraw prescribed dose from bottle using oral syringes provided
Mix in a small glass of water just prior to administration or, alternatively, may be swallowed directly from the syringe
After each use, close the bottle and rinse the syringe with warm water and allow it to dry thoroughly
Oral Administration
Take with or without food
Oral suspension and film-coated tablets may be interchanged at equal doses
Storage
Oral suspension
- Store at room temperature, 25°C (77°F); excursions permitted to 15-30°C (59-86°F)
- Use within 7 weeks of first opening bottle
Tablets
- Store at room temperature, 25°C (77°F); excursions permitted to 15-30°C (59-86°F)
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Patient Handout
Formulary
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