Oxcarbazepine
Oxcarbazepine
Trileptal (IR), Oxtellar XR
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Summary
Common uses
Partial-onset seizures (FDA, adult monotherapy and adjunct, pediatric ≥2)0, Trigeminal neuralgia (off-label, often preferred over carbamazepine for better tolerability)0, Bipolar I disorder (off-label, similar utility to carbamazepine)0
Pharmacy
Starting dose
Adult monotherapy: 300 mg PO BID, titrate by 300 mg every 3 days. Pediatric: weight-based titration starting 8-10 mg/kg/day divided BID
Preparations
IR tablets 150, 300, 600 mg; oral suspension 60 mg/mL; XR tablets 150, 300, 600 mg (Oxtellar)
US FDA Max
2400 mg/day (adult)
Pharmacology
Routes
Oral
Onset
Anticonvulsant effect within days at therapeutic plasma level
Duration
BID dosing (IR); once-daily (XR)
Half-life
Oxcarbazepine 2 hours; 10-monohydroxy active metabolite (MHD) ~9 hours (the agent that produces essentially all of the clinical effect)[2]
Bioavailability
~100% (oral)[2]
Pregnancy
Teratogenic signal less than carbamazepine but present; folate supplementation and effective contraception are appropriate in reproductive-age patients[2]
Legal status
Rx-only in US
Purported mechanism
The 10-monohydroxy active metabolite (MHD) is the clinically active species, a voltage-gated sodium channel blocker in the inactivated state. Compared to its parent compound carbamazepine, oxcarbazepine has substantially less CYP3A4 autoinduction, fewer cytochrome-mediated interactions, no clinically significant aplastic anemia or agranulocytosis signal, and a cleaner overall tolerability profile.0 Retains the HLA-B*15:02 cross-sensitivity of carbamazepine for Stevens-Johnson syndrome and toxic epidermal necrolysis risk in Asian populations; CPIC and FDA recommend pre-treatment HLA-B*15:02 testing. Hyponatremia is more common than with carbamazepine, particularly in elderly patients; sodium monitoring during titration is standard[1].
References
- ↑ CPIC Guideline for HLA Genotype and Use of Carbamazepine and Oxcarbazepine, 2017. https://cpicpgx.org/guidelines/guideline-for-carbamazepine-and-hla-b/
- ↑ 2.0 2.1 2.2 FDA Prescribing Information, Trileptal (oxcarbazepine), Novartis, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021014s036lbl.pdf