Oxcarbazepine: Difference between revisions
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{{MedTemplate | {{MedTemplate | ||
| generic | | generic = Oxcarbazepine | ||
| brand | | brand = Trileptal (IR), Oxtellar XR | ||
| structure | | structure = | ||
| classes | | classes = [[:Category:Anticonvulsants|Anticonvulsant]], [[:Category:Mood stabilizers|Mood stabilizer (off-label)]], [[:Category:Sodium channel blockers|Sodium channel blocker]] | ||
| | | uses = <vote slug="partial-seizures-monotherapy-use">Partial-onset seizures (FDA, adult monotherapy and adjunct, pediatric ≥2)</vote>, <vote slug="trigeminal-neuralgia-use">Trigeminal neuralgia (off-label, often preferred over carbamazepine for better tolerability)</vote>, <vote slug="bipolar-disorder-oxcarbazepine-use">Bipolar I disorder (off-label, similar utility to carbamazepine)</vote> | ||
| uses | | 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 | ||
| starting_dose | | preparations = IR tablets 150, 300, 600 mg; oral suspension 60 mg/mL; XR tablets 150, 300, 600 mg (Oxtellar) | ||
| preparations | | fda_max = 2400 mg/day (adult) | ||
| fda_max = | | pill_id = | ||
| routes | | routes = Oral | ||
| onset | | onset = Anticonvulsant effect within days at therapeutic plasma level | ||
| duration | | duration = BID dosing (IR); once-daily (XR) | ||
| halflife | | halflife = Oxcarbazepine 2 hours; '''10-monohydroxy active metabolite (MHD) ~9 hours''' (the agent that produces essentially all of the clinical effect)<ref name="trileptal-label">FDA Prescribing Information, Trileptal (oxcarbazepine), Novartis, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021014s036lbl.pdf</ref> | ||
| bioavailability | | bioavailability = ~100% (oral)<ref name="trileptal-label" /> | ||
| pregnancy | | pregnancy = Teratogenic signal less than carbamazepine but present; folate supplementation and effective contraception are appropriate in reproductive-age patients<ref name="trileptal-label" /> | ||
| legal | | legal = [[USLegal:Prescription only|Rx-only]] in US | ||
| | | mechanism = <vote slug="oxcarbazepine-mech-claim">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.</vote> '''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<ref name="cpic-hla">CPIC Guideline for HLA Genotype and Use of Carbamazepine and Oxcarbazepine, 2017. https://cpicpgx.org/guidelines/guideline-for-carbamazepine-and-hla-b/</ref>. | ||
| | |||
}} | }} | ||
[[Category: | == References == | ||
<references /> | |||
[[Category:Anticonvulsants]] | |||
[[Category:Mood stabilizers]] | |||
[[Category:Sodium channel blockers]] | [[Category:Sodium channel blockers]] | ||
Latest revision as of 07:24, 23 May 2026
Oxcarbazepine
Trileptal (IR), Oxtellar XR
Experience
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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