Oxcarbazepine


Concise Prescribing Info
Indications/Uses
Partial seizures.
Dosage/Direction for Use
Adult : PO As monotherapy or adjunctive therapy: Initial: 600 mg/day in 2 divided doses, may increase if necessary in max increments of 600 mg/day at wkly interval. Maintenance: 600-1,200 mg/day or up to 2,400 mg/day in adjunctive therapy or in refractory patients switched from other antiepileptics.
Dosage Details
Oral
Partial seizures
Adult: As monotherapy or adjunctive therapy: Initially, 600 mg daily in 2 divided doses, may increase if necessary in max increments of 600 mg daily at wkly intervals. Maintenance dose: 600-1,200 mg daily or up to 2,400 mg daily in adjunctive therapy or in refractory patients switched from other antiepileptics.
Child: ≥6 yr 8-10 mg/kg daily in 2 divided doses, may increase if necessary in increments of 10 mg/kg daily at wkly intervals. Maintenance dose: 30 mg/kg daily in adjunctive therapy. Max: 46 mg/kg/day.
Special Patient Group
Pharmacogenomics:

Human leukocyte antigen B (HLA-B) variant allele HLA-B*15:02 is associated with the development of serious cutaneous adverse reactions [e.g. Stevens-Johnson syndrome (SJS) or toxic epidermal necrolysis (TEN)] to aromatic anticonvulsants (e.g. carbamazepine, lamotrigine, phenytoin, phenobarbital). The prevalence of this allele has been estimated in 6.9% of East Asians, 5.5% of Oceanians, 4.6% of South/Central Asians, <1% of Japanese, <2.5% of Koreans, rare in Africans, and <1% of African Americans, Middle Easterners, Caucasians, Hispanic/South Americans.

Patients who are positive to HLA-B*15:02 allele may have greater risk of developing SJS/TEN when treated with oxcarbazepine. CPIC strongly recommends avoiding use of oxcarbazepine, and cautiously consider alternative aromatic anticonvulsant therapy in these patients. Consider genetic screening prior to initiation of therapy.

The latency period for SJS/TEN is short with continuous dosing of approx 4-28 days, and ADR usually occur within 3 months of use. Therefore, if patient previously used oxcarbazepine consistently for more than 3 months without incidence of SJS/TEN, cautiously consider use of oxcarbazepine in the future. However, tolerance to oxcarbazepine is not indicative of tolerance to other aromatic anticonvulsants.
Renal Impairment
CrCl (mL/min)
Dosage
<30 Initially, 300 mg daily, increased at wkly intervals or longer.
Administration
May be taken with or without food.
Contraindications
Lactation.
Special Precautions
Patient carrying the HLA-B*1502 allele. Avoid abrupt withdrawal. Severe renal and hepatic impairment. Pregnancy.
Adverse Reactions
Hyponatraemia; suicidal behaviour or ideation; neuropsychiatric effects (e.g. impaired cognitive or psychomotor performance, somnolence or fatigue, incoordination); dizziness, somnolence, diplopia, fatigue, nausea, vomiting, ataxia, abnormal vision, abdominal pain, tremor, dyspepsia, abnormal gait, hypothyroidism. Rarely, pancytopenia, agranulocytosis, leucopenia.
Potentially Fatal: Stevens-Johnson syndrome, toxic epidermal necrolysis; anaphylaxis, angioedema; Drug Reaction w/ Eosinophilia and Systemic Symptoms (DRESS).
Patient Counseling Information
May impair ability to drive or operate machinery.
MonitoringParameters
Monitor seizure frequency, serum Na, symptoms of CNS depression, hypersensitivity reactions, serum levels of concomitant antiepileptic drugs during titration; periodic thyroid function test and CBC.
Overdosage
Symptoms: Somnolence, dizziness, nausea, vomiting, hyperkinesia, hyponatraemia, ataxia and nystagmus. Management: Symptomatic and supportive treatment. Employ gastric lavage and/or administer activated charcoal to facilitate removal of medicinal product.
Drug Interactions
May increase plasma concentrations of other anticonvulsants (e.g. phenobarbital, phenytoin). May decrease plasma concentrations of OC and Ca channel blockers. Decreased plasma concentrations w/ potent inducers of CYP isoenzymes (e.g. carbamazepine, phenytoin, phenobarbital).
Food Interaction
Additive sedative effect w/ alcohol.
Lab Interference
May depress serum T4 w/o affecting T3 or TSH.
Action
Description: Oxcarbazepine and monohydroxy derivative (MHD) block voltage-sensitive Na channels, stabilising hyperexcited neuronal membranes, inhibiting repetitive firing, and decreasing the propagation of synaptic impulses. These actions are believed to prevent the spread of seizures. Oxcarbazepine and MHD also increase K conductance and modulate the activity of high-voltage activated Ca channels.
Pharmacokinetics:
Absorption: Completely absorbed from the GI tract. Time to peak plasma concentration: 4.5 hr (tab); 6 hr (oral susp).
Distribution: Widely distributed throughout the body. Crosses the placenta and enters breast milk. Plasma protein binding: Approx 40%, mainly albumin.
Metabolism: Hepatic; rapidly and extensively metabolised to the principal metabolite, 10, 11-dihydro-10-hydroxy-carbamazepine (MHD).
Excretion: Via urine, mainly as metabolites, and <1% as unchanged drug. Plasma half-life: Approx 2 hr (oxcarbazepine); approx 9 hr (monohydroxy metabolite).
Chemical Structure

Chemical Structure Image
Oxcarbazepine

Source: National Center for Biotechnology Information. PubChem Database. Oxcarbazepine, CID=34312, https://pubchem.ncbi.nlm.nih.gov/compound/Oxcarbazepine (accessed on Jan. 22, 2020)

Storage
Store at 25°C.
MIMS Class
ATC Classification
N03AF02 - oxcarbazepine ; Belongs to the class of carboxamide derivatives antiepileptic.
References
Anon. Oxcarbazepine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 20/09/2018.

Anon. Oxcarbazepine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/09/2018.

Buckingham R (ed). Oxcarbazepine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/09/2018.

Buckingham R (ed). Oxcarbazepine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/01/2015.

Clinical Annotation for HLA-B*15:02:01 related to Oxcarbazepine. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/ . Accessed 20/09/2018.

Joint Formulary Committee. Oxcarbazepine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/09/2018.

McEvoy GK, Snow EK, Miller J et al (eds). Oxcarbazepine . AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 28/01/2015.

Oxcarbazepine Tablet, Film-coated (Jubilant Cadista Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/01/2015.

Trileptal Tablets and Oral Suspension. U.S. FDA. https://www.fda.gov/. Accessed 28/01/2015.

Disclaimer: This information is independently developed by MIMS based on Oxcarbazepine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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