CNS Drugs

, Volume 18, Issue 1, pp 57–61 | Cite as

Spotlight on Oxcarbazepine in Epilepsy

  • Lynne M. BangEmail author
  • Karen L. Goa
Adis Spotlight


Oxcarbazepine (Trileptal®, Timox®) is structurally related to carbamazepine and has anticonvulsant activity. Studies suggest that the anticonvulsant activity of oxcarbazepine is mediated via the blocking of neuronal ion channels.

In patients aged <18 years, the efficacy of oxcarbazepine monotherapy was similar to that of phenytoin in children with partial onset or generalised tonic-clonic seizures in a 48-week trial. Additional supporting findings demonstrated that 43–71% of patients with partial onset, generalised or undetermined epilepsy were seizure free after oxcarbazepine monotherapy (mean dosage 27.7–50 mg/kg/ day; duration 1–5 years). In contrast, one small nonblind trial showed more patients treated with oxcarbazepine monotherapy than with carbamazepine monotherapy had recurrent seizures during 16 months of therapy (although the conclusions that can be drawn from this trial are limited).

As adjunctive therapy, oxcarbazepine was significantly better than placebo at reducing seizure frequency in children and adolescents with refractory partial onset seizures with or without secondary generalisation: the median percentage change in partial onset seizure frequency was 35% versus 9%, respectively, during 16 weeks of therapy. In noncomparative trials of adjunctive oxcarbazepine (mean dosage of 34.5–56.7 mg/kg/day), 7–11% of patients with partial onset or generalised seizures were seizure free during treatment, and 20–54% had seizure reductions of ≥50%.

Oxcarbazepine was generally well tolerated during monotherapy and adjunctive therapy; 2.5% and 10% of patients withdrew from well controlled trials of oxcarbazepine monotherapy and adjunctive therapy. Oxcarbazepine monotherapy was better tolerated than phenytoin and events observed in oxcarbazepine-treated patients were transient.

Oxcarbazepine metabolism is largely unaffected by induction of the cytochrome (CYP) P450 system. However, oxcarbazepine can inhibit CYP2C19 and induce CYP3A4 and CYP3A5, thereby interfering with the metabolism of other drugs (e.g. phenytoin). In addition, oxcarbazepine decreases plasma levels of oral contraceptives and alternative contraceptive methods should be used.

In conclusion, oxcarbazepine (as both monotherapy and adjunctive therapy) has shown efficacy in the treatment of partial onset seizures in children with epilepsy. Nevertheless, the generally favorable tolerability profile and relatively low potential for drug interactions of oxcarbazepine make it a valuable option in the treatment of childhood epilepsy. 1 This Spotlight is derived from abstract and summary text of an Adis Drug Evaluation originally published in full in Pediatric Drugs 2003; 5 (8): 557-573. Reviewers of the original full text article are listed in the Acknowledgements section.


Adjunctive Therapy Oxcarbazepine Anticonvulsant Activity Partial Onset Seizure Major Active Metabolite 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



The full text article in Pediatric Drugs 2003; 5(8): 557-73 was reviewed by: M. Brodie, Epilepsy Unit, Western Infirmary, Glasgow, Scotland; S. Crecco, School of Pharmacy, Massachusetts College of Pharmacy and Health Sciences, Boston, Massachusetts, USA; E. Faught, Department of Neurology, University of Alabama School of Medicine, Birmingham, Alabama, USA; E. Gaily, Hospital for Children and Adolescents, University of Helsinki, Helsinki, Finland; M. Kalis, School of Pharmacy, Massachusetts College of Pharmacy and Health Sciences, Boston, Massachusetts, USA; D. Schmidt, Epilepsy Research Group, Berlin, Germany; P.E. Smith, Epilepsy Unit, University Hospital of Wales, Cardiff, Wales; E. Tecoma, UCSD Epilepsy Center, University of California, San Diego, California, USA.


  1. 1.
    Tecoma ES. Oxcarbazepine. Epilepsia 1999; 40 Suppl. 5: S37–46PubMedCrossRefGoogle Scholar
  2. 2.
    Wamil AW, Schmutz M, Portet C, et al. Effects of oxcarbazepine and 10-hydroxycarbamazepine on action potential firing and generalized seizures. Eur J Pharmacol 1994; 271: 301–8PubMedCrossRefGoogle Scholar
  3. 3.
    Stefani A, Pisani, De Murtas M, et al. Action of GP 47779, the active metabolite of oxcarbazepine, on the corticostriatal system II: modulation of high-voltage-activated calcium currents. Epilepsia 1995; 36(10): 997–1002PubMedCrossRefGoogle Scholar
  4. 4.
    Calabresi P, De Murtas M, Stefani A, et al. Action of GP 47779, the active metabolite of oxcarbazepine, on the corticostriatal system I: modulation of corticostriatal synaptic transmission. Epilepsia 1995; 36(10): 990–6PubMedCrossRefGoogle Scholar
  5. 5.
    Curran HV, Java R. Memory and psychomotor effects of oxcarbazepine in healthy human volunteers. Eur J Clin Pharmacol 1993; 44: 529–33PubMedCrossRefGoogle Scholar
  6. 6.
    Sabers A, Møller A, Dam M, et al. Cognitive function and anticonvulsant therapy: effect of monotherapy in epilepsy. Acta Neuro Scand 1995; 92: 19–27CrossRefGoogle Scholar
  7. 7.
    Rättyä J, Vainionpaa L, Knip M, et al. The effects of valproate, carbamazepine, and oxcarbazepine on growth and sexual maturation in girls with epilepsy. Pediatrics 1999 Mar; 103(3): 588–93PubMedCrossRefGoogle Scholar
  8. 8.
    Dam M, Østergaard LH. Oxcarbazepine. In: Levy RH, Mattson RH, Meldrum BS, editors. Antiepileptic Drugs. 4th ed. New York: Raven Press, 1995: 987–95Google Scholar
  9. 9.
    Pariente-Khayat A, Tran A, Vauzelle-Kervuroedan F, et al. Pharmacokinetics of oxcarbazepine as add-on therapy in epileptic children [abstract]. Epilepsia 1994; 35 Suppl. 8: 119Google Scholar
  10. 10.
    Dulac O, D’Souza J, Motte J, et al. Multicenter study of oxcarbazepine pharmacokinetics and tolerability in children with refractory epilepsy [abstract no. P14]. Ann Neurol 2001 Sep; 50Suppl. 1: S104Google Scholar
  11. 11.
    Novartis Pharmaceuticals Corporation. Trileptal (oxcarbazepine) prescribing information [online]. Available from URL: [Accessed 2003 Mar 20]
  12. 12.
    Grant SM, Faulds D. Oxcarbazepine: a review of its pharmacology and therapeutic potential in epilepsy: trigeminal neuralgia and affective disorders. Drugs 1992; 43: 873–88PubMedCrossRefGoogle Scholar
  13. 13.
    Stroink H, Tang KT, Van Parys JAP, et al. Steady-state pharmacokinetics of oxcarbazepine in children [abstract]. Epilepsia 1998; 39 Suppl. 6: 48Google Scholar
  14. 14.
    Jung H, Noguez A, Mayet L, et al. The distribution of 10-hydroxy carbamazepine in blood compartments. Biopharm Drug Dispos 1997; 18: 17–23PubMedCrossRefGoogle Scholar
  15. 15.
    Van Parys JAP, Meinardi H. Survey of 260 epileptic patients treated with oxcarbazepine (Trileptal) on a named-patient basis. Epilepsy Res 1994; 19(1): 79–85PubMedCrossRefGoogle Scholar
  16. 16.
    Schachter SC. Oxcarbazepine: current status and clinical applications. Expert Opin Invest Drug 1999; 8(7): 1103–12CrossRefGoogle Scholar
  17. 17.
    Dickinson RG, Hooper WD, Dunstan PR, et al. First dose and steady state pharmacokinetics of oxcarbazepine and its 10-hydroxy metabolite. Eur J Clin Pharmacol 1989; 37: 69–74PubMedGoogle Scholar
  18. 18.
    Volosov A, Xiaodong S, Perucca E, et al. Enantioselective pharmacokinetics of 10-hydroxycarbamazepine after oral administration of oxcarbazepine to healthy Chinese subjects. Clin Pharmacol Ther 1999; 66: 547–53PubMedGoogle Scholar
  19. 19.
    Rouan MC, Lecaillon JB, Godbillon J, et al. The effect of renal impairment on the pharmacokinetics of oxcarbazepine and its metabolites. Eur J Clin Pharmacol 1994; 47: 161–7PubMedCrossRefGoogle Scholar
  20. 20.
    Emilien G, Maloteaux JM. Pharmacological management of epilepsy: mechanism of action, pharmacokinetic drug interactions and new drug discovery possibilities. Int J Clin Pharmacol Ther 1998; 36: 181–94PubMedGoogle Scholar
  21. 21.
    Sallas W, Hossain M, D’Souza J. Population pharmacokinetics analysis of oxcarbazepine (Trileptal) in children with epilepsy [abstract]. Epilepsia 1999; 40 Suppl. 7: 102Google Scholar
  22. 22.
    McKee PJW, Blacklaw J, Forrest G, et al. A double-blind, placebo-controlled interaction study between oxcarbazepine and carbamazepine, sodium valproate and phenytoin in epileptic patients. Br J Clin Pharmacol 1994; 37: 27–32PubMedCrossRefGoogle Scholar
  23. 23.
    Hossain M, Sallas W, Gasparini M, et al. Drug-drug interaction profile of oxcarbazepine in children and adults [abstract no. P06-118]. Neurology 1999 Apr 12; 52Suppl. 2: A525Google Scholar
  24. 24.
    Tartara A, Galimberti CA, Manni R, et al. The pharmacokinetics of oxcarbazepine and its active metabolite 10-hydroxy-carbazepine in healthy subjects and in epileptic patients treated with phenobarbitone or valproic acid. Br J Clin Pharmacol 1993; 36(4): 366–8PubMedCrossRefGoogle Scholar
  25. 25.
    Guerreiro MM, Vigonius U, Pohlmann H, et al. A double-blind controlled clinical trial of oxcarbazepine versus phenytoin in children and adolescents with epilepsy. Epilepsy Res 1997 Jun; 27(3): 205–13PubMedCrossRefGoogle Scholar
  26. 26.
    Dizdarer G, Kangin M, Sutcuoglu S, et al. A comparison of carbamazepine and oxcarbazepine in partial epilepsies [abstract]. Epilepsia 2000; 41 Suppl.: 67–8Google Scholar
  27. 27.
    Matheisel A, Mazurkiewicz-Beldzinska M, Mankowska B. Oxcarbazepine monotherapy in childhood epilepsy [abstract]. Epilepsia 2002; 43 Suppl. 8: 184Google Scholar
  28. 28.
    Gaily E, Granstrom M-L, Liukkonen E. Oxcarbazepine in the treatment of early childhood epilepsy. J Child Neurol 1997 Nov; 12(8): 496–8PubMedCrossRefGoogle Scholar
  29. 29.
    Ferraro SM, Daraio C, Solis S, et al. Oxcarbazepine in early childhood [abstract]. Epilepsia 1997; 38 Suppl. 8: 96Google Scholar
  30. 30.
    Glauser TA, Nigro M, Sachdeo R, et al. Adjunctive therapy with oxcarbazepine in children with partial seizures. Oxcarbazepine Pediatric Study Group. Neurology 2000 Jun 27; 54(12): 2237–44PubMedCrossRefGoogle Scholar
  31. 31.
    Mandelbaum DE, Kugler SL, Wenger E, et al. The safety and efficacy of oxcarbezepine as adjunctive therapy in children: an open-label study [abstract]. Ann Neurol 1998 Sep; 44: 580Google Scholar
  32. 32.
    Korn-Merker E, Holtmann M, Krause M, et al. Oxcarbazepine: experiences in 142 children and adolescents with difficult-to-treat epilepsies [abstract]. Epilepsia 2001; 42 Suppl. 7: 181Google Scholar
  33. 33.
    Borusiak P, Korn-Merker E, Holert N, et al. Oxcarbazepine in treatment of childhood epilepsy: a survey of 46 children and adolescents. J Epilepsy 1998; 11: 355–60CrossRefGoogle Scholar
  34. 34.
    Sachdeo R, Glauser T, Wheless J, et al. Oxcarbazepine adjunctive therapy in children is effective whether used with carbamazepine or other antiepileptic drugs [abstract]. Ann Neurol 2002 Sep; 52 Suppl. 1: 119Google Scholar
  35. 35.
    Woster P, Carrazana EJ. Oxcarbazepine and hyponatremia [letter]. Am J Health Syst Pharm 2002 Mar 1; 59(5): 467PubMedGoogle Scholar
  36. 36.
    Antiepileptics. British National Formulary No. 40. London: The Pharmaceutical Press, 2000: 222–39Google Scholar

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© Adis Data Information BV 2004

Authors and Affiliations

  1. 1.Adis International LtdAucklandNew Zealand

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