Oxcarbazepine
- Atc Codes:N03AF02
- CAS Codes:28721-07-5
- PHARMGKB ID:28721-07-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Oxcarbazepin, Trileptal; Belgium: Oxcarbazepine, Trileptal; Bulgaria: Trileptal; Cyprus: Trileptal; Czech Republic: Oxkarbazepin, Trileptal; Denmark: Apydan, Oxcarbazepin, Trileptal; Estonia: Apydan, Oxcarbazepine, Trileptal; Finland: Apydan, Oxcarbazepine, Trileptal; France: Oxcarbazepine, Trileptal; Germany: Apydan, Desidox, Oxcarb, Oxcarbazepin, Oxlep, Oxleptal, Timox, Trileptal; Greece: Oxcarbazepine, Trileptal; Hungary: Apydan, Trileptal; Ireland: Oxcarbazepine, Trileptal; Italy: Tolep; Lithuania: Oxcarbazepine; Luxembourg: Trileptal; Netherlands: Oxcarbazepine, Trileptal; Poland: Apydan, Karbagen, Trileptal; Portugal: Epilfarmo, Proaxen, Trileptal, Zigabal; Romania: Trileptal; Slovakia: Trileptal; Slovenia: Karbox; Spain: Epilexter, Oxcarbazepina, Trileptal; Sweden: Oxcarbazepin, Trileptal; UK: Trileptal.
North America
Canada: Oxcarbazepine, Trileptal; USA: Oxcarbazepine, Trileptal.
Latin America
Argentina: Aurene, Oxcarbazepina, Rupox, Trileptal; Brazil: Auram, Oxcarb, Oxcarbazepina, Trileptal; Mexico: Actinium, Deprectal, Oxetol, Trileptal.
Drug combinations
Chemistry
Oxcarbazepine: C~15~H~12~N~2~O~2~. Mw: 252.27. (1) 5H-Dibenz[b,f]azepine-5-carboxamide, 10,11-dihydro-10-oxo-; (2) 10,11-Dihydro-10-oxo-5H-dibenz[b,f]azepine-5-carboxamide. CAS-28721-07-5 (2002).
Pharmacologic Category
Anticonvulsants, Miscellaneous. (ATC-Code: N03AF02).
Mechanism of action
Pharmacological activity results from both oxcarbazepine and its monohydroxy metabolite (MHD). Oxcarbazepine and MHD block voltage-sensitive sodium channels, stabilizing hyperexcited neuronal membranes, inhibiting repetitive firing, and decreasing propagation of synaptic impulses. These actions are believed to prevent spread of seizures. Oxcarbazepine and MHD also increase potassium conductance and modulate activity of high-voltage activated calcium channels. Protects against electrically induced tonic extension seizures and, to a lesser degree, chemically-induced clonic seizures. May abolish or reduce frequency of chronically recurring focal seizures.
Therapeutic use
Partial seizures in adults and children ≥4 years of age. Adjunctive therapy in treatment of partial seizures in children ≥2 years of age with epilepsy.
Pregnancy and lactiation implications
Oxcarbazepine crosses human placenta. Teratogenic effects observed in animals. There are no adequate studies in pregnant women. Use during pregnancy only if benefit to mother outweighs potential risk to fetus. Enters breast milk (not recommended in nursing women).
Unlabeled use
Bipolar disorder. Neuropathic pain.
Contraindications
Hypersensitivity to oxcarbazepine or any component of the formulation.
Warnings and precautions
Use associated with CNS-related adverse events (psychomotor slowing, difficulty with concentration, and speech or language problems, somnolence or fatigue, and coordination abnormalities). May produce potentially serious, sometimes fatal, dermatologic reactions (Stevens-Johnson, toxic epidermal necrolysis). Rare cases of anaphylaxis and angioedema reported (caution in previous hypersensitivity to carbamazepine; fatal multiorgan hypersensitivity reactions also reported). Clinically-significant hyponatremia (sodium <125 mmol/L) can develop during use. Half-life of primary active metabolite prolonged 3-4 fold and AUC doubled in CrCl <30 mL/minute. May reduce efficacy of oral contraceptives. Effects with other sedative drugs or ethanol may be potentiated. Anticonvulsants should not be discontinued abruptly (risk of increasing seizure frequency). May depress serum T~4~ without affecting T~3~ levels or TSH.