Eslicarbazepine
- Atc Codes:N03AF04
- CAS Codes:236395-14-5
- PHARMGKB ID:236395-14-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Exalief, Zebinix; Bulgaria: Exalief, Zebinix; Czech Republic: Exalief, Zebinix; Denmark: Zebinix; Estonia: Exalief, Zebinix; Germany: Exalief, Zebinix; Greece: Zebinix; Hungary: Zebinix; Ireland: Exalief, Zebinix; Latvia: Zebinix; Lithuania: Exalief, Zebinix; Malta: Exalief, Zebinix; Netherlands: Exalief, Zebinix; Poland: Exalief, Zebinix; Portugal: Exalief, Zebinix; Romania: Exalief, Zebinix; Slovakia: Exalief, Zebinix; Slovenia: Exalief, Zebinix; Sweden: Exalief, Zebinix; UK: Zebinix.
Drug combinations
Chemistry
Eslicarbazepine Acetate: C~17~H~16~N~2~O~3~. Mw: 296.32. (1) [S-(-)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide]; (2) BIA 2-093. CAS-236395-14-5.
Pharmacologic Category
Anticonvulsants, Miscellaneous. Antiepileptics, Carboxamide Derivatives. (ATC-Code: N03AF04).
Mechanism of action
The precise mechanisms of action of eslicarbazepine acetate are unknown. However, in vitro electrophysiological studies indicate that both eslicarbazepine acetate and its metabolites stabilize the inactivated state of voltage-gated sodium channels, preventing their return to the activated state and thereby sustaining repetitive neuronal firing.
Therapeutic use
Adjunctive therapy in adults with partial-onset seizures with or without secondary generalization.
Pregnancy and lactiation implications
There are no data from the use of eslicarbazepine acetate in pregnant women. Studies in animals have shown reproductive toxicity. Minimum effective doses should be given, and monotherapy whenever possible should be preferred at least during the first three months of pregnancy. Patients should be counseled regarding the possibility of an increased risk of malformations and given the opportunity to antenatal screening. Antiepileptic medicinal products may contribute to folic acid deficiency, a possible contributory cause of fetal abnormality (folic acid supplementation is recommended before and during pregnancy). Bleeding disorders in the newborn caused by antiepileptic medicinal products have been reported (vitamin K~1~ should be administered as a preventive measure in the last few weeks of pregnancy and to the newborn). Eslicarbazepine acetate adversely interacts with oral contraceptives (an alternative, effective and safe method of contraception should be used during treatment and up to the end of the current menstrual cycle after treatment has been stopped). Breast-feeding should be discontinued during treatment with eslicarbazepine acetate.
Unlabeled use
Contraindications
Hypersensitivity to the active substance, to other carboxamide derivatives (e.g. carbamazepine, oxcarbazepine) or to any of the excipients. Known second- or third-degree atrioventricular (AV) block.
Warnings and precautions
Has been associated with some central nervous system adverse reactions, such as dizziness and somnolence, which could increase the occurrence of accidental injury. May decrease the effectiveness of hormonal contraceptives. If eslicarbazepine is to be discontinued it is recommended to withdraw it gradually to minimize the potential of increased seizure frequency. Rash has developed as an adverse reaction (if signs or symptoms of hypersensitivity develop, therapy must be discontinued). Presence of HLA-B*1502 allele in individuals of Han Chinese and Thai origin has been shown to be strongly associated with the risk of developing Stevens-Johnson syndrome when treated with carbamazepine. Hyponatremia has been reported (in patients with pre-existing renal disease leading to hyponatremia, or in patients concomitantly treated with medicinal products which may themselves lead to hyponatremia (e.g. diuretics, desmopressin). Serum sodium levels should be examined before and during treatment; if clinically relevant hyponatremia develops, therapy should be discontinued. Use not recommended in patients with primary generalized seizures. Prolongations in PR interval have been observed in clinical studies with eslicarbazepine acetate. Suicidal ideation and behavior have been reported in patients treated with anti-epileptic active substances in several indications (patients should be monitored for signs of suicidal ideation and behaviors and appropriate treatment should be considered).