Eslicarbazepine
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Handling and access
NIOSH hazardous drug
Table 2NIOSH lists eslicarbazepine as a hazardous drug. AHFS class: 28:12.92 anticonvulsants, miscellaneous.
- Meets the NIOSH definition of a hazardous drug (carcinogenicity, developmental or reproductive toxicity, organ toxicity at low doses, or genotoxicity) without MSHI or a Group 1 or 2A carcinogen classification.
- Only a developmental and/or reproductive hazard: precautions matter most for workers who are pregnant, breastfeeding, or trying to conceive.
Handle with the precautions your facility uses for hazardous drugs (USP <800>). NIOSH's Managing Hazardous Drug Exposures lists controls by drug form and activity.
Dosing in kidney impairment
Dosage Modifications in Patients with Renal Impairment In patients with moderate and severe renal impairment (i.e., creatinine clearance < 50 mL/min), the initial, titration, and maintenance dosages should generally be reduced by 50%. Titration and maintenance dosages may be adjusted according to clinical response [see Use in Specific Populations and Clinical Pharmacology].
Dosing in liver impairment
Patients with Hepatic Impairment Dose adjustments are not required in patients with mild to moderate hepatic impairment. Use of APTIOM in patients with severe hepatic impairment has not been studied, and use in these patients is not recommended [see Use in Specific Populations and Clinical Pharmacology].
Preparation and administration
Important Administration Instructions Instruct patients to administer APTIOM either as whole or as crushed tablets. Instruct patients to take APTIOM either with or without food. The APTIOM dosing regimen depends on age, weight, and renal function.
Drug interactions
Check eslicarbazepine against a medication listLabel text (5 paragraphs)
Carbamazepine: May need dose adjustment for APTIOM or carbamazepine. ( 2.3 , 5.6 , 7.1 ) Phenytoin: Higher dosage of APTIOM may be necessary and dose adjustment may be needed for phenytoin. ( 2.3 , 7.1 , 7.2 ) Phenobarbital or Primidone: Higher dosage of APTIOM may be necessary. ( 2.3 , 7.1 ) Hormonal Contraceptives: APTIOM may decrease the effectiveness of hormonal contraceptives. ( 7.4 , 8.3 )
7.1 Other Antiepileptic Drugs Several AEDs (e.g., carbamazepine, phenobarbital, phenytoin, and primidone) can induce enzymes that metabolize APTIOM and can cause decreased plasma concentrations of eslicarbazepine [see Clinical Pharmacology ( 12.3 )]. Higher doses of Aptiom may be needed [see Dosage and Administration ( 2.4 )].
7.2 CYP2C19 Substrates APTIOM can inhibit CYP2C19, which can cause increased plasma concentrations of drugs that are metabolized by this isoenzyme (e.g., phenytoin, clobazam, and omeprazole) [see Clinical Pharmacology ( 12.3 )]. Dose adjustment may be needed.
7.3 CYP3A4 Substrates In vivo studies suggest that APTIOM can induce CYP3A4, decreasing plasma concentrations of drugs that are metabolized by this isoenzyme (e.g., simvastatin, lovastatin) [see Clinical Pharmacology ( 12.3 )]. Dose adjustment of simvastatin and lovastatin may be needed if a clinically significant change in lipids is noted.
7.4 Oral Contraceptives Because concomitant use of APTIOM and ethinylestradiol and levonorgestrel is associated with lower plasma levels of these hormones, females of reproductive potential should use additional or alternative non-hormonal birth control.
Contraindications
4 CONTRAINDICATIONS APTIOM is contraindicated in patients with a hypersensitivity to eslicarbazepine acetate or oxcarbazepine [see Warnings and Precautions ( 5.2 , 5.3 , and 5.4 )]. Hypersensitivity to eslicarbazepine acetate or oxcarbazepine. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
DLikelihood score D: Possible rare cause of clinically apparent liver injury.
Eslicarbazepine is an aromatic anticonvulsant similar to oxcarbazepine that is used in combination with other antiepileptic agents as therapy of partial onset seizures. Eslicarbazepine is associated with a low rate of transient serum enzyme elevations during therapy and has been implicated in rare instances of clinically apparent liver injury.
ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to AEDs, such as APTIOM, during pregnancy. Encourage women who are taking APTIOM during pregnancy to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling 1-888-233-2334 or visiting http://www.aedpregnancyregistry.org. Risk Summary Limited available data with APTIOM use in pregnant women are insufficient to inform a drug-associated risk of adverse developmental outcomes.
In oral studies conducted in pregnant mice, rats, and rabbits, eslicarbazepine acetate demonstrated developmental toxicity, including increased incidence of malformations (mice), embryolethality (rats), and fetal growth retardation (all species), at clinically relevant doses (see Data). Advise a pregnant woman of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. The background risk of major birth defects and miscarriage for the indicated population is unknown.
Data Animal Data When eslicarbazepine acetate was orally administered (150, 350, 650 mg/kg/day) to pregnant mice throughout organogenesis, increased incidences of fetal malformations was observed at all doses and fetal growth retardation was observed at the mid and high doses. A no-effect dose for adverse developmental effects was not identified. At the lowest dose tested, plasma eslicarbazepine exposure (C max , AUC) is less than that in humans at the maximum recommended human dose (MRHD, 1600 mg/day).
Oral administration of eslicarbazepine acetate (40, 160, 320 mg/kg/day) to pregnant rabbits throughout organogenesis resulted in fetal growth retardation and increased incidences of skeletal variations at the mid and high doses. The no-effect dose (40 mg/kg/day) is less than the MRHD on a mg/m 2 basis. Oral administration to pregnant rats (65, 125, 250 mg/kg/day) throughout organogenesis resulted in embryolethality at all doses, increased incidences of skeletal variations at the mid and high doses, and fetal growth retardation at the high dose. The lowest dose tested (65 mg/kg/day) is less than the MRHD on a mg/m 2 basis.
When eslicarbazepine acetate was orally administered to female mice during pregnancy and lactation (150, 350, 650 mg/kg/day), the gestation period was prolonged at the highest dose tested. In offspring, a persistent reduction in offspring body weight and delayed physical development and sexual maturation…
Breastfeeding (LactMed)
One mother breastfed two infants while taking eslicarbazepine with no adverse effects. Additionally, eslicarbazepine is the active metabolite of oxcarbazepine. Limited information indicates that oxcarbazepine or eslicarbazepine would not be expected to cause any adverse effects in breastfed infants, especially if the infant is older than 2 months. Monitor the infant for drowsiness, adequate weight gain, and developmental milestones, especially in younger, exclusively breastfed infants and when using combinations of anticonvulsants.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
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