Dosage Form Proportionality and Food Effect of the Final Tablet Formulation of Eslicarbazepine Acetate

Ribeiro, Carlos; Macedo, T.R.A.; Nunes, Teresa; Neta, Carla; Vasconcelos, Teófilo; Cerdeira, Rui; Lima, Ricardo; Rocha, José‐Francisco; Falcão, Amı́lcar; Almeida, Luís; Soares-da-Silva, Patrı́cio

doi:10.2165/0126839-200809060-00007

Cited by 17 publications

(4 citation statements)

References 10 publications

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“…In contrast, ESL is a prodrug that is converted only to S-MHD, which is also known as S-licarbazepine or ESL. 113 , 114 The pharmacokinetics of ESL are not affected by factors such as food consumption, 115 , 116 age, 117 or gender. 118 Our results showed ESL 1200 mg/d was ranked seventh in terms of seizure response.…”

Section: Discussionmentioning

confidence: 99%

Efficacy, tolerability and safety of add-on third-generation antiseizure medications in treating focal seizures worldwide: a network meta-analysis of randomised, placebo-controlled trials

Chen,

Li,

et al. 2024

eClinicalMedicine

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Section: Discussionmentioning

confidence: 99%

Efficacy, tolerability and safety of add-on third-generation antiseizure medications in treating focal seizures worldwide: a network meta-analysis of randomised, placebo-controlled trials

Chen,

Li,

et al. 2024

eClinicalMedicine

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“…Plasma levels of parent drug (ESL) are usually undetectable. In the present study an achiral method was used, thus not allowing to distinguish between eslicarbazepine and its minor metabolite, ( R )-licarbazepine; in such cases, the mixture is reported as BIA 2-005 [19, 20]. …”

Section: Methodsmentioning

confidence: 99%

“…Prior to shipment to the laboratory for the analytical assays (Swiss Bioanalytics AG, Birsfelden, Switzerland), the resulting plasma was separated into aliquots of 0.75 mL and stored at −20 °C. The lowest level of quantification (LLOQ) was at 10 ng/mL [19, 20]. …”

Section: Methodsmentioning

confidence: 99%

Bioequivalence of Eslicarbazepine Acetate from Two Different Sources of its Active Product Ingredient in Healthy Subjects

et al. 2013

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Purpose To compare the bioavailability (BA) and pharmacokinetic (PK) properties and to demonstrate the bioequivalence (BE) between two active product ingredient (API) sources of eslicarbazepine acetate (ESL) in healthy volunteers. Design, subjects and methods Forty healthy male and female subjects aged 18-40 years were randomized to treatment with 400 or 800 mg ESL marketed (MF) formulation [current active pharmaceutical ingredient (API) source] and 400 or 800 mg ESL to-be-marketed (TBM) formulation (new API source) under a gender-balanced, two-period, two-sequence crossover open-label study design. Subjects were assigned to receive either 400 or 800 mg ESL dose strengths, and each was randomly administered on two occasions-either a single oral tablet of MF or a single oral tablet of TBM-separated by a washout period of at least 7 days. Formulations were to be considered bioequivalent if, for both 400 or 800 mg ESL dosage strengths, the test (TBM)/reference (MF) geometric mean ratios (GMR) and 90 % confidence intervals (90 % CI) of the area under the plasma concentration-time curve (AUC) and peak plasma concentration (C max ) were within the predetermined range of 80-125 %. Results Test/reference GMR (90 % CI) for the C max and AUC was respectively 100 % (94-109 %) and 96 % (94-98 %) following 400 mg ESL and 100 % (95-105 %) and 100 % (97-103 %) following 800 mg ESL. Conclusion Oral tablet formulations of either 400 or 800 mg ESL from the new API source were found to be bioequivalent to the corresponding marketed Zebinix Ò formulation according to the regulatory definition of bioequivalence.

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“…Therefore, the authors concluded that dose adjustments of ESL based on gender will not be required 39. Finally, studies concerning possible influences of warfarin (at a subtherapeutic level)40 or food41 on ESL pharmacokinetics in healthy volunteers revealed no influence of either on ESL pharmacokinetics, but did show a small and statistically significant reduction in systemic exposure to S-warfarin, with no effect on R-warfarin, on the International Normalized Ratio 40,41…”

Section: Drug Interactionsmentioning

confidence: 99%

Update on treatment of partial onset epilepsy: role of eslicarbazepine

Rauchenzauner

Luef²

2010

NDT

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Partial epilepsy comprises simple partial seizures, complex partial seizures, and secondarily generalized seizures, and covers more than 60% of patients with epilepsy. Antiepileptic drugs are generally considered to be the major therapeutic intervention for epilepsy but, despite a broad range of commonly used antiepileptic drugs, approximately 30% of adult patients and approximately 25% of children with epilepsy have inadequate seizure control. Eslicarbazepine acetate (ESL) is a novel voltage-gated sodium channel-blocking agent with presumed good safety and efficacy for adjunctive treatment of patients with drug-resistant partial epilepsy. ESL is a prodrug of eslicarbazepine (the active entity responsible for pharmacologic effects), and is rapidly and extensively hydrolyzed during first pass by liver esterases after oral administration. The half-life of eslicarbazepine at steady-state plasma concentrations is 20–24 hours, compatible with once-daily administration. ESL 800 mg and 1200 mg significantly reduces seizure frequency and shows a favorable safety profile in adult patients with drug-resistant partial-onset seizures, as demonstrated in previous Phase II and III trials. In children, ESL showed a clear dose-dependent decrease in seizure frequency with good tolerability. The most commonly reported adverse events associated with ESL are dizziness, somnolence, nausea, diplopia, headache, vomiting, blurred vision, vertigo, and fatigue. In conclusion, these characteristics suggest that ESL might be a valid and well tolerated treatment option for patients with drug-resistant partial-onset epilepsy. The convenience of once-daily dosing and a short, simple titration regimen would be of special interest for children, although conclusive published data are lacking to date. Hence, there is an urgent need to establish the therapeutic value of ESL in this special population in the near future.

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Dosage Form Proportionality and Food Effect of the Final Tablet Formulation of Eslicarbazepine Acetate

Cited by 17 publications

References 10 publications

Efficacy, tolerability and safety of add-on third-generation antiseizure medications in treating focal seizures worldwide: a network meta-analysis of randomised, placebo-controlled trials

Efficacy, tolerability and safety of add-on third-generation antiseizure medications in treating focal seizures worldwide: a network meta-analysis of randomised, placebo-controlled trials

Bioequivalence of Eslicarbazepine Acetate from Two Different Sources of its Active Product Ingredient in Healthy Subjects

Update on treatment of partial onset epilepsy: role of eslicarbazepine

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