Effect of renal impairment on the pharmacokinetics of eslicarbazepine acetate

Maia, Joana; Almeida, Luís; Falcão, Amílcar; Soares, Eva; Mota, Fernando; Potgieter, M. A.; Potgieter, Johané; Soares‐da‐Silva, Patrício

doi:10.5414/cpp46119

Cited by 80 publications

(68 citation statements)

References 6 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…In the same way, the ratio of conversion to R-licarbazepine, as well as to OXC, is also notably low when comparing ESL with OXC (Hainzl et al, 2001). The pharmacodynamic and pharmacokinetic profiles of ESL differ significantly from those of CBZ and OXC Almeida and Soares-da-Silva, 2004;Bialer and Soares-da-Silva, 2012;Doeser et al, 2014;Elger et al, 2013;Falcão et al, 2007Falcão et al, , 2012FontesRibeiro et al, 2008;Maia et al, 2008;Perucca et al, 2011), with lower affinity for the voltage-gated sodium channel resulting in higher selectivity for rapid firing epileptic neurons. The most frequent adverse events related to ESL are usually dose-dependent (Zaccara et al, 2013), and no clinically relevant effects on cognitive http://dx.doi.org/10.1016/j.eplepsyres.2015.06.013 0920-1211/© 2015 Elsevier B.V. All rights reserved.…”

Section: Introductionmentioning

confidence: 87%

Assessing long-term effects of eslicarbazepine acetate on lipid metabolism profile, sodium values and liver function tests

et al. 2015

View full text Add to dashboard Cite

Section: Introductionmentioning

confidence: 87%

Assessing long-term effects of eslicarbazepine acetate on lipid metabolism profile, sodium values and liver function tests

et al. 2015

View full text Add to dashboard Cite

“…Approximately two-thirds of urinary eslicarbazepine is in unconjugated form (free form) and a third is conjugated with glucuronic acid (glucuronyl conjugate) [13,34]. Renal impairment decreases the clearance of eslicarbazepine and its metabolites, whereas mild-to-moderate liver dysfunction seems to not affect glucuronidation and formation of metabolites in vivo [13,14,34,37].…”

Section: Phase II Studiesmentioning

confidence: 97%

Eslicarbazepine acetate for partial-onset seizures

Rauchenzauner

Luef

2011

Expert Review of Neurotherapeutics

View full text Add to dashboard Cite

Eslicarbazepine acetate (ESL), a new voltage-gated sodium channel blocker that is chemically related to carbamazepine and partially metabolized to oxcarbazepine, has attracted attention as results of previous Phase II and III studies demonstrated and confirmed efficacy and tolerability of ESL 800 and 1200 mg once daily as add-on therapy for adult patients with drug-resistant partial-onset seizures. In children, efficacy data point towards a dose-dependent decrease in seizure frequency and tolerability analyses showed a low incidence of mild drug-related adverse effects at 5 and 15 mg/kg/day. The most frequently reported adverse effects were dizziness, somnolence, headache, diplopia, nausea and vomiting. The convenience of once-daily dosing and a short/simple titration regimen in combination with a comparative efficacy and tolerability profile might promote ESL as a valid alternative to the current adjunctive antiepileptic drug therapy armamentarium for drug-resistant partial seizures in adults. Since clinical trials in children and adolescents on ESL efficacy and safety are ongoing and data already published are far from conclusive, the therapeutic value of ESL in this special population has to be established in the near future.

show abstract

“…24 Subjects with mild renal impairment (n = 8) eliminate eslicarbazepine more slowly than healthy controls (10.2 mL/min vs 17.3 mL/min in controls), but this not clinically significant. 26 However, subjects with moderate (n = 8) or severe renal impairment (n = 8) clear eslicarbazepine much more slowly (3.7 mL/min and 1.5 mL/min, respectively). 26 Eslicarbazepine is cleared with dialysis in subjects with end-stage kidney disease requiring dialysis.…”

mentioning

confidence: 99%

“…26 However, subjects with moderate (n = 8) or severe renal impairment (n = 8) clear eslicarbazepine much more slowly (3.7 mL/min and 1.5 mL/min, respectively). 26 Eslicarbazepine is cleared with dialysis in subjects with end-stage kidney disease requiring dialysis. 26 Enantiomer-specific levels can be measured with high performance liquid chromatography separation and ultraviolet light detection method.…”

mentioning

confidence: 99%

See 1 more Smart Citation

Role of eslicarbazepine in the treatment of epilepsy in adult patients with partial-onset seizures

Brown¹,

El‐Mallakh

2010

TCRM

View full text Add to dashboard Cite

Eslicarbazepine is a new dibenzazepine antiepileptic agent. It is a high affinity antagonist of the voltage-gated sodium channel. It is closely related to both carbamazepine and oxcarbazepine. Eslicarbazepine has similar affinity to inactivated sodium channels (channels in just activated neurons) as carbamazepine, and greater efficacy in animal models of seizure than oxcarbazepine. In human placebo-controlled trials of a single daily dose of eslicarbazepine added to other anti-epileptic agents, significant seizure reductions occurred with 800 and 1200 mg daily, with nearly half of the patients experiencing a greater than 50% reduction in seizure frequency. Adverse events (AEs) occurred in over 50% of patients receiving therapeutic doses of eslicarbazepine (compared to 31.4%-44.7% of placebo-treated subjects), but were generally mild or moderate. Eight to 19.6% of eslicarbazepine treated patients discontinued due to AEs (compared to 3.9%-8.5% of placebo-treated subjects). In these patients receiving combination anticonvulsant therapy, the most common AEs were dizziness, nausea and vomiting, somnolence, and diplopia. Eslicarbazepine is an effective and reasonably well-tolerated adjunct in patients with suboptimal control of their partial seizures.

show abstract

Effect of renal impairment on the pharmacokinetics of eslicarbazepine acetate

Cited by 80 publications

References 6 publications

Assessing long-term effects of eslicarbazepine acetate on lipid metabolism profile, sodium values and liver function tests

Assessing long-term effects of eslicarbazepine acetate on lipid metabolism profile, sodium values and liver function tests

Eslicarbazepine acetate for partial-onset seizures

Role of eslicarbazepine in the treatment of epilepsy in adult patients with partial-onset seizures

Contact Info

Product

Resources

About