In this study we evaluated the neurotoxicity of eslicarbazepine acetate (ESL), and of its in vivo metabolites eslicarbazepine (S-Lic) and R-licarbazepine (R-Lic), as compared to the structurally-related compounds carbamazepine (CBZ) and oxcarbazepine (OXC), in an in vitro model of cultured rat hippocampal neurons. The non-related antiepileptic drugs (AEDs) lamotrigine (LTG) and sodium valproate (VPA) were also ...
Background Etamicastat is a novel, potent, and reversible peripheral dopamine-β-hydroxylase inhibitor that has been administered orally at doses up to 600 mg once daily for 10 days to male healthy volunteers and appears to be well tolerated. Objective The aim of this study was to investigate the effect of food on the pharmacokinetics of etamicastat. Material and Methods A single-center, open-label, randomized...
Background: Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor. Coadministration of a COMT inhibitor with levodopa and a dopa-decarboxylase inhibitor (carbidopa or benserazide) increases levodopa exposure and its therapeutic effect. Objectives: The primary objective of this study was to investigate the effect of nebicapone (50, 100, and 200 mg), compared with placebo, on levodopa pharmacok...
The stereoselective disposition of S-licarbazepine (S-Lic) and R-licarbazepine (R-Lic) was investigated in plasma, brain, liver, and kidney tissues after their individual administration (350 mg/kg) to mice by oral gavage. Plasma, brain, liver, and kidney concentrations of licarbazepine enantiomers and their metabolites were determined over the time by a validated chiral HPLC-UV method. The mean concentration da...
The stereoselective disposition of S-licarbazepine (S-Lic) and R-licarbazepine (R-Lic) was investigated in plasma, brain, liver, and kidney tissues after their individual administration (350 mg/kg) to mice by oral gavage. Plasma, brain, liver, and kidney concentrations of licarbazepine enantiomers and their metabolites were determined over the time by a validated chiral HPLC-UV method. The mean concentration da...
Purpose. To determine the effect of gender on the pharmacokinetics of eslicarbazepine acetate, a novel voltage-gated sodium channel blocker in the development for the treatment of epilepsy and bipolar disorder. Methods. Single-centre, open-label, parallel-group study in 12 female and 12 male healthy subjects. The study consisted of a single-dose (600 mg) period and a multiple-dose (600 mg, oncedaily, for 8 days...
To investigate the effect of eslicarbazepine acetate, a new voltage-gated sodium channel blocker, on the steady-state pharmacokinetics of digoxin ; AES Proceedings Annual Meeting of the American Epilepsy Society
The objective was to determine the pharmacokinetics of eslicarbazepine acetate following single and repeated doses. ; AES Proceedings Annual Meeting of the American Epilepsy Society
To investigate the bioavailability and bioequivalence of three formulations of eslicarbazepine acetate: 50 mg/mL oral suspension (Test 1), 200 mg tablets (Test 2) and 800 mg tablets (Reference) ; AES Proceedings of the Annual Meeting of the American Epilepsy Society
Eslicarbazepine acetate is a novel voltage-gated sodium channel blocker in development for the treatment of epilepsy, bipolar disorder and neuropathic pain. The objective of this study was to determine the effect of age and gender on the pharmacokinetics of eslicarbazepine acetate. ; AES Proceedings of the Annual Meeting of the American Epilepsy Society
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