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Catechol-O-methyltransferase and its inhibitors in Parkinson's disease.
The current knowledge on the enzyme catechol-O-methyltransferase (COMT) and the role of COMT inhibitors in PD are reviewed and conversion of levodopa to dopamine at the target region in the brain and facilitation of the continuous action of this amine at the receptor sites are reviewed. Expand
Pharmacokinetic and safety profile of trans-resveratrol in a rising multiple-dose study in healthy volunteers.
In conclusion, repeated administration was well-tolerated but produced relatively low plasma concentrations of trans-resveratrol, despite the high doses and short dosing interval used. Expand
Eslicarbazepine acetate (BIA 2-093)
Eslicarbazepine acetate (ESL) is a novel central nervous system (CNS)-active compound with anticonvulsant activity that behaves as a voltage-gated sodium channel (VGSC) blocker and is currently under clinical development for the treatment of epilepsy and bipolar disorder. Expand
Pharmacokinetics and drug interactions of eslicarbazepine acetate
Eslicarbazepine acetate (ESL) is a novel once‐daily antiepileptic drug (AED) approved in Europe since 2009 that was found to be efficacious and well tolerated in a phase III clinical program in adultExpand
Eslicarbazepine acetate as adjunctive therapy in adult patients with partial epilepsy
Treatment with once-daily eslicarbazepine acetate 800 mg and 1200 mg was more effective than placebo and generally well tolerated in patients with partial-onset seizures refractory to treatment with 1 to 3 concomitant AEDs. Expand
Metabolism of two new antiepileptic drugs and their principal metabolites S(+)- and R(−)-10,11-dihydro-10-hydroxy carbamazepine
It was found that both drugs were almost instantly hydrolysed to the corresponding 10-hydroxy compounds in mice, rats and rabbits and BIA 2-059 seem to be preferable drugs over OXC since they most likely exhibit a 'cleaner' metabolism. Expand
Mechanisms of Action of Carbamazepine and Its Derivatives, Oxcarbazepine, BIA 2-093, and BIA 2-024
The available data indicate that the anticonvulsant efficacy of these AEDs is mainly due to the inhibition of sodium channel activity, which is in line with previous reports on these drugs. Expand
Single‐Dose and Steady‐State Pharmacokinetics of Eslicarbazepine Acetate (BIA 2–093) in Healthy Elderly and Young Subjects
This drug is chemically related to carbamazepine andoxcarbazepine but has been specifically designed to avoid the production of toxic metabolites and to overcome enantiomeric impurity and the unnecessary production of enantiomers ordiastereoisomers of metabolites and conjugates. Expand
Opicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjects.
Despite its short elimination half-life, opicapone markedly and sustainably inhibited erythrocyte S-COMT activity making it suitable for a once daily regimen. Expand
Efficacy and safety of eslicarbazepine acetate as adjunctive treatment in adults with refractory partial‐onset seizures: A randomized, double‐blind, placebo‐controlled, parallel‐group phase III study
To study the efficacy and safety of eslicarbazepine acetate as adjunctive therapy for refractory partial seizures in adults with ≥4 partial‐onset seizures despite treatment with 1–2 antiepileptic drugs (AEDs). Expand