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Effect of Food on the Pharmacokinetic Profile of Etamicastat (BIA 5-453)

Vaz-da-Silva, Manuel; Nunes, Teresa; Rocha, José F.; Falcão, Amílcar; Almeida, Luis; Soares-da-Silva, Patricio

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...


Pharmacokinetic-pharmacodynamic interaction between Nebicapone and controlled-r...

Nunes, Teresa; Rocha, José F.; Fernendes-Lopes, Carlos; Costa, Raquel; Torrão, Leonel; Loureiro, Ana I.; Falcão, Amílcar; Vaz-da-Silva, Manuel

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...


Intranasal drug delivery: how, why and what for?

Pires, Anaísa; Fortuna, Ana; Alves, Gilberto; Falcão, Amílcar

Over the recent decades the interest in intranasal delivery as a non-invasive route for drugs is increased. Since the nasal mucosa offers numerous benefits as a target tissue for drug delivery, a wide variety of therapeutic compounds may be administered intranasally for topic, systemic and central nervous system action. We have, herein, outlined the relevant aspects of nasal anatomy, physiology and histology, a...


The maximal electroshock seizure (MES) model in the preclinical assessment of p...

Castel-Branco, M. M.; Alves, G. L.; Figueiredo, I. V.; Falcão, Amílcar; Caramona, M. M.

The choice of appropriate animal models for the initial in vivo testing of potential anticonvulsant compounds is one of the most important steps in the successful search for new antiepileptic drugs. The purpose of this paper is to describe the most important aspects to take into account when performing the maximal electroshock seizure (MES) test in the routine laboratory screening of new antiepileptics: the con...


Stereoselective Disposition of S- and R-Licarbazepine in Mice

Alves, Gilberto; Figueiredo, Isabel; Falcão, Amílcar; Castel-Branco, Margarida; Caramona, Margarida; Soares-da-Silva, Patrício

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...


Stereoselective disposition of S and R-licarbazepine in mice

Alves, Gilberto; Figueiredo, Isabel; Falcão, Amílcar; Castel-Branco, Margarida; Caramona, Margarida; Soares-da-Silva, Patrício

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...


Aspirina como antiagregante plaquetar. “Resistência à Aspirina” – diagnóstico e...

Moreira, José Afonso; Figueiredo, Isabel Vitória; Falcão, Amílcar


Aspirina como antiagregante plaquetar: mecanismos de resistência à Aspirina

Moreira, José Afonso; Figueiredo, Isabel Vitória; Falcão, Amílcar


Performance of gentamicin population kinetic parameters in Portuguese neonates

Rocha, Marília J.; Almeida, Anabela M.; Falcão, Amílcar C.; Caramona, Margarida M.

Aim: To evaluate the performance of eight different sets of gentamicin populational pharmacokinetic parameters, regarding potential implementation in clinical pharmacokinetic software as prior information. Methods: The study involved 49 patients of 31.3±4.1 weeks of gestational age (GA), receiving gentamicin, and for whom peak and trough concentrations were obtained. Accuracy and precision were assessed by mean...


Enantioselective HPLC-UV method for determination of eslicarbazepine acetate (B...

Alves, Gilberto; Figueiredo, Isabel; Castel-Branco, Margarida; Loureiro, Ana; Fortuna, Ana; Falcão, Amílcar; Caramona, Margarida

Eslicarbazepine acetate (BIA 2-093) is a novel central nervous system drug undergoing clinical phase III trials for epilepsy and phase II trials for bipolar disorder. A simple and reliable chiral reversed-phase HPLC-UV method was developed and validated for the simultaneous determination of eslicarbazepine acetate, oxcarbazepine, S-licarbazepine and R-licarbazepine in human plasma. The analytes and internal sta...


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Fundação para a Ciência e a Tecnologia Universidade do Minho   Governo Português Ministério da Educação e Ciência Programa Operacional da Sociedade do Conhecimento União Europeia