Abstract
Eslicarbazepine acetate is a promising antiepileptic drug structurally related to carbamazepine and oxcarbazepine, which is in the final phase of clinical development. The metabolism of eslicarbazepine acetate is clearly species dependent and, in this case, among small laboratory animals, the mouse seems to be the most relevant species to humans. Hence, the aim of this study was to investigate the plasma, brain and liver disposition of eslicarbazepine acetate in mice to better understand its disposition in humans. Adult male CD-1 mice were treated orally with a single dose of eslicarbazepine acetate 350 mg/kg. Blood samples, brain and liver tissues were taken at 0.25, 0.5, 0.75, 1, 2, 4, 6, 10, 16 and 24 h post-dose. Plasma and tissue levels of eslicarbazepine acetate and its metabolites (S-licarbazepine, R-licarbazepine and oxcarbazepine) were assessed by using high-performance liquid chromatography-ultraviolet detection. Both eslicarbazepine acetate and R-licarbazepine concentrations were below the limit of quantification of the assay in all matrices. Eslicarbazepine acetate was rapidly and extensively metabolized to S-licarbazepine (major metabolite), which was oxidized to oxcarbazepine to a small extent. The brain/plasma ra...Continue Reading
References
Oct 2, 1992·Journal of Chromatography·G FleschP H Degen
Jan 1, 1994·Epilepsia·M SchmutzH R Olpe
Jan 1, 1994·Epilepsia·M J McLeanK F Feldmann
Jul 20, 1999·Journal of Medicinal Chemistry·J BenesP Soares-da-Silva
Jul 6, 2000·Archives of Medical Research·D F González-EsquivelH Jung-Cook
Apr 28, 2001·Epilepsy Research·D HainzlP Soares-da-Silva
Jul 17, 2001·British Journal of Pharmacology·X Tong, P N Patsalos
Apr 12, 2002·Seizure : the Journal of the British Epilepsy Association·Patrick Kwan, Martin J Brodie
Sep 4, 2003·Drugs in R&D·Luis Almeida, Patrício Soares-da-Silva
Sep 10, 2003·Clinical Pharmacokinetics·Theodor W MayBernhard Rambeck
Nov 25, 2003·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Csilla Misl'anová, Milan Hutta
Jan 27, 2004·Seizure : the Journal of the British Epilepsy Association·M J McEwanJulie Metcalfe
Aug 3, 2004·Journal of Clinical Pharmacology·Luis Almeida, Patrício Soares-da-Silva
Dec 2, 2004·Epilepsy Research·Meir BialerTorbjörn Tomson
Mar 31, 2005·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·C ArellanoG Houin
Apr 30, 2005·The Journal of Pharmacology and Experimental Therapeutics·Ralph ClinckersYvette Michotte
Jul 5, 2005·Drugs in R&D·Joana MaiaPatricio Soares-da-Silva
Jul 5, 2005·Expert Opinion on Investigational Drugs·S C Schachter
Aug 16, 2005·Journal of Clinical Pharmacology·Luis AlmeidaPatrício Soares-da-Silva
Sep 30, 2005·Epilepsia·Nicola MarchiAnnamaria Vezzani
Oct 26, 2005·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·C ArellanoG Houin
Dec 3, 2005·BMJ : British Medical Journal·Martin J Brodie, Patrick Kwan
May 31, 2006·Expert Opinion on Investigational Drugs·Meir Bialer
Dec 13, 2006·Seizure : the Journal of the British Epilepsy Association·Alla B GuekhtEugeny I Gusev
Dec 13, 2006·Epilepsy Research·Meir BialerTorbjörn Tomson
Jan 3, 2007·Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics·Luis Almeida, Patrício Soares-da-Silva
Feb 27, 2007·Epilepsia·Christian ElgerPatrício Soares-da-Silva
May 19, 2007·Lancet Neurology·Tu Luong MacChong Tin Tan
May 23, 2007·Clinical Drug Investigation·Gérard Flesch
Jul 10, 2007·Analytica Chimica Acta·Gilberto AlvesMargarida Caramona
Feb 2, 2008·Journal of Pharmaceutical Sciences·Jun ShenClinton F Stewart
Citations
Feb 3, 2016·International Journal of Pharmaceutics·Joana BickerAmílcar Falcão
Dec 21, 2014·BMC Neuroscience·Germán Sierra-ParedesPatrício Soares-da-Silva
Mar 22, 2012·Medicinal Research Reviews·Patrick Vlieghe, Michel Khrestchatisky
Sep 21, 2013·Epilepsy Research·Ana FortunaAmílcar Falcão
Dec 19, 2013·Epilepsy Research·Heidrun PotschkaPatrício Soares-da-Silva
May 11, 2011·Journal of Separation Science·Ana FortunaPatrício Soares-da-Silva
Nov 1, 2011·Drugs·Cinzia Fattore, Emilio Perucca
Oct 16, 2015·Anesthesia and Analgesia·Maja A TomicRadica M Stepanovic-Petrovic
Mar 1, 2012·Epilepsia·Ana FortunaPatrício Soares-da-Silva
Feb 7, 2020·Psychopharmacology·Uroš PecikozaRadica Stepanović-Petrović
Oct 5, 2021·British Journal of Pharmacology·Laura MonniPawel Fidzinski