Author(s):
Falcão, Amílcar 
; Maia, Joana ; Almeida, Luís ; Mazur, Dago ; Gellert, Manfred ; Soares-da-Silva, Patrício
Date: 2007
Persistent ID: http://hdl.handle.net/10316/2806
Origin: Estudo Geral - Universidade de Coimbra
Subject(s): eslicarbazepine acetate; gender effects; pharmacokinetics
Description
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) period, separated by 4 days.
Results. Eslicarbazepine acetate was rapidly and extensively metabolized to eslicarbazepine
(S-licarbazepine), the main active metabolite. Following a single-dose, arithmetic mean eslicarbazepine
maximum plasma concentrations (Cmax) and area under the plasma concentration-time
curve over 24 h (AUC0 24) and from 0 to infinity (AUC0 1) were, respectively, 9.3 mg/ml,
128.5 mg h/ml and 171.9 mg h/ml in male subjects and 10.1 mg/ml, 150.1 mg h/ml and 205.0 mg h/ml
in female subjects. At steady-state, Cmax, AUC0 24 and AUC0 1 were 15.5 mg/ml, 207.8 mg h/ml and
295.8 mg h/ml in male subjects, and 16.8 mg/ml, 214.5 mg h/ml and 295.2 mg h/ml in female subjects.
Steady-state plasma concentrations were attained at 4 to 5 days of administration in both groups.
Eslicarbazepine Cmax, AUC0 24 and AUC0 1 female:male geometric mean ratios (90%CI) were,
respectively, 1.09 (0.94; 1.24), 1.16 (1.00; 1.33) and 1.17 (0.99; 1.38) following single-dose, and 1.10
(0.97; 1.25), 1.04 (0.92; 1.17) and 1.01 (0.88; 1.16) at steady-state.
Conclusion. At steady-state, the pharmacokinetic profile of eslicarbazepine acetate was not
affected by gender.
