Agomelatine is a novel melatonergic antidepressant, with a non-monoaminergic mechanism of action. The aim of this study was to evaluate its plasma concentrations after a single oral dose of 300 mg/dog in fasted and fed status. The research was carried out in 6 adult healthy Labrador dogs according to a randomized open, single-dose, two-treatment, two-phase, paired 2 × 2 cross-over study. At the end of the study all the animals had received the drug in fasted and fed conditions. The drug concentrations were detected in plasma by a validated LC-MS/MS analytical method. The plasma concentrations of agomelatine were found to be extremely variable in both groups as well as the pharmacokinetic profiles. Due to these variable findings the only reliable pharmacokinetic parameters were assessed as C_max (31.8 vs 15.7 ng/mL), T_max (0.75 vs 4 h) and AUC (155 vs 52 ng h/mL) in fasted and fed status, respectively. Unfortunately, as a pioneer study, the small animal sample size used along with the unanticipated variability did not allow to neither statistically estimate if food can affect the pharmacokinetics of agomelatine nor recommend agomelatine for off-label therapies in canine species. Further studies are warranted to clarify this issue.

阿戈美拉汀是一种新型褪黑激素抗抑郁药，具有非单胺能作用机制。本研究的目的是评估其在禁食和进食状态下单次口服剂量 300 mg/狗后的血浆浓度。根据一项随机开放、单剂量、两次治疗、两阶段、配对 2 × 2 交叉研究，该研究在 6 只成年健康拉布拉多犬中进行。在研究结束时，所有动物都在禁食和进食条件下接受了药物。通过验证的 LC-MS/MS 分析方法检测血浆中的药物浓度。发现阿戈美拉汀的血浆浓度在两组以及药代动力学曲线上都存在极大差异。由于这些可变的发现，唯一可靠的药代动力学参数被评估为 C _max (31.8空腹和进食状态下分别为15.7 ng/mL)、T _max (0.75 vs 4 h) 和 AUC (155 vs 52 ng h/mL)。不幸的是，作为一项开创性研究，使用的小动物样本量以及未预料到的变异性既不能从统计学上估计食物是否会影响阿戈美拉汀的药代动力学，也不能推荐阿戈美拉汀用于犬科动物的标签外治疗。需要进一步的研究来澄清这个问题。