University of Coimbra, Faculty of Pharmacy, Coimbra, Portugal; University of Coimbra, Coimbra Institute for Biomedical Imaging and Translational Research, Coimbra, Portugal.
University of Coimbra, Faculty of Pharmacy, Coimbra, Portugal; University of Coimbra, Coimbra Institute for Biomedical Imaging and Translational Research, Coimbra, Portugal.
Life Sci. 2021 Jun 15;275:119342. doi: 10.1016/j.lfs.2021.119342. Epub 2021 Mar 11.
Epilepsy is one of the most common brain disorders, affecting more than 50 million people worldwide. Although its treatment is currently symptomatic, the last generation of anti-seizure drugs is characterized by better pharmacokinetic profiles, efficacy, tolerability and safety. Lacosamide is a third-generation anti-seizure drug that stands out due to its good efficacy and safety profile. It is used with effectiveness in the treatment of partial-onset seizures with or without secondary generalization, primary generalized tonic-clonic seizures and off-label in status epilepticus. Despite scarcely performed until today, therapeutic drug monitoring of lacosamide is proving to be advantageous by allowing the control of inter and intra-individual variability and promoting a successful personalized therapy, particularly in special populations. Herein, the pharmacology, pharmacokinetics, and clinical data of lacosamide were reviewed, giving special emphasis to the latest molecular investigations underlying its mechanism of action and therapeutic applications in pathologies besides epilepsy. In addition, the pharmacokinetic characteristics of lacosamide were updated, as well as current literature concerning the high pharmacokinetic variability observed in special patient populations and that must be considered during treatment individualization.
癫痫是最常见的脑部疾病之一，影响着全球超过 5000 万人。尽管目前的治疗方法是对症治疗，但上一代抗癫痫药物的特点是更好的药代动力学特性、疗效、耐受性和安全性。拉科酰胺是一种第三代抗癫痫药物，由于其良好的疗效和安全性而脱颖而出。它在治疗部分发作性癫痫，伴有或不伴有继发性全身发作、原发性全面强直阵挛发作以及癫痫持续状态中的应用具有有效性。尽管直到今天才进行了很少的研究，但拉科酰胺的治疗药物监测证明是有利的，因为它可以控制个体内和个体间的变异性，并促进成功的个体化治疗，特别是在特殊人群中。本文综述了拉科酰胺的药理学、药代动力学和临床数据，特别强调了其作用机制和在除癫痫以外的疾病中的治疗应用的最新分子研究。此外，还更新了拉科酰胺的药代动力学特征，以及目前关于特殊患者人群中观察到的高药代动力学变异性的文献，在个体化治疗时必须考虑这些变异性。
