Patyar Sazal, Medhi Bikash
Department of Pharmacology, Postgraduate Institute of Medical Education & Research, Chandigarh, India.
Neurosciences (Riyadh). 2010 Jan;15(1):3-6.
Lacosamide (LCM) is a newer antiepileptic drug with a dual mode of action. It selectively enhances slow inactivation of voltage-gated sodium channels without affecting fast inactivation, and modulates collapsing response mediator protein 2 (CRMP-2). It has a high oral bioavailability of approximately 100%. It has shown potent and broad neuroprotective effects in vitro and in vivo animal models making it a potential candidate for long term treatment of epilepsy. In addition to this, it has demonstrated analgesic activity in various animal models. Apart from this, LCM has demonstrated potent effects in animal models for a variety of CNS disorders like schizophrenia and stress induced anxiety. Various safety pharmacology and toxicology studies have shown that LCM is well tolerated. Clinical trials have also suggested that LCM is a safe, effective, and well tolerated adjunctive treatment for reduction of seizure frequency in patients with highly refractory, partial seizures. Other potential indications of LCM are being investigated.
拉科酰胺（LCM）是一种新型抗癫痫药物，具有双重作用模式。它选择性增强电压门控钠通道的缓慢失活而不影响快速失活，并调节塌陷反应调节蛋白2（CRMP - 2）。它具有约100%的高口服生物利用度。在体外和体内动物模型中它已显示出强大而广泛的神经保护作用，使其成为癫痫长期治疗的潜在候选药物。除此之外，它在各种动物模型中已表现出镇痛活性。此外，LCM在动物模型中对多种中枢神经系统疾病如精神分裂症和应激诱导的焦虑症已显示出显著效果。各种安全药理学和毒理学研究表明LCM耐受性良好。临床试验也表明，LCM是一种安全、有效且耐受性良好的辅助治疗药物，可降低高度难治性部分性癫痫患者的癫痫发作频率。LCM的其他潜在适应症正在研究中。
