Department of Clinical Pharmacology and Therapeutics, Tokushima University Graduate School of Biomedical Sciences, Japan; Department of Pharmacy, Tokushima University Hospital, Japan.
Department of Drug Information Analysis, College of Pharmaceutical Sciences, Matsuyama University, Japan.
Eur J Pharmacol. 2021 Jul 5;902:174099. doi: 10.1016/j.ejphar.2021.174099. Epub 2021 Apr 25.
Despite the availability of more than 20 clinical antiepileptic drugs, approximately 30% of patients with epilepsy do not respond to antiepileptic drug treatment. Therefore, it is important to develop antiepileptic products that function via novel mechanisms. In the present study, we evaluated data from one of the largest global databases to identify drugs with antiepileptic effects, and subsequently attempted to understand the effect of the combination of antiepileptic drugs and valacyclovir in epileptic seizures using a kindling model. To induce kindling in mice, pentylenetetrazol at a dose of 40 mg/kg was administered once every 48 h. Valacyclovir was orally administered 30 min before antiepileptic drug injection in kindled mice, and behavioral seizures were monitored for 20 min following pentylenetetrazol administration. Additionally, c-Fos expression in the hippocampal dentate gyrus was measured in kindled mice. Valacyclovir showed inhibitory effects on pentylenetetrazol-induced kindled seizures. In addition, simultaneous use of levetiracetam and valacyclovir caused more potent inhibition of seizure activity, and neither valproic acid nor diazepam augmented the anti-seizure effect in kindled mice. Furthermore, kindled mice showed increased c-Fos levels in the dentate gyrus. The increase in c-Fos expression was significantly inhibited by the simultaneous use of levetiracetam and valacyclovir. The findings of the present study indicate that a combination of levetiracetam and valacyclovir had possible anticonvulsive effects on pentylenetetrazol-induced kindled epileptic seizures. These results suggest that valacyclovir may have an antiseizure effect in patients with epilepsy.
尽管有 20 多种临床抗癫痫药物可供使用,但大约 30%的癫痫患者对抗癫痫药物治疗没有反应。因此,开发作用机制新颖的抗癫痫产品非常重要。本研究我们评估了来自全球最大的数据库之一的数据,以确定具有抗癫痫作用的药物,随后尝试使用点燃模型了解抗癫痫药物和伐昔洛韦联合治疗癫痫发作的效果。为了在小鼠中诱导点燃,每 48 小时给予戊四氮 40mg/kg 一次。在点燃小鼠中给予抗癫痫药物前 30 分钟口服伐昔洛韦,并在给予戊四氮后监测 20 分钟的行为性癫痫发作。此外,还测量了点燃小鼠海马齿状回中的 c-Fos 表达。伐昔洛韦对戊四氮诱导的点燃性癫痫发作具有抑制作用。此外,同时使用左乙拉西坦和伐昔洛韦会引起更强的抑制作用,而丙戊酸钠和地西泮均不会增强点燃小鼠的抗癫痫作用。此外,点燃小鼠的齿状回中 c-Fos 水平升高。同时使用左乙拉西坦和伐昔洛韦可显著抑制 c-Fos 表达的增加。本研究的结果表明,左乙拉西坦和伐昔洛韦的联合使用可能对戊四氮诱导的点燃性癫痫发作具有抗惊厥作用。这些结果表明伐昔洛韦可能对癫痫患者具有抗癫痫作用。