地高辛在亚心脏强直剂量下调节丙戊酸、左乙拉西坦和托吡酯在实验性原发性全身性癫痫发作中的抗惊厥电位。

Q3 Pharmacology, Toxicology and Pharmaceutics
Ceska a Slovenska Farmacie Pub Date : 2022-01-01
Vadim Tsyvunin, Sergiy Shtrygol, Mariia Mishchenko, Diana Shtrygol
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引用次数: 0

摘要

癫痫在世界人口中的流行,以及对现有抗癫痫药物(aed)有很高耐药性的患者比例,促使人们不断寻找治疗该病的新方法。先前,在戊四唑和最大电击诱发癫痫发作的筛选模型中,通过增强低剂量aed的弱活性,证实了心糖苷地高辛具有显著的抗惊厥潜力。本研究旨在探讨地高辛在不同神经化学机制的原发性全身性癫痫模型中对丙戊酸、左乙拉西坦和托吡酯抗惊厥活性的影响。总共使用了264只随机繁殖的雄性白化小鼠。在癫痫诱导前30分钟,以条件有效(ED50)和亚有效(½ED50)剂量给药一次aed:丙戊酸钠和托吡酯,剂量分别为300和150 mg/kg;左乙拉西坦-剂量为100和50毫克/公斤。地高辛在诱发癫痫发作前10-15分钟皮下给药一次,剂量为0.8 mg/kg体重(1/10 LD50)。Picrotoxin(水溶液2.5 mg/kg,皮下注射)、thiosemicarbazide(水溶液25 mg/kg,腹腔注射)、士的宁(水溶液1.2 mg/kg,皮下注射)、樟脑(油溶液1000 mg/kg,腹腔注射)作为惊厥剂用于诱导癫痫发作。发现地高辛在微毒素、硫代氨基卡酰胺、士的宁、樟脑致原发性全身性癫痫发作的情况下,不仅表现出自身较强的抗惊厥活性,而且显著增强了经典AEDs丙戊酸钠、左乙曲西坦、托吡酯的抗惊厥电位。所得结果证实了地高辛作为抗惊厥药物的进一步深入研究,特别是对其作用的神经化学机制的深入研究的方便性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Digoxin at sub-cardiotonic dose modulates the anticonvulsive potential of valproate, levetiracetam and topiramate in experimental primary generalized seizures.

The prevalence of epilepsy in the world population together with a high percentage of patients resistant to existing antiepileptic drugs (AEDs) stimulates the constant search for new approaches to the treatment of the disease. Previously a significant anticonvulsant potential of cardiac glycoside digoxin has been verified by enhancing a weak activity of AEDs in low doses under screening models of seizures induced by pentylenetetrazole and maximal electroshock. The aim of the present study is to investigate the influence of digoxin at a sub-cardiotonic dose on the anticonvulsant activity of valproate, levetiracetam, and topiramate in models of primary generalized seizures with different neurochemical mechanisms. A total of 264 random-bred male albino mice have been used. AEDs were administered 30 min before seizure induction once intragastrically at conditionally effective (ED50) and sub-effective (½ ED50) doses: sodium valproate and topiramate - at doses of 300 and 150 mg/kg; levetiracetam - at doses of 100 and 50 mg/kg. Digoxin was administered once subcutaneously at a dose of 0.8 mg/kg body weight (1/10 LD50) 10-15 min before seizure induction. Picrotoxin (aqueous solution 2.5 mg/kg, subcutaneously), thiosemicarbazide (aqueous solution 25 mg/kg, intraperitoneally), strychnine (aqueous solution 1.2 mg/kg, subcutaneously), camphor (oil solution 1000 mg/kg, intraperitoneally) have been used as convulsive agents for seizure induction. It was found that under the conditions of primary generalized seizures induced by picrotoxin, thiosemicarbazide, strychnine, and camphor, digoxin not only shows its own strong anticonvulsant activity but also significantly enhances the anticonvulsant potential of classical AEDs sodium valproate, levetiracetam, and topiramate. The obtained results substantiate the expediency of further in-depth study of digoxin as an anticonvulsant drug, in particular, the in-depth study of neurochemical mechanisms of its action.

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来源期刊
Ceska a Slovenska Farmacie
Ceska a Slovenska Farmacie Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
0.90
自引率
0.00%
发文量
22
期刊介绍: Přehledový článek je zaměřen zejména na metody přípravy, charakterizaci mikročástic a dále na charakteristiku a příklady jejich možného využití ve farmakoterapii. Mikročástice jako...
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