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verapamil

心血管

关键词心血管 药物 钙离子通道阻滞剂

词汇介绍

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解析

Verapamil [və'ræpə,mɪl] 

释义   n. 戊脉安;异搏定(一种冠状动脉扩张药)

例句   To study the pharmacokinetics and pharmacodynamics of verapamil in patients with hypertension. 

研究维拉帕米在高血压患者的药代动力学及药效学。


概述

维拉帕米,又名异搏定、戊脉安、凡拉帕米,系钙拮抗剂中的苯烷基胺类受体拮抗剂。作用机制为抑制窦房结和房室交界区的4相自动除极化,对窦房结自律性、窦房和房室传导性均有选择性抑制作用;它能抑制钙离子内流,影响兴奋收缩偶联,使心肌产生负性肌力和血管平滑肌松弛作用,因此,本药对心脏有负性频率、负性传导及使心肌收缩减低,血管扩张血压下降。毒理维拉帕米为钙离子通道阻滞剂,口服30~45分钟血中药物浓度达峰值,120分钟起效,高峰作用时间3~4小时,血清药效浓度为80~300 mg/L,半衰期3~7小时,主

Prevention of Severe Hypoglycemia-Induced Brain Damage and Cognitive Impairment with Verapamil复制标题

维拉帕米预防严重低血糖引起的脑损伤和认知障碍

发表时间:2018-10-05

影响因子:7.2

作者: David A Jackson

期刊:Diabetes

Hypoglycemia is the rate-limiting treatment barrier for people with insulin-treated diabetes. With an increased emphasis on glycemic control, the risk of severe hypoglycemia for insulin-treated patient rises markedly. Severe, life-threatening hypoglycemia occurs, on average, once per year for insulin-treated patients with diabetes. The increased morbidity resulting from severe hypoglycemia is mediated by brain glucose deprivation leading to seizures, coma, and brain damage. In clinical and pre-clinical studies, hypoglycemia-induced brain damage results in significant cognitive impairments characterized by deficits in spatial and orientation memory. Hypoglycemia induces a surge of stimulatory signals (excitotoxicity) leading to an inability of neurons to repolarize and control calcium influx. Excess calcium influx from the endoplasm reticulum and extracellular space initiates a positive feedback loop that leads to brain cell necrosis. Consistent with a major role of calcium influx in mediating other types of brain damage, treatment with the calcium channel blocker, verapamil, has been shown to reduce neural damage by up to 96% in other models of brain injury.

译文

低血糖症是胰岛素治疗糖尿病患者的限速治疗障碍。随着对血糖控制的日益重视,胰岛素治疗患者严重低血糖的风险显着增加。对于胰岛素治疗的糖尿病患者,平均每年一次发生严重的危及生命的低血糖症。由严重低血糖引起的发病率增加是由脑葡萄糖剥夺介导的,导致癫痫发作,昏迷和脑损伤。在临床和临床前研究中,低血糖诱导的脑损伤导致显着的认知障碍,其特征在于空间和方向记忆缺陷。低血糖症引起刺激信号(兴奋性毒性)的激增,导致神经元不能再复极化并控制钙内流。来自内质网和细胞外空间的过量钙流入引发正反馈回路,导致脑细胞坏死。与钙流入在介导其他类型脑损伤中的主要作用一致,钙通道阻滞剂维拉帕米治疗已被证明可以在其他脑损伤模型中将神经损伤降低多达96%。