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The Current Role of Clevidipine in the Management of Hypertension
American Journal of Cardiovascular Drugs ( IF 2.8 ) Pub Date : 2021-09-02 , DOI: 10.1007/s40256-021-00494-6
Bo Xu 1 , Zhen Chen 1 , Gaorui Tang 1
Affiliation  

Acute hypertension, which may damage blood vessels, causes irreversible organ damage to the vasculature, central nervous system, kidney, and heart. Clevidipine, the first third-generation calcium channel antagonist approved by the Food and Drug Administration (FDA) in the past 20 years, is an ultra-short-acting calcium channel blocker that inhibits L-type calcium channels with high clearance and low distribution, can be rapidly metabolized into the corresponding inactive acid, and is rapidly hydrolyzed into inactive metabolites by esterase in arterial blood. Clevidipine is the same as nicardipine in that the main physiological effect is vasodilation and the main target is the arterial system, which has a limited effect on capacitor vessels. Unlike nitroglycerin, clevidipine has a limited effect on preload. In contrast to other direct-acting vasodilators, clevidipine has an ultra-short half-life due to metabolism by nonspecific blood and tissue esterases. Clevidipine trials conducted in adult populations have proven that it can rapidly control blood pressure in cardiac surgery situations and that adverse reactions to clevidipine are similar to those with other antihypertensive agents. In recent years, clinical trials have shown that clevidipine has excellent blood pressure-lowering capability in patients with acute neurological injury (hemorrhage, stroke, and subarachnoid and acute intracerebral hemorrhage), those undergoing coronary artery bypass graft or spinal surgery, and in those with cerebral aneurysm/pheochromocytoma, acute heart failure, acute aortic syndromes, or renal insufficiency with severe hypertension, and it is equivalent to commonly used blood pressure-lowering medicines such as nicardipine or nitroglycerin. However, there is a lack of large-scale clinical trial data on the efficacy and safety of clevidipine in children during the perioperative period.



中文翻译:

目前氯维地平在高血压治疗中的作用

急性高血压可能会损害血管,会对脉管系统、中枢神经系统、肾脏和心脏造成不可逆的器官损害。氯维地平是近20年来美国食品药品监督管理局(FDA)批准的第一个第三代钙通道拮抗剂,是一种超短效钙通道阻滞剂,抑制L型钙通道,清除率高,分布低,能迅速代谢成相应的无活性酸,在动脉血中被酯酶迅速水解成无活性代谢物。氯维地平与尼卡地平相同,主要生理作用是血管舒张,主要作用靶点是动脉系统,对电容血管的作用有限。与硝酸甘油不同,氯维地平对前负荷的影响有限。与其他直接作用的血管扩张剂相比,由于非特异性血液和组织酯酶的代谢,氯维地平具有超短的半衰期。在成人人群中进行的氯维地平试验证明,它可以在心脏手术情况下快速控制血压,并且对氯维地平的不良反应与其他降压药相似。近年来,临床试验表明,氯维地平对急性神经损伤(出血、中风、蛛网膜下腔和急性脑出血)患者、冠状动脉旁路移植术或脊柱手术患者以及患有脑动脉瘤/嗜铬细胞瘤、急性心力衰竭、急性主动脉综合征或肾功能不全伴严重高血压,相当于常用的降血压药,如尼卡地平或硝酸甘油。然而,目前尚缺乏关于氯维地平在儿童围手术期的疗效和安全性的大规模临床试验数据。

更新日期:2021-09-02
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