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血管加压素受体拮抗剂:一类用于治疗低钠血症的新型药物。

Vasopressin-receptor antagonists: a new class of agents for the treatment of hyponatremia.

作者信息

Olson Beatriz R

机构信息

Endocrinology and Metabolism, 850 Straits Turnpike, Suite 204, Middlebury, CT 06762, USA.

出版信息

Endocr Metab Immune Disord Drug Targets. 2006 Sep;6(3):249-58. doi: 10.2174/187153006778249985.

DOI:10.2174/187153006778249985
PMID:17017976
Abstract

Hyponatremia is a very common electrolyte disorder often caused by the dysregulation of arginine vasopressin (AVP) secretion and the effects of the hormone at its receptors and is associated with significant morbidity and mortality. Recent developments in the understanding of water homeostasis and AVP actions at the kidney, both in normal circumstances and in pathologic conditions, has created the possibility of new therapies that directly target the inappropriate excess of AVP stimulation of vasopressin V(2) receptors (V2Rs) in the kidney. Preclinical and clinical trial results indicate that AVP V2R antagonism is a highly promising and rational approach for the treatment of dilutional hyponatremia caused by excessive retention of water. This review of hyponatremia and its therapy is intended to educate clinicians who manage patients who have hyponatremia and its complications. Background information on hyponatremia is presented and the pertinent published literature with regard to the diagnosis and therapy of this disorder is summarized with a specific focus on AVP-receptor antagonists. Agents that antagonize AVP V2Rs and promote aquaresis, the electrolyte-sparing excretion of free water, are likely to be effective and well tolerated therapies for the treatment of dilutional hyponatremia.

摘要

低钠血症是一种非常常见的电解质紊乱,通常由精氨酸加压素(AVP)分泌失调及其在受体处的激素作用引起,且与显著的发病率和死亡率相关。在正常和病理情况下,对肾脏水稳态及AVP作用的最新认识发展,使得直接针对肾脏中AVP对血管加压素V2受体(V2R)的不适当过度刺激的新疗法成为可能。临床前和临床试验结果表明,AVP V2R拮抗作用是治疗因水潴留过多导致的稀释性低钠血症的一种极有前景且合理的方法。这篇关于低钠血症及其治疗的综述旨在教育管理低钠血症及其并发症患者的临床医生。文中介绍了低钠血症的背景信息,并总结了有关该疾病诊断和治疗的相关已发表文献,特别关注AVP受体拮抗剂。拮抗AVP V2R并促进水利尿(即游离水的保电解质排泄)的药物可能是治疗稀释性低钠血症的有效且耐受性良好的疗法。

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