Detroit Medical Center/Wayne State University, Harper University Hospital, 3990 John R, Suite 9370, Detroit, MI 48201, USA.
Expert Opin Investig Drugs. 2011 Jun;20(6):831-48. doi: 10.1517/13543784.2011.579102. Epub 2011 May 9.
Hypervolemia and hyponatremia are common features in heart failure and have been associated with increased morbidity and mortality. Stimulation of arginine vasopressin (AVP) plays an important role in the development of both hypervolemia and hyponatremia. Lixivaptan is a selective vasopressin type 2 (V(2)) receptor antagonist that has been demonstrated to have the ability to induce aquaresis, the electrolyte sparing excretion of water, resulting in fluid removal as well as correction of hyponatremia.
This article describes the prevalence, pathophysiology and current treatment limitations of hyponatremia, highlights the importance of arginine vasopressin and the potential role of arginine vasopressin antagonists and reviews all available literature on lixivaptan, a selective V(2) receptor antagonist.
The available experience of lixivaptan in heart failure, although limited, is encouraging. Its aquaretic effect provides the basis for its use to correct hypervolemia and hyponatremia in patients with heart failure, and the absence of neurhormonal stimulation provides positive signal for the exploration of its potential in improving outcomes.
血容量过多和低钠血症是心力衰竭的常见特征，与发病率和死亡率的增加有关。精氨酸加压素（AVP）的刺激在血容量过多和低钠血症的发展中都起着重要作用。利昔伐坦是一种选择性血管加压素 2（V2）受体拮抗剂，已被证明具有诱导水利尿（即电解质保水的水排泄）的能力，从而导致液体清除和低钠血症的纠正。
本文描述了低钠血症的流行率、病理生理学和当前治疗限制，强调了精氨酸加压素的重要性和精氨酸加压素拮抗剂的潜在作用，并回顾了所有关于利昔伐坦（一种选择性 V2 受体拮抗剂）的可用文献。
尽管利昔伐坦在心力衰竭方面的可用经验有限，但令人鼓舞。其利尿作用为其在心力衰竭患者中纠正血容量过多和低钠血症提供了依据，而无神经激素刺激为探索其在改善结局方面的潜力提供了积极信号。
