Zulkifli Amin Hilman, Suridanda Danny Siska
Faculty of Medicine, Universitas Indonesia, Jakarta, Indonesia.
Department of Cardiology and Vascular Medicine, Faculty of Medicine, Universitas Indonesia, Jakarta, Indonesia.
J Tehran Heart Cent. 2016 Jan 13;11(1):1-5.
Heart failure (HF) is still a major problem worldwide with high morbidity and mortality rates. The recently developed medication for HF is still incapable of reducing its morbidity and mortality, and clinical data supporting the efficacy and safety of its mainstay therapy remain insufficient. Arginine-vasopressin (AVP) plays important roles in circulatory and water homeostasis, one of which is water retention through the V2 receptor. In patients with HF, there is an increased level of AVP, contributing to such symptoms as edema, dyspnea, and congestion. Tolvaptan as a selective V2 receptor antagonist, in addition to the conventional therapy, has been shown to cause an increase in net fluid loss, a decrease in body weight, and a reduction in the rate of HF exacerbation. Such evidence has been provided by the Acute and Chronic Therapeutic Impact of a Vasopressin Antagonist (ACTIV) in Congestive Heart Failure (CHF), Efficacy of Vasopressin Antagonism in Heart Failure Outcome Study With Tolvaptan (EVEREST), Acute Heart Failure Volume Control Multicenter Randomized (AVCMA), and Study of Ascending Levels of Tolvaptan in hyponatremia 1and 2 (SALT-1 and SALT-2) trials. Tolvaptan can be an alternative diuretic in conjunction with other standard therapies for HF and has already been proved to be able to decrease morbidity and mortality, especially in HF patients with hyponatremia.
心力衰竭（HF）仍是一个全球性的重大问题，发病率和死亡率都很高。最近研发的用于治疗HF的药物仍无法降低其发病率和死亡率，支持其主要治疗方法有效性和安全性的临床数据仍然不足。精氨酸加压素（AVP）在循环和水稳态中发挥着重要作用，其中之一是通过V2受体潴留水分。在HF患者中，AVP水平升高，会导致水肿、呼吸困难和充血等症状。托伐普坦作为一种选择性V2受体拮抗剂，除常规治疗外，已被证明可导致净失液量增加、体重减轻以及HF恶化率降低。血管加压素拮抗剂在充血性心力衰竭（CHF）中的急性和慢性治疗影响（ACTIV）、托伐普坦心力衰竭结局研究中的血管加压素拮抗作用疗效（EVEREST）、急性心力衰竭容量控制多中心随机试验（AVCMA）以及托伐普坦在低钠血症1和2中的升阶水平研究（SALT-1和SALT-2）试验都提供了此类证据。托伐普坦可作为一种替代利尿剂，与其他治疗HF的标准疗法联合使用，并且已被证明能够降低发病率和死亡率，尤其是在伴有低钠血症的HF患者中。
