Aghel Arash, Tang W H Wilson
Section of Heart Failure and Cardiac Transplantation Medicine, Department of Cardiovascular Medicine, Cleveland Clinic, Cleveland, Ohio, USA.
Core Evid. 2008 Jun;3(1):31-43. doi: 10.3355/ce.2008.010.
Acute heart failure syndrome (AHFS) is one of the leading causes of hospital admission in the US. Tolvaptan is a vasopressin V(2) receptor antagonist that blocks the effect of arginine vasopressin (AVP) in reabsorbing water from the collecting ducts of the nephrons in congestive heart failure.
To review the evidence for utilizing tolvaptan in the treatment of AHFS.
Several clinical trials have sought to assess the clinical effects of tolvaptan in heart failure. Compared with placebo, tolvaptan has been shown to reduce bodyweight and improve serum sodium in patients with AHFS without worsening renal function. Tolvaptan appeared to be well tolerated with a good safety profile. It caused a significant reduction in pulmonary capillary wedge pressure compared with placebo, but has yet to demonstrate reversal of cardiac remodeling. A large-scale mortality trial showed no differences in long-term mortality rates between tolvaptan and placebo, although early symptom relief was apparent with tolvaptan and lower diuretic use.
Tolvaptan has shown to be safe and effective in treating congestion in AHFS. Free water excretion in fluid-overloaded patients vulnerable to cardiorenal compromise with standard diuretic therapy makes V(2) vasopressin receptor blockade an attractive adjunct to standard medical therapy aimed at reducing congestion in AHFS.
急性心力衰竭综合征（AHFS）是美国住院治疗的主要原因之一。托伐普坦是一种血管加压素V(2)受体拮抗剂，可阻断精氨酸血管加压素（AVP）在充血性心力衰竭中从肾单位集合管重吸收水分的作用。
综述托伐普坦用于治疗AHFS的证据。
多项临床试验试图评估托伐普坦在心力衰竭中的临床效果。与安慰剂相比，托伐普坦已被证明可降低AHFS患者的体重并改善血清钠水平，且不会使肾功能恶化。托伐普坦耐受性良好，安全性高。与安慰剂相比，它可显著降低肺毛细血管楔压，但尚未证明能逆转心脏重塑。一项大规模死亡率试验表明，托伐普坦和安慰剂的长期死亡率无差异，尽管托伐普坦能早期缓解症状且利尿剂使用量较低。
托伐普坦已被证明在治疗AHFS的充血方面安全有效。对于易因标准利尿治疗而出现心肾损害的液体超负荷患者，自由水排泄使V(2)血管加压素受体阻断成为旨在减轻AHFS充血的标准药物治疗的一种有吸引力的辅助手段。
