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静脉注射考尼伐坦

Intravenous conivaptan.

作者信息

Moen Marit D, Keating Gillian M

机构信息

Wolters Kluwer Health | Adis, Auckland, New Zealand.

出版信息

Am J Cardiovasc Drugs. 2008;8(5):341-8; discussion 349. doi: 10.2165/00129784-200808050-00006.

Abstract

*Conivaptan is an arginine vasopressin V1A and V2 receptor antagonist. The intravenous formulation is approved in the US for use in the treatment of euvolemic and hypervolemic hyponatremia. Conivaptan produces a dose-dependent electrolyte-sparing aquaresis (solute-free water excretion), increasing serum sodium levels. *In a randomized, double-blind, parallel-group, placebo-controlled, multicenter trial in adults with euvolemic or hypervolemic hyponatremia, the area under the serum sodium concentration-time curve over a 4-day treatment duration (primary endpoint) was significantly greater in intravenous conivaptan 40 mg/day recipients than in placebo recipients. *The total time during treatment that patients had serum sodium levels > or = 4 mEq/L above baseline was significantly longer in intravenous conivaptan than placebo recipients. In conivaptan recipients, an increase in serum sodium levels of > or = 4 mEq/L above baseline was achieved approximately 1 day after the first dose of the drug. *In addition, the mean change from baseline in free water clearance and effective water clearance over the first day of treatment was significantly greater with intravenous conivaptan than with placebo. *Given the nature of the treatment, the tolerability profile for intravenous conivaptan was generally acceptable in patients with hyponatremia. The most common adverse events were injection related (e.g. injection-site phlebitis), hypotension, and pyrexia.

摘要

考尼伐坦是一种精氨酸血管加压素V1A和V2受体拮抗剂。其静脉制剂在美国被批准用于治疗等容性和高容性低钠血症。考尼伐坦可产生剂量依赖性的保电解质利水作用(无溶质水排泄),提高血清钠水平。在一项针对等容性或高容性低钠血症成人患者的随机、双盲、平行组、安慰剂对照、多中心试验中,接受40 mg/天静脉注射考尼伐坦的患者在4天治疗期间血清钠浓度-时间曲线下面积(主要终点)显著大于接受安慰剂的患者。在治疗期间,静脉注射考尼伐坦的患者血清钠水平高于或等于基线水平4 mEq/L的总时间显著长于接受安慰剂的患者。在考尼伐坦治疗的患者中,首次给药后约1天血清钠水平比基线水平升高≥4 mEq/L。此外,治疗第一天静脉注射考尼伐坦的患者自由水清除率和有效水清除率较基线的平均变化显著大于安慰剂组。鉴于治疗的性质,静脉注射考尼伐坦的耐受性在低钠血症患者中总体上是可以接受的。最常见的不良事件与注射有关(如注射部位静脉炎)、低血压和发热。

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