Phase III clinical pharmacology study of tolvaptan

被引：39
作者：
Inomata T. [1 ]
Izumi T. [1 ]
Matsuzaki M. [2 ]
Hori M. [3 ]
Hirayama A. [4 ]
机构：
[1] Department of Cardio-Angiology, Kitasato University School of Medicine, Minamiku 252-0373, Sagamihara, Kanagawa
[2] Department of Medicine and Clinical Science, Yamaguchi University Graduate School of Medicine, Ube
[3] Osaka Medical Center for Cancer and Cardiovascular Diseases, Osaka
[4] Division of Cardiovascular Medicine, Department of Medicine, Nihon University School of Medicine, Tokyo
来源：
Cardiovascular Drugs and Therapy | 2011年 / 25卷 / Suppl 1期
关键词：
Chronic heart failure; Tolvaptan; Vasopressin V2 receptor; Volume overload; Water diuresis;
D O I：
10.1007/s10557-011-6349-x
中图分类号：
学科分类号：
摘要：
Purpose: This study aimed to investigate the pharmacokinetics, pharmacodynamics, efficacy and safety of tolvaptan, an orally effective vasopressin V2-receptor antagonist. Methods: This was a multicenter, randomized, double-blind, parallel group study. Tolvaptan was administered at 7.5 or 15 mg, in combination with furosemide, for 7 days in Japanese heart failure (HF) patients with volume overload that had not resolved despite receiving furosemide. Results: The blood concentration of tolvaptan was maintained at a higher concentration for a longer time in patients who received 15 mg/day when compared with patients who received 7.5 mg/day. Tolvaptan increased urine volume and increased weight loss dose-dependently when used in combination with furosemide. Importantly, tolvaptan enhanced water diuresis without affecting blood electrolyte levels. Conclusion: Tolvaptan exerts diuretic effects and causes body weight loss at the low dose of 7.5 mg; however, these effects were less than those elicited by 15 mg tolvaptan. © 2011 Springer Science+Business Media, LLC.
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页码：S57 / S65
页数：8
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