Phase III clinical pharmacology study of tolvaptan.
Author(s): Inomata T, Izumi T, Matsuzaki M, Hori M, Hirayama A; Tolvaptan Investigators.
Affiliation(s): Department of Cardio-Angiology, Kitasato University School of Medicine, 1-15-1
Kitasato, Minamiku, Sagamihara, Kanagawa, 252-0373, Japan.
inotaka@med.kitasato-u.ac.jp
Publication date & source: 2011, Cardiovasc Drugs Ther. , 25 Suppl 1:S57-65
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.
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