Phase III Clinical Pharmacology Study of Tolvaptan

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 com...

Full description

Saved in:
Bibliographic Details
Published in:Cardiovascular drugs and therapy 2011-12, Vol.25 (Suppl 1), p.57-65
Main Authors: Inomata, Takayuki, Izumi, Tohru, Matsuzaki, Masunori, Hori, Masatsugu, Hirayama, Atsushi
Format: Article
Language:English
Subjects:
Aged
Aged, 80 and over
Antidiuretic Hormone Receptor Antagonists
Asian Continental Ancestry Group
Benzazepines - blood
Benzazepines - pharmacokinetics
Benzazepines - pharmacology
Body Weight - drug effects
Calcium - urine
Cardiology
Creatinine - blood
Creatinine - urine
Diuretics - blood
Diuretics - pharmacokinetics
Diuretics - pharmacology
Double-Blind Method
Drug Therapy, Combination
Edema, Cardiac - blood
Edema, Cardiac - drug therapy
Edema, Cardiac - urine
Female
Furosemide - pharmacology
Humans
Magnesium - urine
Male
Medicine
Medicine & Public Health
Middle Aged
Potassium - blood
Potassium - urine
Sodium - blood
Sodium - urine
Uric Acid - urine
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0920-3206
1573-7241
DOI:10.1007/s10557-011-6349-x