Tolvaptan: a selective vasopressin type 2 receptor antagonist in congestive heart failure
Umamahesh C Rangasetty1, Mihai Gheorghiade, Barry F Uretsky
1University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555-0553, USA.
Abstract:
The neurohormone arginine vasopressin plays a significant role in the regulation of volume homeostasis, which is mediated via vasopressin type 2 (V2) receptors in the collecting tubules of the kidney. Diseases that are accompanied by abnormal volume homeostasis, including congestive heart failure and cirrhosis, are a frequent cause of hospital admissions and increasing healthcare costs. Recently, several nonpeptide V2 receptor antagonists have emerged as promising agents in the management of these conditions with the advantage of having no electrolyte abnormalities, neurohormonal activation or worsening renal insufficiency. Tolvaptan, a highly selective nonpeptide V2 receptor antagonist, has demonstrated an improvement in the volume status, osmotic balance and haemodynamic profile in preclinical and Phase II trials in patients with congestive heart failure and is currently undergoing testing in Phase III trials. This review discusses the evidence for the potential uses of tolvaptan, and its pharmacology and pharmacokinetics, particularly in congestive heart failure.
Related Concept Videos
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
Heart Failure Drugs: Diuretics
Heart Failure Drugs: Inotropic Agents
Antihypertensive Drugs: Angiotensin II Receptor Blockers
Heart Failure Drugs: β-Blockers
Heart Failure VI: Adjunct Therapies

