Drug intelligence / Profile preview

conivaptan + furosemide

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Conivaptan + furosemide is a combination of two pharmaceutical agents used primarily in the management of fluid overload and hyponatremia, particularly in hospitalized patients with heart failure or other conditions associated with volume excess. Conivaptan is a nonpeptide dual antagonist of arginine vasopressin (AVP) V1A and V2 receptors. It promotes aquaresis by blocking the action of AVP on renal collecting ducts, leading to increased excretion of free water without significant loss of sodium or potassium. Furosemide is a loop diuretic that inhibits the sodium-potassium-chloride cotransporter (solute carrier family 12 member 1) in the thick ascending limb of Henle’s loop, resulting in increased excretion of sodium, chloride, potassium, and water. When used together, conivaptan augments both the diuretic and natriuretic response to furosemide without adversely affecting hemodynamics or renal function[4][6]. This combination may be considered for patients with acute decompensated heart failure who require aggressive fluid removal.

02

Targets

NKCC2 (Sodium-potassium-chloride cotransporter 2)AVPR1A (Arginine vasopressin receptor 1A)AVPR2 (Arginine vasopressin V2 receptor)

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