Mechanism of Action

Tolvaptan is a selective vasopressin V2 receptor antagonist. By inhibiting these receptors in the kidneys, it promotes aquaresis (increased urine output without electrolyte loss), reducing water reabsorption in the collecting ducts. This action helps manage hyponatremia and volume overload in conditions like heart failure and liver cirrhosis.

Indication

Indicated for the treatment of clinically significant hypervolemic and euvolemic hyponatremia, such as that associated with heart failure and the syndrome of inappropriate antidiuretic hormone secretion (SIADH).