Medicines
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Brand: Samsca
Tolvaptan is a selective vasopressin V2-receptor antagonist indicated for the treatment of clinically significant hypervolemic and euvolemic hyponatremia, including patients with heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone secretion (SIADH). It works by blocking the binding of vasopressin to V2 receptors in the kidneys, thereby promoting aquaresis (excretion of electrolyte-free water) and increasing serum sodium levels.
For the treatment of hyponatremia associated with heart failure, cirrhosis, and SIADH.
Rapid increases in serum sodium concentration have been reported with tolvaptan, and have been associated with central pontine myelinolysis. Tolvaptan should be initiated in the hospital setting so that serum sodium can be monitored closely. The rate of correction should not exceed 12 mEq/L over 24 hours.
Outcome:
Increased tolvaptan concentrations
Mechanism:
Inhibition of tolvaptan metabolism
Outcome:
Additive effects on fluid and electrolyte balance
Mechanism:
Synergistic diuresis
Outcome:
Slightly decreased tolvaptan absorption
Mechanism:
Changes in gastric pH
Most likely new formulation: extended-release formulation (Year: 2026, 60% confidence)
Based on current usage trends and safety profile, there is a low ( <5%) likelihood of regulatory changes impacting tolvaptan's availability in the near future.
Vasopressin Receptor Antagonist
Benzazepine