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Related Experiment Video

Updated: Jun 15, 2026

Continuous IV Infusion is the Choice Treatment Route for Arginine-vasopressin Receptor Blocker Conivaptan in Mice to Study Stroke-evoked Brain Edema

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Tolvaptan.

Greg L Plosker¹

¹Adis, Auckland, New Zealand. demail@adis.co.nz

|March 9, 2010

Summary

Tolvaptan effectively increases serum sodium levels in patients with hyponatremia. This selective vasopressin V(2) receptor antagonist demonstrated significant improvements in clinical trials for heart failure, cirrhosis, and SIADH.

Area of Science:

Nephrology
Endocrinology
Cardiology

Background:

Hyponatremia, characterized by low serum sodium levels (<135 mmol/L), is often associated with conditions like heart failure, cirrhosis, and SIADH.
Selective vasopressin V(2) receptor antagonists offer a therapeutic approach to manage hyponatremia by increasing free water excretion.

Purpose of the Study:

To evaluate the efficacy and safety of tolvaptan in correcting serum sodium levels in patients with hypervolemic or euvolemic hyponatremia.
To assess the impact of tolvaptan on serum sodium levels across different baseline severity in multicenter trials.

Main Methods:

Two identical randomized, double-blind, placebo-controlled trials (SALT-1 and -2) involving patients with hyponatremia.
Tolvaptan (15-60 mg daily, titrated) or placebo administered for up to 30 days, with serum sodium levels monitored.

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Main Results:

Tolvaptan significantly improved serum sodium levels compared to placebo from baseline to day 4 and day 30 in SALT-1 and -2.
Benefits were observed in patients with both mild (<135 mmol/L) and marked (<130 mmol/L) baseline hyponatremia.
Tolvaptan also showed superiority in increasing serum sodium in a subgroup of EVEREST trial patients hospitalized for heart failure.

Conclusions:

Tolvaptan is an effective oral treatment for increasing serum sodium levels in patients with hyponatremia.
The drug is generally well-tolerated, with thirst and dry mouth being the most common side effects.