Vasopressin receptor antagonists: Characteristics and clinical role

Best Pract Res Clin Endocrinol Metab. 2016 Mar;30(2):289-303. doi: 10.1016/j.beem.2016.02.004. Epub 2016 Feb 16.


Hyponatremia, the most common electrolyte disorder in hospitalized patients is associated with increased risk of mortality even when mild and apparently asymptomatic. Likewise morbidity manifested as attention deficits, gait disturbances, falls, fractures, and osteoporosis is more prevalent in hyponatremic subjects. Hyponatremia also generates a significant financial burden. Therefore, it is important to explore approaches that effectively and safely treat hyponatremia. Currently available strategies are physiologically sound and affordable but lack evidence from clinical trials and are limited by variable efficacy, slow response, and/or poor compliance. The recent emergence of vasopressin receptor antagonists provides a class of drugs that target the primary pathophysiological mechanism, namely vasopressin mediated impairment of free water excretion. This review summarizes the historical development, pharmacology, clinical trials supporting efficacy and safety, shortcomings, as well as practical suggestions for the use of vasopressin receptor antagonists.

Keywords: antidiuretic hormone receptor antagonists; hyponatremia; vasopressin.

Publication types

  • Review

MeSH terms

  • Antidiuretic Hormone Receptor Antagonists / administration & dosage
  • Antidiuretic Hormone Receptor Antagonists / adverse effects
  • Antidiuretic Hormone Receptor Antagonists / pharmacology
  • Antidiuretic Hormone Receptor Antagonists / therapeutic use*
  • Clinical Trials as Topic
  • Humans
  • Hyponatremia / drug therapy*
  • Water-Electrolyte Balance


  • Antidiuretic Hormone Receptor Antagonists