Vasopressin receptor antagonists

Kidney Int. 2006 Jun;69(12):2124-30. doi: 10.1038/ Epub 2006 May 3.


The first non-peptide vasopressin receptor antagonist (VRA) was recently approved by the United States Food and Drug Administration, and several others are now in late stages of clinical development. Phase 3 trials indicate that these agents predictably reduce urine osmolality, increase electrolyte-free water excretion, and raise serum sodium concentration. They are likely to become a mainstay of treatment of euvolemic and hypervolemic hyponatremia. Although tachyphylaxis to the hydro-osmotic effect of these agents does not appear to occur, their use is accompanied by an increase in thirst, and they do not always eliminate altogether the need for water restriction during treatment of hyponatremia. Experience with use of these agents for treatment of acute, severe, life-threatening hyponatremia as well as chronic hyponatremia is limited. Further studies are needed to determine how they are best used in these situations, but the risk of overly rapid correction of hyponatremia seems low. Results of long-term trials to determine the ability of VRAs to reduce morbidity or mortality in congestive heart failure or to slow the progression of polycystic kidney disease are awaited with great interest.

Publication types

  • Review

MeSH terms

  • Antidiuretic Hormone Receptor Antagonists*
  • Azepines / therapeutic use
  • Benzamides / therapeutic use
  • Benzazepines / therapeutic use*
  • Clinical Trials as Topic
  • Diabetes Insipidus, Nephrogenic / drug therapy
  • Diabetes Insipidus, Nephrogenic / physiopathology
  • Fibrosis / drug therapy
  • Fibrosis / physiopathology
  • Heart Failure / drug therapy
  • Heart Failure / physiopathology
  • Humans
  • Hyponatremia / blood
  • Hyponatremia / drug therapy*
  • Hyponatremia / physiopathology
  • Osmolar Concentration
  • Polycystic Kidney Diseases / drug therapy
  • Polycystic Kidney Diseases / physiopathology
  • Pyrroles
  • Receptors, Vasopressin / chemistry
  • Receptors, Vasopressin / physiology
  • Sodium / blood
  • Tolvaptan
  • United States
  • United States Food and Drug Administration
  • Vasopressins / physiology


  • Antidiuretic Hormone Receptor Antagonists
  • Azepines
  • Benzamides
  • Benzazepines
  • Pyrroles
  • Receptors, Vasopressin
  • conivaptan
  • Vasopressins
  • Tolvaptan
  • lixivaptan
  • Sodium