Vasopressin receptor antagonist

Most commonly VRAs are used in the treatment of hyponatremia, especially in patients with congestive heart failure, liver cirrhosis or SIADH.

It has been suggested that cardiovascular mortality may be reduced by selective V2RA such as tolvaptan in the higher risk group with kidney function impairment or severe congestive findings.

Given the potential hyperstimulation of V1R, V2RA may have additional secondary preventative benefits in patients with cirrhosis through a reduction in portal pressure and a decreased risk of variceal bleeding.

[10] Polycystin defects increase intracellular cAMP, secondary messenger for vasopressin acting at V2R, leading to cyst development.

[9] Full scale therapeutic trials of V2RAs in patients with autosomal dominant polycystic kidney disease are currently ongoing.

[9] Thus V1R and/or V2R antagonists may serve as molecular chaperones to mitigate misfolding defects in selected patients with type 2 NDI.