VRA and liver

Q: Which of the following vasopressin receptor antagonists should not be used in patients with liver cirrhosis?

A) tolvaptan

B) mozavaptan

C) satavaptan

D) lixivaptan

E) conivaptan

Answer: A

Vasopressin receptor antagonists act on three receptors i.e., V1a, V1b, and V2 receptors. 

• V1a and V1b receptors cause vasoconstriction and adrenocorticotropic hormone (ACTH) release
• V2 receptors mediates the antidiuretic response

All oral formulations i.e., tolvaptan, mozavaptan, satavaptan, and lixivaptan are V2 selective. Conivaptan is the only parenteral formulation, and acts on both V2 and V1a receptors. 

Tolvaptan is contraindicated in patients with liver issues.

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References:

1. Verbalis JG, Goldsmith SR, Greenberg A, et al. Hyponatremia treatment guidelines 2007: expert panel recommendations. Am J Med 2007; 120:S1.

2. Greenberg A, Verbalis JG. Vasopressin receptor antagonists. Kidney Int 2006; 69:2124.

3. Schrier RW, Gross P, Gheorghiade M, et al. Tolvaptan, a selective oral vasopressin V2-receptor antagonist, for hyponatremia. N Engl J Med 2006; 355:2099.