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Conivaptan, sold under the brand name Vaprisol, is a non-peptide inhibitor of the receptor for anti-diuretic hormone, also called vasopressin. It was approved in 2004 for hyponatremia (low blood sodium levels).
Tolvaptan, sold under the brand name Samsca among others, is an aquaretic drug that functions as a selective, competitive vasopressin receptor 2 (V 2) antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH).
The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors (V 1A, V 1B and V 2).These receptors have a variety of functions, with the V 1A and V 2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V 1A and V 1B receptors are expressed in the central nervous system.
Vasopressin receptor antagonists include the new class of "vaptan drugs" such as conivaptan, tolvaptan, mozavaptan, lixivaptan, satavaptan etc. References
Synthetic aquaretics are vasopressin receptor antagonists and include conivaptan, tolvaptan, demeclocycline, and mozavaptan (OPC-31260), as well as lithium. Conivaptan hydrochloride and tolvaptan have been approved by the FDA for treating syndrome of inappropriate antidiuretic hormone. [4] [5] Mozavaptan is approved in Japan. [citation needed]
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Vasopressin receptor antagonists that are selective for the V2 receptor include: . Tolvaptan (FDA-approved); Lixivaptan; Mozavaptan; Satavaptan; Their main uses are in hyponatremia, such as that caused by syndrome of inappropriate antidiuretic hormone (SIADH) and heart failure, however these agents should be avoided in patients with cirrhosis.
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