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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).
Tolvaptan phosphate is a drug used for the treatment of cardiac edema. It is a prodrug of tolvaptan, [1] [2] formulated as the salt tolvaptan sodium phosphate, for intravenous administration. Tolvaptan phosphate is converted into the active drug tolvaptan in the human body following administration.
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.
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]
Tolvaptan, an aquaretic drug, is a vasopressin receptor 2 (V2) antagonist. [9] Pre-clinical studies had suggested that the molecule cAMP could be involved in the enlargement of ADPKD cysts, [ 42 ] and studies on rodents confirmed the role of vasopressin in increasing the levels of cAMP in the kidney, which laid the basis for the conduction of ...
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Palladio conducted the ELiSA Phase II study with lixivaptan in 31 ADPKD patients. In this study, the proportion of study subjects who showed a urine osmolality response consistent with full vasopressin V 2 receptor inhibition was qualitatively and quantitatively similar to the published effect seen in clinical studies conducted with tolvaptan. [13]
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).