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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.
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]
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.
From or to a drug trade name: This is a redirect from (or to) the trade name of a drug to (or from) the international nonproprietary name (INN).
Tolvaptan is a racemic small molecule drug (Molecular Weight of 448.9 g.mol-1) and is a lipophilic drug, is essentially insoluble in water, and has fair oral absorption (>40% bioavailable). Tolvaptan hsa a plasma half-life of around 12 hours, a volume of distribution of 3L/kg, and has high plasma protein binding at 99%.
ATC code C03 Diuretics is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
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).