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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 .
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.
554 12000 Ensembl ENSG00000126895 ENSMUSG00000031390 UniProt P30518 O88721 RefSeq (mRNA) NM_000054 NM_001146151 NM_001276298 NM_001276299 NM_019404 RefSeq (protein) NP_000045 NP_001139623 NP_001263227 NP_001263228 NP_062277 Location (UCSC) Chr X: 153.9 – 153.91 Mb Chr X: 72.94 – 72.94 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Vasopressin receptor 2 (V2R), or arginine ...
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%.
Autosomal dominant polycystic kidney disease (ADPKD) is one of the most common, life-threatening inherited human disorders and the most common hereditary kidney disease. [1] [2] It is associated with large interfamilial and intrafamilial variability, which can be explained to a large extent by its genetic heterogeneity and modifier genes. [1]