|Trade names||Samsca, Jinarc, Jynarque, others|
|Drug class||Vasopressin-2 receptor (V2) antagonist|
|Main uses||Low sodium, autosomal dominant polycystic kidney disease (ADPKD)|
|Side effects||Thirst, nausea, high sodium, osmotic demyelination syndrome, liver failure, high potassium|
|Bioavailability||Unknown (40% absorbed)|
|Elimination half-life||12 hours (terminal)|
|Chemical and physical data|
|Molar mass||448.95 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Tolvaptan, sold under the brand name Samsca among others, is a medication used to treat low sodium due to heart failure or syndrome of inappropriate antidiuretic hormone (SIADH). It is also used for autosomal dominant polycystic kidney disease (ADPKD). It is taken by mouth. Effects begin within 4 hours.
Common side effects include thirst, nausea, and rapid increase in sodium. Other complications may include osmotic demyelination syndrome, liver failure, and high potassium. It is a vasopressin-2 receptor (V2) antagonist which works by increasing urine production.
Tolvaptan was approved for medical use in the United States and Europe in 2009. A generic version was approved in 2020, though was not available commercially as of 2021. In the United States 10 tablets of 30 mg costs about 3,800 USD as of 2021. This amount in the United Kingdom costs the NHS about £750.
Tolvaptan is indicated for the treatment of significant hypervolemic and euvolemic hyponatremia.
The FDA has determined that tolvaptan should not be used for longer than 30 days and should not be used in patients with underlying liver disease because it can cause liver injury, potentially leading to liver failure. When using to treat hyponatremia, it may cause too rapid correction of hyponatremia resulting in osmotic demyelination syndrome.
|Enantiomers of tolvaptan|
CAS number: 331947-66-1
CAS number: 331947-44-5
The U.S. Food and Drug Administration (FDA) granted tolvaptan a fast track designation for clinical trials investigating its use for the treatment of polycystic kidney disease. The FDA granted Jynarque an orphan drug designation in April 2012, for the treatment of autosomal dominant polycystic kidney disease.
Society and culture
The brand Jynarque, was granted approval for medical use in the United States in April 2018.
In Ontario Canada in 2013 it was found to be not cost effective at 250 CAD per day and was therefore not covered.
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