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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).
It has been suggested that cardiovascular mortality may be reduced by selective V 2 RA such as tolvaptan in the higher risk group with kidney function impairment or severe congestive findings. [9] But until FDA indication is granted for use in CHF with or without accompanying hyponatremia, VRAs are not recommended in patients with CHF. [9]
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. It was developed by Otsuka Pharmaceutical Co. and was approved for use in Japan in 2022. [3]
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).
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In 2014, Japan was the first country in the world to approve a pharmacological treatment for ADPKD [33] followed by Canada and Europe, which approved the drug tolvaptan for ADPKD patients in the beginning of 2015. The USA FDA approved the use of tolvaptan in the treatment of ADPKD in 2018. [41]