Tolvaptan is a selective, competitive vasopressin receptor 2 antagonist with an IC
50 of 1.28µM for the inhibition of AVP-induced platelet aggregation. Tolvaptan is used to treat hyponatremia associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone. Tolvaptan is also in fast-track clinical trials for polycystic kidney disease. Treatment with Tolvaptan causes rapid and sustained body weight reductions concurrent with increases in urine output, improves and/or normalizes serum sodium in hyponatremic patients, reduces signs and symptoms of congestion and increases thirst. However, Tolvaptan has not been shown to decrease heart failure re-hospitalization or mortality. As an adjunct to standard therapy, Tolvaptan is unique in that it is virtually the only novel agent tested in patients hospitalized for acute heart failure syndrome to reach its primary end point for short-term efficacy without causing deleterious side effects.
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