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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 .
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.
Abbrev. [1]Meaning [1] Latin (or Neo-Latin) origin [1]; a.c. before meals: ante cibum a.d., ad, AD right ear auris dextra a.m., am, AM morning: ante meridiem: nocte ...
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Vasopressin receptor antagonists that are selective for the V2 receptor include: . Tolvaptan (FDA-approved); Lixivaptan; Mozavaptan; Satavaptan; Their main uses are in hyponatremia, such as that caused by syndrome of inappropriate antidiuretic hormone (SIADH) and heart failure, however these agents should be avoided in patients with cirrhosis.
Tolvaptan and conivaptan antagonize the effects of antidiuretic hormone (vasopressin), thereby promoting the specific excretion of free water, directly ameliorating the volume overloaded state, and counteracting the hyponatremia that occurs due to the release of neuroendocrine hormones in an attempt to counteract the effects of heart failure.
Tolvaptan, an aquaretic drug, is a vasopressin receptor 2 (V2) antagonist. [9] Pre-clinical studies had suggested that the molecule cAMP could be involved in the enlargement of ADPKD cysts, [ 42 ] and studies on rodents confirmed the role of vasopressin in increasing the levels of cAMP in the kidney, which laid the basis for the conduction of ...
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