Know and Understand Antagonistic Vasopressin


Antagonist vasopressin is a drug that binds to vasopressin receptors (V1A, V1B, and V2) and blocks the action of vasopressin (antidiuretic hormone, ADH), which is a hormone released by the pituitary gland. Vasopressin causes vasoconstriction and increases water reabsorption of the kidneys.

V1A and V2 receptors are found peripherally and V1A and V1B receptors are found in the central nervous system. V1A receptors regulate blood pressure and V2 receptors have an effect on kidney function.

Vasopressin antagonists are used to treating hyponatremia, especially in patients with congenital heart failure.

Antagonistic vasopressin has two treatments including conivaptan and tolvaptan.

The role of vasopressin antagonist in the treatment of cardiovascular disease

Vasopressin plays a physiological role in regulating blood pressure, fluid volume, and serum osmolality. In heart failure, insufficient vasopressin release can result in excessive fluid retention and hyponatremia. Vasopressin antagonist receptors are a class of new active drugs targeted to inhibit one or more different vasopressin receptors, such as V1A (vasoconstriction), V1B (excretion of ACTH) and V2 receptors (inhibition of water reabsorption in the kidneys).

In cardiac decompensation with excess fluid, selective V2 (lixivaptan, satavaptan, and tolvaptan) and non-selective V1A / V2 receptor inhibitors (conivaptan) have been shown to be better in standard therapy, because they allow faster weight loss and faster symptoms. improved (example: lack of dyspnea). Inhibition of free water reabsorption without affecting renal sodium excretion vasopressin antagonist receptors allows normalization of serum sodium in euvolemic and controlled hypervolemic hyponatremia.

Antagonistic vasopressin is well tolerated and does not have a negative effect on kidney function and serum potassium, unlike diuretics. Heart rate and blood pressure are not affected by antagonistic vasopressin receptors. However, in addition to the acute clinical effects of excellent long-term treatment with tolvaptan did not result in a lack of mortality in heart failure patients after an average of 9.9 months of clinical research.

The effects of vasopressin are implicated in various water retention diseases and heart disease, including heart failure, hyponatremia, hypertension, kidney disease, syndrome of inappropriate antidiuretic hormone secretion, cirrhosis, and ocular hypertension. Because vasopressin receptors are found in many different tissues, vasopressin antagonists may be useful in the treatment of disorders such as cerebral ischemia and stroke, Raynaud's disease, dysmenorrhea, and tocolytic treatment. Selective V1B antagonist vasopressin discussed its usefulness in the treatment of emotional and psychological disorders. Vaptan is a vasopressin antagonist receptor with V1A (relcovaptan) or V2 (tolvaptan, lixivaptan) selective or non-selective activity (conivaptan) which can be useful in some disorders. V1A / V2 non-selective antagonist vasopressin, conivaptan, is the first vaptan recognized by the FDA for the treatment of euvolemic hyponatremia.

Vasopressin antagonist receptors are a new class of drugs that address the problem of fluid retention, hyponatremia, and kidney dysfunction in heart failure. Increased vasopressin in heart failure can cause myocardial fibrosis, hypertrophy, and vasoconstriction by activating V1A receptors, and also water retention and hyponatremia by activating V2 receptors. Antagonism of the V1A receptor alone is also beneficial. In comparison, antagonism of the V2 receptor results in increased water excretion and sodium concentration. The vasopressin antagonist receptor can be seen as the first new class of agents with a dominant aquaretic effect, compared to the natriuretic effect on diuretics. The predominant action of the antagonist vasopressin receptor is water excretion, without other electrolyte reduction and less neurohormonal stimulation compared to diuretics.

Classified as a neurohormonal antagonist, antagonistic vasopressin receptors can improve blockages and hyponatremia, and prevent the development of left ventricular dysfunction. Some compounds have been evaluated in the final clinical trial program, and at least one can be used to continue standard medical therapy, combining aquaresis for blockage with neurohormonal antagonism for morbidity and mortality. New patents related to heart failure, hyponatremia, antidiuretic hormones and antagonistic vasopressin have been reviewed.

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