Which drug is a selective vasopressin V2 receptor agonist?
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Which drug is a selective vasopressin V2 receptor agonist?
Tolvaptan (Samsca) is an oral V2 receptor antagonist and has been approved by the US Food and Drug Administration (FDA) for use in patients with CHF or cirrhosis and hyponatremia, and is also used in patients with SIADH. Conivaptan (Vaprisol) is also approved by the US FDA for treatment of euvolemic hyponatremia.
Where are V2 receptors found?
the collecting tubules
V2 receptors are found on the basolateral surface of the cells of the collecting tubules. Activation of these receptors initiates the key homeostatic action of vasopressin, namely water reabsorption from the urine.
Where are the receptors for ADH located?
Antidiuretic hormone binds to receptors on cells in the collecting ducts of the kidney and promotes reabsorption of water back into the circulation. In the absense of antidiuretic hormone, the collecting ducts are virtually impermiable to water, and it flows out as urine.
What hormone is the antagonist to ADH?
An antidiuretic hormone inhibitor used to raise serum sodium levels. A selective vasopressin V2-receptor antagonist to slow kidney function decline in patients at risk for rapidly progressing autosomal dominant polycystic kidney disease (ADPKD)….Antidiuretic Hormone Receptor Antagonists.
| Drug | Target | Type |
|---|---|---|
| Tolvaptan | Vasopressin V1a receptor | target |
What is V2R?
V2R. Vehicle-to-Roadside (wireless vehicle communication)
Where are V3 receptors located?
the pituitary
V3 receptors are found mainly in the pituitary. They are Gq-coupled G-protein receptors which increase intracellular calcium when activated.
Where are V1 and V2 receptors found?
V1 receptors are found on various cells including vascular smooth muscle, and V1 stimulation causes vasoconstriction. Kidney collecting duct cells express V2 receptors, which mediate water retention.
What is ADH function?
Antidiuretic hormone (ADH) is a chemical produced in the brain that causes the kidneys to release less water, decreasing the amount of urine produced. A high ADH level causes the body to produce less urine.
What is the mechanism of ADH?
ADH decreases the volume of urine by increasing the reabsorption of water in the kidneys. ADH causes contraction of vascular smooth muscles, constriction of arterioles, and peripheral vasoconstriction.
What drug class is desmopressin?
Desmopressin is in a class of medications called hormones. It works by replacing vasopressin, a hormone that is normally produced in the body to help balance the amount of water and salt.
Is desmopressin an antidiuretic?
Desmopressin (dDAVP), a synthetic analogue of 8-arginine vasopressin (ADH), is an antidiuretic peptide drug modified by deamination of 1-cysteine and substitution of 8-L-arginine by 8-D-arginine. ADH is an endogenous pituitary hormone that has a crucial role in the control of the water content in the body.
Which drugs increase ADH?
Vasopressin (Pitressin) Has vasopressor and ADH activity. Increases water resorption at the distal renal tubular epithelium (ADH effect) and promotes smooth muscle contraction throughout the vascular bed of the renal tubular epithelium (vasopressor effects).
What do ADH antagonists do?
Tolvaptan is a vasopressin receptor antagonist. Vasopressin (a.k.a. ADH or antidiuretic hormone) helps to regulate water retention by absorbing water in the collecting ducts of the nephron. Blocking this receptor will allow water to be excreted more readily.
What are Vaptan drugs?
Vasopressin receptor antagonists (Vaptans) are a new group of nonpeptide drugs which have been used in various clinical conditions with limited success. Whereas conivaptan is to be administered intravenously, the other vaptans like tolvaptan, lixivaptan, and satavaptan are effective as oral medication.
Does vasopressin increase blood pressure?
Vasopressin plays a key role in the regulation of body fluid balance through its antidiuretic action. This action is mediated by renal vasopressin V2-receptors, which are coupled to adenylyl cyclase and the generation of cAMP. Vasopressin is also capable of causing vasoconstriction and increasing blood pressure.
Is vasopressin a vasoconstrictor or vasodilator?
Indeed, it was shown that vasopressin is a more potent vasoconstrictor than angiotensin II or norepinephrine and is capable of increasing systemic vascular resistance in doses less than those required to produce maximum urine concentration.
