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Vasopressin agonists are used therapeutically in various conditions, and its long-acting synthetic analogue desmopressin is used in conditions featuring low vasopressin secretion, as well as for control of bleeding (in some forms of von Willebrand disease and in mild haemophilia A) and in extreme cases of bedwetting by children.
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.
Vasopressin is released into the brain in a circadian rhythm by neurons of the suprachiasmatic nucleus. [21] Vasopressin released from posterior pituitary is associated with nausea. [22] Recent evidence suggests that vasopressin may have analgesic effects. The analgesia effects of vasopressin were found to be dependent on both stress and sex. [23]
Vasopressin receptor antagonists (VRAs) are drugs that block vasopressin receptors. Most commonly VRAs are used to treat hyponatremia caused by syndrome of inappropriate antidiuretic hormone secretion (SIADH), congestive heart failure (CHF) and cirrhosis. [2] Somatostatin is a competitive inhibitor. [5]
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). The compound was discovered by Astellas and marked in 2006. The drug is now marketed by Cumberland Pharmaceuticals, Inc.
A newer class of drugs known as the NK 1 antagonists are a recently developed class of very efficacious drugs for controlling CINV. These drugs are often used alongside 5HT 3 inhibitors and corticosteroids to form a very potent cocktail of antiemetics that verge on achieving a nearly complete patient response (that is, completely stopping CINV ...
Some chemotherapy drugs are used in diseases other than cancer, such as in autoimmune disorders, [166] and noncancerous plasma cell dyscrasia. In some cases they are often used at lower doses, which means that the side effects are minimized, [166] while in other cases doses similar to ones used to treat cancer are used.
Desmopressin (1-deamino-8-D-arginine vasopressin) is a synthetic form of the normal human hormone arginine vasopressin (the antidiuretic hormone, or ADH), a peptide containing nine amino acids. Compared to vasopressin, desmopressin's first amino acid has been deaminated , and the arginine at the eighth position is in the dextro rather than the ...