Vasopressin

Description

Argipressin is a neurohypophysial hormone from the vasopressin hormone family. Its two primary functions are to retain water in the body and to constrict blood vessels. The antidiuretic action of Argipressin is ascribed to increase in reabsorption of water by the renal tubules. Argipressin can cause contraction of smooth muscle of the gastrointestinal tract, gall bladder, urinary bladder and all parts of the vascular bed, especially the capillaries, small arterioles and venules with less effect on the smooth musculature of the large veins. Agripressin for injections is used for use in diabetes insipidus, when this is not of nephrogenic origin and control of bleeding from oesophageal varices. In addition, argipressin is indicated to increase blood pressure in adults with vasodilatory shock (e.g., post-cardiotomy or sepsis) who remain hypotensive despite fluids and catecholamines.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Vasopressin V1a receptor 18	Agonist 2,752	0.24 nM [EC50]
Vasopressin V1b receptor 7	Agonist 2,752	0.05 nM [EC50]
Vasopressin V2 receptor 16	Agonist 2,752	4.3 nM [EC50]

Conditions

Condition	Modality	Highest Phase	Product
Diabetes insipidus 4	Primary	Approved 8,583	Argipressin 20 IU/ml Solution for Injection
Oesophageal varices 2	Primary	Approved 8,583	Argipressin 20 IU/ml Solution for Injection
Vasodilatory shock 2	Primary	Approved 8,583	VASOSTRICT
Post-operative abdominal distention 2	Palliative	Approved 8,583	PITRESSIN
Abdominal roentgenography 2	Diagnostic	Approved 8,583	PITRESSIN

PubMed

Show entries

Title	Date	PubMed
Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.	1998 Dec	9884074
Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women.	1999 Oct	10519430
Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.	2000 Oct	11012895
[1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors.	2002 Dec	12446593

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Patents

Sample Use Guides

In Vivo Use Guide

For treatment of diabetes insipidus: A dose of 0.25ml to 1ml (5 to 20 units) by subcutaneous or intramuscular injection every four hours. For the initial control of variceal bleeding Argipressin should be given intravenously. Argipressin, 20 units diluted in 100ml dextrose 5% w/v may be infused over a 15 minute period.

Route of Administration: Other

In Vitro Use Guide

Agonist activity of compound at the human vasopressin V1aR was determined in a reporter gene assays (RGA) in HEK293 cells by transiently cotransfecting recombinant vasopressin V1aR expression vectors and the reporter plasmid containing a luciferase gene under the control of NFAT response elements (NFAT-luciferase). Argipressin activates V1aR with EC50 of 0.24 nM.