Vasopressin receptor antagonist
Encyclopedia
A vasopressin receptor antagonist is an agent which interferes with action at the vasopressin receptor
s. They can be used in the treatment of hyponatremia
, especially in patients with congestive heart failure
or liver cirrhosis
.
, a tetracycline antibiotic, is sometimes used to block the action of vasopressin in the kidney in hyponatremia due to inappropriately high secretion of vasopressin (SIADH
), when fluid restriction has failed.
s (V1A
, V1B
and V2
). These receptors have a variety of functions, with the V1A and V2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V1A and V1B receptors are expressed in the central nervous system. V1A is expressed in many regions of the brain, and has been linked to a variety of social behaviors in humans and animals.
The vaptan class of drugs contains a number of compounds with varying selectivity, several of which are either already in clinical use or in clinical trials as of 2009.
Unselective (mixed V1A/V2)
V1A selective
V1B selective
V2 selective
Vasopressin receptor
A vasopressin receptor is a cell surface receptor which binds vasopressin. The three types of vasopressin receptor are members of the A6 subfamily of G-protein coupled receptors.-Subtypes:Humans express three subtypes: 1A, 1B and 2-Function:...
s. They can be used in the treatment of hyponatremia
Hyponatremia
Hyponatremia is an electrolyte disturbance in which the sodium concentration in the serum is lower than normal. In the vast majority of cases, hyponatremia occurs as a result of excess body water diluting the serum sodium and is not due to sodium deficiency. Sodium is the dominant extracellular...
, especially in patients with congestive heart failure
Congestive heart failure
Heart failure often called congestive heart failure is generally defined as the inability of the heart to supply sufficient blood flow to meet the needs of the body. Heart failure can cause a number of symptoms including shortness of breath, leg swelling, and exercise intolerance. The condition...
or liver cirrhosis
Cirrhosis
Cirrhosis is a consequence of chronic liver disease characterized by replacement of liver tissue by fibrosis, scar tissue and regenerative nodules , leading to loss of liver function...
.
Tetracyclines
DemeclocyclineDemeclocycline
Demeclocycline is a tetracycline antibiotic.It is derived from a strain of Streptomyces aureofaciens.-In infections:...
, a tetracycline antibiotic, is sometimes used to block the action of vasopressin in the kidney in hyponatremia due to inappropriately high secretion of vasopressin (SIADH
Syndrome of inappropriate antidiuretic hormone
The syndrome of inappropriate antidiuretic hormone hypersecretion is characterized by excessive release of antidiuretic hormone from the posterior pituitary gland or another source. The result is hyponatremia and sometimes fluid overload...
), when fluid restriction has failed.
Vaptans
A class of medication, the "vaptan" drugs, act by inhibiting the action of vasopressin on its receptorReceptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
s (V1A
Arginine vasopressin receptor 1A
Arginine vasopressin receptor 1A is one of the three major receptor types for arginine vasopressin , and is present throughout the brain, as well as in the periphery in the liver, kidney, and vasculature.Arginine vasopressin receptor 1A is also known as:* V1a vasopressin receptor* antidiuretic...
, V1B
Arginine vasopressin receptor 1B
Arginine vasopressin receptor 1B is a protein that acts as receptor for arginine vasopressin. AVPR1B belongs to the subfamily of G-protein coupled receptors...
and V2
Arginine vasopressin receptor 2
Arginine vasopressin receptor 2 is a protein that acts as receptor for arginine vasopressin. AVPR2 belongs to the subfamily of G-protein-coupled receptors...
). These receptors have a variety of functions, with the V1A and V2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V1A and V1B receptors are expressed in the central nervous system. V1A is expressed in many regions of the brain, and has been linked to a variety of social behaviors in humans and animals.
The vaptan class of drugs contains a number of compounds with varying selectivity, several of which are either already in clinical use or in clinical trials as of 2009.
Unselective (mixed V1A/V2)
- ConivaptanConivaptanConivaptan is a non-peptide inhibitor of antidiuretic hormone . It was approved in 2004 for hyponatremia caused by syndrome of inappropriate antidiuretic hormone , and there is some evidence it may be effective in heart failure...
V1A selective
- RelcovaptanRelcovaptanRelcovaptan is a non-peptide vasopressin receptor antagonist, selective for the V1a subtype. It has shown positive initial results in tests against Raynaud's disease, dysmenorrhoea, and tocolysis, although it is not yet approved for clinical use.-References:...
V1B selective
- Nelivaptan
V2 selective
- LixivaptanLixivaptanLixivaptan is a phase III pharmaceutical being developed by Cardiokine, Inc., a specialty pharmaceutical company based in Philadelphia, PA, focused on the development of pharmaceuticals for the treatment and prevention of cardiovascular diseases...
- MozavaptanMozavaptanMozavaptan is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia caused by syndrome of inappropriate antidiuretic hormone due to ADH producing tumors....
- SatavaptanSatavaptanSatavaptan is a vasopressin-2 receptor antagonist undergoing research for the treatment of hyponatremia. It is also being studied for the treatment of ascites....
- TolvaptanTolvaptanTolvaptan , also known as OPC-41061, is a selective, competitive vasopressin receptor 2 antagonist used to treat hyponatremia associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone . Tolvaptan was approved by the U.S...