Conivaptan
Encyclopedia
Conivaptan is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist
). It was approved in 2004 for hyponatremia
(low blood sodium
levels) caused by syndrome of inappropriate antidiuretic hormone
(SIADH), and there is some evidence it may be effective in heart failure. It is marketed by Astellas Pharma Inc
.
Conivaptan inhibits two of the three subtypes of the vasopressin receptor
(V1a
and V2
). Effectively, it causes iatrogenic nephrogenic diabetes insipidus
.
Conivaptan has not been approved by the FDA for the treatment of decompensated congestive heart failure. However, in theory, vasopressin receptor antagonism would be particularly useful in this setting, and an initial study shows that it has some promise.
Vasopressin receptor antagonist
A vasopressin receptor antagonist is an agent which interferes with action at the vasopressin receptors. They can be used in the treatment of hyponatremia, especially in patients with congestive heart failure or liver cirrhosis.-Tetracyclines:...
). It was approved in 2004 for 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...
(low blood sodium
Sodium
Sodium is a chemical element with the symbol Na and atomic number 11. It is a soft, silvery-white, highly reactive metal and is a member of the alkali metals; its only stable isotope is 23Na. It is an abundant element that exists in numerous minerals, most commonly as sodium chloride...
levels) caused by syndrome of inappropriate antidiuretic hormone
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...
(SIADH), and there is some evidence it may be effective in heart failure. It is marketed by Astellas Pharma Inc
Astellas Pharma
is a Japanese pharmaceutical company, formed on 1 April 2005 from the merger of and .Astellas' franchise areas are urology, immunology , dermatology, cardiology, and infectious disease...
.
Conivaptan inhibits two of the three subtypes of the vasopressin receptor
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:...
(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...
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...
). Effectively, it causes iatrogenic nephrogenic diabetes insipidus
Diabetes insipidus
Diabetes insipidus is a condition characterized by excessive thirst and excretion of large amounts of severely diluted urine, with reduction of fluid intake having no effect on the concentration of the urine. There are several different types of DI, each with a different cause...
.
Conivaptan has not been approved by the FDA for the treatment of decompensated congestive heart failure. However, in theory, vasopressin receptor antagonism would be particularly useful in this setting, and an initial study shows that it has some promise.