Conivaptan

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Conivaptan
Systematic (IUPAC) name
N-(4-(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-
6(1H)-yl)carbonyl)phenyl)-
(1,1'-biphenyl)-2-carboxamide
Identifiers
CAS number 210101-16-9
ATC code C03XA02
PubChem 151171
Chemical data
Formula C32H26N4O2 
Mol. mass 498.583
Pharmacokinetic data
Bioavailability N/A
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes iv

Conivaptan (vaprisol, YM 087) is a non-peptide inhibitor of antidiuretic hormone (vasopressin). 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 both isotypes 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.[1]

[edit] See also