Conivaptan

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Conivaptan
Skeletal formula of conivaptan
Space-filling model of 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
Clinical data
Trade names Vaprisol
AHFS/Drugs.com monograph
Pregnancy cat. C (US)
Legal status -only (US)
Routes intravenous
Pharmacokinetic data
Bioavailability N/A
Identifiers
CAS number 210101-16-9 YesY
ATC code C03XA02
PubChem CID 151171
IUPHAR ligand 2203
DrugBank DB00872
ChemSpider 133239 YesY
UNII 0NJ98Y462X YesY
KEGG D01236 N
ChEBI CHEBI:681850 YesY
ChEMBL CHEMBL1755 YesY
Chemical data
Formula C32H26N4O2 
Mol. mass 498.583
 N (what is this?)  (verify)

Conivaptan (YM 087, brand name Vaprisol) 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.[1]

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