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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 [1]
PubChem 151171
ChemSpider 133239
Chemical data
Formula C 32H26N4O2  
Mol. mass 498.583
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability N/A
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes intravenous
 Yes check.svgY(what is this?)  (verify)

Conivaptan (YM 087, brand name Vaprisol) 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 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.[2]

References

  1. ^ WHO International Working Group for Drug Statistics Methodology (August 27, 2008). "ATC/DDD Classification (FINAL): New ATC 5th level codes". WHO Collaborating Centre for Drug Statistics Methodology. http://www.whocc.no/atcddd/new_atc_ddd.html#ATCDDD_FINAL. Retrieved 2008-09-05.  
  2. ^ Udelson JE, Smith WB, Hendrix GH, et al. (November 2001). "Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure". Circulation 104 (20): 2417–23. doi:10.1161/hc4501.099313. PMID 11705818. http://circ.ahajournals.org/cgi/pmidlookup?view=long&pmid=11705818.  
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