Conivaptan

Conivaptan
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
AHFS/Drugs.com monograph
Pregnancy cat.  ?
Legal status  ?
Routes intravenous
Pharmacokinetic data
Bioavailability N/A
Identifiers
CAS number 210101-16-9
ATC code C03XA02 [1]
PubChem CID 151171
DrugBank DB00872
ChemSpider 133239 YesY
UNII 0NJ98Y462X YesY
KEGG D01236
ChEBI CHEBI:681850 YesY
ChEMBL CHEMBL1755 YesY
Chemical data
Formula C32H26N4O2 
Mol. mass 498.583
SMILES eMolecules & PubChem
 YesY(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.[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. Archived from the original on 2008-05-06. http://web.archive.org/web/20080506023243/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. 
v · d · eAntihypertensives: diuretics (C03)
Sulfonamides
(except EA)
CA inhibitors (at PT)
Thiazide-likes (primarily DCT)
Potassium-sparing (at CD)
ESC blockers
Osmotic diuretics (PT, DL)
VAs (DCT and CD)

vaptans: Conivaptan • Mozavaptan • Satavaptan • Tolvaptan

tetracyclines: Demeclocycline
Other
#WHO-EM. ‡Withdrawn from market. Clinical trials: †Phase III. §Never to phase III

M: VAS

anat(a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot

noco/syva/cong/lyvd/tumr, sysi/epon, injr

proc, drug(C2s+n/3/4/5/7/8/9)
v · d · eHypothalamic-pituitary hormones and analogues (H01)
Hypothalamic
Agonists: Gonadorelin • Nafarelin • Histrelin
Antagonists: Cetrorelix • Ganirelix
Agonists: Lanreotide • Octreotide
Anterior pituitary
Agonists: Corticotropin • Cosyntropin • Tetracosactide
Agonists: Thyrotropin
Posterior pituitary
Agonists: Carbetocin • Demoxytocin
Antagonists: Atosiban
Agonists: Argipressin • Desmopressin • Felypressin • Lypressin • Ornipressin • Terlipressin
Antagonists: Conivaptan • Demeclocycline • Lixivaptan • Mozavaptan • Nelivaptan • Relcovaptan • Satavaptan • Tolvaptan

M: END

anat/phys/devp/horm

noco(d)/cong/tumr, sysi/epon

proc, drug (A10/H1/H2/H3/H5)
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