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Conivaptan information


Conivaptan
Skeletal formula of conivaptan
Space-filling model of conivaptan
Clinical data
Trade namesVaprisol
Other namesYM 087
AHFS/Drugs.comMonograph
License data
  • US DailyMed: Conivaptan
Routes of
administration
Intravenous
ATC code
  • C03XA02 (WHO)
Legal status
Legal status
  • US: ℞-only
Pharmacokinetic data
BioavailabilityN/A
Identifiers
IUPAC name
  • N-(4-((4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin- 6(1H)-yl)carbonyl)phenyl)- (1,1'-biphenyl)-2-carboxamide
CAS Number
  • 210101-16-9 checkY
PubChem CID
  • 151171
IUPHAR/BPS
  • 2203
DrugBank
  • DB00872 checkY
ChemSpider
  • 133239 checkY
UNII
  • 0NJ98Y462X
KEGG
  • D01236 ☒N
ChEBI
  • CHEBI:681850 checkY
ChEMBL
  • ChEMBL1755 checkY
CompTox Dashboard (EPA)
  • DTXSID80175220 Edit this at Wikidata
Chemical and physical data
FormulaC32H26N4O2
Molar mass498.586 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • c1ccccc1-c2ccccc2C(=O)Nc3ccc(cc3)C(=O)N4c5ccccc5-c6[nH]c(C)nc6CC4
InChI
  • InChI=1S/C32H26N4O2/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37) checkY
  • Key:IKENVDNFQMCRTR-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Conivaptan, sold under the brand name Vaprisol, is a non-peptide inhibitor of the receptor for anti-diuretic hormone, also called vasopressin. It was approved in 2004 for hyponatremia (low blood sodium levels). The compound was discovered by Astellas and marked in 2006. The drug is now marketed by Cumberland Pharmaceuticals, 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 American Food and Drug Administration 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]

  1. ^ 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.

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Conivaptan

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Conivaptan, sold under the brand name Vaprisol, is a non-peptide inhibitor of the receptor for anti-diuretic hormone, also called vasopressin. It was approved...

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Aquaretic

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receptor antagonists and include conivaptan, tolvaptan, demeclocycline, and mozavaptan (OPC-31260), as well as lithium. Conivaptan hydrochloride and tolvaptan...

Word Count : 208

Vasopressin receptor antagonist

Last Update:

clinical use or in clinical trials as of 2009. Unselective (mixed V1A/V2) Conivaptan V1A selective (V1RA) Relcovaptan V1B selective (V3RA) Nelivaptan V2 selective...

Word Count : 1059

Mozavaptan

Last Update:

(November 20, 2006). "Neue Wirkstoffe - Conivaptan". Österreichische Apothekerzeitung (in German) (24/2006). "Conivaptan hydrochloride". Molecule of the Month...

Word Count : 72

Hyponatremia

Last Update:

tentative evidence that vasopressin receptor antagonists (vaptans), such as conivaptan, may be slightly more effective than fluid restriction in those with high...

Word Count : 4313

Heart failure

Last Update:

Vasopressin receptor antagonists can also be used to treat heart failure. Conivaptan is the first medication approved by US Food and Drug Administration for...

Word Count : 15556

Vasopressin

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 3871

Diuretic

Last Update:

Selective vasopressin V2 antagonist (sometimes called aquaretics) tolvaptan, conivaptan Competitive vasopressin antagonism leads to decreased number of aquaporin...

Word Count : 2001

Desmopressin

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 1518

Oxytocin receptor agonist

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 264

Vasopressin receptor

Last Update:

receptor antagonists include the new class of "vaptan drugs" such as conivaptan, tolvaptan, mozavaptan, lixivaptan, satavaptan etc. Holmes CL, Landry...

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Atosiban

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 1724

Tolvaptan

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 763

Oxytocin

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 11649

Astellas Pharma

Last Update:

pancreatic cancer – marketed with Hoffmann-La Roche (Genentech). Vaprisol (conivaptan) – Hyponatremia Veozah (fezolinetant) - Hot Flashes (vasomotor symptoms)...

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CYP3A4

Last Update:

amiodarone (class III antiarrhythmic), aprepitant, (antiemetic) ciprofloxacin, conivaptan, crizotinib, rutin (in vitro) (dietary flavonoid), tofisopam, some calcium...

Word Count : 7814

Daridorexant

Last Update:

daridorexant include the strong CYP3A4 inhibitors boceprevir, clarithromycin, conivaptan, indinavir, itraconazole, ketoconazole, lopinavir, nefazodone, nelfinavir...

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Lithium carbonate

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 2641

Suvorexant

Last Update:

suvorexant include the strong CYP3A4 inhibitors boceprevir, clarithromycin, conivaptan, indinavir, itraconazole, ketoconazole, lopinavir, nefazodone, nelfinavir...

Word Count : 8958

Syndrome of inappropriate antidiuretic hormone secretion

Last Update:

cirrhosis to avoid initiation or potentiation of hepatic encephalopathy. Conivaptan – an antagonist of both V1A and V2 vasopressin receptors. Tolvaptan –...

Word Count : 4047

Primary polydipsia

Last Update:

sympatholytic beta blocker Vasopressin receptor antagonists, such as conivaptan Acetazolamide, a carbonic anhydrase inhibitor Lithium was previously used...

Word Count : 3024

Hypotonic hyponatremia

Last Update:

also be treated with specific antagonists of the ADH receptors, such as conivaptan or tolvaptan. Another cause is psychogenic polydipsia. A third group of...

Word Count : 750

Terlipressin

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 584

Uterotonic

Last Update:

(argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Balovaptan Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LIT-001 LY-307174 PF-184563 Relcovaptan...

Word Count : 2321

Bellergal

Last Update:

avoided when prescribing. Moderate CYP3A4 inhibitors such as berotralstat, conivaptan, crizotinib, diltiazem, dronedarone, duvelisib, fedratinib, fluconazole...

Word Count : 936

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