conivaptan ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasopressin receptor antagonists 732 168626-94-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • conivaptan
  • conivaptan hydrochloride
  • vaprisol
  • YM-087
  • conivaptan HCl
  • Molecular weight: 498.59
  • Formula: C32H26N4O2
  • CLOGP: 5
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 78.09
  • ALOGS: -5.45
  • ROTB: 4

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.15 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.15 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 42 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.76 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 6.70 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 2005 FDA CUMBERLAND PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03XA02 CARDIOVASCULAR SYSTEM
DIURETICS
OTHER DIURETICS
Vasopressin antagonists
FDA MoA N0000020044 Vasopressin Receptor Antagonists
MeSH PA D065092 Antidiuretic Hormone Receptor Antagonists
MeSH PA D045283 Natriuretic Agents
FDA EPC N0000178376 Vasopressin Receptor Antagonist
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
CHEBI has role CHEBI:59680 vasopressin receptor antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hyponatremia indication 89627008
Anuria contraindication 2472002 DOID:2983
Hypovolemia contraindication 28560003
Demyelination contraindication 32693004
Hypernatremia contraindication 39355002
Chronic heart failure contraindication 48447003
Acute nephropathy contraindication 58574008
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Osmotic Central Pontine Myelinolysis contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.9 acidic
pKa2 12.5 acidic
pKa3 6.37 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Vasopressin V1a receptor GPCR ANTAGONIST Ki 9.37 CHEMBL CHEMBL
Vasopressin V2 receptor GPCR ANTAGONIST Ki 9.44 CHEMBL CHEMBL
Oxytocin receptor GPCR Ki 7.35 CHEMBL
Vasopressin V2 receptor GPCR Ki 8.52 CHEMBL
Vasopressin V1a receptor GPCR Ki 9.32 CHEMBL

External reference:

IDSource
4025087 VUID
N0000175346 NUI
D01236 KEGG_DRUG
1294548 RXNORM
4025087 VANDF
4025088 VANDF
C0966107 UMLSCUI
CHEBI:681850 CHEBI
CHEMBL1755 ChEMBL_ID
CHEMBL1201108 ChEMBL_ID
DB00872 DRUGBANK_ID
C106389 MESH_SUPPLEMENTAL_RECORD_UI
151171 PUBCHEM_CID
2203 IUPHAR_LIGAND_ID
7947 INN_ID
0NJ98Y462X UNII
20826 MMSL
73959 MMSL
d05699 MMSL
011178 NDDF
011179 NDDF
421516006 SNOMEDCT_US
421858002 SNOMEDCT_US
425602003 SNOMEDCT_US
210101-16-9 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vaprisol HUMAN PRESCRIPTION DRUG LABEL 1 0469-1601 LIQUID 5 mg INTRAVENOUS NDA 23 sections
Vaprisol HUMAN PRESCRIPTION DRUG LABEL 1 0469-1602 SOLUTION 20 mg INTRAVENOUS NDA 23 sections
VAPRISOL DEXTROSE IN PLASTIC CONTAINER HUMAN PRESCRIPTION DRUG LABEL 1 66220-160 INJECTION, SOLUTION 20 mg INTRAVENOUS NDA 24 sections