vasopressin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasoconstrictors, vasopressin derivatives 2810 113-79-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vasopressin
  • 8-L-arginine vasopressin
  • synthetic vasopressin
  • 8-L-Arginine-vasopressin
  • argipressin
  • vasopressin tannate
  • vasopressin injection
  • antidiuretic hormone
  • pitressin tannate
  • Molecular weight: 1084.24
  • Formula: C46H65N15O12S2
  • CLOGP: -3.82
  • LIPINSKI: 3
  • HAC: 27
  • HDO: 15
  • TPSA: 461.43
  • ALOGS: -3.93
  • ROTB: 19

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 5 % Benet LZ, Broccatelli F, Oprea TI

Approvals:

DateAgencyCompanyOrphan
None FDA PARKE DAVIS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D050034 Antidiuretic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D003029 Coagulants
MeSH PA D006401 Hematologic Agents
MeSH PA D006490 Hemostatics
MeSH PA D045283 Natriuretic Agents
MeSH PA D014662 Vasoconstrictor Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Nocturnal enuresis indication 8009008
Hereditary factor VIII deficiency disease indication 28293008 DOID:12134
von Willebrand disorder indication 128105004 DOID:12531
Partial Central Diabetes Insipidus indication
Cardiac arrest off-label use 410429000 DOID:0060319
Uremic Bleeding Tendency off-label use
Chronic glomerulonephritis contraindication 20917003
Migraine contraindication 37796009 DOID:6364
Hypertensive disorder contraindication 38341003 DOID:10763
Uremia contraindication 44730006 DOID:4676
Heart failure contraindication 84114007 DOID:6000
Epilepsy contraindication 84757009 DOID:1826
Asthma contraindication 195967001 DOID:2841
Disorder of coronary artery contraindication 414024009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.65 acidic
pKa2 12.19 acidic
pKa3 12.56 acidic
pKa4 12.85 acidic
pKa5 13.19 acidic
pKa6 13.43 acidic
pKa7 13.76 acidic
pKa8 10.75 Basic
pKa9 6.4 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
200UNITS/10ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 Dec. 17, 2016 RX SOLUTION INTRAVENOUS 9375478 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 Dec. 17, 2016 RX SOLUTION INTRAVENOUS 9687526 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 Dec. 17, 2016 RX SOLUTION INTRAVENOUS 9744209 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 Dec. 17, 2016 RX SOLUTION INTRAVENOUS 9744239 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 Dec. 17, 2016 RX SOLUTION INTRAVENOUS 9937223 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 April 17, 2014 RX SOLUTION INTRAVENOUS 9375478 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 April 17, 2014 RX SOLUTION INTRAVENOUS 9687526 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 April 17, 2014 RX SOLUTION INTRAVENOUS 9744209 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/ML (20UNITS/ML) VASOSTRICT PAR STERILE PRODUCTS N204485 April 17, 2014 RX SOLUTION INTRAVENOUS 9744239 Jan. 30, 2035 TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Vasopressin V1b receptor GPCR AGONIST Ki 9.31 CHEMBL CHEMBL
Vasopressin V2 receptor GPCR AGONIST Ki 8.92 CHEMBL CHEMBL
Vasopressin V1a receptor GPCR AGONIST Ki 9.59 CHEMBL CHEMBL
Oxytocin receptor GPCR Ki 8.78 CHEMBL
Vasopressin V2 receptor GPCR Kd 8.82 CHEMBL
Vasopressin V1b receptor GPCR Ki 9.54 CHEMBL
Vasopressin V1a receptor GPCR Kd 9.19 CHEMBL
Vasopressin V1 receptor GPCR Kd 9.19 CHEMBL
Vasopressin V2 receptor GPCR IC50 8.48 CHEMBL
Oxytocin receptor GPCR Ki 8.93 CHEMBL
Vasopressin V2 receptor GPCR Ki 9.35 CHEMBL

External reference:

IDSource
4018654 VUID
N0000179795 NUI
C1705480 UMLSCUI
D00101 KEGG_DRUG
4R069M4O1P UNII
77671006 SNOMEDCT_US
772208008 SNOMEDCT_US
4018654 VANDF
11149 RXNORM
3144 MMSL
5667 MMSL
d00398 MMSL
002126 NDDF
002122 NDDF
CHEMBL373742 ChEMBL_ID
DB00067 DRUGBANK_ID
CHEBI:9937 CHEBI
1482 INN_ID
CHEMBL1201528 ChEMBL_ID
CHEMBL2108986 ChEMBL_ID
644077 PUBCHEM_CID
2168 IUPHAR_LIGAND_ID
C016671 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
VASOPRESSIN HUMAN PRESCRIPTION DRUG LABEL 1 52584-302 INJECTION, SOLUTION 20 [USP'U] INTRAMUSCULAR unapproved drug other 10 sections
Vasopressin HUMAN PRESCRIPTION DRUG LABEL 1 63323-302 INJECTION, SOLUTION 20 [USP'U] INTRAMUSCULAR unapproved drug other 11 sections