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

Stem definitionDrug idCAS RN
vasoconstrictors, vasopressin derivatives 2967 14636-12-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • terlipressin
  • glycylpressin
  • glypressin
  • remestyp
  • Triglycyl-8-lysine-vasopressin
An inactive peptide prodrug that is slowly converted in the body to lypressin. It is used to control bleeding of ESOPHAGEAL VARICES and for the treatment of HEPATORENAL SYNDROME.
  • Molecular weight: 1227.38
  • Formula: C52H74N16O15S2
  • CLOGP: -4.07
  • LIPINSKI: 3
  • HAC: 31
  • HDO: 16
  • TPSA: 512.85
  • ALOGS: -3.87
  • ROTB: 25

Drug dosage:

DoseUnitRoute
12 mg P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.24 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.20 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC H01BA04 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
POSTERIOR PITUITARY LOBE HORMONES
Vasopressin and analogues
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014662 Vasoconstrictor Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.65 acidic
pKa2 11.89 acidic
pKa3 12.32 acidic
pKa4 12.71 acidic
pKa5 12.98 acidic
pKa6 13.08 acidic
pKa7 13.57 acidic
pKa8 13.58 acidic
pKa9 13.67 acidic
pKa10 13.96 acidic
pKa11 10.31 Basic
pKa12 7.93 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D000077585 MESH_DESCRIPTOR_UI
C0145185 UMLSCUI
D06672 KEGG_DRUG
325927008 SNOMEDCT_US
004053 NDDF
57048 RXNORM
395899009 SNOMEDCT_US
7Z5X49W53P UNII
5114 INN_ID
DB02638 DRUGBANK_ID
CHEBI:135905 CHEBI
CHEMBL2135460 ChEMBL_ID
72081 PUBCHEM_CID

Pharmaceutical products:

None