U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Description

Terlipressin (Glypressin) is indicated for the treatment of bleeding oesophageal varices and in some countries for the treatment of hepato-renal syndrome type 1. It is a prodrug and is converted to the lysine vasopressin in the circulation after the N-triglycyl residue is cleaved by endothelial peptidases. This results in a ‘slow release’ of the vasoactive lysine vasopressin. Terlipressin exerts its action by activating V1a, V1b and V2 vasopressin receptors.

Approval Year

Unknown
127998
Targets

Targets

Primary TargetPharmacologyConditionPotency
Vasopressin V1a receptor
16
Target ID: P37288
Gene ID: 552.0
Gene Symbol: AVPR1A
Target Organism: Homo sapiens (Human)
Partial Agonist
283
 852.0 nM [Ki]
Vasopressin V1b receptor
6
Target ID: P47901
Gene ID: 553.0
Gene Symbol: AVPR1B
Target Organism: Homo sapiens (Human)
Agonist
2637
 1115.0 nM [Ki]
Vasopressin V2 receptor
15
Target ID: P30518
Gene ID: 554.0
Gene Symbol: AVPR2
Target Organism: Homo sapiens (Human)
Agonist
2637
 1580.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8307
GLYPRESSIN

Approved Use

GLYPRESSIN is used to treat Bleeding Oesophageal Varices (BOV), bleeding veins in the lower end of the food-pipe in people with serious liver disease. GLYPRESSIN is also used to treat hepatorenal syndrome, type 1 (HRS-1).
Primary
Approved
8307
GLYPRESSIN

Approved Use

GLYPRESSIN is used to treat Bleeding Oesophageal Varices (BOV), bleeding veins in the lower end of the food-pipe in people with serious liver disease. GLYPRESSIN is also used to treat hepatorenal syndrome, type 1 (HRS-1).
PubMed

PubMed

TitleDatePubMed
European Society of Intensive Care Medicine 14th annual congress, 30 September-3 October 2001, Geneva, Switzerland.
2001 Dec
Life, death, and varices.
2001 Nov
Terlipressin in patients with cirrhosis and type 1 hepatorenal syndrome: a retrospective multicenter study.
2002 Apr
Update on ascites and hepatorenal syndrome.
2002 Aug
Renal failure in cirrhotic patients: role of terlipressin in clinical approach to hepatorenal syndrome type 2.
2002 Dec
Terlipressin-induced vasoconstriction reversed with N-acetylcysteine: a case for combined use in hepatorenal syndrome?
2002 Dec
Effect of terlipressin (Glypressin) on hepatorenal syndrome in cirrhotic patients: results of a multicentre pilot study.
2002 Feb
Double-blind randomized, comparative multicenter study of the effect of terlipressin in the treatment of acute esophageal variceal and/or hypertensive gastropathy bleeding.
2002 Jul-Aug
Terlipressin inhibits in vivo aortic iNOS expression induced by lipopolysaccharide in rats with biliary cirrhosis.
2002 Nov
Terlipressin and arterial blood volume after paracentesis for tense ascites in cirrhosis.
2002 Nov
Terlipressin therapy with and without albumin for patients with hepatorenal syndrome: results of a prospective, nonrandomized study.
2002 Oct
Terlipressin for haemodynamic support in septic patients: a double-edged sword?
2002 Oct 19
[Comparison of Doppler ultrasonography and hepatic venous pressure gradient in assessing portal hypertension in liver cirrhosis].
2002 Sep
Management of acute variceal bleeding.
2003
[Drug therapy of portal hypertension].
2003 Apr
Terlipressin and albumin for the hepatorenal syndrome.
2003 Apr
Comparison of Doppler ultrasonography and the hepatic venous pressure gradient in assessing portal hypertension in liver cirrhosis.
2003 Apr
Terlipressin and albumin combination treatment in hepatorenal syndrome.
2003 Dec
Portal hypertensive bleeding.
2003 Dec
Effects of the V1a vasopressin agonist F-180 on portal hypertension-related bleeding in portal hypertensive rats.
2003 Dec
Terlipressin in chronic hyperdynamic endotoxic shock: is it safe?
2003 Feb
[Hepatorenal syndrome: from physiopathology to treatment].
2003 Jan
Patient with a sudden drop in blood pressure.
2003 Jan
Low-dose terlipressin improves systemic and splanchnic hemodynamics in fluid-challenged endotoxic rats.
2003 Jan
Systematic review: terlipressin in acute oesophageal variceal haemorrhage.
2003 Jan
Hepatorenal syndrome.
2003 Jan-Mar
When endoscopic therapy or pharmacotherapy fails to control variceal bleeding: what should be done? Immediate control of bleeding by TIPS?
2003 Jul
Cyclooxygenase expression in splanchnic hyposensitivity to glypressin of bleeding portal hypertensive rats.
2003 Jun
Terlipressin versus norepinephrine to correct refractory arterial hypotension after general anesthesia in patients chronically treated with renin-angiotensin system inhibitors.
2003 Jun
Emergency sclerotherapy versus vasoactive drugs for variceal bleeding in cirrhosis: a Cochrane meta-analysis.
2003 May
Comment on "Terlipressin in chronic hyperdynamic endotoxic shock: is it safe?" by P. Asfar.
2003 May
Terlipressin infusion in catecholamine-resistant shock.
2003 Oct
[Vasopressin and its analogues in the therapy of shock].
2004
Vasopressors for shock.
2004
[Acute upper gastrointestinal variceal bleeding: vasoactive agents].
2004 Apr
Effects of terlipressin on systemic and regional haemodynamics in catecholamine-treated hyperkinetic septic shock.
2004 Apr
Effects of terlipressin on systolic pulmonary artery pressure of patients with liver cirrhosis: an echocardiographic assessment.
2004 Aug 1
Somatostatin, somatostatin analogues and other vasoactive drugs in the treatment of bleeding oesophageal varices.
2004 Feb
Terlipressin and gelafundin: safe therapy of hepatorenal syndrome.
2004 Feb 27
Effects of treatment of hepatorenal syndrome before transplantation on posttransplantation outcome. A case-control study.
2004 Jan
Role of vasopressin in the management of septic shock.
2004 Jul
Pressure or flow?
2004 Jun
Clinical review: influence of vasoactive and other therapies on intestinal and hepatic circulations in patients with septic shock.
2004 Jun
Terlipressin for cerebral perfusion pressure support in a patient with septic shock.
2004 Jun
[Refractory hypotension during anesthesia in a patient treated with angiotensin receptor blockers].
2004 Jun-Jul
A long-acting vasopressin analog for septic shock: brilliant idea or dangerous folly?
2004 Mar
Terlipressin for catecholamine-resistant septic shock in children.
2004 Mar
Effect of terlipressin on blood volume distribution in patients with cirrhosis.
2004 May
A prospective double blind randomized study comparing the need for blood transfusion with terlipressin or a placebo during early excision and grafting of burns.
2004 May
Terlipressin in patients with septic shock: friend or foe?
2004 May

Sample Use Guides

In Vivo Use Guide
The maximum dose is 1.7 mg given every 4 hours for up tp 48 hours (bleeding oesophageal varices) or every 6 hours for up to 2 weeks (hepatorenal syndrome, type 1).
Route of Administration: Intravenous
In Vitro Use Guide
Isolated perfused mesenteric arteries of portal vein ligated and sham-operated rats were contracted by methoxamine (3 nmol-3 mumol) and then treated with nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester (100 microM), terlipressin or the selective V2 receptor agonist desmopressin (each 0.5 uM). Terlipressin alone reduced and in combination with NG-nitro-L-arginine methyl ester abolished the difference in reactivity to methoxamine between the portal vein ligated and sham-operated groups.
Substance Class Protein
Created
by admin
on Sat Dec 17 10:43:46 UTC 2022
Edited
by admin
on Sat Dec 17 10:43:46 UTC 2022
Protein Sub Type
Sequence Type COMPLETE
Record UNII
7Z5X49W53P
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TERLIPRESSIN
DASH   INN   MART.   MI   USAN   WHO-DD  
USAN   INN  
Official Name English
GLY-GLY-GLY-CYS-TYR-PHE-GLN-ASN-CYS-PRO-LYS-GLY-NH2 (4-9 DISULFIDE)
Common Name English
Terlipressin [WHO-DD]
Common Name English
terlipressin [INN]
Common Name English
GLYCYLPRESSIN
Common Name English
N-(N-(N-GLYCYLGLYCYL)GLYCYL)-8-L-LYSINEVASOPRESSIN
Common Name English
TERLIPRESSIN [MART.]
Common Name English
TERLIPRESSIN [USAN]
Common Name English
TERLIPRESSIN [MI]
Common Name English
GLYCYLGLYCYLGLYCYL(8-L-LYSINE)VASOPRESSIN
Common Name English
TERLIPRESSIN [EP MONOGRAPH]
Common Name English
VASOPRESSIN, N-(GLYCYLGLYCYLGLYCYL)-8-L-LYSINE-
Common Name English
GLYPRESSIN
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 580417
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
FDA ORPHAN DRUG 534216
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
FDA ORPHAN DRUG 11785
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
WHO-VATC QH01BA04
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
FDA ORPHAN DRUG 191804
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
WHO-ATC H01BA04
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
NCI_THESAURUS C80212
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
Code System Code Type Description
ChEMBL
CHEMBL2135460
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
DAILYMED
7Z5X49W53P
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
WIKIPEDIA
TERLIPRESSIN
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
FDA UNII
7Z5X49W53P
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
ECHA (EC/EINECS)
238-680-8
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
NCI_THESAURUS
C77387
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
RXCUI
57048
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY RxNorm
CAS
14636-12-5
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
USAN
SS-34
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
MERCK INDEX
M10580
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY Merck Index
MESH
C012078
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
EVMPD
SUB10927MIG
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
EPA CompTox
DTXSID7048952
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
DRUG CENTRAL
2967
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
INN
5114
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
PUBCHEM
72081
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
DRUG BANK
DB02638
Created by admin on Sat Dec 17 10:43:46 UTC 2022 , Edited by admin on Sat Dec 17 10:43:46 UTC 2022
PRIMARY
Related Record Type Details
TERLIPRESSIN ACETATE
SALT/SOLVATE -> PARENT
Related Record Type Details
LYPRESSIN
METABOLITE ACTIVE -> PARENT
Believed to behave as a prodrug
IN-VIVO
PLASMA
LYPRESSIN
METABOLITE ACTIVE -> PARENT
IN-VIVO
PLASMA
Related Record Type Details
TERLIPRESSIN
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:SEQUENCE(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966