TERLIPRESSIN

Possibly Marketed Outside US

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252 | http://www.nps.org.au/__data/cmi_pdfs/CMR10462.pdf

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

Targets

Primary Target	Pharmacology	Potency
Vasopressin V1a receptor 16 Target ID: P37288 Gene ID: 552.0 Gene Symbol: AVPR1A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252	Partial Agonist 288	852.0 nM [Ki]
Vasopressin V1b receptor 6 Target ID: P47901 Gene ID: 553.0 Gene Symbol: AVPR1B Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252	Agonist 2662	1115.0 nM [Ki]
Vasopressin V2 receptor 15 Target ID: P30518 Gene ID: 554.0 Gene Symbol: AVPR2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252	Agonist 2662	1580.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hepatorenal syndrome, type 1 3 Sources: https://www.old.health.gov.il/units/pharmacy/trufot/alonim/Glypressin_dr_1293447055647.pdf	Primary		Approved 8360	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).
Bleeding oesophageal varices 3 Sources: https://www.old.health.gov.il/units/pharmacy/trufot/alonim/Glypressin_dr_1293447055647.pdf	Primary		Approved 8360	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

Title	Date	PubMed
Update on treatment of variceal hemorrhage.	2002	12566616
Management of acute variceal bleeding.	2003	12837994
[Drug therapy of portal hypertension].	2003 Apr	12793061
Terlipressin and albumin for the hepatorenal syndrome.	2003 Apr	12668990
Comparison of Doppler ultrasonography and the hepatic venous pressure gradient in assessing portal hypertension in liver cirrhosis.	2003 Apr	12653891
Terlipressin plus hydroxyethyl starch infusion: an effective treatment for hepatorenal syndrome.	2003 Aug	12867805
Review article: the management of acute variceal bleeding.	2003 Aug 1	12895210
Terlipressin and albumin combination treatment in hepatorenal syndrome.	2003 Dec	15244209
Portal hypertensive bleeding.	2003 Dec	14696298
Effects of the V1a vasopressin agonist F-180 on portal hypertension-related bleeding in portal hypertensive rats.	2003 Dec	14647048
Terlipressin dose response in healthy and endotoxemic sheep: impact on cardiopulmonary performance and global oxygen transport.	2003 Feb	12594590
Beneficial effects of terlipressin in hepatorenal syndrome: a prospective, randomized placebo-controlled clinical trial.	2003 Feb	12542598
Acute renal failure in patients with cirrhosis: perspectives in the age of MELD.	2003 Feb	12540770
Patient with a sudden drop in blood pressure.	2003 Jan	12545047
Low-dose terlipressin improves systemic and splanchnic hemodynamics in fluid-challenged endotoxic rats.	2003 Jan	12545018
Hepatorenal syndrome.	2003 Jan-Mar	15094702
[Vasodilatory septic shock refractory to catecholamines: is there a role for terlipressin?].	2003 Jul	12946495
Is spontaneous bacterial peritonitis an inducer of vasopressin analogue side-effects? A case report.	2003 Jul	12870738
When endoscopic therapy or pharmacotherapy fails to control variceal bleeding: what should be done? Immediate control of bleeding by TIPS?	2003 Jul	12728322
Cyclooxygenase expression in splanchnic hyposensitivity to glypressin of bleeding portal hypertensive rats.	2003 Jun	12795648
Terlipressin versus norepinephrine to correct refractory arterial hypotension after general anesthesia in patients chronically treated with renin-angiotensin system inhibitors.	2003 Jun	12766641
[Acute upper gastrointestinal hemorrhage. Diagnosis and management].	2003 May	12966782
Emergency sclerotherapy versus vasoactive drugs for variceal bleeding in cirrhosis: a Cochrane meta-analysis.	2003 May	12730868
Comment on "Terlipressin in chronic hyperdynamic endotoxic shock: is it safe?" by P. Asfar.	2003 May	12655391
Terlipressin infusion in catecholamine-resistant shock.	2003 Oct	14601280
[Vasoconstrictive Therapies for Bleeding Esophageal Varices and their Mechanisms of Action].	2003 Oct	14562199
[Vasopressin and its analogues in the therapy of shock].	2004	15305765
Vasopressors for shock.	2004	15266497
[Acute upper gastrointestinal variceal bleeding: vasoactive agents].	2004 Apr	15150493
Effects of terlipressin on systemic and regional haemodynamics in catecholamine-treated hyperkinetic septic shock.	2004 Apr	14673520
Effects of terlipressin on systolic pulmonary artery pressure of patients with liver cirrhosis: an echocardiographic assessment.	2004 Aug 1	15259082
Somatostatin, somatostatin analogues and other vasoactive drugs in the treatment of bleeding oesophageal varices.	2004 Feb	15077917
Medical management of variceal bleeding in patients with cirrhosis.	2004 Feb	14997222
Science Review: Vasopressin and the cardiovascular system part 2 - clinical physiology.	2004 Feb	14975041
Worsening of cerebral hyperemia by the administration of terlipressin in acute liver failure with severe encephalopathy.	2004 Feb	14768000
Terlipressin and gelafundin: safe therapy of hepatorenal syndrome.	2004 Feb 27	15090293
Systemic, portal and renal effects of terlipressin in patients with cirrhotic ascites: pilot study.	2004 Jan	14675246
Effects of treatment of hepatorenal syndrome before transplantation on posttransplantation outcome. A case-control study.	2004 Jan	14672625
Role of vasopressin in the management of septic shock.	2004 Jul	15103461
Pressure or flow?	2004 Jun	15264750
Clinical review: influence of vasoactive and other therapies on intestinal and hepatic circulations in patients with septic shock.	2004 Jun	15153235
Terlipressin for cerebral perfusion pressure support in a patient with septic shock.	2004 Jun	15144312
[Refractory hypotension during anesthesia in a patient treated with angiotensin receptor blockers].	2004 Jun-Jul	15303535
A long-acting vasopressin analog for septic shock: brilliant idea or dangerous folly?	2004 Mar	15080105
Terlipressin as rescue therapy for intractable hypotension during neonatal septic shock.	2004 Mar	14987339
Terlipressin bolus induces systemic vasoconstriction in septic shock.	2004 Mar	14987338
Terlipressin for catecholamine-resistant septic shock in children.	2004 Mar	14767584
Effect of terlipressin on blood volume distribution in patients with cirrhosis.	2004 May	15180188
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	15082350
Terlipressin in patients with septic shock: friend or foe?	2004 May	15048551

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 `Thu Jul 06 06:57:29 UTC 2023` Edited by `admin` on `Thu Jul 06 06:57:29 UTC 2023`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	7Z5X49W53P
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TERLIPRESSIN

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