TERLIPRESSIN

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 17 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 290	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 2678	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 2678	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 8429	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 8429	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
Pharmacologic therapy for portal hypertension.	2001 Feb	11177691
[Physiopathology of refractory ascites and the hepatorenal syndrome].	2002	12107916
Management of esophageal varices.	2002	12055714
Increased plasma levels of neuropeptide Y in hepatorenal syndrome.	2002 Mar	11867178
Terlipressin therapy with and without albumin for patients with hepatorenal syndrome: results of a prospective, nonrandomized study.	2002 Oct	12297842
Terlipressin plus hydroxyethyl starch infusion: an effective treatment for hepatorenal syndrome.	2003 Aug	12867805
Terlipressin dose response in healthy and endotoxemic sheep: impact on cardiopulmonary performance and global oxygen transport.	2003 Feb	12594590
Successful resuscitation of serious bupivacaine intoxication in a patient with pre-existing heart failure.	2003 Jan	12514153
[Vasodilatory septic shock refractory to catecholamines: is there a role for terlipressin?].	2003 Jul	12946495
When endoscopic therapy or pharmacotherapy fails to control variceal bleeding: what should be done? Immediate control of bleeding by TIPS?	2003 Jul	12728322
Emergency sclerotherapy versus vasoactive drugs for variceal bleeding in cirrhosis: a Cochrane meta-analysis.	2003 May	12730868
Effects of terlipressin on systemic and regional haemodynamics in catecholamine-treated hyperkinetic septic shock.	2004 Apr	14673520
Effects of treatment of hepatorenal syndrome before transplantation on posttransplantation outcome. A case-control study.	2004 Jan	14672625
Terlipressin bolus induces systemic vasoconstriction in septic shock.	2004 Mar	14987338

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 16 00:32:37 GMT 2023` Edited by `admin` on `Sat Dec 16 00:32:37 GMT 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