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 | Condition | Potency |
---|---|---|---|
Target ID: P37288 Gene ID: 552.0 Gene Symbol: AVPR1A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252 |
852.0 nM [Ki] | ||
Target ID: P47901 Gene ID: 553.0 Gene Symbol: AVPR1B Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252 |
1115.0 nM [Ki] | ||
Target ID: P30518 Gene ID: 554.0 Gene Symbol: AVPR2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252 |
1580.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | GLYPRESSIN Approved UseGLYPRESSIN 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). |
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Primary | GLYPRESSIN Approved UseGLYPRESSIN 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 |
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Update on treatment of variceal hemorrhage. | 2002 |
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Management of acute variceal bleeding. | 2003 |
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[Drug therapy of portal hypertension]. | 2003 Apr |
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Terlipressin and albumin for the hepatorenal syndrome. | 2003 Apr |
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Comparison of Doppler ultrasonography and the hepatic venous pressure gradient in assessing portal hypertension in liver cirrhosis. | 2003 Apr |
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Terlipressin plus hydroxyethyl starch infusion: an effective treatment for hepatorenal syndrome. | 2003 Aug |
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Review article: the management of acute variceal bleeding. | 2003 Aug 1 |
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Terlipressin and albumin combination treatment in hepatorenal syndrome. | 2003 Dec |
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Portal hypertensive bleeding. | 2003 Dec |
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Effects of the V1a vasopressin agonist F-180 on portal hypertension-related bleeding in portal hypertensive rats. | 2003 Dec |
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Terlipressin dose response in healthy and endotoxemic sheep: impact on cardiopulmonary performance and global oxygen transport. | 2003 Feb |
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Beneficial effects of terlipressin in hepatorenal syndrome: a prospective, randomized placebo-controlled clinical trial. | 2003 Feb |
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Acute renal failure in patients with cirrhosis: perspectives in the age of MELD. | 2003 Feb |
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Patient with a sudden drop in blood pressure. | 2003 Jan |
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Low-dose terlipressin improves systemic and splanchnic hemodynamics in fluid-challenged endotoxic rats. | 2003 Jan |
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Hepatorenal syndrome. | 2003 Jan-Mar |
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[Vasodilatory septic shock refractory to catecholamines: is there a role for terlipressin?]. | 2003 Jul |
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Is spontaneous bacterial peritonitis an inducer of vasopressin analogue side-effects? A case report. | 2003 Jul |
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When endoscopic therapy or pharmacotherapy fails to control variceal bleeding: what should be done? Immediate control of bleeding by TIPS? | 2003 Jul |
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Cyclooxygenase expression in splanchnic hyposensitivity to glypressin of bleeding portal hypertensive rats. | 2003 Jun |
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Terlipressin versus norepinephrine to correct refractory arterial hypotension after general anesthesia in patients chronically treated with renin-angiotensin system inhibitors. | 2003 Jun |
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[Acute upper gastrointestinal hemorrhage. Diagnosis and management]. | 2003 May |
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Emergency sclerotherapy versus vasoactive drugs for variceal bleeding in cirrhosis: a Cochrane meta-analysis. | 2003 May |
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Comment on "Terlipressin in chronic hyperdynamic endotoxic shock: is it safe?" by P. Asfar. | 2003 May |
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Terlipressin infusion in catecholamine-resistant shock. | 2003 Oct |
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[Vasoconstrictive Therapies for Bleeding Esophageal Varices and their Mechanisms of Action]. | 2003 Oct |
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[Vasopressin and its analogues in the therapy of shock]. | 2004 |
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Vasopressors for shock. | 2004 |
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[Acute upper gastrointestinal variceal bleeding: vasoactive agents]. | 2004 Apr |
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Effects of terlipressin on systemic and regional haemodynamics in catecholamine-treated hyperkinetic septic shock. | 2004 Apr |
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Effects of terlipressin on systolic pulmonary artery pressure of patients with liver cirrhosis: an echocardiographic assessment. | 2004 Aug 1 |
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Somatostatin, somatostatin analogues and other vasoactive drugs in the treatment of bleeding oesophageal varices. | 2004 Feb |
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Medical management of variceal bleeding in patients with cirrhosis. | 2004 Feb |
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Science Review: Vasopressin and the cardiovascular system part 2 - clinical physiology. | 2004 Feb |
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Worsening of cerebral hyperemia by the administration of terlipressin in acute liver failure with severe encephalopathy. | 2004 Feb |
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Terlipressin and gelafundin: safe therapy of hepatorenal syndrome. | 2004 Feb 27 |
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Systemic, portal and renal effects of terlipressin in patients with cirrhotic ascites: pilot study. | 2004 Jan |
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Effects of treatment of hepatorenal syndrome before transplantation on posttransplantation outcome. A case-control study. | 2004 Jan |
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Role of vasopressin in the management of septic shock. | 2004 Jul |
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Pressure or flow? | 2004 Jun |
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Clinical review: influence of vasoactive and other therapies on intestinal and hepatic circulations in patients with septic shock. | 2004 Jun |
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Terlipressin for cerebral perfusion pressure support in a patient with septic shock. | 2004 Jun |
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[Refractory hypotension during anesthesia in a patient treated with angiotensin receptor blockers]. | 2004 Jun-Jul |
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A long-acting vasopressin analog for septic shock: brilliant idea or dangerous folly? | 2004 Mar |
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Terlipressin as rescue therapy for intractable hypotension during neonatal septic shock. | 2004 Mar |
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Terlipressin bolus induces systemic vasoconstriction in septic shock. | 2004 Mar |
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Terlipressin for catecholamine-resistant septic shock in children. | 2004 Mar |
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Effect of terlipressin on blood volume distribution in patients with cirrhosis. | 2004 May |
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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 |
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Terlipressin in patients with septic shock: friend or foe? | 2004 May |
Sample Use Guides
In Vivo Use Guide
Sources: http://www.nps.org.au/__data/cmi_pdfs/CMR10462.pdf
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8835750
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
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Sequence Type | COMPLETE |
Record UNII |
7Z5X49W53P
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Validated (UNII)
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FDA ORPHAN DRUG |
580417
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FDA ORPHAN DRUG |
534216
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FDA ORPHAN DRUG |
11785
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FDA ORPHAN DRUG |
191804
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WHO-VATC |
QH01BA04
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WHO-ATC |
H01BA04
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NCI_THESAURUS |
C80212
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CHEMBL2135460
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7Z5X49W53P
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TERLIPRESSIN
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238-680-8
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C77387
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57048
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14636-12-5
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SS-34
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M10580
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C012078
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DB02638
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SALT/SOLVATE -> PARENT |
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METABOLITE ACTIVE -> PARENT |
Believed to behave as a prodrug
IN-VIVO
PLASMA
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METABOLITE ACTIVE -> PARENT |
IN-VIVO
PLASMA
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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MOL_WEIGHT:SEQUENCE(CALCULATED) | CHEMICAL |
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Molecular Formula | CHEMICAL |
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