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) |
852.0 nM [Ki] | ||
Target ID: P47901 Gene ID: 553.0 Gene Symbol: AVPR1B Target Organism: Homo sapiens (Human) |
1115.0 nM [Ki] | ||
Target ID: P30518 Gene ID: 554.0 Gene Symbol: AVPR2 Target Organism: Homo sapiens (Human) |
1580.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| 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). |
|||
| 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 |
|---|---|---|
| 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 in chronic hyperdynamic endotoxic shock: is it safe? | 2003 Feb |
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| Terlipressin dose response in healthy and endotoxemic sheep: impact on cardiopulmonary performance and global oxygen transport. | 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 |
|
| 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 |
|
| 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 |
|
| [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 |
|
| Terlipressin infusion in catecholamine-resistant shock. | 2003 Oct |
|
| [Vasoconstrictive Therapies for Bleeding Esophageal Varices and their Mechanisms of Action]. | 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 |
|
| Medical management of variceal bleeding in patients with cirrhosis. | 2004 Feb |
|
| Science Review: Vasopressin and the cardiovascular system part 2 - clinical physiology. | 2004 Feb |
|
| Worsening of cerebral hyperemia by the administration of terlipressin in acute liver failure with severe encephalopathy. | 2004 Feb |
|
| Terlipressin and gelafundin: safe therapy of hepatorenal syndrome. | 2004 Feb 27 |
|
| Systemic, portal and renal effects of terlipressin in patients with cirrhotic ascites: pilot study. | 2004 Jan |
|
| 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 as rescue therapy for intractable hypotension during neonatal septic shock. | 2004 Mar |
|
| Terlipressin bolus induces systemic vasoconstriction in septic shock. | 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
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
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.
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NCI_THESAURUS |
C80212
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DBSALT002332
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SUB04727MIG
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139032838
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100000091321
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4U092XZF0K
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C99153
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ACTIVE MOIETY
SUBSTANCE RECORD