Terlipressin
Also known as: Glypressin, INN: terlipressin, Lysine vasopressin prodrug, Terlipressine, Terlivaz, TLP, Triglycyl-lysine-vasopressin
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Summary
Terlipressin is a synthetic analogue of vasopressin approved for prescription use as an intravenous or subcutaneous vasoconstrictor. It is primarily employed, together with albumin, to treat type 1 hepatorenal syndrome (HRS‑1) in patients with advanced cirrhosis, aiming to improve kidney function by counteracting the severe splanchnic vasodilation that characterises this condition.
Mechanism of Action
Terlipressin acts as a vasopressin‑like agonist at V1 receptors on vascular smooth muscle, especially in the splanchnic circulation. Activation of these receptors induces potent vasoconstriction, reducing blood pooling in the gut, raising effective arterial volume, and thereby enhancing renal perfusion and glomerular filtration in HRS‑1 patients.
What the Research Shows
Clinical research has focused on terlipressin’s role in HRS‑1. A phase 3, double‑blind trial (CONFIRM) randomised 300 patients to terlipressin plus albumin or placebo plus albumin for up to 14 days; verified HRS reversal occurred in 32% of terlipressin recipients versus 17% with placebo (P=0.006). Secondary analyses showed 39% overall reversal versus 18% with placebo. Review articles note that terlipressin‑albumin regimens achieve renal‑function recovery in roughly 40‑50% of cases, positioning the drug as a likely first‑line therapy in Europe. The vasoactive‑inotropic score (VIS) literature now includes terlipressin as a component for quantifying hemodynamic support.
Reported Benefits
Evidence from the CONFIRM trial and subsequent reviews indicates terlipressin improves renal function in HRS‑1, with significantly higher rates of serum‑creatinine reduction and HRS reversal compared with placebo. When combined with albumin, it can achieve renal recovery in up to half of treated patients, offering a bridge to liver transplantation and potentially improving short‑term outcomes.
Limitations of the Evidence
Response rates remain modest; many patients do not achieve reversal and overall mortality stays high. The drug is studied only for HRS‑1, and data on long‑term survival or use in other indications are lacking. Safety concerns, especially respiratory failure, limit its applicability in patients with pulmonary disease. Comparative data with alternative vasoconstrictors (e.g., norepinephrine) are limited.
Safety Considerations
Adverse events reported more frequently with terlipressin include abdominal pain, nausea, diarrhoea, and notably respiratory failure, which contributed to higher 90‑day respiratory‑related deaths (11% vs 2% with placebo). Clinicians should monitor respiratory status, fluid balance, and signs of ischemia, and exercise caution in patients with underlying lung disease or cardiovascular compromise.
How It Is Administered
Terlipressin is administered intravenously or subcutaneously, typically as a bolus or short infusion repeated every 4–6 hours, and is given alongside intravenous albumin. The formulation is a synthetic cyclic peptide supplied in sterile solution for parenteral use.
Routes of Administration
Goals & Uses
- Acute variceal bleedingGastrointestinalHigh
- Prevention of post-hepatectomy liver failureSurgical/HepaticLow
- Esophageal variceal bleeding controlGastroenterology/HemostasisHigh
- Hepatorenal syndromeRenalHigh
- Septic shock (off‑label)Critical CareModerate
- Gastric variceal bleedingGastroenterology/HemostasisModerate
- Hepatorenal syndrome type 1 (HRS-1) treatmentRenal/HepaticHigh
- Septic shock (vasopressor support)Critical CareModerate
Contraindications
- Respiratory failure / hypoxiaPulmonaryHigh
- Ischemic heart diseaseCardiovascularModerate
- Hyponatremia (severe)Metabolic/ElectrolyteModerate
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Sepsis with high output statesInfectious/Critical CareModerate
- Peripheral arterial occlusive diseaseVascularHigh
- Uncontrolled hypertensionCardiovascularModerate
- Known hypersensitivity to terlipressinAllergyHigh
- Severe cardiovascular disease / ischemic heart diseaseCardiovascularHigh
Adverse Effects
- Myocardial infarctionCardiovascularRare
- HypertensionCardiovascularCommonHigh blood pressure
- Peripheral ischemiaVascularUncommon
- Respiratory failure / pulmonary edemaPulmonaryUncommon
- Abdominal cramps / painGastrointestinalCommon
- Abdominal cramps / diarrheaGastrointestinalCommon
- Peripheral ischemia / skin necrosisVascularUncommon
- Bradycardia / cardiac arrhythmiaCardiovascularUncommon
- HyponatremiaElectrolyteCommon
Drug Interactions
- NitroglycerinModerate
- Beta-blockersModerate
- Drugs prolonging QT intervalModerate
- NSAIDsModerateMay increase renal risk in susceptible patients
- Vasopressors (norepinephrine, vasopressin)High
- Other vasoconstrictors (e.g., norepinephrine)High
Population Constraints
- PregnancyReproductive SafetyRelative
- Pediatric patientsAgeRelative
- ElderlyAgeRelative
- Patients with severe hyponatremia (Na < 130 mEq/L)MetabolicRelative
- Elderly patientsAgeRelative
- Pregnant womenReproductiveAbsolute
- Patients with hypoxia or respiratory compromisePulmonaryAbsolute
Regulatory Status
- European UnionApprovedApproved: hepatorenal syndrome, acute variceal bleedingMarketing authorization granted; prescription only
- United StatesUnapprovedInvestigational use under IND for hepatorenal syndrome; not FDA‑approved
- United KingdomApprovedApproved: hepatorenal syndrome, acute variceal bleedingAuthorized via MHRA; prescription only
Not approved by the US FDA; approved in the European Union, United Kingdom, Japan, and several Asian countries for hepatorenal syndrome and variceal hemorrhage.
Evidence & Sources
- Journal ArticleModerateBelletti A, et al.2021-01-01T00:00:00.000000Z
- Journal ArticleModerateWong F, et al.2021-01-01T00:00:00.000000Z
- Journal ArticleModerateBelcher JM2023-01-01T00:00:00.000000Z
- Journal ArticleModerateKhemichian S, Nadim MK, Terrault NA2025-01-01T00:00:00.000000Z
- Journal ArticleModerateFrancoz C, et al.2019-01-01T00:00:00.000000Z
- Journal ArticleModerateTapper EB, Parikh ND2023-01-01T00:00:00.000000Z
Frequently Asked Questions
What condition is terlipressin approved to treat?
Terlipressin is approved for use, together with albumin, in adults with type 1 hepatorenal syndrome—a severe kidney dysfunction that occurs in advanced cirrhosis.
How does terlipressin improve kidney function?
By activating V1 vasopressin receptors, terlipressin constricts splanchnic vessels, reduces blood pooling in the gut, raises effective arterial volume, and thereby enhances renal perfusion and glomerular filtration.
What are the main safety concerns?
Clinical trials reported higher rates of abdominal discomfort, nausea, diarrhoea, and serious respiratory failure. Monitoring for respiratory compromise and ischemic complications is recommended.
Is terlipressin given alone or with other drugs?
It is administered together with intravenous albumin, which helps expand plasma volume and supports the vasoconstrictive effect on renal perfusion.
Can terlipressin be used for conditions other than HRS‑1?
Current evidence and regulatory approval are limited to HRS‑1; its use for other indications remains investigational and is not supported by the cited literature.
What is Terlipressin?
Terlipressin is a synthetic analogue of vasopressin approved for prescription use as an intravenous or subcutaneous vasoconstrictor. It is primarily employed, together with albumin, to treat type 1 hepatorenal syndrome (HRS‑1) in patients with advanced cirrhosis, aiming to improve kidney function by counteracting the severe splanchnic vasodilation that characterises this condition.
What is Terlipressin used for?
Terlipressin is educationally associated with: Acute variceal bleeding, Prevention of post-hepatectomy liver failure, Esophageal variceal bleeding control, Hepatorenal syndrome, Septic shock (off‑label), Gastric variceal bleeding, Hepatorenal syndrome type 1 (HRS-1) treatment, Septic shock (vasopressor support). Educational only — not medical advice.
How is Terlipressin administered?
Recorded routes of administration: Intramuscular, Intravenous, Subcutaneous.
What are the potential side effects of Terlipressin?
Reported adverse effects include: Myocardial infarction, Hypertension, Peripheral ischemia, Respiratory failure / pulmonary edema, Abdominal cramps / pain, Abdominal cramps / diarrhea, Peripheral ischemia / skin necrosis, Bradycardia / cardiac arrhythmia, Hyponatremia. This list is not exhaustive — consult a qualified clinician.
Who should avoid Terlipressin?
Recorded contraindications: Respiratory failure / hypoxia, Ischemic heart disease, Hyponatremia (severe), Pregnancy, Sepsis with high output states, Peripheral arterial occlusive disease, Uncontrolled hypertension, Known hypersensitivity to terlipressin, Severe cardiovascular disease / ischemic heart disease. Consult a qualified clinician before use.