Terlipressin

Synthetic Vasopressin Analogue (cyclic Peptide)Rx: PrescriptionCompound: Approved

Also known as: Glypressin, INN: terlipressin, Terlipressine, Terlivaz, Triglycyl-lysine-vasopressin

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Terlipressin is a synthetic vasopressin analogue used primarily for the treatment of hepatorenal syndrome type 1 (HRS-1), esophageal variceal bleeding, and bleeding from gastric varices. It reduces portal pressure through splanchnic vasoconstriction and has a longer half-life than vasopressin due to its prodrug design.

Mechanism of Action

Terlipressin is a prodrug that is cleaved in vivo to lysine-vasopressin. It acts primarily as a V1 receptor agonist on vascular smooth muscle, causing splanchnic and systemic vasoconstriction, thereby reducing portal hypertension and hepatic venous pressure gradient. It also has mild V2 receptor activity.

Routes of Administration

IntravenousSubcutaneous

Goals & Uses

  • Prevention of post-hepatectomy liver failureSurgical/HepaticLow
  • Esophageal variceal bleeding controlGastroenterology/HemostasisHigh
  • Gastric variceal bleedingGastroenterology/HemostasisModerate
  • Hepatorenal syndrome type 1 (HRS-1) treatmentRenal/HepaticHigh
  • Septic shock (vasopressor support)Critical CareModerate

Contraindications

  • Respiratory failure / hypoxiaPulmonaryHigh
  • Hyponatremia (severe)Metabolic/ElectrolyteModerate
  • PregnancyPopulationHighPotential fetal risk or insufficient safety data
  • Sepsis with high output statesInfectious/Critical CareModerate
  • Peripheral arterial occlusive diseaseVascularHigh
  • Severe cardiovascular disease / ischemic heart diseaseCardiovascularHigh

Adverse Effects

  • HypertensionCardiovascularCommonHigh blood pressure
  • Respiratory failure / pulmonary edemaPulmonaryUncommon
  • Abdominal cramps / diarrheaGastrointestinalCommon
  • Peripheral ischemia / skin necrosisVascularUncommon
  • Bradycardia / cardiac arrhythmiaCardiovascularUncommon
  • HyponatremiaElectrolyteCommon

Drug Interactions

  • Beta-blockersModerate
  • Drugs prolonging QT intervalModerate
  • NSAIDsModerateMay increase renal risk in susceptible patients
  • Vasopressors (norepinephrine, vasopressin)High

Population Constraints

  • Pediatric patientsAgeRelative
  • Patients with severe hyponatremia (Na < 130 mEq/L)MetabolicRelative
  • Elderly patientsAgeRelative
  • Pregnant womenReproductiveAbsolute
  • Patients with hypoxia or respiratory compromisePulmonaryAbsolute

Regulatory Status

  • European UnionApprovedApproved: Esophageal variceal bleeding, Hepatorenal syndromeLong-standing approval in EU member states (Glypressin and generics); approved for variceal hemorrhage and HRS.
  • United StatesApprovedApproved: Hepatorenal syndrome type 1 (HRS-1) with rapid progression of renal failureFDA approved Terlivaz (terlipressin) in August 2022. Not approved for variceal bleeding. Carries REMS program requirement.
  • United KingdomApprovedApproved: Esophageal variceal bleeding, Hepatorenal syndromeApproved and used widely in UK clinical practice for portal hypertension-related complications.

Approved by the FDA in 2022 (Terlivaz) for hepatorenal syndrome with rapid progression of renal failure. Previously approved in many European and other countries for variceal bleeding and HRS. Not FDA-approved for variceal bleeding indications.

Evidence & Sources

No sources recorded yet.

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