Terlipressin is a synthetic vasopressin analog (MW ~1227.4 g/mol) that acts as a prodrug, slowly converted by tissue peptidases to the active metabolite lysine vasopressin. It was FDA-approved in September 2022 (Terlivaz) for hepatorenal syndrome type 1 (HRS-1), making it the first pharmacotherapy specifically approved for this indication in the United States. Terlipressin has been used in Europe for decades for variceal bleeding and hepatorenal syndrome. It acts primarily via V1a receptors to cause splanchnic vasoconstriction, improving renal perfusion in the context of portal hypertension.
Category: Reproductive / Hormonal. Evidence rating: A (strong human clinical data).
Clinical status: FDA-approved (Terlivaz for hepatorenal syndrome type 1, September 2022)
Terlipressin is a triglycyl-lysine vasopressin prodrug. After injection, endopeptidases in the liver, kidney, and vascular endothelium cleave the triglycyl moiety to release lysine vasopressin (the active metabolite) over several hours. Lysine vasopressin preferentially activates V1a receptors on…
Research base: 0 registered clinical trials and 1 indexed publication reference Terlipressin.
Safety considerations: Respiratory failure: observed in 11% of terlipressin-treated patients vs 2% placebo in CONFIRM trial; FDA boxed warning for serious or fatal respiratory failure; Abdominal pain and diarrhea (common); Peripheral ischemia: digital ischemia, skin necrosis, and intestinal ischemia reported.
Reviewed by the PeptideAtlas Editorial Team. Last reviewed: 2026-08-12.
Related peptides: Kisspeptin, Gonadorelin, Oxytocin.
Compare: Terlipressin vs Kisspeptin, Terlipressin vs Gonadorelin, Terlipressin vs Oxytocin.
Hepatorenal syndrome (HRS) is a life-threatening form of kidney failure occurring in patients with advanced liver disease and portal hypertension. Splanchnic vasodilation leads to reduced effective blood volume and renal vasoconstriction. Terlipressin constricts splanchnic blood vessels, redirecting blood flow to improve renal perfusion, with the goal of reversing kidney failure.
In the CONFIRM trial, 11% of terlipressin-treated patients developed respiratory failure vs 2% on placebo. Terlipressin increases venous return, which in patients with impaired cardiac function and portal hypertension can precipitate pulmonary edema. Oxygen monitoring and respiratory assessment are required during treatment.
Terlipressin is a prodrug that is slowly converted to lysine vasopressin, providing a longer duration of action (~6 hours vs ~30 minutes) and allowing intermittent IV bolus dosing every 6 hours rather than continuous infusion. It has relatively greater V1a selectivity.