Terlipressin

Terlivaz / Glypressin

Terlipressin is a synthetic analog of vasopressin designed as a slow-release prodrug: three glycine residues are added to the vasopressin structure, and after injection they are gradually cleaved to release the active peptide lysine-vasopressin over hours. This 'prohormone' design gives a longer, smoother duration of action than native vasopressin, allowing intermittent bolus dosing or continuous infusion in a hospital setting rather than the tight titration a short-acting vasopressor requires. Unlike desmopressin — which is engineered for V2 (antidiuretic) selectivity — terlipressin retains meaningful activity at the vasopressin V1 receptor, which constricts blood vessels. In advanced liver disease (cirrhosis), the splanchnic circulation around the gut becomes abnormally dilated, which lowers effective blood volume reaching the kidneys and drives the dangerous kidney failure called hepatorenal syndrome (HRS). By constricting these splanchnic vessels, terlipressin redirects blood flow, raises perfusion pressure to the kidney, and can reverse the kidney injury. The same splanchnic vasoconstriction reduces pressure in the portal vein, which is why terlipressin is also used to control acute bleeding from esophageal varices. Terlipressin received US FDA approval in 2022 (as Terlivaz) for hepatorenal syndrome with rapid kidney-function decline, and it has long been used in Europe and elsewhere for HRS and variceal bleeding. It is administered by clinicians in a monitored inpatient environment, usually alongside albumin, because its vasoconstrictor action carries real risks — including reduced blood flow to fingers, toes, or the intestines, fluid overload, and respiratory complications. It is a specialist hospital drug, not something used outside supervised care.