terlipressin

Terlipressin is a synthetic vasopressin prodrug used as a vasoactive medication to reduce portal hypertension and to improve renal function in certain liver-related conditions. It is a prodrug of vasopressin (lysine vasopressin) that is cleaved in vivo to the active hormone.

Mechanism and pharmacology: It acts primarily as a vasopressin V1 receptor agonist, causing constriction of both systemic and splanchnic vessels, which lowers portal venous pressure and redirects blood flow toward the systemic circulation. In patients with cirrhosis, this can increase effective arterial blood volume, supporting renal perfusion.

Indications and regulatory status: It is used to treat acute variceal bleeding due to portal hypertension; in some countries it is also used for hepatorenal syndrome in adults, typically in combination with albumin. Regulatory approval varies by country, and practice patterns differ accordingly.

Administration and dosing: Terlipressin is given by intravenous injection or infusion. Onset is rapid after dosing; duration is limited, as vasopressin activity lasts only a few hours per dose. Dosing regimens commonly involve 2 mg IV every 4 hours, adjusted for response and tolerability, and continued for several days depending on indication and guidelines.

Safety and adverse effects: Cautions include cardiovascular disease, peripheral vascular disease, mesenteric ischemia, and high risk of myocardial ischemia. Adverse effects include hypertension, headache, abdominal cramps, hyponatremia, chest pain, arrhythmias, and potential for ischemic events; monitoring of blood pressure, electrolytes, and signs of ischemia is recommended.

History and notes: After administration, terlipressin is rapidly converted to vasopressin. It was developed in the late 20th century and has been used especially in Europe and other regions of the world.