Terlipressin

Indications:

• Treatment of bleeding esophageal varices in patients with cirrhosis.
• Treatment of hepatorenal syndrome (HRS), particularly type 1 HRS.

Mechanism of Action: Terlipressin is a prodrug of lysine vasopressin (LVP). Upon administration, it is hydrolyzed to release LVP. LVP then acts on vasopressin V1 receptors, leading to splanchnic vasoconstriction. This helps reduce portal blood flow and pressure, thereby reducing or stopping esophageal variceal bleeding. In the case of HRS, the vasoconstrictive effect helps improve renal function.

Pharmacokinetics:

• Absorption: After intravenous administration, terlipressin is rapidly hydrolyzed to LVP.
• Distribution: Distributed throughout the body, mainly in the kidneys, liver, and vascular endothelium.
• Metabolism: Rapidly metabolized, primarily in the liver.
• Excretion: Excreted primarily through the kidneys.

Form: Terlipressin API is usually available as a white to off-white lyophilized powder.