Terlipressin is a synthetic, long-acting analogue of vasopressin (antidiuretic hormone). It is a prodrug that is slowly converted in vivo to lysine-vasopressin. It is primarily used in the management of bleeding esophageal varices in patients with portal hypertension due to cirrhosis and, more recently, for the treatment of hepatorenal syndrome type 1 (HRS-1). Its mechanism involves causing vasoconstriction of the splanchnic circulation, thereby reducing portal venous pressure and blood flow to esophageal varices.
Adult: For Variceal Bleed: 2 mg IV bolus every 4-6 hours until bleeding is controlled (up to 72 hours), then 1 mg every 4-6 hours for prevention of rebleeding. For HRS-1: 1 mg IV every 6 hours; dose may be increased to 2 mg every 6 hours if no response (no reduction in serum creatinine >25%) after 3 days.
Note: For Intravenous Use Only. Reconstitute the 1 mg lyophilized powder with 5 mL of Sterile Water for Injection. Administer as a slow IV bolus over 1 minute. Do not mix with other medications. Must be administered in a hospital setting with continuous monitoring of blood pressure, heart rate, ECG, fluid balance, and serum sodium.
Terlipressin is a prodrug for lysine-vasopressin. It acts as a potent agonist at vascular V1 receptors, causing vasoconstriction of the splanchnic (intestinal) blood vessels. This reduces portal venous inflow and pressure, thereby decreasing the pressure within esophageal varices and controlling bleeding. In HRS-1, it reverses the splanchnic arterial vasodilation, improving effective arterial blood volume and renal perfusion.
Pregnancy: Category B3 (Australian Category). Contraindicated. May cause uterine contractions and fetal hypoxia. Use only if potential benefit justifies the potential risk to the fetus, typically in life-threatening maternal hemorrhage.
Driving: Not relevant. Patients are hospitalized and critically ill during therapy. Dizziness or headache may affect ability to drive post-treatment; caution advised.
| Beta-blockers (e.g., Propranolol) | Additive bradycardia; may reduce heart rate excessively. | Major |
| Other Vasoconstrictors (e.g., Noradrenaline) | Additive hypertensive and ischemic effects. | Major |
| Corticosteroids (e.g., Hydrocortisone) | May enhance the hypertensive effect of terlipressin. Often used together in HRS-1 therapy. | Moderate |
| Drugs causing QT prolongation (e.g., Fluoroquinolones) | Potential additive effect on QT interval; monitor ECG. | Moderate |
| Diuretics (e.g., Furosemide) | Increased risk of electrolyte disturbances (hyponatremia, hypokalemia). | Moderate |
| Glyceryl Trinitrate (GTN) | Often co-administered to mitigate ischemic side effects; requires careful hemodynamic monitoring. | Moderate |
Same composition (Terlipressin (1mg)), different brands: