Adult: As powder and solvent for solution for inj: Initially, 1-2 mg, then 1 mg 4-6 hourly. Max duration of treatment: 72 hours. As solution for inj: Initially, 2 mg 4 hourly, maintain until bleeding is controlled for 24 hours or up to max of 48 hours. Subsequent doses may be reduced to 1 mg 4 hourly in patients weighing <50 kg or if adverse reaction occur.
Intravenous Hepatorenal syndrome type 1
Adult: Initially, 1 mg 6 hourly via slow bolus inj, may be increased up to max 2 mg 4-6 hourly if serum creatinine has not been reduced by at least 25% after 3 days. Max duration of treatment: 2 weeks.
Reconstitution
Powder for solution for inj: Slowly add the contents of the solvent ampoule to the powder vial and roll gently until completely dissolved. Dilute further with 10 mL NaCl 0.9% solution for inj.
Symptoms: Acute hypertensive crisis, bradycardia. Management: Symptomatic and supportive treatment with a vasodilator-type α-blocker (e.g. clonidine) and atropine.
Drug Interactions
Increases the hypotensive effect of non-selective β-blockers. Concomitant use of drugs known to induce bradycardia (e.g. propofol, sufentanil) may lower heart rate and cardiac output. May trigger ventricular arrhythmias, including Torsade de pointes, when used with drugs that can prolong QT interval (e.g. class IA and III antiarrhythmics, erythromycin, certain antihistamines and TCAs), or with drugs that may cause hypokalaemia or hypomagnesaemia.
Action
Description: Mechanism of Action: Terlipressin, an inactive prodrug, is converted via enzymatic cleavage to lysine-vasopressin. The active vasopressin selectively causes splanchnic and extrarenal vasoconstriction by stimulation of V1 receptors on vascular smooth muscle, thereby reducing splanchnic blood flow and portal pressure. It also increases systemic mean arterial pressure and decrease heart rate. It has minimal action on V2 receptors responsible for its antidiuretic effects. Duration: 4-6 hours. Pharmacokinetics: Absorption: Time to peak plasma concentration: Approx 2 hours. Distribution: Volume of distribution: Approx 0.5 L/kg. Metabolism: Almost completely metabolised in the liver and kidneys by endo- and exopeptidases. Excretion: Via urine (<1% as unchanged drug and <0.1% as lypressin). Elimination half-life: 50-80 minutes.
Chemical Structure
Storage
Solution for inj: Store between 2-8°C. Powder for solution for inj: Store below 25°C. Protect from light.