TERLIVAZ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TERLIVAZ (TERLIVAZ).

How it works

Terlipressin is a synthetic vasopressin analog that acts as a prodrug, converting to lysine-vasopressin in the body. It selectively constricts splanchnic blood vessels via V1 receptors, reducing portal pressure and treating variceal bleeding. It also increases renal perfusion via V2 receptors, improving renal function in hepatorenal syndrome.

What the body does with it

Metabolism	Terlipressin is rapidly converted to its active metabolite lysine-vasopressin via exopeptidases in the liver and kidneys. Further metabolism occurs via peptidases in various tissues.
Excretion	Primarily renal (approximately 60% as unchanged drug and metabolites); biliary/fecal excretion accounts for about 20%.
Half-life	Terminal elimination half-life is approximately 2.5 hours; in patients with renal impairment, half-life may be prolonged.
Protein binding	Approximately 50% bound to plasma proteins, primarily albumin.
Volume of Distribution	Approximately 0.5 L/kg; indicates distribution primarily in extracellular fluid.
Bioavailability	Subcutaneous: approximately 80% relative to intravenous administration.
Onset of Action	Intravenous bolus: within 1–2 minutes; subcutaneous: within 10–15 minutes.
Duration of Action	Approximately 4–6 hours after intravenous administration; clinical effect duration is dose-dependent.

Classification & Brands

Dosing & administration

Initial dose: 1-2 mg intravenous bolus every 4-6 hours; titrate to 4 mg every 4-6 hours as needed for variceal bleeding. Max daily dose: 12 mg.

Dosage form	POWDER
Renal impairment	No specific dose adjustment for GFR; use caution in severe renal impairment (GFR <30 mL/min) due to potential sodium retention and volume overload.
Liver impairment	Child-Pugh A/B: No dose adjustment. Child-Pugh C: Initial dose of 1 mg intravenous bolus every 6 hours; titrate cautiously due to increased risk of hepatic encephalopathy.
Pediatric use	Safety and efficacy not established in pediatric patients; no weight-based dosing available.
Geriatric use	Start at lower end of dosing range (1-2 mg) due to age-related decrease in renal function and increased cardiovascular risk; monitor for fluid overload and hypertension.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TERLIVAZ (TERLIVAZ).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for at least 48 hours after last dose.
Teratogenic Risk	Terlipressin is contraindicated in pregnancy due to risk of uterine contractions, fetal hypoxia, and miscarriage. Animal studies show embryotoxicity and teratogenicity. First trimester: high risk of spontaneous abortion. Second and third trimesters: risk of preterm labor, placental insufficiency, and fetal distress.

Warnings & precautions

■ FDA Black Box Warning

Terlipressin can cause serious or fatal ischemic adverse reactions including cardiac, mesenteric, peripheral, and digital ischemia. Use is contraindicated in patients with ischemic cardiovascular or cerebrovascular disease.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to terlipressin or any component","Uncontrolled hypertension","Ischemic cardiovascular disease (e.g., coronary artery disease)","Cerebrovascular disease","Peripheral vascular disease","Mesenteric ischemia","Severe asthma or chronic obstructive pulmonary disease (COPD)","Lactic acidosis","Ongoing septic shock","Known pregnancy (may cause fetal harm)"]

Clinical Precautions

Precautions

["Risk of ischemic events (cardiac, mesenteric, peripheral)","Fluid overload and electrolyte disturbances","Respiratory failure and dyspnea","Fetal harm if used during pregnancy","Monitor blood pressure, oxygenation, and electrolytes"]

Clinical Tips & Counseling

Drug interactions

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TERLIVAZ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TERLIVAZ (TERLIVAZ).

How it works

What the body does with it

Metabolism	Terlipressin is rapidly converted to its active metabolite lysine-vasopressin via exopeptidases in the liver and kidneys. Further metabolism occurs via peptidases in various tissues.
Excretion	Primarily renal (approximately 60% as unchanged drug and metabolites); biliary/fecal excretion accounts for about 20%.
Half-life	Terminal elimination half-life is approximately 2.5 hours; in patients with renal impairment, half-life may be prolonged.
Protein binding	Approximately 50% bound to plasma proteins, primarily albumin.
Volume of Distribution	Approximately 0.5 L/kg; indicates distribution primarily in extracellular fluid.
Bioavailability	Subcutaneous: approximately 80% relative to intravenous administration.
Onset of Action	Intravenous bolus: within 1–2 minutes; subcutaneous: within 10–15 minutes.
Duration of Action	Approximately 4–6 hours after intravenous administration; clinical effect duration is dose-dependent.

Classification & Brands

Dosing & administration

Initial dose: 1-2 mg intravenous bolus every 4-6 hours; titrate to 4 mg every 4-6 hours as needed for variceal bleeding. Max daily dose: 12 mg.

Dosage form	POWDER
Renal impairment	No specific dose adjustment for GFR; use caution in severe renal impairment (GFR <30 mL/min) due to potential sodium retention and volume overload.
Liver impairment	Child-Pugh A/B: No dose adjustment. Child-Pugh C: Initial dose of 1 mg intravenous bolus every 6 hours; titrate cautiously due to increased risk of hepatic encephalopathy.
Pediatric use	Safety and efficacy not established in pediatric patients; no weight-based dosing available.
Geriatric use	Start at lower end of dosing range (1-2 mg) due to age-related decrease in renal function and increased cardiovascular risk; monitor for fluid overload and hypertension.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TERLIVAZ (TERLIVAZ).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for at least 48 hours after last dose.
Teratogenic Risk	Terlipressin is contraindicated in pregnancy due to risk of uterine contractions, fetal hypoxia, and miscarriage. Animal studies show embryotoxicity and teratogenicity. First trimester: high risk of spontaneous abortion. Second and third trimesters: risk of preterm labor, placental insufficiency, and fetal distress.