Generic
Terlipressin
2 brands available in the market
At a glance
Terlipressin is a vasopressin analog used for the short-term management of bleeding esophageal varices and type 1 hepatorenal syndrome. It controls bleeding by reducing splanchnic blood flow and portal pressure.
Description
Terlipressin is an inactive prodrug that is converted to lysine-vasopressin via enzymatic cleavage. Active vasopressin causes splanchnic and extrarenal vasoconstriction by stimulating V1 receptors on vascular smooth muscle, reducing splanchnic blood flow and portal pressure. It increases systemic mean arterial pressure and decreases heart rate.
Indications
- Bleeding esophageal varices (short-term management)
- Type 1 hepatorenal syndrome (IAC criteria)
Therapeutic class
Other Preparations
Pharmacological class
Vasopressin Analog
Pharmacology
Terlipressin is a prodrug converted to lysine-vasopressin, which activates V1 receptors. It reduces splanchnic blood flow, decreases portal pressure, increases systemic arterial pressure, and decreases heart rate. Minimal V2 receptor activity results in low antidiuretic effects.
Mechanism of action
Reduces portal pressure and bleeding by vasoconstriction.
Dosage
Adult Dose (IV):
- Bleeding esophageal varices: Start 2 mg every 4 hours (until bleeding controlled for 24 hours, max 48 hours); <50 kg or adverse effects: 1 mg every 4 hours
- Type 1 hepatorenal syndrome: 3-4 mg every 24 hours (3-4 administrations); if serum creatinine not reduced by 25% after 3 days, discontinue; target: creatinine <130 µmol/L or ≥30% reduction; average treatment 10 days
Administration
- IV injection/infusion only; IV bolus
- Administered by a healthcare professional in a hospital
- Do not self-administer
Missed dose
If you miss a dose, skip it and continue with your normal schedule; do not double the dose.
Side effects
Common Side Effects:
- Paleness (skin)
- Increased blood pressure
- Abdominal pain, nausea, diarrhea
- Headache
- Abdominal cramps
Serious:
- QT prolongation, Torsade de pointes
- Bradycardia
- Cardiac arrhythmias
Precautions & warnings
- Do not use in unstable angina, recent MI, septic shock with low cardiac output
- Caution in hypertension, heart disease, renal dysfunction, cerebrovascular disease
- Monitor ECG, BP, HR, electrolytes, and fluid balance during treatment
- Caution with QT-prolonging drugs
Contraindications
- Pregnancy
- Hypersensitivity to terlipressin or excipients
Drug interactions
- Non-selective beta-blockers: Increased hypotensive effect on portal vein
- Bradycardia-inducing drugs (propofol, sufentanil): Decreased heart rate and cardiac output
- QT-prolonging drugs (Class IA/III antiarrhythmics, erythromycin, certain antihistamines, TCAs): Risk of Torsade de pointes
Food interactions
It is not known whether alcohol is safe with Terlipressin; consult your doctor.
Use in pregnancy
Use in Pregnancy: Highly unsafe; may cause uterine contractions and decreased fetal blood flow; do not use; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; decide based on benefits of breastfeeding and therapy; consult your doctor.
Pediatric use
Limited experience in pediatric patients; no dosage recommendation
Geriatric use
Limited experience in elderly patients; no dosage recommendation
Renal / hepatic impairment
Renal Impairment: Caution in renal dysfunction; consult your doctor.
Hepatic Impairment: Limited information; consult your doctor.
Overdose effects
Overdose may cause severe circulatory adverse effects; elevated BP can be controlled with clonidine 150 mcg IV; bradycardia treated with atropine.
Storage conditions
Store at 2-8°C in a refrigerator, protected from light in the original carton; keep out of reach of children.
Chemical structure
Terlipressin