Pharmacology · Vasopressin and its analogues
Terlipressin !
A long-acting vasopressin prodrug given IV. It constricts gut vessels and improves kidney blood flow in hepatorenal syndrome.
Updated 2026-11-01
Mechanism of action
Terlipressin (triglycyl-lysine vasopressin) is a prodrug: enzymes slowly cut off its glycine residues, releasing lysine vasopressin. This acts mainly on V1a receptors of vascular smooth muscle, constricting splanchnic arterioles. Blood is shifted from the dilated gut circulation back to the central circulation, which raises effective arterial volume and improves kidney perfusion in hepatorenal syndrome. It also has some V2 (antidiuretic) action.
- Enzymes slowly convert terlipressin into lysine vasopressin
- Lysine vasopressin activates V1a receptors in splanchnic vessels
- Splanchnic vasoconstriction returns blood to the central circulation
- Kidney perfusion and function improve
Pharmacokinetics
- Absorption
- Given IV after the powder is reconstituted
- Metabolism
- Prodrug cleaved by peptidases into lysine vasopressin
- Half-life
- Longer-acting than vasopressin because the active form is released gradually
Indications
- Hepatorenal syndrome with rapid loss of kidney function in adults with advanced liver disease Cirrhosis →
Adverse effects
Common
- Abdominal pain
- Nausea and diarrhoea
- Shortness of breath
Contraindications
- Low blood oxygen or worsening breathing problems
- Active coronary, mesenteric or peripheral ischaemia
Key interactions
- Albumin and other IV fluids
- Volume overload raises the risk of respiratory failure; fluids are reduced if overload appears
What is monitored
- Oxygen saturation and breathing
- Fluid balance and signs of overload
- Creatinine and urine output
- Heart rate, chest pain and skin or limb colour
Administration and safety
- Reconstituted and given IV by health professionals
- Oxygen saturation is assessed with pulse oximetry before starting and during treatment
- Not started in patients with hypoxia or worsening breathing
Nursing care
- Check oxygen saturation and breathing before and during treatment
- Watch for shortness of breath, crackles or rapid weight gain (fluid overload)
- Look for chest pain, abdominal pain or bluish fingers and skin
- Record urine output and creatinine
Pregnancy and breastfeeding
May cause fetal harm; the treating team is told at once if pregnancy is possible.
Test yourself
Think of the answer, then tap the question to see it.
How does terlipressin improve kidney function in hepatorenal syndrome?
V1 vasoconstriction of dilated splanchnic vessels returns blood to the central circulation, raising effective volume and renal perfusion.
What is the boxed warning of terlipressin?
Serious or fatal respiratory failure, more likely with fluid overload; oxygenation is checked before each dose.
Why does terlipressin act longer than vasopressin?
It is a prodrug: lysine vasopressin is released gradually as enzymes remove its glycine residues.
Related drugs
Related conditions
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Terlipressin Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Farmacología básica y clínica (Katzung), 16.ª ed., cap. 37 (McGraw Hill, 2025).
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