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Terlipressin: quick citable summary
Terlipressin is listed by PeptaHub as a other peptide with a prescription legal-status classification. The page summarizes mechanism, research context, common routes, safety notes, and references for writers and AI answer engines.
PeptaHub. “Terlipressin: Mechanism, Research Context, Safety.” peptahub.com, 2026. https://peptahub.com/peptides/terlipressin. Licensed CC BY 4.0.
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What is Terlipressin?
Terlipressin (Terlivaz) is the first FDA-approved treatment for hepatorenal syndrome with rapid kidney function reduction (HRS-AKI), approved September 2022. It is a vasopressin analog prodrug that produces splanchnic vasoconstriction to restore renal perfusion in advanced liver disease.
Overview
Terlipressin is a synthetic vasopressin analogue and the first FDA-approved medication (approved September 2022) for hepatorenal syndrome with rapid reduction of kidney function (HRS-AKI). It acts as a prodrug that is cleaved in vivo to release lysine-vasopressin, producing potent splanchnic vasoconstriction and improving renal perfusion in the setting of advanced liver disease.
Mechanism of action
Terlipressin is a prodrug consisting of three glycine residues attached to lysine-vasopressin (N-triglycyl-8-lysine-vasopressin). Tissue peptidases cleave the N-terminal glycyl residues, releasing the active moiety lysine-vasopressin. Lysine-vasopressin binds to V1 receptors in splanchnic and peripheral vascular smooth muscle, causing potent vasoconstriction. In hepatorenal syndrome, the underlying pathology is severe splanchnic vasodilation driven by portal hypertension and circulatory dysfunction; by reversing this vasodilation, terlipressin reduces effective arterial blood volume depletion, suppresses the renin-angiotensin-aldosterone and sympathetic nervous systems, and restores renal perfusion. This mechanism is distinct from other vasopressors in its preferential splanchnic action and prolonged duration.
Reported study ranges
| Purpose | Route | Reported range | Frequency | Notes |
|---|---|---|---|---|
| hepatorenal syndrome (HRS-AKI) | intravenous | 0.85–1.7 mg | every 6 hours for up to 14 days | Per the FDA label: 0.85 mg IV every 6 hours on days 1-3. On day 4, assess the change in serum creatinine from baseline — if it has decreased by at least 30%, continue 0.85 mg every 6 hours; if by less than 30%, increase to 1.7 mg every 6 hours; if it is at or above baseline, discontinue. Continue until 24 hours after two consecutive creatinine values of 1.5 mg/dL or less, to a maximum of 14 days. Do not initiate if oxygen saturation is below 90%. |
Reported ranges are for research context only. Consult a qualified healthcare professional before using any peptide.
Convert Terlipressin research-range units
Need to convert mg to mcg, dose volume, or U-100 syringe units? The Terlipressin dose calculator is preloaded with these ranges, or use the general dose unit converter.
Research summary
In the pivotal CONFIRM trial (Wong et al., N Engl J Med 2021; Phase 3, n=300, randomized 2:1 to terlipressin plus albumin or placebo), verified reversal of HRS-1 occurred in 32% of terlipressin patients versus 17% on placebo (P=0.008). More adverse events occurred with terlipressin, including abdominal pain, nausea, diarrhea, and respiratory failure. It had been used in Europe and Asia for over two decades before FDA approval. A meta-analysis of terlipressin RCTs in hepatorenal syndrome (Fabrizi et al., Aliment Pharmacol Ther 2006) supports efficacy versus placebo/albumin. Respiratory failure is the central safety concern and is the subject of a boxed warning; patients with hypoxia or with acute-on-chronic liver failure Grade 3 are at elevated risk.[1][2][3][4]
Evidence grading
Each claimed benefit is graded by the strength of available evidence. Grades reflect study quality, not effect size.
Strong = multiple RCTs · Moderate = limited trials or observational · Preliminary = animal or in vitro only · Insufficient = anecdotal or no published data
Side effects
Side effects vary by individual. This is not an exhaustive list. Report unusual symptoms to a healthcare professional.
Common stacks
Peptides commonly paired with Terlipressin for synergistic effects.
Legal status
FDA-approved September 2022 (Terlivaz) to improve kidney function in adults with hepatorenal syndrome with rapid reduction in kidney function. Carries a BOXED WARNING for serious or fatal respiratory failure. Do not initiate in patients with hypoxia (oxygen saturation below 90%) until oxygenation improves; discontinue if saturation falls below 90%. Contraindicated in patients with ongoing coronary, peripheral, or mesenteric ischemia. Patients with serum creatinine above 5 mg/dL are unlikely to benefit. Given only in hospital settings with continuous pulse-oximetry monitoring. Previously approved in 40+ countries including EU member states.
Sourcing & access
Prescription required
Terlipressin is an FDA-approved prescription medication available through licensed healthcare providers, pharmacies, and label-appropriate access programs; compounded access depends on current FDA shortage status and compounding rules.
Frequently asked questions
Terlipressin (brand name Terlivaz) is a synthetic vasopressin analog prodrug approved by the FDA in September 2022 for hepatorenal syndrome with rapid reduction in kidney function (HRS-AKI). It had been used in Europe and Asia for over two decades prior to US approval.
Terlipressin is cleaved by tissue peptidases to release lysine-vasopressin, which binds V1 receptors causing splanchnic vasoconstriction. In hepatorenal syndrome, this reverses the severe splanchnic vasodilation driven by portal hypertension, suppresses the renin-angiotensin system, and restores renal perfusion.
Terlipressin carries a boxed warning for serious or fatal respiratory failure, with higher risk in patients who have hypoxia or acute-on-chronic liver failure Grade 3. It should not be started if oxygen saturation is below 90%, and it is contraindicated in patients with ongoing coronary, peripheral, or mesenteric ischemia. Other serious risks include peripheral ischemia and skin necrosis; common effects include abdominal pain, nausea, diarrhea, dyspnea, hyponatremia, and bradycardia. Patients with serum creatinine above 5 mg/dL are unlikely to benefit.
In the pivotal CONFIRM Phase 3 trial of 300 patients (Wong et al., NEJM 2021), 32% of terlipressin-treated patients achieved verified reversal of HRS-1 versus 17% on placebo. A meta-analysis of terlipressin trials in hepatorenal syndrome supports benefit over albumin alone.
Research references
- Terlipressin plus Albumin for the Treatment of Type 1 Hepatorenal Syndrome (CONFIRM)PubMed
- Terlipressin and albumin vs albumin in patients with cirrhosis and hepatorenal syndrome: a randomized studyPubMed
- Meta-analysis: terlipressin therapy for the hepatorenal syndromePubMed
- Terlipressin Plus Albumin Is More Effective Than Albumin Alone in Improving Renal Function in Patients With Cirrhosis and Hepatorenal Syndrome Type 1PubMed