Terlipressin acetate injection, as a first-line emergency pharmacotherapy strongly recommended by major international and domestic practical medical guidelines, plays a pivotal role in the rescue and standardized treatment of gastroesophageal and gastric variceal rupture hemorrhage. This critical practical medical condition is a severe, life-threatening portal hypertensive crisis, predominantly triggered by decompensated liver cirrhosis and persistent elevated portal pressure. It is typically marked by abrupt onset, sudden massive upper gastrointestinal hemorrhage, rapid progression of hemodynamic instability, and an alarmingly high short-term mortality rate, which brings enormous difficulties and severe challenges to emergency rescue and practical medical comprehensive management.
Our Products Description
Terlipressin Acetate COA
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| Certificate of Analysis | ||
| Compound name | Terlipressin Acetate | |
| Grade | Pharmaceutical grade | |
| CAS No. | 14636-12-5 | |
| Quantity | 36g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090086 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.54% |
| Loss on drying | ≤1.0% | 0.42% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.98% |
| Single impurity | <0.8% | 0.52% |
| Total microbial count | ≤750cfu/g | 95 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 500ppm |
| Storage |
Store in a sealed, dark, and dry place below -20°C |
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| Chemical Formula | C52H74N16O15S2 |
| Exact Mass | 1226.50 |
| Molecular Weight | 1227.38 |
| m/z | 1226.50 (100.0%), 1227.50 (56.2%), 1228.50 (15.5%), 1228.49 (9.0%), 1227.49 (5.9%), 1229.50 (5.1%), 1228.50 (3.3%), 1228.50 (3.1%), 1229.51 (2.8%), 1229.50 (1.7%), 1227.50 (1.6%), 1230.50 (1.4%) |
| Elemental Analysis | C, 50.89; H, 6.08; N, 18.26; O, 19.55; S, 5.22 |
Once acute variceal bleeding occurs, patients are exposed to extremely high risks of subsequent complications including hemorrhagic shock, hepatic encephalopathy, spontaneous infection and multiple organ dysfunction syndrome, rendering timely, standardized and targeted practical medical intervention extremely critical to improve survival outcomes. The core therapeutic objectives in the acute bleeding phase center on achieving rapid and sustained haemostasis, stabilizing systemic circulatory homeostasis, lowering abnormally elevated portal venous tension, and blocking the continuous deterioration of liver function and systemic condition.
As a synthetic vasopressin analog with definite pharmacological activity, tarlipressin acetate injection can effectively constrict splanchnic regional blood vessels, reduce splanchnic blood perfusion volume, and further lower portal venous pressure, thereby markedly decreasing the blood flow and perfusion pressure inside gastroesophageal and gastric varices to exert a stable and reliable hemostatic effect.It exerts a key therapeutic value throughout the entire management process, including controlling acute massive bleeding, maintaining hemostatic stability, and reducing the risk of early rebleeding. With its stable efficacy and favorable safety profile, this injection significantly improves the success rate of emergency treatment, lowers mortality, and provides essential support for improving the long‑term prognosis of patients with cirrhosis‑related variceal bleeding.
The core pharmacological mechanism of Tarlipressin regulating bleeding
It achieves precise targeting to control gastroesophageal and gastric variceal bleeding, and the specific mechanism can be divided into two points:
The drug releases active metabolites after enzymatic hydrolysis in the body, selectively stimulating the V1 receptor of the visceral microcirculation arterial plexus, mediating moderate spasm of vascular smooth muscle, reducing the amount of portal system reflux bloodstream, downregulating portal tension from the root, relieving bloodstream stasis in varicose veins, and reducing bloodstreamflow shock at the site of vascular rupture. Compared with endogenous vasopressin.
Its affinity for V1 receptor is significantly increased, and its action site is more concentrated in the visceral vascular area, avoiding non selective constriction of systemic bloodstream vessels.
This not only ensures the accuracy of portal tension regulation, but also reduces the risk of tissue hypoperfusion caused by extensive vascular constriction, laying a pharmacological foundation for rapid control of acute bleeding.
For the bloodstream supply branches of gastroesophageal and gastric varices, it can regulate the tension of bloodstream vessel walls, contract abnormally dilated collateral circulation vessels, reduce the perfusion of diseased veins, accelerate the contraction and closure of small bloodstream vessels around the hemorrhage lesion, promote the initiation of coagulation mechanism, achieve rapid haemostasis, and have minimal non-specific impact on the peripheral vascular system of the whole body.
This drug can directly act on the vascular smooth muscle cells around varicose veins, inducing vasoconstriction by regulating intracellular calcium ion concentration. It can not only directly block the blood flow supply to the hemorrhage lesion, but also create favorable conditions for platelet adhesion and coagulation factor aggregation by improving the local hemodynamic environment. Under the dual action, it can achieve rapid closure of the hemorrhage lesion, and the long-acting properties of its metabolites can maintain the continuity of hemostatic effect and reduce hemostatic failure caused by vascular tension fluctuations.
Information source:
Xinmiao Zhou, et al. Tarlipressin for the treatment of acute variceal bleeding: A systematic review and meta-analysis of randomized controlled trials[J]. Medicine (Baltimore), 2018, 97(45): e13437.
Garcia-Tsao G, Bosch J. Management of varices and variceal hemorrhage in cirrhosis[J]. N Engl J Med, 2010, 362(9): 823-832.
Carbonell N, Pauwels A, Serfaty L, et al. Improved survival after variceal hemorrhage in patients with cirrhosis over the past two decades[J]. Hepatology, 2004, 40(3): 652-659.
The first-line emergency efficacy of acute massive bleeding
In the emergency scenario of acute massive hemorrhage caused by gastroesophageal and gastric variceal rupture, the first-line intervention value of terlipressin acetate injection is mainly reflected in three aspects:
(I)Efficient haemostasis
Its active metabolites have a long half-life and a sustained and stable effect.
After a single loading dose, most patients can achieve effective control of hemorrhage within 48 hours. The haemostasis response speed and stability of action are better than traditional vasopressin drugs, reducing the risk of recurrent bleeding.
Practical medical data shows that after administration of it, significant relief of hemorrhage signs can be observed within an average of 12 hours.
Compared to vasopressin, which has a haemostasis onset time of about 24 hours, this drug can more quickly block the hemorrhage process, reduce the risk of severe complications such as hemorrhagic shock and multiple organ failure, and its stable action curve avoids severe fluctuations in vascular tension caused by sudden increases and decreases in drug concentration, further reducing the probability of haemostasis failure.
(II)Adaptation to severe cases
For critically ill patients with massive hemorrhage and pre shock symptoms, this drug can quickly regulate portal tension while supplementing bloodstream volume, block hemorrhage progression, and provide a window for subsequent interventions such as endoscopy; It has a mild impact on blood tension and a low incidence of cardiovascular adverse reactions, making it suitable for high-risk patients with underlying cardiovascular diseases. For patients with pre shock symptoms such as bloodstream loss exceeding 1000ml, skin dampness and coldness, and increased heart rate, terlipressin acetate injection can quickly reduce portal tension to a safe range on the basis of liquid resuscitation, reducing the risk of venous rebleeding. At the same time, its contraction effect on coronary and peripheral bloodstream vessels is mild, and it will not worsen the basic condition of coronary heart disease and high blood pressure patients. Even if combined with cirrhosis related cardiovascular disease, it can be safely used, greatly expanding the scope of application for critically ill patients.
(III)Convenient practical medical operation
Medication can be administered through intravenous infusion or intermittent infusion, without the need for continuous intravenous pumping. The process is simple and suitable for multiple scenarios such as primary medical institutions and emergency transportation, making it easy to implement emergency interventions. In the conventional emergency plan, it only requires the initial intravenous infusion of a loading dose, followed by maintenance doses at fixed intervals, without the need for complex infusion pump control equipment. Primary healthcare institutions do not require additional specialized infusion equipment to carry out treatment; During the emergency transportation process, the intermittent administration mode is not limited by the transportation environment, and the administration rhythm can be adjusted at any time to ensure the continuous hemostatic effect during transportation, providing key guarantees for patients to be transported to higher-level hospitals for further treatment.
Information source:
S Walker, HP Kreichgauer, JC Bode. Tarlipressin versus somatostatin in the treatment of hemorrhage gastroesophageal varices--final report of a placebo-controlled, double-blind study[J]. Dig Dis Sci, 1997, 42(11): 2298-2304.
Su Xue, Zheng Sheng, Huang Yuanfei, etc Research progress on vasoactive drug therapy for gastroesophageal and gastric variceal hemorrhage [J]. Chinese Journal of Hepatology (Electronic Edition), 2024, 16 (2): 45-52
Terlipressin acetate injection therefore occupies an irreplaceable and core position in the whole-process emergency management and early intervention of esophagogastric variceal rupture and bleeding. Its stable pharmacological activity, precise hemodynamic regulatory mechanism and favorable practical medical safety tolerability enable it to quickly control acute massive hemorrhage, effectively reverse unstable circulatory status, and significantly reduce the incidence of life-threatening complications such as hemorrhagic shock, hepatic encephalopathy and multiple organ failure. Meanwhile, it can remarkably elevate the short-term survival rate of critically ill patients with decompensated liver cirrhosis and create valuable time for subsequent endoscopic treatment, interventional therapy and comprehensive liver protection management.
With the continuous advancement of practical medical research, gradual optimization of standardized medication procedures and continuous accumulation of real-world practical medical evidence, tarlipressin acetate injection will further consolidate its authoritative core status in the emergency treatment of portal hypertensive bleeding. It also provides a solid and reliable pharmacological basis for formulating more refined, individualized and standardized rescue regimens, and brings more guaranteed prognostic benefits to a wide range of liver cirrhosis patients with high bleeding risk.
References
Tripathi D, Stanley AJ, Hayes PC, et al. U.K. guidelines on the management of variceal haemorrhage in cirrhotic patients[J]. Gut, 2015, 64(11): 1680-1704.
Hepatology Group, Digestive Disease Branch, Chinese Medical Association Diagnosis and treatment guidelines for gastroesophageal and gastric variceal hemorrhage in patients with cirrhosis (2022 edition) [J]. Chinese Journal of Gastroenterology, 2022, 42 (12): 793-803
Lui HF, Chan AC. Tarlipressin in the management of acute gastroesophageal variceal bleeding: An update[J]. World J Gastroenterol, 2020, 26(38): 5892-5905.
Li Xinghai Observation of the therapeutic effect of injectable tarlipressin on gastroesophageal and gastric variceal hemorrhage [J]. Chinese Medical Guidelines, 2016, 14 (1): 131-132
European Association for the Study of the Liver. EASL practical medical Practice Guidelines on the management of variceal hemorrhage in cirrhosis[J]. J Hepatol, 2018, 69(1): 187-203.
FAQ
It mainly acts on the V1 receptors which are predominantly located in the arterial smooth muscle within the splanchnic circulation, thereby reducing the splanchnic bloodstream flow and portal tension and controlling AVB. Several meta-analyses about it for AVB have been published (Supplementary Table 1)
Tarlipressin acetate is a synthetic long-acting vasopressin analogue peptide drug. It acts on vascular V1 receptors to constrict visceral blood vessels, lower portal venous pressure, and also has mild antidiuretic effects. It features longer half-life and more stable efficacy than natural vasopressin for practical medical emergency use.
The exact mechanism of action of this is not fully understood; however, it works to cause vasoconstriction in shock and other conditions associated with vasodilation.
It is mainly used for acute gastroesophageal variceal bleeding and hepatorenal syndrome caused by portal high blood pressure. During use, blood pressure and heart rate should be monitored closely; it is contraindicated for patients with cardiovascular disease and drug hypersensitivity, and should be used cautiously in elderly and hepatorenal impaired patients.
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