Terlipressin

Terlipressin
Cat. No.
BT17493
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 98.0% as determined by:
(a) Analysis by RP-HPLC.
(b) Analysis by SDS-PAGE.
Usage
Prospec's products are furnished for LABORATORY RESEARCH USE ONLY. The product may not be used as drugs, agricultural or pesticidal products, food additives or household chemicals.
Shipped with Ice Packs
In Stock

Description

Terlipressin contains 12 amino acids Gly-Gly-Gly-c[Cys-Tyr-Phe-Gln-Asn-Cys]-Pro-Lys-Gly-NH2 and having a molecular weight of 1227.37 Dalton.

Product Specs

Introduction
Terlipressin, a synthetic analog of the naturally occurring hormone antidiuretic hormone (ADH) or vasopressin, exerts its effects through two primary mechanisms. Firstly, it induces vasoconstriction, narrowing blood vessels and thereby restricting blood flow to specific areas of the body. Secondly, it acts on renal receptors to promote water retention, preventing excessive water loss through urine. Terlipressin finds clinical application in the management of bleeding esophageal varices, which are fragile, dilated veins that can develop in various parts of the body, including the esophagus. These varices arise due to increased blood pressure, often associated with conditions like severe liver disease, and pose a risk of rupture and life-threatening bleeding. By constricting blood vessels and limiting blood flow to the varices, terlipressin effectively controls bleeding.
Description
Terlipressin is a peptide composed of 12 amino acids with the sequence Gly-Gly-Gly-c[Cys-Tyr-Phe-Gln-Asn-Cys]-Pro-Lys-Gly-NH2. Its molecular weight is 1227.37 Daltons.
Physical Appearance
Terlipressin appears as a sterile, white powder obtained through lyophilization (freeze-drying).
Formulation
The lyophilized powder contains a concentration of 1 mg/ml of terlipressin protein without any additional additives.
Solubility
To reconstitute lyophilized Terlipressin, it is recommended to dissolve it in 18MΩ-cm H2O to a concentration of at least 100 µg/ml. Further dilutions can be made in other aqueous solutions as needed.
Stability
Lyophilized Terlipressin exhibits stability at room temperature for up to 3 weeks; however, it is recommended to store it desiccated at temperatures below -18°C. After reconstitution, Terlipressin should be stored at 4°C for a period of 2-7 days. For longer-term storage, freezing at temperatures below -18°C is recommended. To enhance long-term stability, adding a carrier protein (0.1% HSA or BSA) is advised. Avoid repeated freeze-thaw cycles.
Purity
The purity of Terlipressin is greater than 98.0%, as determined by two analytical methods: Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC) and Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis (SDS-PAGE).

Product Science Overview

Chemical Structure and Mechanism of Action

Terlipressin is a prodrug of lypressin, also known as lysine vasopressin. Compared to endogenous vasopressin, terlipressin has a longer half-life and increased selectivity for the V1 receptor . This selectivity makes it a potent vasopressor, meaning it can constrict blood vessels and increase blood pressure effectively .

Medical Uses

Terlipressin is indicated for several medical conditions, including:

  • Hepatorenal Syndrome (HRS): Terlipressin is used to improve kidney function in adults with hepatorenal syndrome, particularly those with a rapid reduction in kidney function . It is important to note that patients with a serum creatinine level greater than 5 mg/dL are unlikely to benefit from this treatment .
  • Esophageal Varices Bleeding: Terlipressin is effective in treating bleeding caused by esophageal varices, which are enlarged veins in the esophagus that can rupture and bleed .
Approval and Availability

Terlipressin was first approved by the U.S. Food and Drug Administration (FDA) in September 2022 . It is available under various brand names, including Terlivaz . The drug is also available in several countries, including the United States, New Zealand, Australia, the European Union, India, Pakistan, and the UAE .

Contraindications and Precautions

Terlipressin is contraindicated in individuals experiencing hypoxia or worsening respiratory symptoms, as well as those with ongoing coronary, peripheral, or mesenteric ischemia . Additionally, it may cause fetal harm when used during pregnancy .

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