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English name: Terlipressin acetate

CAS number: 14636-12-5

Molecular formula: C52H74N16O15S2

Molecular weight: 1227.37

EINECS Number: 238-680-8

Melting point:>170°C(dec.)

Boiling point: 1824.0±65.0°C (Predicted)

Density: 1.46±0.1g/cm3(Predicted)

Terlipressin (trade names Teripress by New Medicon Pharma and Glypressin by Ferring Pharmaceuticals) is an analogue of vasopressin used as a vasoactive drug in the management of hypotension. It has been found to be effective when norepinephrine does not help.
Indications for use include norepinephrine-resistant septic shock and hepatorenal syndrome. In addition, it is used to treat bleeding esophageal varices.
 
Between the patients with cirrhosis of the liver into the portal circulation of each vein and venous congestion can occur in vascular anastomosis, portal vein pressure rise phenomenon. The most frequently appeared in the azygos vein anastomosis with lower esophageal varices, instant tube.

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Application

This product is pressurized prodrug hormone, vasopressin glycyl in injection into the blood after enzymatic hydrolysis in the molecule is produced a continuous low level. The portal venous pressure it generates the desired effect, but the changes of arterial blood pressure than the use of vasopressin after much smaller, and the blood of a few do not increase the fibrinolytic. Push once its role can be maintained for about 4 ~ 6h.

Terlipressin, whose chemical name is triglycyllysine vasopressin, is a new synthetic long-acting vasopressin preparation. It is a kind of prodrug, which is inactive by itself. It is acted by aminopeptidase in vivo to slowly "release" the active lysine vasopressin after removing the three glycyl residues at its N-terminus. Therefore, terlipressin acts as a reservoir that releases lysine vasopressin at a steady rate.

Terlipressin can improve liver and kidney function, reverse HRS, and prolong the survival time of HRS patients, so it prolongs the waiting time for liver transplantation. At the same time, terlipressin is an important treatment drug for patients with esophageal variceal bleeding in emergency situations, and it is the only drug that has been shown to prolong the survival time of patients with esophageal varices bleeding. In addition, terlipressin has a certain effect in the treatment of refractory shock, cirrhotic ascites, intraoperative hypotension and cardiac arrest in children, and has a good clinical application prospect.