Quality Inspection for Cephapirinbenzathine - Terlipressin Acetate for Esophageal Variceal Bleeding – Gentolex

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Quality Inspection for Cephapirinbenzathine - Terlipressin Acetate for Esophageal Variceal Bleeding – Gentolex Detail:

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Name	N-(N-(N-Glycylglycyl)glycyl)-8-L-lysinevasopressin
CAS number	14636-12-5
Molecular formula	C52H74N16O15S2
Molecular weight	1227.37
EINECS Number	238-680-8
Boiling point	1824.0±65.0 °C (Predicted)
Density	1.46±0.1 g/cm3(Predicted)
Storage conditions	Keep in dark place, Inert atmosphere, Store in freezer, under -15°C.
Acidity coefficient	(pKa) 9.90±0.15 (Predicted)

Synonyms

[N-α-Triglycyl-8-lysine]-vasopressin;130:PN: WO2010033207SEQID:171claiMedprotein; 1-Triglycyl-8-lysineVasopressin; Nα-Glycyl-glycyl-glycyl-[8-lysine]-vasopressin; Nα-Glycyl-glycyl-glycyl-lysine-vasopressin; Nα-Glycylglycylglycyl-vasopressin; Nα-Gly-Gly-Gly-8-Lys-vasopressin; Terlipressin, Terlipressine, Terlipressina, Terlipressinum.

Description

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.

The pharmacological effect of terlipressin is to contract splanchnic vascular smooth muscle and reduce splanchnic blood flow (such as reducing blood flow in the mesentery, spleen, uterus, etc.), thereby reducing portal blood flow and portal pressure. On the other hand, it can also reduce plasma The effect of renin concentration, thereby increasing renal blood flow, improving renal function and increasing urine output in patients with hepatorenal syndrome. Terlipressin is currently the only drug that can improve the survival rate of patients with esophageal variceal hemorrhage. It was mainly used in the clinical treatment of variceal hemorrhage. In addition, terlipressin has also been successfully used in the liver and kidney. In general, it is likely to play a beneficial role in coexisting refractory shock and cardiopulmonary resuscitation. Compared with vasopressin, it has a long-lasting effect, does not cause dangerous complications, including fibrinolysis and serious complications in the cardiovascular system, and is simple to use (intravenous injection), which is more suitable for acute and critical care. Rescue and treatment of critically ill patients.

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