Terlipressin Acetate Salt CAS 14636-12-5

Terlipressin acetate Introduction

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Terlipressin acetate is a novel artificially synthesized long-acting vasopressin preparation with high selectivity for vasopressin V1 receptor. Its CAS number: 14636-12-5; Molecular formula: C52H74N16O15S2; Molecular weight: 1227.38; EINECS Number: 238-680-8.It is a Preparatory productthat is inherently inactive. After undergoing the action of aminopeptidase in the body, the N-terminal three glycyl residues are removed, and active lysine vasopressin is slowly "released". Therefore, Terlipressin Acetate salt is equivalent to a reservoir that can release lysine vasopressin at a stable rate. High purity t-GLVP is a white or off white block or powder, or a colorless clear solution. In clinical practice, it can rapidly reduce HVPG and provide faster, stronger, and more durable treatment for complications of portal hypertension.

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What are the pharmacological effects of Terlipressin Acetate salt ?

Terlipressin Acetate salt powder is a synthetic polypeptide, which is an analogue of hormone secreted by the posterior pituitary gland. After use, its triglyceride will be cut off by enzymes in vivo and slowly release active substances such as vasopressin, which will contract smooth muscle for 10 hours. Compared with the same dose of vasopressin, its activity can only be maintained for 20-40 minutes, which is a great advantage. Moreover, due to the slow enzymolysis speed of this product, the circulating lysine vasopressin can not reach the poisoning level, so it not only has a good function of maintaining the effect of the product, but also is very safe, and it is difficult to cause adverse consequences due to the frequent use of conventional vasopressin to maintain the effect. In addition, terlipressin acetate has two functions: first, it has obvious vasoconstrictive effect, especially reducing the contraction of visceral vascular smooth muscle, reducing visceral blood flow (such as reducing the blood flow of mesentery, spleen, uterus, etc.), so that venous blood flows to the hepatic portal vein system, which reduces portal vein blood pressure and has hemostatic effect; Second, this product can also reduce the plasma renin concentration, and act on some receptors on the kidney, thus increasing the renal blood flow of patients with hepatorenal syndrome, preventing excessive loss of water in urine, and having anti-enuresis function.

What is the evaluation of the clinical effect of Terlipressin acetate?

Terlipressin is the only product that can improve the survival rate of patients with esophageal variceal bleeding. It used to be mainly used to treat esophageal variceal bleeding in clinic. In addition,Hot sales Terlipressin has been successfully used in comprehensive treatment of liver and kidney, and it is likely to play a beneficial role in refractory shock and cardiopulmonary resuscitation. Compared with conventional vasopressin, it has a long-lasting effect, does not cause dangerous complications, including fibrinolysis and serious complications in cardiovascular system, and is simple in use and low in frequency, so it is very suitable for the rescue and treatment of critical patients. In the treatment of hepatorenal syndrome, the best-selling terlipressin can improve liver and kidney function, reverse HRS and prolong the survival time of HRS patients, so it can also prolong the waiting time of liver transplantation. As a highly selective vasopressin V1 receptor agonist, it has a better development prospect in the study of Norepinephrine-resistant septic shock. In addition, Terlipressin Acetate salt has certain anti-inflammatory and antioxidant effects, and has a certain role in the treatment of refractory shock, ascites due to cirrhosis, hypotension during operation and cardiac arrest in children, which has a good clinical application prospect.

What are the side effects of Terlipressin Acetate salt?

The use of terlipressin to treat esophageal variceal bleeding may result in the following adverse reactions:
Due to its ability to constrict blood vessels, patients may experience facial and surface pallor, as well as a slight increase in blood pressure (more pronounced in hypertensive patients).
2. A small number of patients may experience arrhythmia, bradycardia, and insufficient coronary artery blood supply.
3. Occasional headaches or local necrosis may occur.
4. It may enhance peristaltic movement and cause abdominal pain, nausea, and diarrhea.
5. In some cases, bronchial muscle spasms may occur, which may lead to difficulty breathing.
6. There may be uterine muscle spasms and blood circulation disorders in the uterine muscles and endometrium.
Although the antidiuretic activity of terlipressin acetate is only 3% of that of natural vasopressin, there have been very few reported cases of hyponatremia and hypocalcemia, especially in patients with fluid imbalance.

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FAQ:

Q1:What makes Terlipressin acetate more effective than the body's own "vasopressin"?
It is equivalent to a "slow-release" product. After use, the enzymes in the body will gradually remove the three amino acids at the end of it, releasing the active substances gradually. Therefore, the effect is more stable and lasting, unlike natural oxytocin which comes on strong and has significant side effects. This design is very ingenious, turning itself into a "storage facility".
Q2:How did it stop the massive bleeding in the esophagus?

Its mechanism of stopping bleeding is quite straightforward: it forcefully constricts the blood vessels in the internal organs. Esophageal varices are like balloons that have been blown too large. Once they rupture, blood will flow continuously. Terlipressin acetate can cause the blood vessels supplying these varicose veins to constrict, reducing the blood flow into the portal vein, thereby lowering the pressure and relieving the pressure on the ruptured "balloon", achieving the purpose of stopping the bleeding.

Q3:What feelings or reactions will occur after using it?

The most common symptom is a pale complexion and skin, as the peripheral blood vessels constrict. At the same time, blood pressure will rise, and may be accompanied by abdominal pain, nausea, diarrhea and headache.

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