Description
Terlipressin acetate is a novel synthetic long-acting vasopressin preparation. It is a kind of prodrug, which is inactive by itself. After the action of aminopeptidase in the body, after removing the three glycyl residues at its N-terminus, it slowly "releases" the active lysine vasopressin. Therefore, terlipressin acts as a reservoir that releases lysine vasopressin at a steady rate.
Chemical Properties
N-(N-(N-Glycylglycyl)glycyl)-8-L-lysinevasopressin is White Solid
Uses
N-(N-(N-Glycylglycyl)glycyl)-8-L-lysinevasopressin is an analogue of vasopressin used as a vasoactive drug in the management of hypotension. N-(N-(N-Glycylglycyl)glycyl)-8-L-lysinevasopressin is used norepinephrine-resistant septic shock and hepatorenal syndrome. N-(N-(N-Glycylglycyl)glycyl)-8-L-lysinevasopressin is also used in the treatment of acute variceal bleeding.
Definition
ChEBI: Terlipressin is a polypeptide.
Clinical Use
Treatment of bleeding oesophageal varices
Side effects
In clinical trials, the most common side effects of terlipressin administration were paleness, increased blood pressure, peripheral ischemia, abdominal pain, nausea, diarrhea, and headache.
Terlipressin related adverse events are common and most of terlipressin related adverse events were mild or moderate, which can be resolved spontaneously without any intervention. As terlipressin acts mainly on the splanchnic vessels, the incidence of severe ischemic complications is lower with terlipressin than with vasopressin. However, it may cause serious complications such as myocardial infarction, intestinal ischemia, peripheral cyanosis, and skin necrosis[1].
Drug interactions
Potentially hazardous interactions with other drugs
None known
Metabolism
Terlipressin is metabolised by tissue peptidases resulting
in the slow release of lypressin. Terlipressin is almost
completely metabolised in the kidneys and liver, with less
than 1% of terlipressin and less than 0.1% of lypressin
excreted in the urine.
References
[1] Chiang C, et al. Terlipressin-Induced Peripheral Cyanosis in a Patient with Liver Cirrhosis and Hepatorenal Syndrome. American Journal of Case Reports, 2019.
