Introduction
Terlipressin is an analogue of vasopressin used as a vasoactive drug in the management of hypotension which has been found to be effective when norepinephrine fails.
Uses
Terlipressin is a drug used to treat bleeding caused by esophageal varices.
Commonly used to stop bleeding of varices in the food pipe (oesophagus).
Associated Conditions
Pharmacodynamics
Terlipressin is a medicine similar to a naturally occurring hormone present in the body, known as antidiuretic hormone (ADH) or vasopressin. ADH has two main effects in the body. Firstly, it causes narrowing of blood vessels (vasoconstriction), thereby limiting blood flow to a particular area of the body. It also acts on receptors in the kidney to retain water in the body, which helps to prevent excessive loss of water in the urine.
Mechanism of Action
Terlipressin, an analogue of vasopressin, acts on three different receptors, vasopressin receptor V1a (which initiates vasoconstriction, liver gluconeogenesis, platelet aggregation and release of factor VIII), vasopressin receptor V1b (which mediates corticotrophin secretion from the pituitary) and vasopressin receptor V2 which controls free water reabsorption in the renal medullar. The binding of terlipressin to the V2 receptor activates adenylate cyclase which causes the release of aquaporin 2 channels into the cells lining the renal medullar duct. This allows water to be reabsorbed down an osmotic gradient so the urine is more concentrated.
Protein Binding
Approximately 30%
Dosage
occur.
In type 1 hepatorenal syndrome: An i.v. injection 3 to 4 mg (3x8.5ml to 4x8.5ml) terlipressin acetate every 24 hours as 3 or 4 administrations. In the absence of any reduction of the serum creatinine after 3 days of treatment, cessation of Varipress IV Injection 1 mg/8.5 ml treatment is advised. In other cases, Varipress IV Injection 1 mg/8.5 ml treatment is to be pursued until the obtaining either of a serum creatinine less than 130 µmol/litre or of a drop of at least 30% in the serum creatinine with respect to the value measured at the time of diagnosis of hepatorenal syndrome. The standard average duration of treatment is 10 days.
