Core pharmacology

Class Group

Vasopressin Analogue

Legacy Cicm Level

Level 2

Introduction

analogue of vasopressin – Prodrug
Peiptidases  Lysine vasopressin

used as a vasoactive drug in the management of hypotension. It has been found to be effective when norepinephrine does not help

Longer duration of action than Vasopressin

Indications Uses

Commonly used to stop bleeding of varices in the food pipe (oesophagus).

Hepatorenal syndrome

Chemical Pharmaceutics

Prodrug of lysine Vasopressin

Presentation

IV

Main Action

Acts at the GPCR Vasopressin receptors

Mechanism of action

Acts at the GPCR Vasopressin receptors
V1 on vascular smooth muscle - vasoconstrictive
V1 on platelets - increase platelet aggregation
V2 on the nephron - antidiuretic actions

Physiological effects

Vasoconstriction
Increased platelet aggregation
Antidiuretic

Adverse Effects Toxicity

Hyponatraemia with H2O retention
May cause severe vasoconstriction -CVC only
Arrhythmias at higher doses
GIT smooth muscle constriction
cramping, nausea, diarrhoea

Absorption

IV only

Protein binding

30%

Volume of distribution

0.5 L/kg
Biphasic plasma curve

Metabolism

minimal

Excretion

urine

Half-life

50-70min

Route And Dose

IV
1-2mg terlipressin acetate (0.85-1.7mg Terlipressin) Q6 hourly