Terlipressin acetate

Terlipressin is a prodrug form of the vasopressin peptide lysipressin and a partial agonist of the vasopressin V_1A receptor (K_i = 0.85 ?M).¹ It is also an agonist of vasopressin V_1B and V₂ receptors (K_is = 1.11 and 1.58 ?M, respectively). It increases mean arterial pressure (MAP) and decreases mortality in a rat model of uncontrolled hemorrhagic shock when administered at a dose of 15 ?g/kg.² Terlipressin (2.6 ?g/kg per hour), in combination with norepinephrine, improves vascular reactivity and increases survival time in a rat model of cecal ligation and puncture-induced septic shock and a rabbit model of LPS-induced septic shock.³ It also increases MAP in a rat model of liver cirrhosis with portal hypertension, arterial hypotension, high cardiac output, and low systemic vascular resistance.⁴

1.Colson, P.H., Virsolvy, A., Gaudard, P., et al.Terlipressin, a vasoactive prodrug recommended in hepatorenal syndrome, is an agonist of human V1, V2 and V1B receptors: Implications for its safety profilePharmacol. Res.113(Pt A)257-264(2016) 2.Lee, C.C., Lee, M.T., Chang, S.S., et al.A comparison of vasopressin, terlipressin, and lactated ringers for resuscitation of uncontrolled hemorrhagic shock in an animal modelPLoS One9(4)e95821(2014) 3.Xiao, X., Zhu, Y., Zhen, D., et al.Beneficial and side effects of arginine vasopressin and terlipressin for septic shockJ. Surg. Res.195(2)568-579(2015) 4.Fernández-Varo, G., Oró, D., Cable, E.E., et al.Vasopressin 1a receptor partial agonism increases sodium excretion and reduces portal hypertension and ascites in cirrhotic ratsHepatology63(1)207-216(2016)