Drug intelligence / Profile preview

hypertonic saline + terlipressin

Development stage
Phase 3
Lead developer
Mallinckrodt
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination therapy consisting of hypertonic saline and terlipressin. Terlipressin is a vasopressin analogue with a longer half-life that can be administered by bolus injection. It acts on vasopressin receptors, causing vasoconstriction in the splanchnic vasculature, which helps reverse splanchnic arterial vasodilation, reduce portal hypertension, and increase effective arterial blood volume and mean arterial pressure. Hypertonic saline is often used in combination with albumin in some clinical contexts. The combination of hypertonic saline, albumin, and terlipressin has been studied in animal models of hemorrhagic shock. One important clinical consideration is that terlipressin can induce hyponatremia, and in such cases, hypertonic saline (3% sodium chloride) may be administered to prevent continuous decrease in serum sodium. In clinical practice, terlipressin is typically administered by intravenous bolus or continuous IV infusion, with dosages varying based on the specific condition being treated. For hepatorenal syndrome, the initial dosage is often 0.85 mg every 6 hours by slow intravenous bolus injection, with potential adjustments based on serum creatinine response. Research has shown that in pediatric animal models of hypovolemic shock, the combination of terlipressin with hypertonic albumin did not produce better results than hypertonic albumin alone in terms of hemodynamic and perfusion parameters.

02

Targets

AVPR1A (Arginine vasopressin receptor 1A)AVPR2 (Arginine vasopressin V2 receptor)

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