Drug intelligence / Profile preview

hydroxyzine + lorazepam + melatonin

Development stage
Preclinical
Lead developer
UCB
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous, Sublingual, Transdermal
01

Overview

This is a combination of three agents—hydroxyzine, lorazepam, and melatonin—each with distinct mechanisms of action. Hydroxyzine is a first-generation antihistamine with sedative and anxiolytic properties, acting as an antagonist at the histamine H1 receptor. Lorazepam is a benzodiazepine that enhances the effect of gamma-aminobutyric acid (GABA) at GABA-A receptors in the central nervous system, producing anxiolytic, sedative, muscle relaxant, and anticonvulsant effects. Melatonin is an endogenous hormone regulating circadian rhythms; as a supplement it acts as an agonist at melatonin receptors to promote sleep onset. The combination may be used off-label for severe insomnia or anxiety but carries significant risk for additive central nervous system depression (excessive sedation, respiratory depression), especially in older adults or those with comorbidities[1][3][5].

02

Targets

MTNR1A (MT1)MTNR1B (Melatonin Receptor 2)HRH1 (Histamine H1 Receptor)GABAA (Gamma-aminobutyric acid receptor)

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