Drug intelligence / Profile preview

zolpidem + lorazepam

Development stage
Preclinical
Lead developer
Sequential Medicine
Modality
Small Molecules
Administration
Oral
01

Overview

Zolpidem + lorazepam is a non-standard, investigational combination of two central nervous system depressant drugs: zolpidem, a non-benzodiazepine hypnotic used for short-term management of insomnia, and lorazepam, a benzodiazepine used primarily for anxiety, sedation, and as an adjunct for insomnia. Zolpidem acts as a positive allosteric modulator at the GABA(A) receptor, selectively binding to the benzodiazepine-1 (BZ1) site, thereby enhancing GABAergic neurotransmission which leads to sedation and hypnotic effects. Lorazepam also binds to the benzodiazepine site on the GABA(A) receptor, broadly potentiating GABA’s inhibitory effects throughout the brain to decrease anxiety, cause sedation, muscle relaxation, and provide anticonvulsant effects. The pharmacological combination would result in additive or supra-additive CNS depressant effects, increasing risks of sedation, respiratory depression, psychomotor impairment, falls, and dependence. There is no known approved fixed-dose combination of these two drugs, but a clinical trial (SM-A-02) has investigated the efficacy of combined zolpidem and lorazepam for sleep induction.

Other names
zolpidem 5 mg / lorazepam 0.5 mg combination
02

Targets

TSPO (Translocator Protein (18 kDa))Gamma-aminobutyric acid type A receptor alpha-2/alpha-3 subunit-containing benzodiazepine site (GABA-A R alpha-2/alpha-3 BZD site)GABA-A α/γ interface (Gamma-aminobutyric acid type A receptor (GABA-A receptor) alpha/gamma subunit interface)

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