Mechanism of action

Mechanism of action

Zolpidem binds with high affinity to the α₁ containing GABA_A receptors, about 10-fold lower affinity for those containing the α₂, α₃-GABA_A receptor subunits, and with no appreciable affinity for α₅ subunit containing receptors.^[20] Like the vast majority of benzodiazepine like molecules, zolpidem has no affinity for α₄ and α₆ subunit containing receptors.^[21] Zolpidem positively modulates GABA_A receptors, probably by increasing the GABA_a receptor complexes apparent affinity for GABA, without effect desensitization, or peak current.^[22]

A meta-analysis of the randomised controlled clinical trials which compared benzodiazepines against Z drugs has shown that there are few consistent differences between zolpidem and benzodiazepines in terms of sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia and daytime alertness.^[23]