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Zolpidem (SL800750)

Sanofi · FDA-approved active Small molecule

Zolpidem is a sedative-hypnotic that selectively binds to benzodiazepine receptors on GABA-A channels in the central nervous system to promote sleep onset.

Zolpidem is a sedative-hypnotic that selectively binds to benzodiazepine receptors on GABA-A channels in the central nervous system to promote sleep onset. Used for Insomnia (sleep onset and maintenance), Short-term treatment of insomnia in adults.

At a glance

Generic nameZolpidem (SL800750)
SponsorSanofi
Drug classNon-benzodiazepine hypnotic (Z-drug)
TargetGABA-A receptor (alpha-1 subunit selective)
ModalitySmall molecule
Therapeutic areaNeurology / Sleep Medicine
PhaseFDA-approved

Mechanism of action

Zolpidem acts as a positive allosteric modulator of GABA-A receptors, enhancing the inhibitory effects of gamma-aminobutyric acid (GABA) and increasing chloride ion influx into neurons. This hyperpolarizes neuronal membranes and reduces neuronal excitability, leading to sedation and sleep induction. It has selective affinity for the alpha-1 subunit of GABA-A receptors, which contributes to its hypnotic properties with relatively less muscle relaxation or anticonvulsant activity compared to non-selective benzodiazepines.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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