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Zolpidem (Myslee®)

Astellas Pharma Inc · FDA-approved active Small molecule

Zolpidem is a selective benzodiazepine receptor agonist that enhances inhibitory GABA signaling in the central nervous system to promote sleep onset.

Zolpidem is a selective benzodiazepine receptor agonist that enhances inhibitory GABA signaling in the central nervous system to promote sleep onset. Used for Insomnia (sleep onset and maintenance).

At a glance

Generic nameZolpidem (Myslee®)
Also known asMyslee, FK199B
SponsorAstellas Pharma Inc
Drug classSelective benzodiazepine receptor agonist (non-benzodiazepine hypnotic)
TargetGABA-A receptor (alpha-1 subunit selective)
ModalitySmall molecule
Therapeutic areaNeurology / Sleep Medicine
PhaseFDA-approved

Mechanism of action

Zolpidem binds preferentially to the alpha-1 subunit of GABA-A receptors in the brain, potentiating the effect of the inhibitory neurotransmitter GABA. This increases chloride ion influx into neurons, hyperpolarizing the cell membrane and reducing neuronal excitability. The result is sedation and facilitation of sleep initiation with minimal muscle relaxation or anticonvulsant effects 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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