Small molecule
PubChem CID 5732
Zolpidem
Ambien
- Mechanism of action
- GABA-A receptor positive modulator (non-benzodiazepine hypnotic)
- In plain language
- Boosts the effect of GABA, the brain's main natural 'slow down' chemical, at one specific type of receptor closely tied to falling asleep, without belonging to the older class of benzodiazepine sedatives.
- How it works
- Zolpidem (Ambien) is a non-benzodiazepine hypnotic of the imidazopyridine class. Per the FDA label, it is a GABA-A receptor positive modulator presumed to exert its therapeutic effect in the short-term treatment of insomnia through binding to the benzodiazepine site of alpha-1 subunit-containing GABA-A receptors, increasing the frequency of chloride channel opening and inhibiting neuronal excitation. Zolpidem binds with greater affinity to alpha-1-containing receptors relative to alpha-2 and alpha-3 subtypes and has no appreciable affinity for alpha-5-containing receptors, which may explain the relative absence of myorelaxant effects seen in animal studies.
- Therapeutic applications
- Zolpidem (Ambien) is FDA-indicated for the short-term treatment of insomnia characterized by difficulties with sleep initiation; efficacy in decreasing sleep latency has been demonstrated in controlled trials of up to 35 days. It is a Schedule IV controlled substance. It carries a boxed warning for complex sleep behaviors, including sleep-walking, sleep-driving, and engaging in other activities while not fully awake, some of which have resulted in serious injury or death; the label directs that zolpidem be discontinued immediately if a patient experiences a complex sleep behavior.
- Class
- Small molecule
- Therapeutic area
- CNS / Sleep
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