Eszopiclone
Eszopiclone is the active (S)-enantiomer of zopiclone, licensed (as Lunesta) for insomnia. It reduces sleep latency and improves sleep maintenance and is one of the Z-drugs studied for somewhat longer-term use. It shares the class risks of dependence and complex sleep behaviours.
01 Overview
Eszopiclone is the single active enantiomer of zopiclone and is marketed in the United States as Lunesta. Clinical trials support its use for both sleep-onset and sleep-maintenance insomnia, and it has been studied over longer treatment periods than most hypnotics.
It acts at the GABA-A benzodiazepine site. Like other Z-drugs it can cause dependence, next-day impairment and complex sleep behaviours such as sleep-driving with amnesia. An unpleasant taste is a frequently reported effect.
02 Mechanism
Positive allosteric modulator at the GABA-A benzodiazepine receptor site (active S-enantiomer of zopiclone), enhancing inhibitory neurotransmission to promote sleep.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Therapeutic (adult) | 1–3 mg/day | Oral | At bedtime; start at 1 mg, elderly typically 1-2 mg. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Reduced sleep latencyFalls asleep faster, shown in controlled trials. | Clinical | ||
| Improved sleep maintenanceFewer awakenings and longer sleep, including in longer-term studies. | Clinical | ||
| SedationCNS depression that can persist into the morning. | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Dependence and rebound insomniaTolerance and dependence with continued use; rebound insomnia on stopping. | Moderate | Common with prolonged use | Clinical | |
| Complex sleep behavioursSleep-driving, sleep-walking and related behaviours with amnesia, prompting an FDA boxed warning for the Z-drug class. | Severe | Rare | Observational | |
| Next-day impairmentResidual drowsiness impairing driving and coordination. | Moderate | Common | Clinical | |
| Additive respiratory depressionDangerous with opioids or alcohol. | Life-threatening | High risk in combination | Clinical |