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Mechanism of Action

LUNESTA (eszopiclone) is a
non-benzodiazepine hypnotic agent
that acts upon the GABA-A Receptor*

The effects of eszopiclone are due to modulation of gamma-aminobutyric acid (GABA)-A-receptor macromolecular complexes, containing alpha-1, alpha-2, alpha-3 and alpha-5 sub-units. This increases chloride conductance resulting in neuronal hyperpolarization, inhibiting neuronal transmission and causing sleep.1

Racemic zopiclone:
Effects predominantly
mediated through α1†

Eszopiclone:
Effects predominantly
mediated through α2 and α3†

Eszopiclone Molecule
Eszopiclone MOA

GABA-A Receptor: subunit composition
and eszopiclone binding site

Select Pharmacokinetics of LUNESTA*

Absorption1

Eszopiclone is rapidly absorbed

  • Time to peak concentration (tmax):
    approximately 1 hour
  • Terminal-phase elimination half-life (t1/2):
    approximately 7 hours

In healthy adults, LUNESTA does not accumulate with once-daily administration, and its exposure is dose-proportional over the range of 1 to 6 mg.

Food Effects1

  • In healthy adults, the rate of absorption of eszopiclone (tmax) was delayed by approximately 1 hour after a high fat meal
Lunesta Butterfly

Tap to see

tmax of Eszopiclone and Zopiclone1,2†

Absorption (tmax)

1 Hour Clock Less Than 2 Hours Clock

Adapted from the Product Monograph.

Absorption (tmax>)

1 Hour Clock Less Than 2 Hours Clock

Adapted from the product monograph.

*Clinical significance has not been established.

†Comparative clinical significance has not been established.

References: 1. LUNESTA® Product Monograph. Sunovion Pharmaceuticals Canada Inc. October 6, 2022. 2. Imovane® Product Monograph. Sanofi-Aventis Canada Inc. April 6, 2022.