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Eszopiclone (Lunesta)

Non-Benzodiazepine Hypnoticprescriptionoral · inferred

S-isomer of zopiclone — cyclopyrrolone non-benzodiazepine hypnotic that selectively binds GABA-A receptors at the alpha-1 subunit. Unlike zolpidem, FDA-approved for long-term use (6-month efficacy data). Improves both sleep onset and sleep maintenance. Metabolized by CYP3A4 and CYP2E1. Metallic taste is the most common side effect. Schedule IV controlled substance.

Projected serum levels — 2 mg, once daily

Eszopiclone (Lunesta)
Eszopiclone (Lunesta) modeled serum levels, 2 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 0.25 0.50 0.75 1 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 2 mg once daily (oral).

Modeled steady state after ~1 days: peak ≈ 0.71 mg, trough ≈ 0.011 mg body load. Population-based estimate over 15 days for a 2 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Non-Benzodiazepine Hypnotic
Route modeled
Oral
Model confidence
inferred
Half-life
6 h
Common dose
2 mg
Suggested maximum
3 mg/day
Reference dose range
0.50–3 mg (single dose)
Suggested cadence
once daily
Validated against
3 mg oral — Cmax 0.030 mg/L at 1 h

Documented interactions

  • contraindicated
    Efavirenz (Sustiva) + Eszopiclone (Lunesta) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Eszopiclone (Lunesta) AUC by ~0.16x

  • contraindicated
    Rifampin + Eszopiclone (Lunesta) CYP induction

    Rifampin inducer of CYP3A4 predicted to change Eszopiclone (Lunesta) AUC by ~0.16x

  • danger
    Amlodipine (Norvasc) + Eszopiclone (Lunesta) CYP inhibition

    Amlodipine (Norvasc) reversible_inhibitor of CYP3A4 predicted to change Eszopiclone (Lunesta) AUC by ~2.15x

  • danger
    Ashwagandha (KSM-66) + Eszopiclone (Lunesta) CYP inhibition

    Ashwagandha (KSM-66) reversible_inhibitor of CYP3A4 predicted to change Eszopiclone (Lunesta) AUC by ~2.15x

  • danger
    Berberine + Eszopiclone (Lunesta) CYP inhibition

    Berberine reversible_inhibitor of CYP3A4 predicted to change Eszopiclone (Lunesta) AUC by ~2.15x

  • danger
    Black Seed Oil (Nigella sativa / Thymoquinone) + Eszopiclone (Lunesta) CYP inhibition

    Black Seed Oil (Nigella sativa / Thymoquinone) reversible_inhibitor of CYP3A4 predicted to change Eszopiclone (Lunesta) AUC by ~2.15x

Serum checks 68 modeled interaction pairings for eszopiclone (lunesta) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Six-month, randomized, double-blind, placebo-controlled study of eszopiclone in patients with chronic insomnia Krystal AD et al. · Sleep, 2003 DOI

    Pivotal 6-month RCT (788 patients) demonstrating eszopiclone 3 mg maintained efficacy without tolerance development, making it the first hypnotic with FDA approval for long-term insomnia treatment.

  2. Pharmacokinetics of eszopiclone: a review Najib J · Clinical Pharmacokinetics, 2006 DOI

    PK review establishing eszopiclone half-life of 6 hours, rapid absorption (tmax ~1h), 52% bioavailability, CYP3A4/2E1 metabolism, and dose-proportional pharmacokinetics across the 1-3 mg range.

2 published studies referenced in the app, each with a plain-language summary.