Eszopiclone

LUNESTA

Open Eszopiclone in the interactive console ↗

What it isNon-benzodiazepine GABA-A modulator; insomnia, particularly sleep maintenance.

Why this oneA longer half-life than zolpidem, so it holds sleep through the night, and it is licensed for long-term use.

What limits itNext-morning impairment and a metallic taste. Complex sleep behaviors as for the class; dose is halved in the elderly.

FDA-approved for

insomnia (2004)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Complex sleep behaviors (sleep-walking, sleep-driving, and other activities while not fully awake) may occur and can cause serious injury or death.

FDA dosing	Population	Start	Target	Max
Insomnia	Adults	1 mg QHS	1-3 mg QHS	3 mg QHS
Insomnia	Elderly / debilitated	1 mg QHS	1-2 mg QHS	2 mg QHS

Renal Undefined

Hepatic Severe hepatic impairment: do not exceed 2 mg

Max 3 mg; do not exceed 2 mg in elderly/debilitated patients, severe hepatic impairment, or with potent CYP3A4 inhibitors

Instructions

Take immediately before bedtime with at least 7-8 hours remaining before awakening
Do not take with or immediately after a heavy, high-fat meal
Taper to discontinue to avoid withdrawal effects

Contraindications

Prior complex sleep behaviors after taking eszopiclone

Cautions

CNS depression and next-day impairment (esp. 3 mg; caution driving)
Anaphylaxis and angioedema (do not rechallenge)
Abnormal thinking and behavioral changes
Worsening depression / suicidal thinking
Withdrawal effects with rapid reduction/discontinuation
Caution in elderly and impaired respiratory/hepatic function

Adverse reactions

Unpleasant taste (dysgeusia)
Headache
Somnolence
Respiratory infection
Dizziness
Dry mouth
Rash
Anxiety
Hallucinations

Pregnancy Insufficient human data; animal studies show offspring toxicity

Lactation Undefined

⚠ BOXED WARNING

Complex sleep behaviors including sleepwalking and sleep-driving

Cost, est. cash$5–$150/month

Generic entry2011

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability3 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityComplex sleep behaviors, next-day impairment and additive CNS depression.

Mechanism of action: Eszopiclone ballicule

Eszopiclone ballicule: receptor binding, kinetics and half-life diagram

Open Eszopiclone in the interactive console ↗

Memory aids: mascots and interaction avatars

Eszopiclone LUNESTA mascot mnemonic cartoon — **“Lunar Easy pic”**
Z-drug

CYP3A4 substrate

Open Eszopiclone in the interactive console ↗