Dosing and uses of Lunesta (eszopiclone)
Dosing Forms & Stengths
tablet: Schedule IV
- 1mg
- 2mg
- 3mg
Insomnia
Starting dose: 1 mg PO HS for nonelderly adults (both men and women)
Dose may be increased to 2-3 mg HS if clinically indicated
Higher doses are known to cause next morning drowsiness/impairment
Dosing Considerations
Data in adults (aged 25-40 yr) taking eszopiclone 3 mg showed blood levels may remain high enough the following morning (7.5 hr after administration) to impair activities that require alertness, including driving
Impairment to driving skills, memory, and coordination persisted as long as 11 hr after the drug was taken
Despite these long-lasting effects, patients were often unaware they were impaired
Dosage modifications
CYP3A inhibitors: Do not exceed starting dose of 1 mg HS; may increase to 2 mg if needed
Renal impairment: No dose adjustment required
Dosage adjustments may be needed when coadministered with other CNS depressants to avoid additive effects
Hepatic impairment
- Mild-to-moderate: No dose adjustment required
- Severe: 1 mg PO HS
Administration
Take immediately before bedtime, with at least 7-8 hr remaining before the planned before awakening
Taking with or immediately after a heavy, high-fat meal results in slower absorption and would be expected to reduce efficacy
Pediatric dosage forms and strengths
Safety and efficacy not established
Geriatric dosage forms and strengths
Insomnia
Starting dose: 1 mg PO HS recommended for elderly or debilitated individuals
Not to exceed 2 mg total dose
Higher doses are known to cause next morning drowsiness/impairment
Lunesta (eszopiclone) adverse (side) effects
>10%
Headache (13-21%)
Unpleasant taste (17-34% in non-elderly)
1-10%
Abnormal dreams (elderly)
Accidental injury (elderly)
Diarrhea
Dizziness
Dry mouth
Dyspepsia
Nervousness
Neuralgia
Pain
Pruritus
Rash (in non-elderly)
Somnolence
Unpleasant taste (elderly)
UTI
<1%
Agitation
Alopecia
Angioedema
Asthma
Anorexia
Cystitis
Dysphagia
Fever
Epistaxis
Hypertension
Hostility
Hypercholesterolemia
Hypokalemia
Postmarketing Reports
Dysosmia
Warnings
Contraindications
Documented hypersensitivity
Cautions
Take immediately before going to bed - taking earlier may cause memory loss, hallucinations, dizziness, lightheadedness
Can impair daytime function in some patients at the higher doses (2 mg or 3 mg), even when used as prescribed; monitor for next day next-day psychomotor impairment
Take only when able to have a full night of sleep (7-8 hr); coadministration with other sedative-hypnotics at bedtime or taking eszopiclone the middle of the night is not recommended because of risk for next-day psychomotor impairment
May cause CNS depression and impair physical and mental abilities
May worsen clinical depression
May cause abnormal thinking & bizarre behavior
May impair ability to drive or operate heavy machinery
Caution in history of drug or substance abuse, respiratory diseases, hepatic impairment
Amnesia may occur
Sleep-driving (sleep-cooking, sleep-eating) may occur
Pregnancy and lactation
Pregnancy category: C
Lactation: excretion in milk unknown; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Lunesta (eszopiclone)
Mechanism of action
Unknown, may interact with GABA receptor complexes at binding domains allosterically couppled to benzodiazepine receptors
Pharmacokinetics
Absorption: Rapid (attenuated by high-fat meal)
Protein Bound: 52-59%
Peak Plasma Time: 1 hr
Half-life, elimination: 6 hr (<65 years old); 9 hr (≥65 years)
Metabolism: Primarily by CYP3A4 & CYP2E1 via oxidation & demethylation
Metabolites: (S)-zopiclone-N-oxide & (S)-N-desmethylzopiclone
Excretion: Urine (85%)
