eszopiclone LUNESTA
Class: Nonbenzodiazepine/CyclopyrroneFDA Indications: Insomnia
Off-Label Use: NONE
Prescribing
FDA Schedule IVForms: 1, 2, 3mg tablet
Dose Range: 1-3 mg/day
Starting: 1 mg qhs for elderly, 2-3 mg qhs otherwise
Stopping: Taper to avoid rebound insomnia
Precautions
Contraindications: None, other than patients with known hypersensitivity to eszopicloneSerious Side Effects: "complex" behaviors i.e., somnambulism, sleep related eating and sleep-driving
Side Effects: dysgeusia, headache, daytime somnolence, amnesia
Pharmacodynamics
1° MOA: GABAAR α1 subunit agonistTarget: GABAA α1
Pharmacokinetics
t½: 6 (6-9)° TMAX: 1°Absorption Rate: Rapid
Substrate of: 3A4; 2E1
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - caution with other CNS-depressants
- - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
Misc
- - longest t½ of the nonbenzodiazepine hypnotics
- - only hypnotoic FDA approved for long-term use
- - preferential binding of GABAAR α1 subunits > α2/α3 subunits → sedation > anxiolysis
Special Populations
Category C—Based on animal data, may cause fetal harm
RID 1.5%; probably safe, but studies incomplete
Start at 1mg qhs, max dose 2 mg
2019 BEE℞S Recommendation: Avoid. Nonbenzodiazepine benzodiazepine receptor agonist hypnotics (ie, Z drugs) have adverse events similar to those of benzodiazepines in older adults (eg, delirium, falls, fractures); increased emergency room visits/ hospitalizations; motor vehicle crashes; minimal improvement in sleep latency and duration.
No dosage adjustment necessary.
No dosage adjustment for mild-moderate impairment; for severe impairment start at 1 mg, max dose 2 mg
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