Sepracor; patent expires 2012.
Indicated for both sleep initiation and sleep maintenance. Indicated for both short-term and chronic insomnia.
Lunesta is the purified S-enantiomer of zopiclone, which is a non-benzodiazepine approved for treating insomnia in 80 countries. Binds to the GABA-benzodiazepine receptor complex, like benzodiazepines, but is more selective for the omega-1 receptor subtype than BZs.
Supplied as 1 mg light blue, 2 mg white, and 3 mg dark blue tablets.
Start at 1 mg QHS for elderly, 2-3 mg QHS otherwise.
No higher than 1 mg in hepatic impairment.
Most common: An unpleasant taste, and somnolence.
Even though it has a long half life, studies have shown little in the way of cognitive impairment even 6 hours after dosing.
Classified as a Schedule IV drug, but abuse potential is likely somewhat less than benzodiazepines.
Pregnancy Category C
Substrate of 3A4, blood level doubled by ketoconazole.
Lunesta does not affect any liver enzymes
A high fat meal delays absorption by an hour
Half life is about 6 hours, 9 hours in the elderly.
One of the few hypnotics FDA approved for long-term use, although it’s likely that all the other non-benzodiazepines are equally safe used chronically.