These agents have a nonbenzodiazepine structure and bind more specifically to the alpha 1 subunit of the GABA Areceptor, which is associated with sedation. This class of drugs is called nonbenzodiazepine receptor agonists. They are excellent choices for treatment of sleep-onset insomnia.
Both eszopiclone and zolpidem-CR are effective for both sleep-onset and sleep-maintenance insomnia, with a reduced abuse potential and long-term efficacy up to 6 months as compared with nonselective benzodiazepine receptor agonists.
Zaleplon (Sonata)
Sedative-hypnotic of pyrazolopyrimidine class; rapid onset of action with ultra-short duration of action; good choice for treatment of sleep-onset insomnia. Second dose can be used during middle of night without residual sedation in morning (believed to be an advantage of this hypnotic over others).
Zolpidem (Ambien, Ambien CR)
Sedative-hypnotic of imidazopyridine class; has rapid onset and duration of action; good first choice for treatment of sleep-onset insomnia; has no significant residual sedation in morning. The extended-release product (Ambien CR) consists of a coated 2-layer tablet and is useful for insomnia characterized by difficulties with sleep onset and/or sleep maintenance. The first layer releases drug content immediately to induce sleep; the second layer gradually releases additional drug to provide continuous sleep.
Eszopiclone (Lunesta)
Nonbenzodiazepine hypnotic pyrrolopyrazine derivative of the cyclopyrrolone class. The precise mechanism of action is unknown but is believed to interact with GABA-receptor at binding domains close to or allosterically coupled to benzodiazepine receptors. Indicated for insomnia to decrease sleep latency and improve sleep maintenance. Short half-life of 6 h. Higher doses (ie, 2 mg for elderly adults and 3 mg for nonelderly adults) are more effective for sleep maintenance, whereas lower doses (ie, 1 mg for elderly adults and 2 mg for nonelderly adults) are suitable for difficulty in falling asleep.
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