Non-benzodiazepine hypnotic (“Z-drug”)
GABA-A receptor agonist that selectively binds to the benzodiazepine-1 (BZ1) receptor subtype, enhancing inhibitory GABAergic activity and promoting sleep onset and maintenance. Compared to other Z-drugs, it has a longer half-life, contributing to its utility in sleep-maintenance insomnia.
Insomnia, particularly when characterized by difficulty falling asleep or staying asleep
Sleep disruption in posttraumatic stress disorder (PTSD) and circadian rhythm disturbances
Oral tablet (1 mg, 2 mg, 3 mg)
Start at 1 mg p.o. nightly, taken immediately before bedtime. May be titrated to 2–3 mg as clinically indicated, using the lowest effective dose to minimize next-day impairment.
1–3 mg p.o. nightly
Half-life of approximately 6 hours, with hepatic metabolism primarily via CYP3A4. Its longer duration of action may benefit sleep maintenance but increases risk of next-day sedation, particularly in older adults.
Dysgeusia (metallic or bitter taste), sedation, dizziness, dry mouth, and next-day drowsiness
Complex sleep behaviors (e.g., sleepwalking, sleep-driving), anterograde amnesia, hallucinations, and rebound insomnia
Monitor for next-day sedation, cognitive or motor impairment, complex sleep behaviors, and mood or behavioral changes
Complex sleep behaviors, including sleepwalking, sleep-driving, and engaging in activities while not fully awake, which may result in serious injury or death.
Use caution in patients with traumatic brain injury (TBI), dementia, or other cognitive disorders due to increased risk of confusion, sedation, and impaired coordination. In older adults, eszopiclone is generally not recommended for long-term use due to risk of cognitive and motor side effects. However, it may be considered in younger patients with sleep-maintenance insomnia who have not responded to non-pharmacologic treatments, with regular reassessment for efficacy and adverse effects.