Polysomnographic and clinical assessment of zaleplon for the treatment of primary insomnia

Abstract

Insomnia is a heterogeneous phenomenon, defined as difficulty in initiating and maintaining sleep, and nonrestorative sleep. Chronic insomnia is a highly prevalent condition with a high level of psychosocial, occupational, health, and economic morbidity. The treatment of insomnia includes both nonpharmacologic and pharmacologic measures. The pharmacologic treatment of insomnia in the last two decades has been revolutionized by the development of the nonbenzodiazepine hypnotics, also known as the Z-drugs, including zopiclone, eszopiclone, zolpidem, and zaleplon. These drugs have proven to offer a more favorable benefit to risk profile than the benzodiazepines that preceded them, owing to their selectivity for the BZ1/ω1 receptor subtype of the GABAA receptor complex. Zaleplon is a hypnotic with a unique pharmacologic profile owing to an ultrashort half life and its selective binding of the BZ1/ω1 receptor subtype of the GABAA receptor complex. A number of studies have demonstrated the polysomnographic and clinical features of zaleplon, many predicted by its unique pharmacologic profile. Zaleplon appears to be effective in the initiation of sleep onset, with less effect on sleep maintenance parameters. It is associated with minimal next day sedative, psychomotor and memory effects, with both evening and middle-of-night dosing. It appears to possess a relatively low potential for tolerance, withdrawal, and rebound effects; abuse potential, respiratory depression, other adverse effects, and sleep architecture changes. Zaleplon, with its unique pharmacologic profile of zaleplon, offers another option to clinicians in the treatment of insomnia.