Zaleplon: A pyrazolopyrimidine sedative-hypnotic agent for the treatment of insomnia

Background: Insomnia is the subjective complaint of poor sleep or an inadeq uate amount of sleep that adversely affects daily functioning. For the past 4 decades, treatment of insomnia has shifted away from the use of barbitur ates toward the use of hypnotic agents: of the benzodiazepine class. Howeve r, problems associated with the latter leg, next-day sedation, rebound inso mnia, dependence, and tolerance) have prompted development of other agents. Objective: This review describes the recently approved nonbenzodiazepine ag ent, zaleplon. Methods: Studies of zaleplon were identified through a search of English-la nguage articles listed in MEDLINE(R) and International Pharmaceutical Abstr acts, with no limitation on year. These were supplemented by educational ma terials from conferences. Results: The efficacy and tolerability of zaleplon have been documented in the literature. Zaleplon has been shown to improve sleep variables in compa rison with placebo. Like most hypnotic agents, zaleplon can be used for pro blems of sleep initiation at the beginning of the night, but its short dura tion of clinical effect may also allow patients to take it later in the nig ht without residual effects the next morning. Zaleplon can be taken less th an or equal to2 hours before awakening without "hangover" effects. It is ge nerally well tolerated, with headache being the most commonly reported adve rse event in clinical trials (15% -18%). Compared with flurazepam, a long-a cting benzodiazepine sedative-hypnotic agent, zaleplon causes significantly less psychomotor and cognitive impairment (P < 0.001). Zaleplon has not be en studied in pregnant women or children. The dose of zaleplon should be in dividualized; the recommended daily dose for most adults is 10 mg. Conclusions: Insomnia has a substantial impact on daily functioning. If pha rmacologic treatment is indicated for insomnia, the choice of an agent Shou ld be guided by individual patient characteristics.