Abstract
▴ Zaleplon is a nonbenzodiazepine sedative-hypnotic which acts as a selective agonist at the benzodiazepine ω1 (type 1) receptor.
▴ In comparison with placebo, zaleplon 10mg taken at bedtime has been shown to significantly reduce sleep latency in both polysomnographic and subjective assessments.
▴ Zaleplon 5 and 10mg significantly reduced median time to sleep onset compared with placebo after the first and second weeks of a randomised double-blind study in 422 elderly patients with insomnia. Similarly, zaleplon 10 and 20mg significantly reduced subjective sleep latency from that with placebo throughout a 4-week trial in 574 patients with insomnia.
▴ There was no evidence of next-day psychomotor impairment with zaleplon 10mg. In contrast, significant impairments were seen with flurazepam 30mg, zolpidem 20mg, triazolam 0.25mg and zopiclone 7.5mg in some comparative trials.
▴ The tolerability profile of zaleplon was similar to that of placebo in clinical trials, and use of zaleplon was not associated with rebound insomnia or other withdrawal effects.
Similar content being viewed by others
References
Becker PM, Jamieson AO, Brown WD. Insomnia. Use of a decision tree to assess and treat. Postgrad Med 1993 Jan; 93(1): 66–80, 85
Wagner J, Wagner ML, Hening WA. Beyond benzodiazepines: alternative pharmacologic agents for the treatment of insomnia. Ann Pharmacother 1998 Jun; 32: 680–91
Kupfer DJ, Reynolds CF III. Management of insomnia. N Engl J Med 1997 Jan 30; 336: 341–6
Beer B, Clody DE, Mangano R, et al. Areview of the preclinical development of zaleplon, a novel non-benzodiazepine hypnotic for the treatment of insomnia. CNS Drug Rev 1997; 3(3): 207–24
Sanger DJ. Behavioural effects of novel benzodiazepine (ω) receptor agonists and partial agonists: increases in punished responding and antagonism of the pentylenetetrazole cue. Behav Pharmacol 1995; 6(2): 116–26
Vanover KE, Barrett JE. Evaluation of the discriminative stimulus effects of the novel sedative-hypnotic CL 284, 846. Psychopharmacology 1994 Jul; 115: 289–96
Walsh JK, Fry J, Erwin CW, et al. Efficacy and tolerability of 14-day administration of zaleplon 5mg and 10mg for the treatment of primary insomnia. Clin Drug Invest 1998 Nov; 16(5): 347–54
Dietrich B, Farr I. Zaleplon: dose-response evaluation in primary insomnia [abstract]. Sleep Res 1995; 24A: 116
Walsh JK, Pollack CP, Scharf MB, et al. Lack of residual sedation following middle-of-the-night zaleplon administration in sleep maintenance insomnia. Philadelphia (PA): Wyeth-Ayerst Research, 1998. (Data on file)
Dietrich B, Emilien G, Salinas E. Efficacy of zaleplon on sleep and daytime performance in a phase-advanced sleep model. Philadelphia (PA): Wyeth-Ayerst Research, 1998. (Data on file)
Troy SM, Lucki I, Unruh MA, et al. Comparison of the effects of zaleplon, zolpidem, and triazolam on memory, learning, and psychomotor performance. Philadelphia (PA): Wyeth-Ayerst Research, 1998. (Data on file)
Ware JC, Allen R, Scharf MB, et al. An evaluation of residual sedation following nighttime administration of 10 or 20 mg of zaleplon, 30 mg of flurazepam, or placebo in healthy subjects [abstract no. 313.C]. Sleep 1998; 21 Suppl. : 263
Vermeeren A, Danjou PE, O’Hanlon JF. Residual effects of evening and middle-of-the-night administration of zaleplon 10 and 20 mg on memory and actual driving performance. Hum Psychopharm 1998 Nov; 13 Suppl. 2: 98–107
Rosen AS, Fournié P, Darwish M, et al. Zaleplon pharmacokinetics and absolute bioavailability. Biopharm Drug Dispos 1999. In press
Greenblatt DJ, Harmatz JS, von Moltke LL, et al. Comparative kinetics and dynamics of zaleplon, zolpidem, and placebo. Clin Pharmacol Ther 1998 Nov; 64(5): 553–61
Lee W-H, Amorusi P, DeMaio W, et al. Metabolic disposition of radiolabeled zaleplon (CL-284,846) in healthy male volunteers. Philadelphia (PA): Wyeth-Ayerst Research, 1998. (Data on file)
Beer B, Ieni JR, Wu W-H, et al. A placebo-controlled evaluation of single, escalating doses of CL 284,846, a non-benzodiazepine hypnotic. J Clin Pharmacol 1994; 34: 335–44
Vanover KE, Mangano RM, Barrett JE. CL 284,846, a novel sedative-hypnotic: evaluation of its metabolites for pharmacological activity in vitro and in vivo. Drug Dev Res 1994 Sep; 33: 39–45
Darwish M, Martin PT, Cevallos WH, et al. Rapid disappearance of zaleplon from breast milk after oral administration to lactating women. J Clin Pharmacol 1999. In press
Élie R, Davignon M, Emilien G. Zaleplon decreases sleep latency in outpatients without producing rebound insomnia after 4 weeks of treatment [abstract no. 151]. J Sleep Res 1998; 7(2 Suppl. ): 76
Hedner J, Emilien G, Salinas E. Improvement in sleep latency and sleep quality with zaleplon in elderly patients with primary insomnia [abstract no. 229]. J Sleep Res 1998; 7(2 Suppl. ): 115
Fry J, Scharf MB, Berkowitz DV, et al. A phase III, 28 day, multicenter, randomized, double-blind comparator-and placebo-controlled, parallel-group safety, tolerability, and efficacy study of 5, 10, and 20 mg of zaleplon, compared with 10 mg of zolpidem or placebo, in adult outpatients with insomnia [abstract no. 312.C]. Sleep 1998; 21 Suppl. : 262
Rush CR, Frey JM, Griffiths RR. Zaleplon and triazolam in humans: acute behavioral effects and abuse potential. Psychopharmacology 1999. In press
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Hurst, M., Noble, S. Zaleplon. Mol Diag Ther 11, 387–392 (1999). https://doi.org/10.2165/00023210-199911050-00006
Published:
Issue Date:
DOI: https://doi.org/10.2165/00023210-199911050-00006