Pharmacodynamic profile of Zaleplon, a new non‐benzodiazepine hypnotic agent

  title={Pharmacodynamic profile of Zaleplon, a new non‐benzodiazepine hypnotic agent},
  author={Alain A. Patat and Isabelle Paty and Ian Hindmarch},
  journal={Human Psychopharmacology: Clinical and Experimental},
The challenge in developing hypnotic agents for the treatment of insomnia is to balance the sedative effect needed at bedtime with the residual sedation on awakening. Zaleplon is a novel pyrazolopyrimidine hypnotic agent that acts as a selective agonist to the brain omega1 receptor situated on the alpha1 subunit of the GABAA receptor complex. Zaleplon was proven to be an effective hypnotic drug as it consistently and significantly reduced latency to persistent sleep in insomniac patients for… 

Comparative Pharmacokinetics and Pharmacodynamics of Short-Acting Hypnosedatives

  • D. Drover
  • Biology
    Clinical pharmacokinetics
  • 2004
While zaleplon may be best indicated for the delayed onset of sleep, zolpidem and zopiclone may be better indicated for maintaining a complete night’s sleep.

Pharmacokinetic Determinants of the Clinical Effects of Benzodiazepine Agonist Hypnotics

O Ongoing pharmaceutical research has the objective of developing drug delivery innovations that can optimize hypnotic drug action by regulation of release and systemic exposure to short half-life BZ agonists.

Forensic Aspects of Hypnotic Drugs

Overall, the non-benzodiazepine hypnotics have a good safety record but professionals involved in healthcare and forensics should be aware of the potential adverse effects.

Low-dose doxepin (3 and 6 mg) for the treatment of insomnia

Low-dose doxepin offers a unique combination of potency and selectivity for H1, which may prove advantageous in the treatment of insomnia and the potential role of this compound in clinical practice is discussed.

chapter Pharmacokinetics, pharmacodynamics, and the pharmacokinetic/pharmaco-dynamic relationship of zolpidem in healthy subjects

For most effects, zolpidem’s short duration of action could be adequately described by both a sigmoid emax model and a transit tolerance model, but for spv and eeg alpha power, the tolerance model seemed less suitable.

Pharmacotherapy for insomnia.

Role of Zolpidem in the Management of Insomnia

Zolpidem is an imidazo‐pyridine compound that enhances the GABAA receptor function by interaction with Omega‐1 receptor subtype that has rapid onset of action, improves total sleep duration, and reduces night‐time awakenings.

Newer hypnotic drugs for the short-term management of insomnia: a systematic review and economic evaluation.

The systematic review provided in this report suggests that an agnostic approach to cost-effectiveness is required for the use of hypnotic drugs for insomnia and it is suggested that further consideration should be given to a formal trial to allow head-to-head comparison of some of the key drugs in a double-blind RCT lasting at least 2 weeks, and of sufficient size to draw reasonable conclusions.

In the Zzz Zone: The Effects of Z-Drugs on Human Performance and Driving

  • N. Gunja
  • Psychology
    Journal of Medical Toxicology
  • 2013
The risk–benefit analysis of Z-drugs in the treatment of insomnia, particularly in the elderly, may not favor treatment due to the increased risks of falls and motor vehicle collisions.



Zolpidem. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential.

While zolpidem aids sedation, and may reduce memory or psychomotor function within the first 2 hours after administration of single oral doses, its use as a surgical premedicant remains to be established.

Zopiclone. A review of its pharmacological properties and therapeutic efficacy as an hypnotic.

Zopiclone is a well established alternative to the benzodiazepine hypnotics and may be particularly beneficial in those patients unable or unwilling to tolerate the residual effects associated with many other hypnotic agents.

Zaleplon: a review of its use in the treatment of insomnia.

Zaleplon 5, 10 and 20 mg administered at bedtime, or later if patients have difficulty sleeping, is an effective and well tolerated hypnotic agent and represents a useful option in the management of patients with insomnia who have difficulties initiating sleep.

Zaleplon and triazolam in humans: acute behavioral effects and abuse potential

Despite its non-benzodiazepine structure and unique benzodiazepin-receptor binding profile, the behavioral pharmacological profile of zaleplon is similar to that of triazolam, according to this double-blind, crossover study.

Clinical Pharmacokinetics and Pharmacodynamics of Zolpidem

Zolpidem is a strong sedative with only minor anxiolytic, myorelaxant and anticonvulsant properties, and has been shown to be effective in inducing and maintaining sleep in adults.

Sleep latency is shortened during 4 weeks of treatment with zaleplon, a novel nonbenzodiazepine hypnotic. Zaleplon Clinical Study Group.

Zaleplon appears to provide a favorable safety profile, as indicated by the absence of rebound insomnia and withdrawal symptoms once treatment was discontinued, and was effective in the treatment of insomnia in outpatients with DSM-III-R insomnia.

A Review of the Preclinical Development of Zaleplon, a Novel Non-Benzodiazepine Hypnotic for the Treatment of Insomnia

The results suggest that the effects of zaleplon are similar in many respects to other compounds acting at the benzodiazepine receptor complex but differ as well from both benzidiazepine and non- benzodiazine drugs.

Efficacy and Tolerability of 14-Day Administration of Zaleplon 5mg and 10mg for the Treatment of Primary Insomnia

Zaleplon appeared to have hypnotic properties consistent with its pharmacokinetic profile, and a low likelihood of undesired effects in a double-blind, placebo-controlled design.

Zaleplon improves sleep without producing rebound effects in outpatients with insomnia

Results show that zaleplon provides effective treatment of insomnia with a favourable safety profile and a significantly greater incidence of withdrawal symptoms and a suggestion of sleep difficulty after treatment discontinuation was seen with zolpidem compared to placebo.