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Cited by 317Sleep and related disordersPharmaceutical Practices and Patient OutcomesObstructive Sleep Apnea Research

Zolpidem: an update of its pharmacology, therapeutic efficacy and tolerability in the treatment of insomnia

Holm, Kristin J., Goa, Karen L.·2000·Drugs
DOI 10.2165/00003495-200059040-00014
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Abstract

Unlabelled Zolpidem is an imidazopyridine agent that is indicated for the short term (< or = 4 weeks) treatment of insomnia (recommended dosage 10 mg/day in adults and 5 or 10 mg/day in the elderly or patients with hepatic impairment). Data have shown that the hypnotic efficacy of zolpidem is generally comparable to that of the benzodiazepines flunitrazepam, flurazepam, nitrazepam, temazepam and triazolam as well as nonbenzodiazepine hypnotic agents such as zopiclone and trazodone in the treatment of elderly and adult patients with insomnia. The comparative efficacy of a recently available nonbenzodiazepine hypnotic zaleplon and zolpidem has yet to be established. There was no evidence of tolerance developing to the hypnotic effects of zolpidem in a number of studies of up to 6 months' duration. However, tolerance has been described in a few patients taking the drug at high dosages for periods of up to several years. Zolpidem is well tolerated in patients with insomnia and the most common adverse events are generally nausea, dizziness and drowsiness. Although zolpidem produced some psychomotor and memory impairment over the first few hours after administration, it had few next-day effects (including effects on daytime well-being and morning coordination). In this respect, it was comparable or superior to flunitrazepam and flurazepam and comparable to other benzodiazepines in patients with insomnia. Zolpidem appears to have a low potential for abuse.Conclusions Zolpidem is effective and well tolerated in patients with insomnia, including the elderly. Studies have shown that zolpidem generally has similar efficacy to other hypnotics including benzodiazepines and zopiclone. Zolpidem appears to have minimal next-day effects on cognition and psychomotor performance when administered at bedtime. In addition, there is little evidence of tolerance to the hypnotic effects of zolpidem, or rebound insomnia or withdrawal symptoms after discontinuation of the drug when it is given as recommended (10 mg/day for < 1 month) or over longer periods.

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Crossref · 10.2165/00003495-200059040-00014

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  • The elevated risk of Z-drug use disorder among older adults is partly attributed to the higher prevalence of sleep and mood disorders in this population, as well as to age-related reductions in drug clearance.

    “This elevated risk among older adults is partly attributed to the higher prevalence of sleep and mood disorders in this population, as well as to age-related reductions in drug clearance.”

    From Z-drug abuse and dependence: Clinical guideline of the Brazilian Academy of Neurology for diagnosis and management (2025) · cites this paper as [51]

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Authors
Holm, K. J., & Goa, K. L.
Corresponding author
Holm, Kristin J.
Venue
Drugs
Publisher
Springer Science and Business Media LLC
Published
2000-04
Volume
59
Issue
4
Pages
865-889
ISSN
0012-6667 (ISSN-L)
DOI
10.2165/00003495-200059040-00014
OpenAlex
W2058537083
Cited by
317
References
138
Citations by year
2026: 5 · 2025: 9 · 2024: 8 · 2023: 8 · 2022: 10 · 2021: 13 · 2020: 9 · 2019: 14 · 2018: 11 · 2017: 9 · 2016: 16 · 2015: 12 · 2014: 15 · 2013: 13 · 2012: 19
FWCI
4.10
Type
journal article
Language
en
Open access
closed
Locations
  • Drugs (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Social Sciences › Psychology › Experimental and Cognitive Psychology › Sleep and related disorders
  • Health Sciences › Medicine › Geriatrics and Gerontology › Pharmaceutical Practices and Patient Outcomes
  • Health Sciences › Medicine › Physiology › Obstructive Sleep Apnea Research
Keywords
insomnia, imidazopyridines, benzodiazepine receptor, GABAA receptor, hypnotic efficacy, non-benzodiazepine hypnotics, zopiclone, zaleplon, adverse events, elderly patients, liver dysfunction, abuse liability, rebound insomnia, withdrawal symptoms, pharmacokinetics
MeSH terms
Zolpidem, Animals, Humans, Hypnotics and Sedatives, Sleep Initiation and Maintenance Disorders, Pyridines

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