Not yet reviewed — this article is pending editorial review by Lyrea.
Dosage & Duration
Dosage
Duration
Subjective Effects
In controlled studies of therapeutic oral doses, zaleplon produced sedation, short-term memory impairment, and psychomotor impairment around the approximately one-hour peak exposure. In the cited studies these measured impairments were absent by 3 to 4 hours, although individual response and next-day risk vary.[cite:url-dailymed-1ef0eb]
Physical
Reported at therapeutic oral doses in the prescribing information.[cite:url-dailymed-1ef0eb]
Cognitive
Reported at therapeutic oral doses in the prescribing information; the label notes that causation for abnormal behaviour reports is often uncertain.[cite:url-dailymed-1ef0eb]
Pharmacology
Pharmacodynamics
Zaleplon interacts with the GABA-benzodiazepine receptor complex and preferentially binds the omega-1 site on alpha-1-containing GABA-A receptors. Modulation of this chloride-channel complex is associated with its hypnotic and sedative effects.1
Pharmacokinetics
After oral administration, zaleplon reaches peak plasma concentration in about 1 hour and has an elimination half-life of about 1 hour. Absolute oral bioavailability is about 30% because of substantial first-pass metabolism.1 Aldehyde oxidase is the primary metabolic pathway, producing 5-oxo-zaleplon; CYP3A4 is a lesser pathway producing desethylzaleplon. The oxidative metabolites are converted to glucuronides, are pharmacologically inactive, and less than 1% of a dose is excreted unchanged in urine.1
Unsafe
AvoidThere is considerable risk of physical harm when taking these combinations, they should be avoided where possible.
Caution
Use cautionThese combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
Tolerance
Harm Potential
Toxicity
Overdose can produce CNS depression ranging from drowsiness and confusion to ataxia, respiratory depression, coma, and very rarely death. Fatal outcomes have been reported most often when additional CNS depressants were also taken.1
History & Culture
The U.S. Food and Drug Administration approved Sonata (zaleplon) capsules under NDA 20-859 on August 13, 1999. The approved indication was short-term treatment of insomnia.2
Legality
By Country
References
Source Pages
Citations
- Zaleplon capsules USP, Preferred Pharmaceuticals Inc.; prescribing information updated October 8, 2025. dailymed.nlm.nih.gov (n.d.). https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=b0476859-07af-47f1-aec7-61aea0d99d241234567891011121314151617181920
- Food and Drug Administration. accessdata.fda.gov (n.d.). https://www.accessdata.fda.gov/drugsatfda_docs/nda/99/20859_Sonata_appltr_prntlbl.pdf1
Further Reading
Automated synthesisInformation aggregated and synthesized using an autonomous workflow built by Josie Kins.
Suggest an edit
Spotted a mistake, an outdated claim, or something missing from the Zaleplon article? Send the editors a private note. Feedback lands in a moderation queue and is never shown on the site.
Wish to give generalised feedback? You can do so here.