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    Zaleplon molecular structure

    Zaleplon Stats & Data

    Depressant Psychedelic
    Sonata
    NPS DataHub
    MW305.34
    FormulaC17H15N5O
    CAS151319-34-5
    IUPACN-[3-(3-cyanopyrazolo[5,1-b]pyrimidin-7-yl)phenyl]-N-ethylacetamide
    SMILESCCN(C(C)=O)c1cccc(c1)c1ccnc2c(C#N)cnn12
    InChIKeyHUNXMJYCHXQEGX-UHFFFAOYSA-N
    Others
    Chemical Class medicine
    Psychoactive Class Depressant / Psychedelic

    Pharmacology

    DrugBank
    Half-life Approximately 1 hour State Solid Vd * 1.4 L/kg Clearance * 1 L/h/kg

    Description

    Zaleplon is a sedative/hypnotic, mainly used for insomnia. It is known as a nonbenzodiazepine hypnotic. Zaleplon interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Zaleplon is a schedule IV drug in the United States.

    Mechanism of Action

    Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. Zaleplon also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding.

    Pharmacodynamics

    Zaleplon is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zaleplon also binds selectively to the CNS GABAA-receptor chloride ionophore complex at benzodiazepine(BZ) omega-1 (BZ1, ο1) receptors.

    Metabolism

    Zaleplon is primarily metabolized by aldehyde oxidase.

    Absorption

    Absorption Zaleplon is rapidly and almost completely absorbed following oral administration.

    Toxicity

    Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness

    Indication

    For the treatment of short-term treatment of insomnia in adults.

    Protein Binding

    Approximately 60% (in vitro plasma protein binding).

    Elimination

    Zaleplon is metabolized primarily by the liver and undergoes significant presystemic metabolism. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Renal excretion of unchanged zaleplon accounts for less than 1% of the administered dose.

    Receptor Profile

    Receptor Actions

    Modulators
    GABA-A receptor positive allosteric modulator (benzodiazepine site)
    Other
    preferential binding to alpha-1 subunit (BZ1/omega-1 receptor)

    Effect Profile

    Curated + 17 Reports
    Psychedelic 4.6

    Strong visuals with low headspace

    Visual Intensity×3
    8
    Headspace Depth×3
    1
    Auditory Effects×1
    0
    Body Load / Somatic Effects×1
    0
    Based on reports from:
    Erowid Experience Reports PsychonautWiki Zaleplon

    Tolerance & Pharmacokinetics

    drugs.wiki

    Tolerance Decay

    Full tolerance 3d Half tolerance 10d Baseline ~14d

    Cross-Tolerances

    Zolpidem
    30% ●○○
    Zopiclone
    30% ●○○

    Experience Report Analysis

    Erowid
    17 Reports
    2001–2018 Date Range
    3 With Age Data
    9 Effects Detected

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Effect Analysis

    Erowid

    Effects aggregated from 17 experience reports (17 Erowid)

    17 Reports
    9 Effects Detected
    6 Positive
    1 Adverse
    2 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Positive Effects 6

    Stimulation 47.1% 70%
    Euphoria 41.2% 70%
    Sedation 29.4% 70%
    Color Enhancement 23.5% 70%
    Focus Enhancement 23.5% 70%
    Tactile Enhancement 17.6% 70%

    Adverse Effects 1

    Motor Impairment 17.6% 70%

    Real-World Dose Distribution

    62K Doses

    From 18 individual dose entries

    Oral (n=9)

    Median: 20.0mg 25th: 10.0mg 75th: 30.0mg 90th: 42.0mg
    mg/kg median: 0.22 mg/kg 75th: 0.353

    Insufflated (n=8)

    Median: 30.0mg 25th: 16.25mg 75th: 40.0mg 90th: 46.0mg
    mg/kg median: 0.401 mg/kg 75th: 0.441

    Form / Preparation

    Most common forms and preparations reported

    Redose Patterns

    Redosing behavior across 14 reports

    14.3% Redosed
    1.3 Avg Doses
    120m Median Interval
    Read full reports on Erowid →

    References

    Cited References

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