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Zaleplon Stats & Data

Depressant Psychedelic

Sonata

PubChem CID 5719

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 GABA_BZ 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 (GABA_BZ) receptor complex. Subunit modulation of the GABA_BZ 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 GABA_A-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.

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)

Toxicity

PubChem DrugBank

Toxicity in a milder form can cause lethargy, drowsiness, and confusion. Severe toxicity can lead to respiratory depression, ataxia, hypotension, hypotonia, loss of consciousness, coma, and rarely death. Management aims at providing supportive treatment, including gastric lavage and IV fluids. Researchers have conducted animal studies that show flumazenil is useful as an antagonist to zaleplon, but there are no clinical trials regarding the use of flumazenil as an antidote to zaleplon overdose. Zaleplon exerts its action through subunit modulation of the GABA<sub>B</sub>Z receptor chloride channel macromolecular complex.

Carcinogenicity

No indication of carcinogenicity to humans (not listed by IARC).

Liver injury risk

No documented concern

FDA LiverTox / DILIrank. Reflects published case reports of liver injury, not absolute risk.

Toxicity (DrugBank)

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

Health effects (PubChem excerpts)

Angina pectoris, bundle branch block, hypertension, hypotension, palpitation, syncope, melena, mouth ulceration, rectal hemorrhage, stomatitis, dysphagia, enteritis, gum hemorrhage, diabetes mellitus, goiter, hypothyroidism, arthrosis, bursitis, hyperesthesia, hyperkinesia, hypotonia, incoordination, insomnia, libido decreased, neuralgia, nystagmus, dry skin, eczema, maculopapular rash, skin hypertrophy, dysuria, hematuria, impotence, kidney calculus, kidney pain, urinary retention, and vaginal hemorrhage (RxList, A308). They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. May cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease.

Effect Profile

Curated + 17 Reports

Psychedelic 4.6

Strong visuals with low headspace

Visual Intensity×3

Headspace Depth×3

Auditory Effects×1

Body Load / Somatic Effects×1

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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