Zaleplon Stats & Data
CCN(C(C)=O)c1cccc(c1)c1ccnc2c(C#N)cnn12HUNXMJYCHXQEGX-UHFFFAOYSA-NPharmacology
DrugBankDescription
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.
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
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
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 + 11 ReportsModerate visuals with low headspace
Tolerance & Pharmacokinetics
drugs.wikiNo tolerance chart. Our decay curves for these drugs were estimates, and a curve can make tolerance look longer-lasting than it is, which is the dangerous direction.
How fast tolerance to these drugs fades after a break has not been measured well enough to draw, so don't count on a dose you used to take still being safe: after time off, start with a much smaller amount and don't use alone. Mixing sedatives with each other, with alcohol or with opioids sharply raises the risk of a fatal overdose. If you've been using regularly, don't stop suddenly: withdrawal from benzodiazepines, alcohol or GHB/GBL can cause seizures or delirium, so get medical help to cut down gradually.
Sources: FRANK: benzodiazepines · Alcohol and Drug Foundation: GHB · FDA 2020: benzodiazepine boxed warning · FDA 2019: gabapentinoids and breathing · NHS: alcohol use disorder
Cross-Tolerances
Experience Report Analysis
ErowidDemographics
Gender Distribution
Too few reports for a chart: gender is known from 17 reports, and a split is drawn only from 20 reports or more. Counts are shown instead. Why 20?
- Male 15 of 17
- Not Specified 2 of 17
Age Distribution
Reports Over Time
Effect Analysis
ErowidEffects aggregated from 11 experience reports (11 single-substance Erowid)
Effect Sentiment Distribution
Confidence Distribution
Each bar is the share of reports mentioning the effect; its whisker, and the band on the rows below, is the 95% interval: where the share could plausibly be with other reports of the same kind.
Too few reports for bars: these effects come from 11 single-substance Erowid reports, and a bar is drawn only from 20 reports or more. With fewer, a percentage cannot tell a common effect from a rare one. Counts are shown instead. Why 20?
Positive Effects 3
Adverse Effects 0
Show 1 neutral or unclassified mention
Real-World Dose Distribution
ErowidFrom 18 of 18 recorded dose entries: those that state a weight (mg, g or µg), in routes with at least five of them. Values above Q3 + 3×IQR, far above what people typically take, are left out; they can include real heavy doses and overdoses, not only mistakes.
Oral (n=9)
Insufflated (n=8)
Form / Preparation
Most common forms and preparations, as a share of the 14 reports that give one
Too few reports for bars: these forms come from 14 reports, and a bar is drawn only from 20 reports or more. With fewer, a percentage cannot tell a common effect from a rare one. Counts are shown instead. Why 20?
- Powder / Crystals 7 of 14
- Capsule 2 of 14
- Ground / Crushed 2 of 14
Redose Patterns
Redosing behavior across 14 reports
Too few reports for a chart: redosing is known from 14 reports, and a split is drawn only from 20 reports or more. Counts are shown instead. Why 20?
- Single dose 12 of 14
- Redosed 2 of 14
References
Cited References
- DrugBank: Zaleplon
- Erowid Experience Vault: Zaleplon
- PsychonautWiki: Zaleplon Talk Page
- StatPearls: Zaleplon
- TripSit Wiki: Drug Combinations
- Wikipedia: Zaleplon
- Zaleplon: A pyrazolopyrimidine sedative-hypnotic agent (2000)
- DrugBank Article: Zaleplon for Insomnia
- DrugBank Article: Zaleplon Efficacy
- DrugBank Article: Zaleplon Adverse Effects