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QuickView for Zaleplon (compound)


PubChem
Name: zaleplon
PubChem Compound ID: 5719
Molecular formula: C17H15N5O
Molecular weight: 305.334 g/mol
Synonyms:
DEA No. 2781; CL 284,846; ZAL 846; Zaleplon (JAN/USAN); CL-284846; D00530; Acetamide, N-(3-(3-cyanopyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-N-ethyl-; Zaleplon [USAN:INN]; Sonata (TN); Sonata.
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DrugBank
Identification
Name: zaleplon
Name (isomeric): DB00962
Drug Type: small molecule
Synonyms:
DEA No. 2781
Brand: Sonata, Zalaplon
Category: Hypnotics and Sedatives, Anxiolytics sedatives and hypnotics, Anticonvulsants
CAS number: 151319-34-5
Pharmacology
Indication: For the treatment of short-term treatment of insomnia in adults.
Pharmacology:
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 (GA...
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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.
Absorption: Absorption Zaleplon is rapidly and almost completely absorbed following oral administration.
Protein binding: Approximately 60% (in vitro plasma protein binding).
Biotransformation: Zaleplon is primarily metabolized by aldehyde oxidase.
Route of 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.
Half Life: Approximately 1 hour
Clearance: 1 L/h/kg
Toxicity: Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
RifampinRifampin decreases the effect of zaleplon
MethotrimeprazineAdditive CNS depressant effects may occur. A dose reduction of zaleplon may be required. Monitor for increased CNS depression during concomitant therapy.
TriprolidineThe CNS depressants, Triprolidine and Zaleplon, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
CimetidineCimetidine may increase the serum concentration of zaleplon by decreasing its metabolism. Reduce the initial dose of zaleplon to 5 mg in patients receiving cimetidine.

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