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🧬 Receptor activity
Mechanism of action
Zaleplon exerts its action through subunit modulation of the GABA<sub>B</sub>Z 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<sub>B</sub>Z) receptor complex. Subunit modulation of the GABA<sub>B</sub>Z 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<sub>A</sub>-receptor chloride ionophore complex at benzodiazepine(BZ) omega-1 (BZ1, ο1) receptors.
Pharmacokinetics
Half-life
Approximately 1 hour
Absorption
Absorption Zaleplon is rapidly and almost completely absorbed following oral administration.
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.
1.4 L/kg
1 L/h/kg
Metabolism
Zaleplon is primarily metabolized by aldehyde oxidase.
Zaleplon has known human metabolites that include Dementhylazed-zaleplon.
Zaleplon is primarily metabolized by aldehyde oxidase. Zaleplon is rapidly and almost completely absorbed following oral administration. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Zaleplon is primarily metabolized by aldehyde oxidase to form 5-oxo-zaleplon. Zaleplon is metabolized to a lesser extent by cytochrome P450 (CYP) 3A4 to form desethylzaleplon, which is quickly converted, presumably by aldehyde oxidase, to 5-oxo-desethylzaleplon. These oxidative metabolites are then converted to glucuronides and eliminated in urine. All of zaleplon's metabolites are pharmacologically inactive (RxList, A308).
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
Protein binding
Approximately 60% (in vitro plasma protein binding).
External links
Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.