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Information about Zaleplon

Zaleplon is a benzodiazepine receptor agonist and hypnotic that is used as a sleeping pill.

Liver safety of Zaleplon

Zaleplon has not been implicated in causing serum enzyme elevations or clinically apparent liver injury.

Mechanism of action of Zaleplon

Zaleplon (zal' e plon) is a non-benzodiazepine, benzodiazepine receptor agonist of the pyrazolopyrimide class that acts by binding to the benzodiazepine (BZ) site on the GABA receptor complex, causing neural inhibition and helping to induce sleep. Zaleplon has selectivity for certain BZ receptor subtypes and does not have the neuromuscular relaxation or anticonvulsant effects of the standard benzodiazepines. Zaleplon has a short half life and rapid onset of action. In multiple placebo-controlled trials, zaleplon was shown to decrease the latency to onset of sleep and improve perceived sleep quality with few next day residual effects and little evidence of rebound insomnia after withdrawal.

FDA approval information for Zaleplon

Zaleplon was approved for use in the United States in 1999 for the short term treatment of insomnia and it remains in wide use.

Dosage and administration for Zaleplon

Zaleplon is available in 5 and 10 mg capsules generically and under the brand name Sonata. The recommended dose is one 5 or 10 mg tablet taken orally immediately before bedtime.

DEA controlled substance classification of Zaleplon

Like the other benzodiazepine receptor agonists, zaleplon is classified as a Schedule IV controlled substance (low potential for abuse and limited physical or psychological dependence).

Side effects of Zaleplon

Side effects are uncommon, usually mild and may include headache, nausea, dizziness and drowsiness.

Sedatives and Hypnotics

Miscellaneous Agents


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