Comparative Pharmacology
Head-to-head clinical analysis: LUNESTA versus ZALEPLON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LUNESTA versus ZALEPLON.
LUNESTA vs ZALEPLON
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nonbenzodiazepine hypnotic that binds to GABA-A receptors at the benzodiazepine binding site, enhancing GABAergic inhibitory neurotransmission.
Selective agonist of the benzodiazepine site on GABA-A receptors, enhancing GABA-mediated chloride conductance and neuronal inhibition. Binds preferentially to the α1 subunit-containing receptors.
1 mg, 2 mg, or 3 mg orally once immediately before bedtime; not to exceed 3 mg/day.
10 mg orally once daily at bedtime; range 5-20 mg.
None Documented
None Documented
Terminal elimination half-life is approximately 6 hours in young adults and about 9 hours in elderly patients. This supports once-nightly dosing for insomnia.
Clinical Note
moderateZaleplon + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Zaleplon is combined with Fluticasone propionate."
Clinical Note
moderateZaleplon + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Zaleplon."
Clinical Note
moderateZaleplon + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Zaleplon."
Clinical Note
moderateZaleplon + Cyclosporine
The terminal elimination half-life is approximately 1 hour (range 0.9–1.1 hours) in healthy adults. This short half-life minimizes next-day residual effects and is consistent with its use for sleep induction without significant morning sedation.
Primarily hepatic metabolism via CYP3A4 and CYP2E1; renal excretion of metabolites accounts for approximately 80% of total clearance, with about 2-4% excreted unchanged in urine. Fecal excretion contributes less than 10%.
Approximately 70% of a dose is excreted as metabolites in urine (primarily as 5-oxo-zaleplon and other oxidative metabolites) and about 30% in feces. Less than 1% is excreted unchanged in urine.
Category C
Category A/B
Non-Benzodiazepine Hypnotic
Non-Benzodiazepine Hypnotic
"The metabolism of Cyclosporine can be decreased when combined with Zaleplon."