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Zaleplon

Also known as: Zaleplon

gamma-Aminobutyric Acid A Receptor AgonistGABA A Agonists

Route: Oral

9 interactions on record⛔ Black Box Warning

Zaleplon has 9 known drug interactions based on U.S. FDA drug labeling data. Notable interactions include combinations with Alcohol, Imipramine, Promethazine. Patients taking Zaleplon should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 9
Moderate: 5
Minor: 2

Moderate (5)

Zaleplon + Alcohol— Zaleplon potentiated CNS-impairing effects of ethanol on balance testing, reaction time, and divided attention for up to…
Zaleplon + Imipramine— Co-administration produced additive effects on decreased alertness and impaired psychomotor performance for 2 to 4 hours…
Zaleplon + Promethazine— Co-administration resulted in 15% decrease in maximal zaleplon plasma concentrations with no change in AUC. Pharmacodyna…
Zaleplon + Rifampin— Multiple-dose rifampin reduced zaleplon Cmax and AUC by approximately 80%, potentially leading to zaleplon ineffectivene…
Zaleplon + Thioridazine— Co-administration produced additive effects on decreased alertness and impaired psychomotor performance for 2 to 4 hours…

Minor (2)

Zaleplon + Paroxetine— Co-administration did not produce any interaction on psychomotor performance. Paroxetine did not alter zaleplon pharmaco…
Zaleplon + Venlafaxine— Co-administration did not result in significant pharmacokinetic changes or pharmacodynamic interaction between zaleplon …

Zaleplon + Alcohol🟡Moderate

Zaleplon potentiated CNS-impairing effects of ethanol on balance testing, reaction time, and divided attention for up to 2.5 hours. Pharmacodynamic interaction without altered ethanol pharmacokinetics.

Zaleplon + Imipramine🟡Moderate

Co-administration produced additive effects on decreased alertness and impaired psychomotor performance for 2 to 4 hours. Pharmacodynamic interaction with no alteration of either drug's pharmacokinetics.

Zaleplon + Promethazine🟡Moderate

Co-administration resulted in 15% decrease in maximal zaleplon plasma concentrations with no change in AUC. Pharmacodynamics not evaluated; caution advised.

Zaleplon + Rifampin🟡Moderate

Multiple-dose rifampin reduced zaleplon Cmax and AUC by approximately 80%, potentially leading to zaleplon ineffectiveness. Alternative non-CYP3A4 substrate hypnotic may be considered.

Zaleplon + Thioridazine🟡Moderate

Zaleplon + Paroxetine🟢Minor

Co-administration did not produce any interaction on psychomotor performance. Paroxetine did not alter zaleplon pharmacokinetics, confirming no role of CYP2D6 in zaleplon metabolism.

Zaleplon + Venlafaxine🟢Minor

Co-administration did not result in significant pharmacokinetic changes or pharmacodynamic interaction between zaleplon and venlafaxine ER.

Zaleplon + Erythromycinℹ️Unknown

Co-administration of single, oral doses of zaleplon with erythromycin (10 mg and 800 mg, respectively), a strong, selective CYP3A4 inhibitor, produced a 34% increase in zaleplon's maximal plasma concentrations and a 20% increase in the area under the plasma concentration time curve. The magnitude of interaction with multiple doses of erythromycin is unknown.

Zaleplon + Ketoconazoleℹ️Unknown

Other strong selective CYP3A4 inhibitors such as ketoconazole can also be expected to increase the exposure of zaleplon.

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine, supplemented with a small number of well-established interactions from curated clinical references. For informational purposes only. Always consult your pharmacist or physician.