About Zaleplon Pyrazolopyrimidine derivative( a nonbenzodiazepine, Sedative-hypnotic. Mechanism of Action of Zaleplon Zaleplon is a non benzodiazepine sedative-hypnotic drug. It binds to the benzodiazepine binding site on GABA-A receptors containing the alpha 1 receptor sub unit and alters the GABA mediated chloride channel opening. This is responsible for sedative effect of the drug. Interactions for Zaleplon Rifampin: It reduces the AUC of zaleplon. Cimetidine: It increases the Cmax and AUC of zaleplon. Food: If zaleplon is taken with or immediately after fatty meal its effect on sleep onset may be reduced.