In recent decades, interest in enzyme inhibition, such as myeloperoxidase (MPO) and glycosidases, has dramatically increased, mainly because these enzymes play a vital role in many biological processes. Based on the biological potential associated with these enzymes, instead of several glycosidase and myeloperoxidase (MPO) inhibitors that have been developed, there are not enough studies on the inhibition effects of widely used types of antivirals (aciclovir, tenofovir), oral antidiabetics (glibenclamide, glibornuride, glurenorm, met-formin), and non-steroidal anti-inflammatory drugs (NSAIDs) active substances (benzydamine HCl, diclofenac, indomethacin, ketorolac tromethamine, paracetamol, salicylic acid) today. For that reason, the aim of our study is to investigate the inhibition effects of these 12 different drug active substances on α-glucosidase and MPO activities. According to the obtained results, the screened drug active substances acyclovir, glibornuride, and paracetamol inhibited α-glucosidase with the lowest IC50 value, while similarly low values for MPO were found by tenofavir, glurenorm, and indomethacin. In our study, we can suggest that these active pharmaceu-tical ingredients may contribute to the pharmaceutical industry due to their inhibitory effects on α-glucosidase and MPO in vitro.