Miconazole inhibits the enzyme 14α-sterol demethylase found exclusively in fungi, resulting in decreased production of ergosterol. Ergosterol is an important component of the mycotic cell wall. Thus, inhibition of ergosterol synthesis leads to dissolution fungal cells. In addition to its antifungal effects, miconazole, like ketoconazole, is known to be an antagonist of the glucocorticoid receptor.
After application to the skin, miconazole can be detected in the skin for up to four days. Less than 1% is absorbed into the bloodstream, where 88.2% is bound to plasma proteins and 10.6% to blood cells. The substance is partially metabolized and excreted mainly in the faeces.