Imidapril is a prodrug for the active metabolite imidaprilat, an angiotensin-converting enzyme (ACE) inhibitor that suppresses the conversion of angiotensin I to angiotensin II (IC₅₀ = 2.6 nM), thereby preventing vasoconstriction and decreasing aldosterone secretion by the adrenal cortex which leads to an increase in sodium excretion and subsequently increases water outflow.