Cellular mechanism of action of loop diuretics: implications for drug effectiveness and adverse effects

Abstract

The loop diuretics inhibit a transport system that moves sodium, potassium and chloride across cell membranes of many tissues, including the thick ascending loop of Henle. This inhibitory effect is responsible for their natriuretic effect. Of the agents available for clinical use, bumetanide is the most powerful; it has an in vitro transport inhibitory potency and an in vivo natriuretic effectiveness that is approximately 50-fold that of furosemide. This increased potency and the consequent decreased dose requirement give bumetanide the potential for increased effectiveness and decreased incidence of adverse effects.