Diuretic effect and metabolism of bumetanide in man

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Abstract
Bumetanide (3‐N‐butylamino‐4‐phenoxy‐5‐sulfamyl‐benzoic acid) is a sulfonamide congener with potent diuretic activity in man. Oral administration of 14[;‐bumetanide (2 mg, 22 t‐LCi) to 4 adult male volunteers was rapidly and almost completely absorbed (>95%). Its average apparent volume of distribution was 25 L. Bumetanide induced a ceiling diuresis at 1 hr, with loss of Na+ and water for 4 to 5 hr. Loss ofK+was minimal. Bumetanide was quickly eliminated by metabolism and urinary excretion with a plasma half‐life of 1.5 hr. The administered radioactivity was almost completely recovered (96%),81% appearing in the urine and the remainder in thefeces. In one subject with biliary T tube, 14.4% of the dose was excreted in the bile which suggested that the radioactivity of the feces came from the bile. Thin‐layer chromatography analysis ofpooled urine, bile, and fecal samples showed the elimination of bumetanide could be explained by excretion oI unchanged drug and side chain oxidative metabolism and conjugation.

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