Abstract

A new diuretic agent, FR 3068 (tienilic acid) was studied for effects on urinevolume, urinary and serum electrolytes and uric acid, for serum and urinary con-centration of unchanged FR 3068 and for tolerability in 33 healthy male volunteers. A single oral dose of 250mg of FR 3068 increased significantly urine volume for 4 hours and urinary excretion of Na and Cl for 6 hours, but didn't cause significant changes in urinary K excretion and serum electrolytes.Urinary excretion of uric acid increased for 4 hours after administration of 125 mg and for 6 hours after 250mg, and serum uric acid at 8 hours after administration decreased significantlyin correlation with dosages of 62.5, 125 and 250mg.Peak serum concentration of unchanged FR 3068 was obtained 1 to 2 hours after a single oral administration and urinary recovery of unchanged FR 3068 in 24 hours was 17.3% after 62.5 mg, 22.3% after 125 mg and 37.9% after 250 mg. Any side effects and abnormalities in laboratory tests, ECG and audiogram were not observed during the study.It is considered that FR 3068 is an unique diuretic agent with a marked urico-suric effect.

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