Azosemide kinetics and dynamics

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Abstract
Azosemide is a loop diuretic that may also affect Na+ reabsorption at the proximal tubule. I.v. and oral doses of the drug were given to normal subjects to examine its kinetic and dynamic parameters. In the fasting state a lag time of absorption of .apprx. 1 h was followed by absorption t1/2 [half-life] and elimination t1/2 of .apprx. 0.75 and 2-2.5 h. Only 2% of an oral dose was excreted unchanged in the urine. After i.v. dosing the elimination t1/2 was approximately 2 h; 20% of a dose was recovered unchanged. Thus azosemide has an estimated bioavailability of 10%. The relationship between urinary azosemide excretion rate (dose) and natriuretic response follows a sigmoid-shaped curve with a dose inducing half-maximal response of 9.3 .+-. 2.6 .mu.g/min, whereas it is 69.8, 12.1 and 1 .mu.g/min for furosemide, piretanide and bumetanide respectively.