Premium
Azosemide kinetics and dynamics
Author(s) -
Brater D Craig,
Day Bart,
Anderson Shirley,
Seiwell Ruth
Publication year - 1983
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1983.197
Subject(s) - bumetanide , chemistry , pharmacology , reabsorption , bioavailability , diuretic , pharmacokinetics , absorption (acoustics) , endocrinology , medicine , sodium , cotransporter , physics , organic chemistry , acoustics
Azosemide is a loop diuretic that may also affect sodium reabsorption at the proximal tubule. We gave intravenous and oral doses of the drug to normal subjects to examine its kinetic and dynamic parameters. In the fasting state a lag time of absorption of approximately 1 hr was followed by absorption t½s and elimination t½s of approximately 0.75 and 2 to 2.5 hr. Only 2% of an oral dose was excreted unchanged in the urine. After intravenous dosing the elimination t½ was approximately 2 hr; 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 μg/min, whereas it is 69.8, 12.1 and 1 μg/min for furosemide, piretanide, and bumetanide respectively. Clinical Pharmacology and Therapeutics (1983) 34, 454–458; doi: 10.1038/clpt.1983.197