Summary
The pharmacokinetics of the antikaliuretic amiloride has been studied in healthy controls and in patients with chronic renal failure or hepatitis. It was 40% bound to protein.
In healthy volunteers 49% of an oral dose was recovered unchanged in the urine. The renal clearance of amiloride was about 3 times the creatinine clearance, which means that it was predominantly excreted via tubular secretion.
Renal impairment reduced the clearance of amiloride, causing a prolongation of the t1/2 and drug accumulation in plasma. In hepatitis the t1/2 of amiloride was prolonged and the AUC increased. Urinary recovery (Ae) of amiloride was greater in hepatitis patients than in controls.
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Spahn, H., Reuter, K., Mutschler, E. et al. Pharmacokinetics of amiloride in renal and hepatic disease. Eur J Clin Pharmacol 33, 493–498 (1987). https://doi.org/10.1007/BF00544242
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DOI: https://doi.org/10.1007/BF00544242