Studies on digitalis; I. Renal excretion of digitoxin and its cardioactive metabolites

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Abstract
Simultaneous serum and urine measurements of digitoxin and its cardioactive metabolites were performed in patients with normal renal function, after a single intravenous dose (5 patients) and on maintenance therapy (22 patients). A modified 86Rb method was used for the measurement of digitoxin in serum and urine. After a single dose of digitoxin intravenously, the mean serum‐tissue equilibration half‐time (T/2) was 71 minutes, the mean serum elimination T/2 8.1 days, and urine concentration T/2,7.2 days. Only 2.8% of the dose was excreted as cardioactive metabolites during the first 24 hours and 15.8% after 8 days. Twenty‐two patients on maintenance dosage had a mean serum concentration of 20.6 ng per milliliter, urine concentration of 24.9 ng per milliliter, and the renal excretion of cardioactive substances during 24 hours was 32.9% of the daily dose. Digitoxin clearance was calculated to be 1 ml per minute. Diuretics did not alter the excretion of digitoxin. There was no significant correlation between urine flow and renal excretion of digitoxin. The results suggest that other cardioactive metabolites of digitoxin are present after single‐dose and maintenance therapy.

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