Enhanced Transformation of Digitoxin to Dihydrodigitoxin in Humans with Renal Failure

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Abstract
A gas-chromatographic mass-spectroscopic technique was used to identify dihydrodigitoxin, a metabolite digitoxin, in the plasma of healthy volunteers and patients with renal failure. Digitoxin and dihydrodigitoxin were extracted from plasma and derivatized with heptafluorbutyric anhydride. In normal subjects, only minimal concentrations of dihydrodigitoxin in plasma were determined (1 ng/ml) after i.v. bolus injection of digitoxin. Under chronic treatment with a daily dose of 0.1 mg digitoxin in 3 of 7 individuals, dihydrodigitoxin plasma levels were detected (0.7, 1.5 and 1.7 ng/ml). In 7 patients with renal failure, high dihydrodigitoxin plasma concentrations (8.9 .+-. 0.9 ng/ml) occurred in a similar range to those of the parent compound (8.7 .+-. 2.2 ng/ml) under maintenance treatment with digitoxin.

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