Pharmacokinetics of beta-methyldigoxin.

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Abstract
Beta-methyldigoxin (β-MD) is a cardiac glycoside widely used to treat heart failure and arrhythmia but its pharmacokinetics is not well known. Pharmacokinetic characteristics of β-MD were studied in five healthy volunteers. After a single oral dose of β-MD (0.2mg), the serum glycoside concentrations and urinary glycoside excretions were measured over seven days. The concentrations of β-MD and its metabolites in serum and urine were deter mined by high performance liquid chromatography-fluorescence polarization immunoassay method. β-MD appeared in serum 15min after administration and reached the peak serum concentration (1.88±0.71ng/ml) at 0.70±0.33hr. Elimination half-life, volume of distribution, and renal clearance were found to be 46.5±14.1hr, 9.5±2.4l/kg, and 46.0±14.3ml/min, respectively. These kinetic parameters were different from data reported previously . Digoxin was the only metabolite observed in serum and its peak concentration was 0.31± 0.07ng/ml at 1.10±0.34hr. The percentages of the β-MD dose renally excreted by 156 hr as β-MD, digoxin, digoxigenin bisdigitoxoside, digoxigenin monodigitoxoside, and digoxigenin were 29.55, 23.42, 1.28, 0.36, and 0.50%, respectively. From serum concentration-time curves, the presence of enterohepatic circulation of β-MD was suggested.

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