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Digoxin biotransformation
Author(s) -
Gault M Henry,
Longerich Linda L,
Loo Jack C K,
Ko Patrick T H,
Fine Adrian,
Vasdev Sudesh C,
Dawe Madonna A
Publication year - 1984
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.1984.11
Subject(s) - digoxin , digoxigenin , chemistry , biotransformation , metabolite , radioimmunoassay , urine , pharmacology , chromatography , endocrinology , medicine , biochemistry , enzyme , heart failure , in situ hybridization , gene expression , gene
Serum digoxin and metabolites were assayed in plasma and urine by HPLC in 10 dialysis‐dependent patients with end‐stage renal failure (group I) and in five patients with comparatively normal renal function (group II) after ingestion of 150 µCi 3 H‐digoxin‐12α. Thirteen patients were on maintenance digoxin therapy and were at steady state. Metabolites found regularly but usually in small amounts, were 3β‐digoxigenin and its mono‐ and bis‐digitoxosides, and 3‐keto and 3α(epi)‐digoxigenin. Quantitatively the most abundant metabolites were polar and averaged 26% (7 to 76) of the radioactivity in plasma 6 hr after drug, and 60% (11 to 88) for digoxin for all 15 patients. Neither values between group I and II for the polar metabolites nor digoxin differed significantly. The metabolites reacted with antibody to digoxin to varying degrees and may make up an important component of the serum digoxin concentration when determined by standard radioimmunoassay. In some patients, digoxin undergoes extensive biotransformation, mainly, we suggest by hydrolysis, oxidation, epimerization, and conjugation to polar end‐metabolites. Clinical Pharmacology and Therapeutics (1984) 35, 74–82; doi: 10.1038/clpt.1984.11