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Decreased digoxin cardioinactive‐reduced metabolites after administration as an encapsulated liquid concentrate
Author(s) -
Rund Deborah G,
Lindenbaum John,
Dobkin Jay F,
Butler Vincent P,
Saha Jnan R
Publication year - 1983
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.1983.243
Subject(s) - digoxin , pharmacology , chemistry , medicine , heart failure
The generation by intestinal bacteria of large amounts of cardioinactive metabolites of digoxin with a reduced lactone ring (digoxin reduction products, or DRP) may be associated with increased dosage requirements. Since DRP excretion varies inversely with bioavailability, we compared the 6‐day urinary excretion (CUE) of digoxin and DRP after 0.4‐mg doses of an encapsulated liquid concentrate and a standard tablet in 22 normal subjects known to form substantial amounts of DRP. Mean (±SE) CUE of digoxin was greater with the capsules than the tablets (195.9 ± 8.6 and 137.5 ± 6.3 μg). CUE of DRP was less after the capsules (60.8 ± 5.5 and 102.7 ± 9.5 μg). Percent DRP was greater after the tablets in every subject (mean for tablets, 41.2 ±2.7%; capsules, 23.5 ± 1.8%). Patterns of DRP excretion differed with the two preparations, probably reflecting differences in the routes whereby digoxin reached the colon. The use of highly bioavailable capsules in subjects with heavy DRP production should minimize metabolic inactivation during digoxin therapy. Clinical Pharmacology and Therapeutics (1983) 34 , 738–743; doi: 10.1038/clpt.1983.243