Decreased digoxin cardioinactive-reduced metabolites after administration as an encapsulated liquid concentrate
| Autor: | John Lindenbaum, Jay F. Dobkin, Vincent P Butler, Deborah G. Rund, Jnan R. Saha |
|---|---|
| Rok vydání: | 1983 |
| Předmět: |
Adult
Male Digoxin Metabolite Biological Availability Capsules Digitalis Pharmacology Dosage form Excretion chemistry.chemical_compound medicine Humans Pharmacology (medical) biology Capsule Metabolism Middle Aged biology.organism_classification Bioavailability chemistry Evaluation Studies as Topic Female Tablets medicine.drug |
| Zdroj: | Clinical Pharmacology and Therapeutics. 34:738-743 |
| ISSN: | 1532-6535 0009-9236 |
| Popis: | 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 |
| Databáze: | OpenAIRE |
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