Biotransformation and elimination of digoxin with normal and minimal renal function.

Abstract

Six subjects with normal renal function (NRF) and 6 patients with minimal renal function (MRF) on 3 times weekly hemodialysis received 150 muCi3H-digoxin-12 alpha orally. Serial urine collections were made for five days or more. Digoxin and metabolites were separated using diethylaminoethyl Sephadex LH-20 column chromatography. Mean cumulative percentages of the ingested radioactivity excreted over five days in NRF and MRF groups were: digoin, 54.5% and 14.7%; bis-digitoxoside of digoxigenin, 2.0% and 0.59%; mono-digitoxoside, 0.8% and 0.19%; digoxigenin, 0.25% and 0.03%; and dihydrodigoxin, 0.3% and 0.03%. Half-lives based on the mean rates of disappearance from urine comparing NRF and MRF groups were: for digoxin 40 hr and 120 hr; for bis-digitoxoside, 11.5 hr and 46 hr; for mono-digitoxoside, 8.5 hr and 12 hr; for digoxigenin, 2 hr and 7.5 hr; and for dihydrodigoxin, 1.2 hr and 7.0 hr. Considering the relationships of the five-day cumulative excretion and half-lives of digoxin and metabolites in the NRF and MRF groups, it appears unlikely that there is a major alteration in the biotransformation of digoxin in advanced renal failure when there appears to be a shift from renal to slower biliary excretion.

• Authors: M H Gault, D Sugden, C Maloney, M Ahmed, M Tweeddale
• Journal: Clinical pharmacology and therapeutics (Clin Pharmacol Ther) Vol. 25 Issue 5 Pt 1 Pg. 499-513 (May 1979) ISSN: 0009-9236 [Print] United States
• PMID: 436354 (Publication Type: Journal Article)

Chemical References

• Digoxin

Topics

• Adult
• Aged
• Bile (metabolism)
• Biotransformation
• Chromatography, Ion Exchange
• Digoxin (metabolism, urine)
• Female
• Half-Life
• Humans
• Kidney Diseases (metabolism)
• Male
• Middle Aged
• Renal Dialysis
• Time Factors