ISSN:
1432-1912
Keywords:
Digoxin and Derivatives
;
Bis- and Monodigitoxosides
;
Biliary Excretion
;
Renal Excretion
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary The metabolism of digoxin (D), 4‴-acetyldigoxin (AD) and 4″-methyldigoxin (MD) was studied in biliary fistula rats by quantitative analysis of the excretion of these glycosides after intraduodenal administration. The total activity excreted within 12 h in bile amounts to 45.1; 40.5; 21.3 and in urine to 11.6; 14.3; 17.6% of the dose of D, AD and MD respectively. AD undergoes a rapid, but incomplete desacetylation in the organism. The highest desacetylation activities were found in liver, in intestinal mucosa and in kidney. Yet considerable amounts of unchanged AD were found in portal vein blood and still another 1–2% of the dose in bile and urine. In contrast MD is very slowly demethylated. 15 min after intraduodenal administration portal vein blood contains almost exclusively MD. A stepwise cleavage of digitoxoses from D as well as of AD and MD is indicated. The absolute amounts of digoxigenin-bis-digitoxoside (4–8% of the dose), digoxigenin-mono-digitoxoside (2.5–8.5%) excreted in bile and urine were in the same range for all three glycosides examined, although the relative amounts of these metabolites in bile and urine were much higher after administration of MD than of the two other glycosides. In addition a water-soluble fraction could be detected in bile and urine after administration of D, AD and MD. The absolute quantities of polar metabolites (4.5–7.0%) excreted in bile and urine were identical for all three glycosides.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00508087
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