Pharmacokinetics and Metabolism of Digitoxin in the Human

Vöhringer, H. F.; Rietbrock, N.

doi:10.1007/978-3-642-66904-0_6

Cited by 5 publications

(2 citation statements)

References 13 publications

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“…Consistent with prev ous studies of digitoxin (Perrier et al, 1977;Ochs et al, 1980b;Haustein, 1981;Vohringer & Rietbrock, 1978), elimination half-life is very long, averaging 8 days in the present study. Digitoxin volume of distribution averaged 0.76 1/kg.…”

Section: Multiple-dose Kineticssupporting

confidence: 92%

Digitoxin accumulation.

Ochs¹,

Pabst²,

and³

et al. 1982

Brit J Clinical Pharma

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1 Nine healthy volunteers received single 1 mg intravenous doses of digitoxin, following which serum digitoxin concentrations were measured at multiple points in time over the next 14 days. 2 Mean kinetic variables for digitoxin were: volume of distribution, 0.761/kg; elimination half-life, 8 days; total clearance, 0.049 ml min-kg-'. 3 After a drug-free interval of at least 4 months, subjects took 0.07 mg of oral digitoxin daily for 28 consecutive days. Serum digitoxin concentrations were measured during the period of dosage and in the 21 day post-dosage washout. 4 Digitoxin accumulation was slow, proceeding with a mean half-life (7.9 days) that was nearly identical to the single-dose half-life. However, the two were not significantly correlated. 5 Mean observed steady-state serum concentrations (15.4 ng/ml) also were nearly identical to those predicted from the single-dose study (15.3 ng/ml), but again the two were not significantly correlated. 6 Steady state is very slowly attained after initiation of maintenance therapy with digitoxin. The kinetic data suggest that a loading dose on the average should be 12 times the maintenance dose.

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Section: Multiple-dose Kineticssupporting

confidence: 92%

Digitoxin accumulation.

Ochs¹,

Pabst²,

and³

et al. 1982

Brit J Clinical Pharma

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“…Knowledge of DT3 metabolism is very limited because the biotransformation is complex, involving conversion of DT3 to form DG3, hydrolysis of sugar side chains of DT3 and DG3, and epimerization at C-3 of the aglycone (15,(20)(21)(22). Furthermore, evidence of conjugates and other polar metabolites of the drug has been found, but the products have not been fully characterized (20).…”

mentioning

confidence: 99%

Reductive inactivation of digitoxin by Eubacterium lentum cultures

Chandrasekaran¹,

Robertson²,

Reuning³

1987

Appl Environ Microbiol

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The obligate anaerobe Eubacterium lentum inactivated the cardiac glycoside digitoxin by reducing the double bond in the lactone ring. This conversion was quantitative when the substrate was incubated at a concentration of 10 ,ug/ml. The reduction reaction coincided with the growth phase of the bacterium. The stereochemical configuration at C-20 of the reduction product dihydrodigitoxin was found to be R. Incubation of digitoxigenin and its mono-and bisdigitoxosides individually with E. lentum led to the formation of their respective dihydro derivatives. The configuration at C-20 of these reduced metabolites was also found to be R.

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Neue Gesichtspunkte zur Digitalistherapie bei Niereninsuffizienz

Krämer¹

1980

Pharmakotherapie Bei Niereninsuffizienz

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Pharmacokinetics and Metabolism of Digitoxin in the Human

Cited by 5 publications

References 13 publications

Digitoxin accumulation.

Digitoxin accumulation.

Reductive inactivation of digitoxin by Eubacterium lentum cultures

Neue Gesichtspunkte zur Digitalistherapie bei Niereninsuffizienz

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