Monograph
C01AA04 - Digitoxin |
Not porphyrinogenic |
NP |
Rationale
Metabolised by CYP3A4. Clinical observation and two references point to non-porphyrinogenicity.The daily dose is beneath the mg range and hepatocyte exposure beneath the micromolar range.
Chemical description
3β-[(O-2,6-Dideoxy-β-d-ribo-hexopyranosyl-(1→4)-O-2,6-dideoxy-β-d-ribo-hexopyranosyl-(1→4)-2,6-dideoxy-β-d-ribo-hexopyranosyl)oxy]-14β-hydroxy-5β-card-20(22)-enolide. M = 764.9
Therapeutic characteristics
Glycoside used for digitalisation in heart failure and arrythmia. Steady-state therapeutic plasma concentrations of digitoxin may range from 10 to 35 nanograms/mL.
Metabolism and pharmacokinetics
40% excreted in bile as conjugates after hydrolysis and hydroxylation where CYP3A is involved. Most metabolites are inactive; the major active metabolite is digoxin. Enterohepatic recycling occurs and about 25-30% is excreted unchanged in urine. Digitoxin is very slowly eliminated from the body. The daily dose is beneath the mg range and hepatocyte exposure beneath the micromolar range.
Personal communication
S. Thunell, 2004. Swedish observations (n=11): tolerated.
Published experience
Tolerance has been described by Kauppinen and Mustajoki (1992).
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Kauppinen and Mustajoki. Prognosis of acute porphyria: Occurrence of acute attacks, precipitating factors,and assocciated diseases. Medicine 1992; 71, 1-13.
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| * | Drug reference publications | |
| 2. | Martindale 2009.
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