Abstract
1. The influence of multiple dose administration of omeprazole on the pharmacokinetics of oral digoxin was studied in 10 healthy male volunteers. 2. In a randomized two-way crossover design a single dose of 1 mg digoxin was administered either alone (control) or on day 8 of an 11 day course of omeprazole 20 mg once daily. 3. Plasma digoxin concentrations were measured over 96 h after digoxin administration with a [125I]-r.i.a. method. 4. On average, Cmax and AUC values for digoxin were approximately 10% higher and tmax tended to be shorter during the administration of omeprazole, while the elimination rate constant was unaffected. 5. The increase in AUC(0,96 h) was statistically significant (P less than 0.05), but within the accepted range for bioequivalence. In two subjects the increase was approximately 30%. 6. It is concluded that co-treatment with omeprazole causes a minor increase in the absorption of oral digoxin. The magnitude of this effect is not considered to be clinically relevant for the majority of patients.
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Selected References
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- Böttcher H., Lüllmann H., Proppe D. Comparison of digoxin with some digitoxin metabolites on cat heart lung preparation. Eur J Pharmacol. 1973 Apr;22(1):109–111. doi: 10.1016/0014-2999(73)90192-1. [DOI] [PubMed] [Google Scholar]
- Gault H., Kalra J., Ahmed M., Kepkay D., Barrowman J. Influence of gastric pH on digoxin biotransformation. I. Intragastric hydrolysis. Clin Pharmacol Ther. 1980 Jan;27(1):16–21. doi: 10.1038/clpt.1980.3. [DOI] [PubMed] [Google Scholar]
- Gault H., Kalra J., Ahmed M., Kepkay D., Longerich L., Barrowman J. Influence of gastric pH on digoxin biotransformation. II. Extractable urinary metabolites. Clin Pharmacol Ther. 1981 Feb;29(2):181–190. doi: 10.1038/clpt.1981.29. [DOI] [PubMed] [Google Scholar]
- Kuhlmann J., Abshagen U., Rietbrock N. Pharmacokinetics and metabolism of digoxigenin-mono-digitoxoside in man. Eur J Clin Pharmacol. 1974;7(2):87–94. doi: 10.1007/BF00561320. [DOI] [PubMed] [Google Scholar]
- Lage G. L., Spratt J. L. Structure-activity correlation of the lethality and central effects of selected cardiac glycosides. J Pharmacol Exp Ther. 1966 Jun;152(3):501–508. [PubMed] [Google Scholar]
- Ochs H. R., Greenblatt D. J., Bodem G., Harmatz J. S. Dose-independent pharmacokinetics of digoxin in humans. Am Heart J. 1978 Oct;96(4):507–511. doi: 10.1016/0002-8703(78)90162-x. [DOI] [PubMed] [Google Scholar]
- Ochs H. R., Greenblatt D. J., Bodem G. Single- and multiple-dose kinetics of intravenous digoxin. Clin Pharmacol Ther. 1980 Sep;28(3):340–345. doi: 10.1038/clpt.1980.171. [DOI] [PubMed] [Google Scholar]
- Somogyi A., Muirhead M. Pharmacokinetic interactions of cimetidine 1987. Clin Pharmacokinet. 1987 May;12(5):321–366. doi: 10.2165/00003088-198712050-00002. [DOI] [PubMed] [Google Scholar]