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Theophylline steady state pharmacokinetics is not altered by omeprazole

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Summary

The effect of omeprazole treatment on theophylline pharmacokinetics was studied in eight, non-smoking healthy male volunteers during repeated administration of a slow release formulation of theophylline. In a randomized double-blind cross-over study, the subjects received theophylline 5 mg·kg−1 per day with omeprazole 20 mg per day or identical placebo during two periods, each of 7 days, separated by a washout period of 7 days.

The oral clearance of theophylline remained unchanged whether it was administered alone or with omeprazole (54.2 ml·min−1). The average urinary excretion of theophylline and its metabolites, 1,3 dimethyluric acid (1,3-DMU), 3-methylxanthine (3-MX), 1-methyluric acid (1-MU) amounted to 9%, 32%, 12% and 22% of the administered dose, respectively, and no significant change occured during concomitant treatment with omeprazole.

Thus, the formation and clearance of the metabolites was not altered by omeprazole. Consequently, omeprazole in the recommended dose of 20 mg daily can safely be administered to patients on theophylline therapy.

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Taburet, A.M., Geneve, J., Bocquentin, M. et al. Theophylline steady state pharmacokinetics is not altered by omeprazole. Eur J Clin Pharmacol 42, 343–345 (1992). https://doi.org/10.1007/BF00266361

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  • DOI: https://doi.org/10.1007/BF00266361

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