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Influence of Omeprazole on Bioavailability of Bismuth following Administration of a Triple Capsule of Bismuth Biskalcitrate, Metronidazole, and Tetracycline
Author(s) -
Spénard Jean,
Aumais Christian,
Massicotte Julie,
Tremblay Claude,
Lefebvre Marc
Publication year - 2004
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270004265643
Subject(s) - omeprazole , cmax , metronidazole , bioavailability , capsule , tetracycline , toxicity , pharmacology , bismuth , chemistry , pharmacokinetics , medicine , gastroenterology , antibiotics , biochemistry , biology , botany , organic chemistry
The objective of this study was to determine the impact of omeprazole on bismuth (Bi) bioavailability when given in a three‐in‐one capsule containing bismuth biskalcitrate, metronidazole, and tetracycline. Thirty‐four healthy volunteers were randomly assigned to receive three capsules (each containing bismuth biskalcitrate 140mg+ metronidazole 125 mg+ tetracycline 125 mg) qid alone × 6 days or the same treatment + omeprazole (OM) 20 mg bid. Blood was drawn at intervals for 24 hours after the last dose. After the last dose, mean (CV) Cmin for plasma bismuth was 2882 pg/mL (36%) and 1195 pg/mL (23%) (p < 0.001), with and without OM, respectively. Mean (CV)Cmax was 25,493 pg/mL (69%) and 8061 pg/mL (28%) (p < 0.001) with and without OM, respectively. AUC0‐24 increased by 2.9 in presence of OM (p < 0.001). Adverse events in both groups were usually mild and of a gastrointestinal nature, and all had resolved by the end of the trial. This study confirms an interaction between Bi biskalcitrate and OM. Risk of Bi toxicity, seen after long‐term use of Bi compounds, is minimal here because plasma levels of Bi remained well below the toxic levels of 50 μg/L, and the treatment period with this triple capsule + OM is only 10 days, a substantially lower number of days compared to that which might produce Bi toxicity.