Omeprazole: Pharmacology, Pharmacokinetics and Interactions

Oosterhuis, B.; Jonkman, J. H. G.

doi:10.1159/000200098

Cited by 30 publications

(24 citation statements)

References 11 publications

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“…Minor elevations of the AUCs by 10% of digoxin and by 21% of nifedipine after pretreatment with omeprazole were ascribed to decreased gastric acidity and regarded as having no clinical significance (11,34). Other studies demonstrated 26 to 54% reductions of the clearance of diazepam and a 19% rise of the AUC of phenytoin after prior administration of omeprazole, which is probably due to a competition for binding sites of the cytochrome P-450 subfamily IIC (2,3,17,36).…”

Section: Discussionmentioning

confidence: 99%

Interaction study of lomefloxacin and ciprofloxacin with omeprazole and comparative pharmacokinetics

Stuht¹,

Lode²,

Koeppe³

et al. 1995

Antimicrob Agents Chemother

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To assess whether or not concomitant omeprazole treatment influences the pharmacokinetics of lomefloxacin and ciprofloxacin, a randomized, double-blind four-way-crossover study was performed. Another objective was to compare the pharmacokinetics of lomefloxacin and ciprofloxacin. Twelve healthy volunteers participated. On days 1 to 4 of each study period, each of them took 20 mg of omeprazole or a placebo orally, and on day 4, each took 400 mg of lomefloxacin or 500 mg of ciprofloxacin orally. Blood and urine samples were collected and assayed for the quinolones by high-pressure liquid chromatography. The mean peak concentrations in plasma (C max ) and the areas under the curves (AUC), respectively, of lomefloxacin and ciprofloxacin, respectively, after prior treatment with placebo were 2.88 ؎ 0.73 (mean ؎ standard deviation) as against 2.60 ؎ 0.76 g/ml and 24.9 ؎ 3.13 as against 11.9 ؎ 1.89 g ⅐ h/ml, and 72.4% ؎ 5.10% as against 36.1% ؎ 7.50% of the doses of lomefloxacin and ciprofloxacin, respectively, were recovered from the urine. None of the pharmacokinetic parameters differed significantly after prior treatment with omeprazole compared with placebo. The C max of lomefloxacin was not significantly higher than that of ciprofloxacin, but lomefloxacin's AUC reached twice that of ciprofloxacin because of its significantly longer half-life in plasma (6.68 ؎ 1.94 as against 4.15 ؎ 0.92 h, respectively, P Յ 0.01). Concomitant therapy with omeprazole did not alter the pharmacokinetics of lomefloxacin or ciprofloxacin in these single-dose studies.The bioavailability of fluoroquinolone antimicrobial agents is markedly reduced by aluminum-magnesium-containing antacids (15,19,20,40) and the aluminum-containing mucousprotective drug sucralfate (13). On the other hand, histamine 2 receptor antagonists exert only minor effects on the pharmacokinetics of the quinolones. One study indicated that cimetidine diminishes the clearance of pefloxacin by inhibiting its hepatic biotransformation (41), and intravenously administered ranitidine led to a 40% reduction in the bioavailability of enoxacin (15), but the pharmacokinetics of ciprofloxacin and ofloxacin were not altered by coadministration of ranitidine per os (20,32).The present randomized, double-blind study was designed to determine the effect of omeprazole, a powerful inhibitor of gastric H ϩ /K ϩ -ATPase (26), on the pharmacokinetics of lomefloxacin and ciprofloxacin. In addition, the pharmacokinetics of the two quinolones, which were administered open labeled, were compared.(Results of this study were presented as a poster at the 18th International Congress of Chemotherapy, Stockholm, 1993 [43]). MATERIALS AND METHODSSubjects. Twelve healthy volunteers participated. Six were females, and six were males. Their mean age, height, weight, and creatinine clearance were 31.8 Ϯ 7.00 years, 1.75 Ϯ 0.09 m, 72.5 Ϯ 9.34 kg, and 112 Ϯ 15.5 ml/min/1.73 m 2 , respectively (means Ϯ standard deviations). Exclusion criteria were a regular use of medication within 4 weeks prior to the ...

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Section: Discussionmentioning

confidence: 99%

Interaction study of lomefloxacin and ciprofloxacin with omeprazole and comparative pharmacokinetics

Stuht¹,

Lode²,

Koeppe³

et al. 1995

Antimicrob Agents Chemother

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“…31 Thus it is expected to have a narrow spectrum of interaction limited to drugs metabolized by this enzyme. However, interactions with diazepam, phenytoin, warfarin, digoxin, or methotrexate are reported as not clinically significant.…”

Section: Drug Interactionsmentioning

confidence: 99%

“…However, interactions with diazepam, phenytoin, warfarin, digoxin, or methotrexate are reported as not clinically significant. [31][32][33][34][35][36] There is no effect of omeprazole on metabolism of several other drugs tested like theophylline, 37,38 propranolol 39 or cyclosporine.…”

Section: Drug Interactionsmentioning

confidence: 99%

Delayed-release oral suspension of omeprazole for the treatment of erosive esophagitis and gastroesophageal reflux disease in pediatric patients: a review

Monzani¹,

Oderda²

2010

CEG

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Abstract:Omeprazole is a proton-pump inhibitor indicated for gastroesophageal reflux disease and erosive esophagitis treatment in children. The aim of this review was to evaluate the efficacy of delayed-release oral suspension of omeprazole in childhood esophagitis, in terms of symptom relief, reduction in reflux index and/or intragastric acidity, and endoscopic and/or histological healing. We systematically searched PubMed, Cochrane and EMBASE (1990 to 2009) and identified 59 potentially relevant articles, but only 12 articles were suitable to be included in our analysis. All the studies evaluated symptom relief and reported a median relief rate of 80.4% (range 35%-100%). Five studies reported a significant reduction of the esophageal reflux index within normal limits (7%) in all children, and 4 studies a significant reduction of intra-gastric acidity. The endoscopic healing rate, reported by 9 studies, was 84% after 8-week treatment and 95% after 12-week treatment, the latter being significantly higher than the histological healing rate (49%). In conclusion, omeprazole given at a dose ranging from 0.3 to 3.5 mg/kg once daily (median 1 mg/kg once daily) for at least 12 weeks is highly effective in childhood esophagitis.

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“…Under physiological acidic conditions, aspirin is absorbed in its lipid state by passive diffusion across the gastric mucosal membrane according to the pH partition hypothesis 6. PPIs exert their antacid effect by inhibiting the H + /K + -exchanging ATPase of the gastric parietal cells, thus raising intragastric pH 7. In fact, the pH potentially rises above the p K a (3.5) of acetylsalicylic acid, causing a pronounced reduction in the lipophilicity of aspirin 8.…”

Section: Introductionmentioning

confidence: 99%

The antiplatelet effect of aspirin is reduced by proton pump inhibitors in patients with coronary artery disease

Würtz

Grove²,

Kristensen³

et al. 2009

Heart

113

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Omeprazole: Pharmacology, Pharmacokinetics and Interactions

Cited by 30 publications

References 11 publications

Interaction study of lomefloxacin and ciprofloxacin with omeprazole and comparative pharmacokinetics

Interaction study of lomefloxacin and ciprofloxacin with omeprazole and comparative pharmacokinetics

Delayed-release oral suspension of omeprazole for the treatment of erosive esophagitis and gastroesophageal reflux disease in pediatric patients: a review

The antiplatelet effect of aspirin is reduced by proton pump inhibitors in patients with coronary artery disease

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