No effects of pantoprazole on the pharmacokinetics of rosuvastatin in healthy subjects.

Purpose: Rosuvastatin disposition is modulated by the expression and activity of several membrane transporters including BCRP (ABCG2). The objective of our study was to investigate the effects of pantoprazole, a previously proposed BCRP inhibitor, on the disposition of rosuvastatin. Methods: The imp...

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Publicado en:European Journal of Clinical Pharmacology Vol. 72; no. 8; pp. 925 - 932
Autores principales: Huguet, J., Lu, J., Gaudette, F., Chiasson, J.-L., Hamet, P., Michaud, V., Turgeon, J.
Formato: clinical trial equations & formulas research tables/charts Journal Article
Publicado: Springer Nature Aug2016
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Aug2016
      vid: 72
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      pub: Springer Nature
      place: New York, New York
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        116775248
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        10.1007/s00228-016-2065-6
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        atl: No effects of pantoprazole on the pharmacokinetics of rosuvastatin in healthy subjects.
      aug:
        au:
          Huguet, J.
          Lu, J.
          Gaudette, F.
          Chiasson, J.-L.
          Hamet, P.
          Michaud, V.
          Turgeon, J.
        affil: CRCHUM, Centre de recherche du Centre hospitalier de l'Université de de Montréal, 900 Saint-Denis Street Montréal H2X 0A9 Canada
      sug:
        subj:
          Rosuvastatin Pharmacokinetics
          Pantoprazole Sodium Contraindications
          Drug Interactions
          Membrane Transport Proteins Antagonists and Inhibitors
          Human
          Descriptive Statistics
          Confidence Intervals
          Odds Ratio
          Rosuvastatin Blood
          Metabolic Clearance Rate Evaluation
          Clinical Trials
      ab: Purpose: Rosuvastatin disposition is modulated by the expression and activity of several membrane transporters including BCRP (ABCG2). The objective of our study was to investigate the effects of pantoprazole, a previously proposed BCRP inhibitor, on the disposition of rosuvastatin. Methods: The impact of pantoprazole (40 mg ID for 2 days) on rosuvastatin pharmacokinetics was evaluated in healthy volunteers ( n = 16) who received a single oral dose of rosuvastatin (10 mg) either alone or with pantoprazole. Rosuvastatin, N-desmethylrosuvastatin, and rosuvastatin lactone levels were quantified in plasma while rosuvastatin and N-desmethylrosuvastatin excretion were measured in urine. Results: Ratios and 90 % standard confidence interval of geometric means for C (1.03 [0.91-1.16]), AUC (1.03 [0.89-1.19]) and renal clearance (0.96 [0.85-1.09]) were all within the pre-specified range of 0.8-1.25, indicating a lack of drug-drug interaction between pantoprazole and rosuvastatin. Conclusions: Concomitant administration of pantoprazole with rosuvastatin did not affect rosuvastatin plasma concentrations. The use of pantoprazole as a BCRP inhibitor should be revisited when characterizing BCRP-mediated transport in humans.
      pubtype: Academic Journal
      doctype:
        clinical trial
        equations & formulas
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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