Omeprazole limited sampling strategies to predict area under the concentration-time curve ratios: implications for cytochrome P450 2C19 and 3A phenotyping.

Purpose: To develop a limited sampling strategy (LSS) to predict area under the concentration-time curve (AUC) ratios of omeprazole (AUC) to its metabolites 5-hydroxyomeprazole (AUC) and omeprazole sulfone (AUC) as phenotyping parameters for cytochrome P450 (CYP) 2C19 and 3A. Methods: Data were obta...

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Publicado en:European Journal of Clinical Pharmacology Vol. 68; no. 4; pp. 407 - 414
Autores principales: Lawson, Eileen, Wu, Jerry, Baldwin, R., Ingelman-Sundberg, Magnus, Rosenborg, Staffan, Yim, Dong-Seok, Yin, Ophelia, Capparelli, Edmund, Ma, Joseph
Formato: research tables/charts Journal Article
Publicado: Springer Nature Apr2012
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Apr2012
      vid: 68
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      pub: Springer Nature
      place: New York, New York
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        atl: Omeprazole limited sampling strategies to predict area under the concentration-time curve ratios: implications for cytochrome P450 2C19 and 3A phenotyping.
      aug:
        au:
          Lawson, Eileen
          Wu, Jerry
          Baldwin, R.
          Ingelman-Sundberg, Magnus
          Rosenborg, Staffan
          Yim, Dong-Seok
          Yin, Ophelia
          Capparelli, Edmund
          Ma, Joseph
        affil: Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego (UCSD), 9500 Gilman Drive, MC 0714 La Jolla 92093-0714 USA
      sug:
        subj:
          Omeprazole Metabolism
          Drug Monitoring Methods
          Omeprazole Pharmacokinetics
          Genotype
          Human
          Secondary Analysis
          Male
          Female
          Descriptive Statistics
          Measurement Issues and Assessments
          Phenotype
          Chromatography, High Pressure Liquid
          Data Analysis Software
          Young Adult
          Adult
          Multiple Linear Regression
          Adult: 19-44 years
          Male
          Female
      ab: Purpose: To develop a limited sampling strategy (LSS) to predict area under the concentration-time curve (AUC) ratios of omeprazole (AUC) to its metabolites 5-hydroxyomeprazole (AUC) and omeprazole sulfone (AUC) as phenotyping parameters for cytochrome P450 (CYP) 2C19 and 3A. Methods: Data were obtained from 37 (4 women) Caucasian, Chinese, and Korean healthy adults from three published studies. The AUC, AUC, and AUC were calculated via noncompartmental analysis. Observed AUC/AUC and AUC/AUC were determined. Plasma concentrations of omeprazole, 5-hydroxyomeprazole, and omeprazole sulfone at 1, 1.5, 2, 3, 4, 6, and 8 h post-dose were used to generate limited sampling strategy (LSS) models to predict AUC/AUC and AUCAUC. Bias and precision were assessed via percentage mean prediction error (%MPE) and percentage mean absolute error (%MAE), with acceptable limits being <15%. Results: For CYP2C19, the AUC/AUC was [mean ± standard deviation (SD)] 2.10 ± 1.63. Five LSS models of AUC/AUC were generated, but none met the bias or precision criteria. Upon stratification by CYP2C19 genotype and ethnicity, a three-timepoint (at 1, 2, and 4 h) LSS model accurately predicted AUC/AUC in Caucasian CYP2C19*1/*1 subjects. For CYP3A, AUC/AUC (mean ± SD) was 1.79 ± 0.67. All LSS models had unacceptable %MAE, even when stratified by CYP2C19 genotype and ethnicity. Conclusions: A LSS model to predict AUC/AUC, and thus CYP2C19 activity, was generated for Caucasian CYP2C19*1/*1 subjects. However, additional model validation is needed prior to general use. LSS models to predict AUC/AUC, and thus CYP3A activity, were not possible, even upon stratification by CYP2C19 genotype and ethnicity.
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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