Kinetics of omeprazole and escitalopram in relation to the CYP2C19*17 allele in healthy subjects.

PURPOSE: Ultrarapid drug metabolism of antidepressants has been associated with therapeutic failures. The CYP2C19*17 allele has been associated with higher levels of CYP2C19 gene transcription and increased rates of omeprazole and mephenytoin metabolism. The aim of this study was to compare the impa...

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Publicado en:European Journal of Clinical Pharmacology Vol. 64; no. 12; pp. 1175 - 1180
Autores principales: Rosenborg SO, Mwinyi J, Andersson M, Baldwin RM, Pedersen RS, Sim SC, Bertilsson L, Ingelman-Sundberg M, Eliasson E
Formato: research Journal Article
Publicado: Springer Nature Dec2008
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Dec2008
      vid: 64
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      pub: Springer Nature
      place: New York, New York
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        10.1007/s00228-008-0529-z
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        atl: Kinetics of omeprazole and escitalopram in relation to the CYP2C19*17 allele in healthy subjects.
      aug:
        au:
          Rosenborg SO
          Mwinyi J
          Andersson M
          Baldwin RM
          Pedersen RS
          Sim SC
          Bertilsson L
          Ingelman-Sundberg M
          Eliasson E
        affil: Karolinska Institutet, Department of Laboratory Medicine, Division of Clinical Pharmacology, Karolinska University Hospital Huddinge, SE-141 86, Stockholm, Sweden. staffan.ohlsson@ki.se
      sug:
        subj:
          Alleles
          Enzymes Pharmacokinetics
          Omeprazole Pharmacokinetics
          Serotonin Uptake Inhibitors Therapeutic Use
          Adult
          Europe
          Female
          Fisher's Exact Test
          Funding Source
          Male
          Mann-Whitney U Test
          Omeprazole Administration and Dosage
          Omeprazole Blood
          Pharmacy and Pharmacology
          Serotonin Uptake Inhibitors Adverse Effects
          Serotonin Uptake Inhibitors Blood
          Serotonin Uptake Inhibitors Metabolism
          T-Tests
          Volunteer Workers
          Human
          Adult: 19-44 years
          Female
          Male
      ab: PURPOSE: Ultrarapid drug metabolism of antidepressants has been associated with therapeutic failures. The CYP2C19*17 allele has been associated with higher levels of CYP2C19 gene transcription and increased rates of omeprazole and mephenytoin metabolism. The aim of this study was to compare the impact of the CYP2C19*17 allele on omeprazole single-dose kinetics with escitalopram exposure at steady state in volunteers genotyped as either CYP2C19*17/*17 or CYP2C19*1/*1. METHODS: Sixteen healthy volunteers participated in both study parts, five homozygous for CYP2C19*17 and 11 homozygous for CYP2C19*1. Individual pharmacokinetic parameters were determined after single-dose omeprazole of 40 mg and after 1 week on escitalopram 5 mg b.i.d. RESULTS: Escitalopram area under the concentration time curve from zero to 12 h (AUC(0-12h)) was 21% lower in homozygous carriers of CYP2C19*17 compared with CYP2C19*1 (p = 0.08). There was a significant correlation between escitalopram exposure at steady state and the single-dose kinetics of omeprazole (Spearman correlation coefficient of 0.67; p = 0.006). CONCLUSION: Based on our investigation using two different CYP2C19 substrates, we concluded that a clinically significant difference in escitalopram or omeprazole kinetics between the genotypes appears unlikely.
      pubtype: Academic Journal
      doctype:
        research
        Journal Article
      ougenre: Article
    language: English
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