The influence of ethnic factors and gender on CYP1A2-mediated drug disposition: A comparative study in Caucasian and Chinese subjects using phenacetin as a marker substrate

A. Bartoli, S. Xiaodong, G. Gatti, G. Cipolla, R. Marchiselli, E. Perucca

Research output: Contribution to journalArticle

Abstract

To assess potential ethnic and gender-related differences in the expression of cytochrome CYPIA2-mediated activity, the pharmacokinetics of phenacetin (a CYPIA2 substrate) and its metabolite paracetamol were compared in 20 Caucasian and 20 Chinese subjects after administration of a single oral 900 mg phenacetin dose. Peak plasma concentrations and apparent oral clearance values for phenacetin did not differ between the two groups (geometric means: 3.4 μg/ml and 1.56 ml h-1 kg-1, respectively, for Caucasians vs. 4.7 μ/ml and 1.25 ml h-1 kg-1 respectively, for Chinese, after excluding one Caucasian with aberrantly low plasma phenacetin values). Pharmacokinetic parameters for metabolically derived paracetamol were also similar in the two groups. When subjects were divided into subgroups according to gender, phenacetin apparent oral clearance values were found to be lower in Chinese women compared with both Chinese men and Caucasian subjects of either sex. It is concluded that there are no major interethnic differences in the expression of CYP1A2-related activity between Caucasians and Chinese, although Chinese women as a subgroup may exhibit comparatively lower enzyme activity.

Original languageEnglish
Pages (from-to)586-591
Number of pages6
JournalTherapeutic Drug Monitoring
Volume18
Issue number5
DOIs
Publication statusPublished - 1996

Keywords

  • Cytochrome CYP1A2
  • Drug metabolism
  • Ethnopharmacology
  • Gender
  • Paracetamol
  • Pharmacogenetics
  • Phenacetin

ASJC Scopus subject areas

  • Toxicology
  • Health, Toxicology and Mutagenesis
  • Pharmacology
  • Biochemistry
  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology (medical)
  • Public Health, Environmental and Occupational Health

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