Studies of acetaminophen and metabolites in urine and their correlations with toxicity using metabolomics

Drug Metab Lett. 2009 Aug;3(3):130-6. doi: 10.2174/187231209789352139. Epub 2009 Aug 1.

Abstract

A LC/MS-based metabolomic assay was utilized to investigate a drug's excretion kinetic profile in urine so that the drug toxicity information could be obtained. Groups of 10 male Sprague-Dawley rats per dose were orally gavaged with a single dose of 0.2% carboxymethylcellulose, 400 mg acetaminophen (APAP)/kg body weight or 1600 mg APAP/kg. UPLC/MS and NMR were used to evaluate the excretion kinetics of major drug metabolites. N-acetyl-L-cysteine acetaminophen (APAP-NAC) had statistically significant correlations with clinical chemistry data, endogenous metabolite concentrations and histopathology data. The potential toxicity of a drug can be assessed through the study of the drug's metabolite profiles.

MeSH terms

  • Acetaminophen / administration & dosage
  • Acetaminophen / analogs & derivatives
  • Acetaminophen / pharmacokinetics
  • Acetaminophen / toxicity*
  • Acetaminophen / urine*
  • Administration, Oral
  • Analgesics, Non-Narcotic / administration & dosage
  • Analgesics, Non-Narcotic / pharmacokinetics
  • Analgesics, Non-Narcotic / toxicity*
  • Analgesics, Non-Narcotic / urine*
  • Animals
  • Biotransformation
  • Chemical and Drug Induced Liver Injury / etiology*
  • Chemical and Drug Induced Liver Injury / metabolism
  • Chemical and Drug Induced Liver Injury / pathology
  • Chromatography, Liquid
  • Creatine / urine
  • Dose-Response Relationship, Drug
  • Liver / drug effects*
  • Liver / metabolism
  • Liver / pathology
  • Magnetic Resonance Spectroscopy
  • Male
  • Mass Spectrometry
  • Metabolomics* / methods
  • Principal Component Analysis
  • Rats
  • Rats, Sprague-Dawley
  • S-Adenosylmethionine / urine
  • Sulfates / urine

Substances

  • Analgesics, Non-Narcotic
  • Sulfates
  • Acetaminophen
  • S-Adenosylmethionine
  • acetaminophen glucuronide
  • Creatine