Paracetamol metabolism, hepatotoxicity, biomarkers and therapeutic interventions: a perspective
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Accepted version
Author(s)
Type
Journal Article
Abstract
After over 60 years of therapeutic use in the UK, paracetamol (acetaminophen, N-acetyl-p-aminophenol, APAP) remains the subject of considerable research into both its mode of action and toxicity. The pharmacological properties of APAP are the focus of some activity, with the role of the metabolite N-arachidonoylaminophenol (AM404) still a topic of debate. However, that the hepatotoxicity of APAP results from the production of the reactive metabolite N-acetyl-p-benzoquinoneimine (NAPQI/NABQI) that can deplete glutathione, react with cellular macromolecules, and initiate cell death, is now beyond dispute. The disruption of cellular pathways that results from the production of NAPQI provides a source of potential biomarkers of the severity of the damage. Research in this area has provided new diagnostic markers such as the microRNA miR-122 as well as mechanistic biomarkers associated with apoptosis, mitochondrial dysfunction, inflammation and tissue regeneration. Additionally, biomarkers of, and systems biology models for, glutathione depletion have been developed. Furthermore, there have been significant advances in determining the role of both the innate immune system and genetic factors that might predispose individuals to APAP-mediated toxicity. This perspective highlights some of the progress in current APAP-related research.
Date Issued
2018-03-06
Date Acceptance
2018-02-07
Citation
Toxicology Research, 2018, 7 (3), pp.347-357
ISSN
2045-452X
Publisher
Royal Society of Chemistry
Start Page
347
End Page
357
Journal / Book Title
Toxicology Research
Volume
7
Issue
3
Copyright Statement
© The Royal Society of Chemistry 2018
Subjects
Science & Technology
Life Sciences & Biomedicine
Toxicology
INDUCED LIVER-INJURY
INDUCED HEPATIC-NECROSIS
ACETAMINOPHEN HEPATOTOXICITY
ISOLATED HEPATOCYTES
GLUTATHIONE DEPLETION
SPECIES-DIFFERENCES
COVALENT BINDING
DRUG-METABOLISM
FAILURE
MICE
Publication Status
Published
Date Publish Online
2018-03-06