Oxidation of Diclofenac to Reactive Intermediates by Neutrophils, Myeloperoxidase, and Hypochlorous Acid

It reacted with glutathione to form a conjugate. 5-Hydroxydiclofenac is a major hepatic metabolite of diclofenac, and we found that rat hepatic microsomes oxidized 5-hydroxydiclofenac to the iminoquinone which was trapped with glutathione

Gohachiro Miyamoto; Nasir Zahid; Jack P. Uetrecht

2002

Scholarcy highlights

  • Diclofenac is associated with a low, but significant, incidence of hepatotoxicity and bone marrow toxicity
  • The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online
  • An alternative hypothesis is that an oxidative reactive metabolite could be responsible for such reactions and such metabolites formed by the enzymes present in neutrophils could be responsible for bone marrow toxicity
  • The same iminoquinone was formed by the oxidation of 5-hydroxydiclofenac
  • It reacted with glutathione to form a conjugate. 5-Hydroxydiclofenac is a major hepatic metabolite of diclofenac, and we found that rat hepatic microsomes oxidized 5-hydroxydiclofenac to the iminoquinone which was trapped with glutathione
  • This reactive metabolite represents another possible cause of the idiosyncratic reactions associated with the use of diclofenac

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