Involvement of human cytochrome P450 2D6 in the bioactivation of acetaminophen.

  title={Involvement of human cytochrome P450 2D6 in the bioactivation of acetaminophen.},
  author={Huajin Dong and Robert L Haining and Kenneth E. Thummel and Allan E Rettie and Sidney D. Nelson},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  volume={28 12},
Acetaminophen (APAP), a widely used analgesic and antipyretic agent, can cause acute hepatic necrosis in both humans and experimental animals when consumed in large doses. It is generally accepted that N-acetyl-p-benzoquinone imine (NAPQI) is the toxic, reactive intermediate whose formation from APAP is mediated by cytochrome P450. Several forms of P450 in humans, including 2E1, 1A2, 2A6, 3A4, have been shown to catalyze the oxidation of APAP to NAPQI. We now present evidence which demonstrates… CONTINUE READING
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