Editors' ChoicePharmacology

Avoiding Acetaminophen Toxicity

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Science's STKE  15 Oct 2002:
Vol. 2002, Issue 154, pp. tw376-TW376
DOI: 10.1126/stke.2002.154.tw376

Acetaminophen is a widely used drug for treating pain, inflammation, and fever. However, because it is metabolized into a toxic compound, high doses can cause liver damage. Zhang et al. show that this toxicity is enhanced when a nuclear receptor called CAR has been activated, which in turn increases the expression of those enzymes that metabolize acetaminophen. However, subsequent treatment of mice exposed to high doses of acetaminophen with a CAR inverse agonist blocked toxicity. The study suggests that CAR inverse agonists could be clinically useful to treat acetaminophen-related hepatoxicity.

J. Zhang, W. Huang, S. S. Chua, P. Wei, D. D. Moore, Modulation of acetaminophen-induced hepatotoxicity by the xenobiotic receptor CAR. Science 298, 422-424 (2002). [Abstract] [Full Text]

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