• J Clin Pharm Ther · Dec 2010

    Review

    What do we (not) know about how paracetamol (acetaminophen) works?

    • K Toussaint, X C Yang, M A Zielinski, K L Reigle, S D Sacavage, S Nagar, and R B Raffa.
    • Temple University School of Pharmacy, Philadelphia, PA 19140, USA.
    • J Clin Pharm Ther. 2010 Dec 1; 35 (6): 617-38.

    What Is Known And BackgroundAlthough paracetamol (acetaminophen), N-(4-Hydroxyphenyl)acetamide, is one of the world's most widely used analgesics, the mechanism by which it produces its analgesic effect is largely unknown. This lack is relevant because: (i) optimal pain treatment matches the analgesic mechanism to the (patho)physiology of the pain and (ii) modern drug discovery relies on an appropriate screening assay.ObjectiveTo review the clinical profile and preclinical studies of paracetamol as means of gaining insight into its mechanism of analgesic action.MethodsA literature search was conducted of clinical and preclinical literature and the information obtained was organized and reviewed from the perspective of its contribution to an understanding of the mechanism of analgesic action of paracetamol.ResultsParacetamol's broad spectrum of analgesic and other pharmacological actions is presented, along with its multiple postulated mechanism(s) of action. No one mechanism has been definitively shown to account for its analgesic activity.What Is New And ConclusionFurther research is needed to uncover the mechanism of analgesic action of paracetamol. The lack of this knowledge affects optimal clinical use and impedes drug discovery efforts.© 2010 The Authors. JCPT © 2010 Blackwell Publishing Ltd.

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