Ibuprofen: Pharmacology, Therapeutics and Side Effects (2012)

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Ibuprofen is probably one of the most successful drugs used worldwide for the treatment of mild to moderate pain and various inflammatory conditions. Since its initial discovery half a century ago in December 1961 by Dr. (now Professor) Stewart Adams, the late Dr. John Nicholson and Mr. Colin Burrows of the Boots Co. Nottingham (UK) (see photo), ibuprofen has been developed in a wide variety of oral and parenteral formulations for use in an amazing variety of indications. My chapter on the “History and Development of Ibuprofen” written in the first monograph (which I also edited) on this drug details the twists and turns that took place in the discovery and development of ibuprofen from initial humble beginnings. It is a great tribute to Stewart Adams and his colleagues that their insight and persistence enabled the pharmacological activities of ibuprofen to be discovered and clinical potential to be realized at a time when little was known about inflammatory processes, let alone the techniques for quantifying clinical responses in arthritic and other painful inflammatory conditions. Indeed, it was only through screening several thousand compounds for anti-inflammatory, analgesic, and antipyretic activity in what were then relatively newly established animal models in guinea pigs and rats that the pharmacological activity of ibuprofen was identified, and found to be uniquely active compared with other compounds including that of aspirin, a reference standard employed at the time. These discoveries were essentially made on an empirical basis. It was a decade or so later before the discovery of prostaglandins and their actions in regulating inflammation. Also, it took longer before assays for detecting anti-inflammatory activity based on prostaglandin synthesis inhibition were developed, conditions understood and then refined as well as validated for screening potential therapeutic agents.

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