Abstract

Salicylates have been used to treat pain and inflammation associated with rheumatism and other conditions since ancient times. The Assyrians initially described the use of willow leaves in treating rheumatism . This practice was continued into the 19th century when the first scientific studies evaluating this remedy were published in Europe. The active ingredient, salicylic acid, was first discovered in 1838 by the Italian chemist Raffaele Piria. Herman Kolbe of Marburg University elucidated the chemical structure and synthesized the compound in 1859 opening the door for industrial production of salicylic acid. However, early preparations of salicylic acid were plagued by side effects, such as unpleasant taste and dyspepsia, leading to discontinuation of treatment in a significant number of patients. This inspired Felix Hoffmann of Friedrich Bayer & Co. to develop a stable and better-tolerated form of the drug: acetylsalicylic acid. This new compound was marketed in 1899 as “Aspirin”. This acetylation step would prove to have consequences that reached well beyond tolerability and pain relief. In fact, it is now clear that it is responsible for aspirin’s widespread clinical use as an antiplatelet agent.

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