The History of Aspirin

Aspirin was the first manufactured drug to relieve fever and aches. Aspirin is acetylsalicylic acid, an industrial synthesis of salicin, which occurs naturally in white willow (Salix alba), a large tree with gray bark. Greek physicians wrote about the benefits of bitter white willow powder more than 2,000 years ago. Ancient Europeans chewed leaves of white willow as a folk remedy in prehistoric times. In the United States, 50 million aspirin tablets are sold annually.

  1. Willow Bark

    • Native Americans and Chinese herbalists used willow bark as early as Europeans did. For example, three nations in the southeastern United States, the Alabama, Houma and Chickasaw, made decoctions (concentrates), poultices and tea of the roots or bark of their regional willows to relieve fevers and aches. In 1876, a British doctor working in South Africa made an anecdotal report to the British medical journal Lancet regarding Hottentot healers who used willow bark to treat fever.

    Identification

    • In 1828, French pharmacist Henri Leroux isolated willow bark's medically active principal, a glucoside (sugar) of o-hydroxybenzyl alcohol. Leroux named it salicin, after the genus Salix. An Italian organic chemist, Raffaele Piria, separated the sugar and oxidized the remaining component to salicylic acid. In 1839, salicylic acid was isolated in Germany from meadowsweet (Filipendula ulmaria), a wildflower. The compound was unsuccessfully marketed in Germany, where side effects included stomach bleeding and diarrhea. In the 1840s, methyl salicylate, a derivative of salicylic acid, was identified as the active principal in the essential oil of wintergreen mint.

    Bayer

    • In 1853, Carl von Gerhardt introduced an acetyl group into a salicylic acid compound, creating stomach-friendly acetylsalicylic acid (ASA), but he did not take the product to market. In 1897, Felix Hoffman, an employee of Bayer in Germany, reviewed Gerhardt's work and recreated a stable ASA. Bayer conducted large-scale studies of the safety and effectiveness of treating pain and fever with Hoffman's ASA. In 1899, Bayer marketed ASA as a white powder sold in glass bottles. To the old genus name, Spiraea, for meadowsweet, Hoffman added an "a" as an abbreviation for acetyl, creating the brand for his product "aspirin."

    Prostaglandins

    • For many years after aspirin reached mass market, the action of aspirin in the body was still not described. In the mid-1900s, prostaglandins (cyclic fatty acids that can act as hormones) were studied for their effect on labor and abortion, fever, inflammation and other metabolic processes. In the 1960s, British chemist John Vane developed "cascade superfusion assay" (test by flooding tissues with substances) protocol to study how some biochemicals influence cell reception of other biochemicals. Vane demonstrated that aspirin inhibited the formation of prostaglandins. He was awarded a Nobel Prize in recognition of his work.

    Heart

    • The Physician's Health Study conducted between 1982 and 1995 used a large voluntary group of physicians to test whether some daily supplements affected myocardial infarction (blood clots entering the heart). The study found that low-dose aspirin reduced risk by 44 percent. Aspirin inhibits the action of prostaglandins that cause blood platelets to aggregate as clots.

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