5 - Nonsteroidal Anti-Inflammatory Drugs and Acetaminophen: Pharmacology for the Future  pp. 53-69


By Jon McCormack and Ian Power

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The nonsteroidal anti-inflammatory drugs (NSAIDs) encompass a heterogeneous group of therapeutic agents used in a wide spectrum of analgesic and anti-inflammatory roles. From aspirin, the first NSAID commercially produced for analgesic prescription over 100 years ago, the conventional NSAIDs were derived, and had been in clinical use for many years before their mechanism of action (ie, inhibiting prostaglandin synthesis) was elucidated. Acetaminophen is an analgesic and antipyretic agent that may be classified as an NSAID by virtue of its mechanism of action on prostaglandin metabolism. The development of the highly selective coxibs has been ongoing since the mid-1990s. This chapter discusses the history, pharmacokinetic properties, perioperative use, and adverse effects of the NSAIDs.

HISTORY

The Salicylates

In the 18th century the bark of the willow tree (Salix alba) was noted to have analgesic properties, whereby a letter from Rev. Mr Edward Stone to the Royal Society in 1763 described “a bark of an English tree, which I have found by experience to be a powerful astringent, and very efficacious in curing anguish and intermitting disorders.” These properties were conferred by a glycoside of salicylic acid, named sialicin, first isolated from natural sources as yellow crystals by Buchner in 1828. German chemists also succeeded in isolating salicylic acid from Meadowsweet (Spirea ulmaria) but it was not until the latter part of the century, in 1860, that Kolbe synthesized salicylic acid and its sodium salt from phenol, carbon dioxide, and sodium.

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