When were NSAIDs first used?
Salicylates have been used for centuries. In the 4th century B.C., Hippocrates, Celsus, Galen, and others recorded the use of willow bark and other plants known to contain salicylates to treat fever and pain. Today, one can find numerous health food stores and herbal websites selling willow bark for use in pill form, tinctures, and a dried form to be used in tea. Purification of the active ingredient and development of modern NSAIDs is outlined below:
- 1760s—Dr. Edward Stone published his experience with willow bark as an antipyretic when dried.
- 1829—salicylic acid isolated from willow bark.
- 1853—Gerhardt buffered salicylic acid with sodium and acetyl chloride, creating sodium salicylate and acetylsalicylic acid.
- 1860—salicylic acid chemically synthesized (Kolbe).
- 1897—acetylsalicylic acid (ASA, aspirin) chemically synthesized (Hoffman; working for Bayer Company).
- 1899—ASA introduced in the United States as a powder (Bayer Company).
- 1949—phenylbutazone, the first alternative to salicylates, introduced.
- 1960s—indomethacin introduced.
- 1970s— J.R. Vane (1971) demonstrated that ASA, indomethacin, and salicylate all exert their effect by COX inhibition (Nobel Prize in Medicine, 1982). Ibuprofen, fenoprofen calcium, naproxen and tolmetin introduced.
- 1990s—introduction of the specific COX-2 inhibitors.