The Story of Ibuprofen

Acute inflammation, though uncomfortable and painful, does have its benefits:

• Acts as a defense mechanism to protect from infection and injury.
• Localizes and eliminates the injurious agent.
• Removes damaged tissue.

Fortunately, the discomfort is temporary and leaves when the inflammatory response has done its job. Problems arise when inflammation is chronic, however, because of some persistent injury or autoimmune condition that results in a constant sensation of pain. This stress interferes with our rest, sleep, and comfort, which are needed to maintain a  healthy body.

For many decades only aspirin or salicylates were found to reliably relieve inflammation and reduce pain without the use of an opioid type of drug that risked the possibility of addiction.  In the 1940’s, cortisone and its successor, prednisone, were discovered to be very effective as anti-inflammatory agents. However, it was found that aspirin caused bleeding problems and ulcers in the gastrointestinal tract, and the long-term use of prednisone or steroids also had many harmful side effects. During the 1950’s and 1960’s there was extensive research devoted to seeking alternative anti-inflammatory drugs. In the 1960’s, a small pharmaceutical company in England, Boots Pure Drug Company Ltd of Nottingham , United Kingdom, discovered ibuprofen after testing hundreds of compounds. The method of testing was a key to its discovery. Until that time testing a drug against inflammation was time consuming, but Boots scientist Dr. Stewart Adams developed a method of screening compounds as anti-inflammatories that was quick and reliable,  allowing hundreds of compounds to be tested instead of a few at a time. Dr. John Nicholson, the lead chemist at Boots,  synthesized the compound. Medicinal chemists are as important in drug discovery as pharmacologists. First, they need to verify the structure of the compound precisely, then determine the best way to produce the compound reliably and in sufficient quantity and quality for economical bulk production.

One interesting item of trivia is the first recorded use of ibuprofen. According to the story, Dr. Adams, the night before he was to give a lecture at a conference, had imbibed too many cocktails and developed a profound headache from a hangover. He took some ibuprofen, believing it was safe, and relieved his headache.

Ibuprofen has been shown to be safer than aspirin and steroids as  an anti-inflammatory pain reliever, but it is still not without its adverse reactions. The main untoward effects are nausea, dyspepsia, gastrointestinal ulceration and bleeding, dizziness, salt and fluid retention and high blood pressure. Though these adverse reactions have been reported with ibuprofen, it is still considered a relatively safe drug. For this reason, it was eventually removed from prescription only status to being sold over-the-counter. Only the 200mg tablet and children’s and infant’s liquid formulations are available without a prescription. Ibuprofen comes in 400mg, 600mg, and 800mg tablets that are prescription only. As a reminder, always read and understand the dosing instructions on the package before using.

Other familiar drugs in this class of nonsteroidal anti-inflammatories (NSAID) have been developed. Some familiar names are naproxen, diclofenac, celecoxib, ketorolac, and indomethacin. Though ibuprofen can be bought without a prescription, it is still a highly effective drug and can cause harm if not used correctly, in the long term.

The story of ibuprofen is the search for something safer than what was available. Through more efficient testing methods and advances in chemistry, scientists were able to accelerate the discovery and bring this medication to market.

Prosper and be in health.