Fighting Arthritis at 105

Like a high-flying Internet stock riding a wave of marketing hype, COX-2 selective inhibitors had their bubble burst in September 2004, sending patients scrambling to ensure the safety of their most valuable of investments: their health. As a result, arthritics have been returning to an old standby, aspirin, whose use has been linked in dozens of studies to a decreased risk of heart attack and thrombotic stroke.

For years, aspirin (acetylsalisylic acid or ASA) had been the only drug available to fight arthritis. According to Bayer's aspirin.com website, Dr. Felix Hoffmann "discovered acetylsalicylic acid in a fortuitous experiment while searching for a remedy that would be better tolerated by his father, who was plagued by rheumatoid arthritis." It still remains one of the first analgesics people reach for, due to its low cost (pennies per use) and widespread availability (wherever a headache can be found). A groundbreaking study in 1971 by John Vane of the Royal College of Surgeons in London showed that aspirin works by suppressing cyclooxygenase, an enzyme responsible for the formation of prostaglandins (which, among other things, help relay pain information to the brain) and thromboxanes (which help clot blood).

Later research showed that there were different versions of the cyclooxygenase enzymes: COX-1 (responsible for maintaining the gastrointestinal tract) and COX-2 (responsible for inflammation and pain throughout the body), that aspirin inhibited equally well. It suppressed the pain arising from the prostaglandins that the COX-2 enzyme produced, but also prevented the gastric-protective COX-1 enzyme from doing its job. The latter, coupled with aspirin's acidic nature, sets the stage for serious gastrointestinal complications.

COX-2 selective inhibitors, like Vioxx (rofecoxib), Bextra (valdecoxib), and Celebrex (celecoxib), were developed with the hope that they would reduce the gastrointestinal side effects without interfering with the COX-1 enzyme. Alas, due to uncertainty surrounding COX-2 inhibitors and adverse cardiovascular events, Vioxx was withdrawn from the market by Merck in September 2004, followed in December by an FDA recommendation calling for the limited use of Celebrex and Bextra. Still, there is hope that other drugs can safely target the COX-2 enzyme, like the prescription drug Mobic (meloxicam) although because of its lower COX-2 selectivity, it is not classified as a COX-2 in the United States, and the emerging COX-2 drugs Arcoxia (etoricoxib), from Merck, and Prexige (lumiracoxib), from Novartis, currently undergoing trials for safety.

Aside from its analgesic qualities, aspirin inhibited blood clotting, the cause of heart attacks and thrombotic stroke. As an anticoagulant, aspirin was a natural candidate to prevent these kinds of events from occurring.

Though it is an over-the counter drug, aspirin can have serious side effects, including ulcers, increased bleeding, and, in children, has been associated to the development of Reye's Syndrome. Patients who are thinking of starting an aspirin regimen to control their arthritis pain should first consult with their doctor.