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COX-2 Inhibitors

In an effort to circumvent the ulcer problem, drug manufacturers developed the Cox-2 inhibitors. These are "super aspirins" that block the Cox-2 enzyme that drives inflammation but don't block the Cox-1 enzyme that releases the prostaglandins protecting the stomach. The drugs don't suppress pain or reverse the ravages of the disease any better than older options, but they have fewer side effects than other arthritis drugs.

At least, that is the claim of their manufacturers. The FDA is not convinced. It approved Searle's Cox-2 inhibitor Celebrex as a good option to relieve arthritis pain but declared there is no proof the drug is easier on patients' stomachs than other drugs. The FDA has required the same warning about side effects as for older painkillers. Potential downsides of Celebrex reported in the Proceedings of the National Academy of Sciences include a reduction in beneficial prostaglandins and an increase in the risk of heart attack.

Despite these drawbacks, in its first three weeks on the market in early 1999 about 142,000 prescriptions were written for Celebrex, making it the second-fastest-selling new drug after the anti-impotence drug Viagra. Over the long run, in fact, Celebrex is expected to fare better than Viagra, since most users take anti-impotence drugs only when the urge strikes them (or when they hope it will). Arthritis victims take arthritis drugs virtually every day; and once they start on one, they are likely to take it for life. In 1998, drug companies sold about $6 billion in brand-name prescription NSAIDs. Sales of Celebrex were projected to reach $1 billion a year later, equivalent to a sixth of the NSAID market. Celebrex costs $2.50 to $3.00 per day for the lowest effective dose (200 mg). This is more than three times the cost of a therapeutically equivalent amount of NSAIDs (ibuprofen or naproxen); while glucosamine and chondroitin sulfates, the most popular nutritional remedies, may be had for as little as twenty cents a day.

Merck, the world's largest drug company, sought government approval for its own Cox-2 inhibitor, Vioxx, in the spring of 1999. Merck hoped to persuade the FDA that Vioxx is superior to Celebrex and does not need any warning label about gastrointestinal effects. But as with Celebrex, the FDA has not permitted Merck to claim that Vioxx is less damaging to the gastrointestinal tract than traditional NSAIDs such as aspirin. The reviewing committee approved the drug for short-term use but observed that its side effects, including swelling, high blood pressure, and elevated potassium levels, increase with increasing doses, suggesting it might not be safe for use long term. The committee advised against its use for chronic pain and said its use for acute pain should be limited to five days, the longest Merck had studied it for that purpose.

If the FDA is heeded, Vioxx won't be much help for arthritis sufferers, since they need long-term relief; but the FDA's warnings probably won't halt its use for arthritis pain. The rule is that once a drug has been approved, a doctor may prescribe it for any purpose deemed in his or her professional judgment to be appropriate. Celebrex, its competitor Cox-2 inhibitor, became the number one prescription arthritis medication a year after it got FDA approval.

The Under-Appreciated Benefits of Inflammation

Even if the Cox-2 inhibitors are not hazardous to the stomach (a matter that remains in dispute), there is a more fundamental problem with these drugs. All arthritis drugs, including Cox-2 inhibitors, relieve the pain of arthritis merely by suppressing some stage of the inflammatory process, thus relieving pressure on the nerves. They do this by inhibiting the synthesis of prostaglandins that cause dilation of the blood vessels. The problem is that this dilation is necessary to increase the blood flow required for the repair of joint structures.

Studies have shown that suppressing inflammation not only doesn't cure arthritis but actually speeds joint deterioration. Inflammation is a natural process by which the body tries to remove dead or damaged tissue cells and lays down the matrix for new cells to replace the old. It does this by a buildup of body fluids that serves to destroy or wall off toxins and injured tissue and carry immune system cells to the site of damage. When this process is interfered with, the already compromised joint simply deteriorates more rapidly. In the hip, the resulting affliction is called "analgesic hip," a progressive degeneration of the joint caused by the very drugs given to treat joint pain. Cartilage and bone degeneration increases, leading to more hyperplasia (abnormal proliferation of normal cells), more joint capsule scarring, and more pain. Animal studies have shown that aspirin, indomethacin, and other NSAIDs promote the rapid breakdown of cartilage. All NSAIDs can also cause sodium and water retention, which is thought to trigger changes in deteriorating cartilage.25 And NSAIDs suppress the production of proteoglycans, a type of glycoprotein found in connective tissue. The stiffness and cushioning ability of cartilage is directly correlated with its content of these substances.

Copyright © 2001 by Ellen Hodgson Brown.

Tags: Arthritis

About the Author

Ellen Hodgson Brown is a health writer who specializes in alternative medicine. Her books include The Alternative Pharmacy (with Dr. Lynne Walker) and The Key to Ultimate Health.