Features October 2007 Issue

Know Your NSAIDs to Reduce Risks, Maximize Relief

Prescription painkillers or over-the-counter meds? Knowing the options can help ease your arthritis discomfort safely.

The use of nonsteroidal anti-inflammatory drugs, or NSAIDs, is as widespread as the arthritis they treat. Yet, despite the common usage of NSAIDs by more than 40 million Americans each day to manage chronic pain, the drugs remain misunderstood and often misused by those who rely on them most.

"Patients over the age of 60 need to be careful not only because of their increased risk for side effects, but also for the negative interactions NSAIDs may have with other medications they’re taking," says Mandy Leonard, Pharm.D., BCPS, a pharmacist and assistant director for Drug Information Services and Formulary Management at Cleveland Clinic. "You should always have a pharmacist review the list of drugs you’re currently taking before

NSAID'S For Reflief
beginning any NSAID therapy."

How they work

For those with moderate to severe arthritis, NSAIDs offer much-needed pain relief. Although they come in more than 20 varieties—a patient may respond better to one drug than another—all NSAIDs offer the same benefits by reducing pain and inflammation, lowering fever, and preventing your blood from clotting. The most popular over-the-counter (OTC) NSAIDs include aspirin (although this is not typically used to treat arthritis), ibuprofen (Motrin and Advil), and naproxen (Aleve), which fall into the "traditional NSAIDs" category.

A newer class of NSAID, called a selective cyclooxygenase 2 (COX-2) inhibitor, or coxib, was introduced in the late 1990s and quickly earned praise for the drug’s ability to offer pain relief in addition to serving as a gastro-protective shield for NSAID users. While coxib drugs were deemed effective, a study of the COX-2 inhibitor rofecoxib (Vioxx) showed that patients taking this drug were at increased risk for heart attack and stroke. Spurred by these findings, two of the three U.S. Food and Drug Administration (FDA)-approved coxibs—Vioxx and Bextra (valdecoxib)—were withdrawn from the market in 2004 and 2005, leaving celecoxib (Celebrex) as the only prescription coxib currently available in the U.S.

There is no doubt that NSAIDs, both traditional and coxib, are beneficial for arthritis sufferers, but understanding how they work can help you avoid both simple and serious side effects. While both traditional and coxib NSAIDs work by inhibiting cyclooxygenase (COX) enzymes within the body, which in turn provides relief of inflammation and pain, traditional NSAIDs block both COX-1 and COX-2 enzymes, while coxib NSAIDs block only the COX-2 enzymes.

"When you think of the enzyme or cyclooxygenase (COX) system, think of it as a seesaw," says Leonard. "On one side you have COX-1 enzymes that help produce certain prostaglandins or fatty acid compounds, which protect the lining of the stomach and help blood clot normally. On the other side, you have COX-2 [enzymes] that also produce prostaglandins, but this type causes inflammation, pain, and fever."

By blocking both COX-1 and COX-2 enzymes, traditional NSAIDS inhibit the bad enzymes (COX-2), but also the good enzymes (COX-1) that help prevent intestinal bleeding and ulcers. The COX-2 inhibitors, such as celecoxib, were developed to inhibit only COX-2 enzymes, explains Leonard.

Prescription or OTC?

Being prescribed a NSAID doesn’t guarantee that the pain and inflammation of your arthritis will be reduced more effectively. The difference between an OTC and prescription NSAID is that OTC drugs are typically available in a lower dose than a prescription NSAID.

"It’s not necessarily about the efficacy of either prescription or OTC NSAIDs, because it’s all relative to dose," Leonard says. "You can’t get Motrin in 600- or 800-milligram dosages over-the-counter. That requires a prescription because of the increased risk of side effects. But you can buy 200-milligram Motrin OTC and take three at once to equal the effectiveness—an option that is recommended only after consulting your physician."

Interestingly, an OTC NSAID can be just as effective as a prescription, with each variation of the drug affecting every person differently, according to Leonard. "Many people try several before finding the drug that is most effective for them," she says.

"If you’re treating osteoarthritis (OA), you may want to give a [OTC] NSAID a two- to three-week trial," says Leonard. "If you’re not getting any pain relief after this period of time, a different OTC can be tried, with a prescription-strength NSAID being the next option."


Conditions and side effects

Before taking a NSAID, review the warnings and precautions on the drug’s label, in addition to talking with your physician or pharmacist to examine possible side effects and the proper dosage for your needs, says Leonard.

Although Cox-2 inhibitor NSAIDs have been shown to increase the risk of heart attack and stroke, all NSAIDs, with the exception of aspirin, present this threat. Even though the risk of serious cardiovascular side effects varies among NSAIDs, the FDA recently added a warning to all prescription and OTC NSAIDs stating that using these drugs increases the risk of heart attacks and strokes.

In an upcoming issue, we’ll tell you how to avoid the most common, as well as most serious, side effects of NSAID use. For now, the American Heart Association recommends that coxibs be the last choice for people with, or at high risk of, heart disease. Patients with high blood pressure should also be monitored closely when taking a NSAID over a long period of time. And to protect the gastrointestinal tract, says Leonard, all NSAIDs should be taken with food or milk.