Use in Gel Form May Offer Safer Joint Pain Relief

SOUTH BEND — A local pharmacist says doctors should take a second look at an old way of delivering pain relief: putting medicine in a gel and rubbing it right where it hurts.

Connie Chalko, of Mar-Main Pharmacy, says non-steroidal anti- inflammatory drugs may have fewer side effects if they’re compounded in a gel and applied topically.

The Mar-Main, a compounding pharmacy, has been mixing up gels containing ketoprofen and other common NSAIDs for years. Some local sports medicine doctors and rheumatologists have been using them to relieve some of their patients’ aching joints.

Older anti-inflammatory medicines taken orally — starting with the oldest of all, aspirin — can cause potentially fatal stomach and intestinal bleeding if used long term at certain doses.

Vioxx was created to be safer for the stomach. But then it had to be pulled from the market last fall when its maker discovered that it increased the risk of heart attack and stroke.

The Food and Drug Administration is reviewing the safety of two other COX-2 drugs that are similar to Vioxx, Celebrex and Bextra, and may rule on their fates as soon as next week.

The disappointing turn of events means that many people are again searching for safe ways to relieve chronic pain for their arthritis.

Medicine rubbed directly on a sore joint rather than swallowed as a pill might be safer because of the way it’s absorbed. Some of it gets into the bloodstream and enters the system. But one study suggests that a much higher concentration stays at the joint, where it’s less likely to cause trouble.

“You have more of a local effect and less side effect,” she said.

In one sense, topical joint relief is a throwback to the old- fashioned medicated liniments, which had a powerful smell and a warming effect on the skin but not much else.

“Oils and liniments for pain relief go all the way back to the Colonial period,” said Gregory Higby, director of the American Institute of the History of Pharmacy, in Madison, Wis. “There were very few effective oral medications for pain until 1899 and the invention of aspirin.”

The pain gel mixed at Mar-Main, of course, is not an old-time liniment. It contains effective anti-inflammatory medicine. And the gel used as the base has been shown to penetrate the skin and deliver medicine directly to joints, Chalko said.

Three local doctors who are using topical ketoprofen said it appears to work well and safely. They’re cautious, however, about saying it’s safe for long-term joint pain relief.

Scientific studies proving either its long-term effectiveness or long-term safety simply have not been done.

“The last time I looked there was … little data about long- term effects,” said Dr. Brent Mohr, a South Bend rheumatologist who said he has used a ketoprofen gel made at Mar-Main and found it to be successful.

The practice of putting anti-inflammatory drugs in gels is also a so-called “off-label use,” one that’s perfectly legal but not specifically approved by the Food and Drug Administration.

“That always raises a red flag,” said Dr. Stephen Simons, a sports physician in South Bend who has been using compounded gels from Mar-Main for 12 years.

Simons said he likes to use ketoprofen gel in patients whose inflammation is close to the surface. Tendonitis of the elbow — tennis elbow — is a good example.

Dr. Mark Lavallee, who also is a sports medicine specialist, said he sometimes orders compounds that include several medicines.

The idea of putting medicines close to the injury appeals to him.

“Why have it go to your ear or your big toe and all the other places you don’t want it to go?” Lavallee said.

While long-term studies have yet to be done, Mohr said one of his patients used ketoprofen gel for six months without any stomach or intestinal bleeding or loss of effectiveness.

Mohr said he recommends the gel approach for patients who have trouble taking pills and have only one or two painful joints.

It’s impractical to expect someone with rheumatoid arthritis pain in all their joints to use a gel, he said.

“They can’t rub a gel all over three times a day,” he said. “It’s too much.”

With the loss of Vioxx and heavy suspicion falling on Celebrex and Bextra, Mohr said his first choice is to prescribe an older NSAID in oral form.

To protect the stomach, he prescribes it in combination with a heartburn medicine such as Prilosec or Nexium.

He’s not happy about that.

“So you’re giving two medicines with two sets of side effects,” he said.

Simons said the safety of the gel form of ketoprofen ultimately comes down to how much of it is absorbed into the bloodstream. If a lot of it is absorbed, then it’s likely to have the same bad side effect as the oral NSAIDS.

Encouragingly, one study done in Italy found that most of the medicine delivered through a gel stays in the joint tissue and joint fluid and only a little makes its way into the bloodstream.

Stephen Scott, an associate professor of pharmacy practice at Purdue University, said locally applied medicines generally have a mostly local effect. But again, the studies are lacking.

“The data will never be developed unless a pharmaceutical company decides to use a topical approach,” he said.

All three physicians interviewed for this story said it’s too soon to give up on Vioxx and its cousins Celebrex and Bextra.

Their risks must be balanced against their benefits for people who face daily debilitating pain.

“My fear is that the FDA is going to take significantly more drugs off the market,” Mohr said. “If they take our tools away, we’re not going to be able to help people.”

Staff writer David Rumbach:

drumbach@sbtinfo.com

(574) 235-6358