Related topics: •  Alternative Medicines for Arthritis •  Arthritis Center •  Managing Arthritis Pain

Here's a look at the drugs commonly prescribed to treat both major types of arthritis. As you'll see, each drug has potential drawbacks. No matter what medication your doctor recommends, make sure you understand the risks and follow the instructions exactly.

It's important to understand which type of arthritis you have. Osteoarthritis is the most common. The main problem in osteoarthritis is that cartilage (the stiff, rubbery substance that provides a cushion between two bones) starts wearing down after years of hard use, causing pain and stiffness. Physical therapy, gentle exercise, and weight loss can help relieve symptoms, but in some cases joint surgery or injections may be necessary. Drugs to treat this condition focus mainly on pain relief.

Rheumatoid arthritis works differently: It often develops at an earlier age and it's believed to be an autoimmune disorder. (The immune system mistakenly attacks your own body's tissue, in this case your joints.) Like other autoimmune conditions, rheumatoid arthritis is more common in women. In rheumatoid arthritis, the synovial membranes of your joints get inflamed (from the immune cells attacking it). The immune cells also release certain enzymes that eventually chew away the cartilage. New studies suggest that rheumatoid arthritis needs to be treated aggressively early on for the best long-term results. Drugs to treat rheumatoid arthritis target the wayward immune response and control pain in the process, with the goal of remission.

Examples: Tylenol, generics

Doctors have known for a long time that acetaminophen -- when used correctly -- is one of the safest pain relievers around. For this reason, it's often doctors' first choice for treating chronic osteoarthritis pain. Since it doesn't help reduce inflammation, people with rheumatic arthritis aren't likely to benefit from taking acetaminophen alone.

Possible side effects: A study reported in the August 2005 edition of the journal Hypertension found that women taking over 500 mg of acetaminophen per day increased their risk of developing high blood pressure by up to 99 percent. Because acetaminophen is an ingredient in many over-the-counter preparations like cold medicines, it's not always easy to be sure how much you're getting in a day, so be sure to read labels carefully. If you take acetaminophen every day, it's a good idea to have your blood pressure checked regularly. Also, the Food and Drug Administration (FDA) estimates that 14,000 people wind up in the emergency room each year with accidental acetaminophen overdoses. So even if you don't have to worry about high blood pressure, be sure you get no more than 4 grams -- or 4,000 milligrams -- a day. (That's eight extra-strength tablets or 12 regular tablets.)

Possible cautions: You should not take acetaminophen if you're a heavy drinker (you regularly have three or more alcoholic drinks a day), and your doctor should also know if you have a history of liver disease. Large doses of acetaminophen can overload and damage your liver -- especially if it has to detoxify alcohol as well.

But whether you drink alcohol regularly or not, it's a good idea to keep tabs on the amount of acetaminophen you take every day. A study reported in the December 2005 issue of the journal Hepatology followed 662 patients with acute liver failure over a period of six years and found that acetaminophen was the most common cause of liver poisoning. Almost half of those cases were unintentional overdoses.

Regularly using this drug can also enhance the action of the blood thinning drug warfarin (Coumadin), possibly leading to internal bleeding.

Examples: aspirin (Anacin, Bayer, and Bufferin) ibuprofen (Advil, Motrin), naproxen (Aleve), ketoprofen (Orudis)

As the name suggests, these drugs ease inflammation as well as pain. For decades, NSAIDs have been the cornerstone of treatment for many different kinds of arthritis. But just because something is available over-the-counter doesn't mean it's perfectly safe. Large doses of NSAIDs -- or smaller doses over a long time -- can cause bleeding stomach ulcers, as well as kidney and liver damage. This is often more of a concern for people with rheumatoid arthritis. If your doctor recommends any standard NSAID, you'll need to have regular checkups to make sure the drugs aren't harming you. Also, taking an antacid, or acid-reducing drug, with NSAIDs lowers the risk of developing ulcers. These include famotidine (Pepcid), omeprazole (Prilosec), and ranitidine (Zantac).

Possible side effects: In April 2005, the US Food and Drug Administration issued a health advisory for both prescription and over-the-counter (OTC) NSAIDs. The FDA requested that manufacturers of prescription NSAIDs add a boxed warning about the potential for serious cardiovascular problems and potentially life-threatening gastrointestinal bleeding that is associated with this class of drugs. The agency also recommended that NSAIDs not be prescribed for anyone who has recently undergone coronary artery bypass surgery.

The FDA says that available evidence doesn’t indicate an increased risk for cardiovascular problems with short-term use of OTC NSAIDs. However, the agency has asked manufacturers of these drugs to revise their labels to include more specific information about the potential for cardiovascular and gastrointestinal problems and possible skin reactions. The agency also wants manufacturers to emphasize the importance of sticking to the recommended dosage and duration of use. One important note: The FDA advises that if your doctor has instructed you to take a daily aspirin to reduce the risk of heart problems, you should NOT stop taking it unless your doctor says so. Aspirin has been shown to have certain heart-protective properties. If you have any questions about your regular aspirin dose, call your doctor, but continue taking it in the meantime.

Here are some other things to be aware of if you take NSAIDs. A 2005 study found that women taking more than 400 mg of NSAIDs per day were up to 78 percent more likely to develop high blood pressure than women who didn't take the medication. So if you take NSAIDs every day, keep tabs on your blood pressure. Let your doctor know if you have an allergy to aspirin or similar drugs. You should tell your doctor if you take a blood thinner such as warfarin (Coumadin) because aspirin is also a blood thinner. High doses of aspirin can cause ringing in the ears. NSAIDs (aspirin in particular) can cause or aggravate asthma, hay fever, and nasal congestion. Other side effects can include stomach cramps, diarrhea, indigestion, vomiting, and headache. (Bleeding can occur without pain, however.) Call your doctor immediately if you notice black stools, which could indicate internal bleeding. If you vomit blood or any substance that looks like coffee grounds, or suddenly feel weak, sweaty, and dizzy, get emergency help.

Like all drugs, NSAIDs are processed in the liver and excreted through the kidneys, so these organs should be monitored carefully. Drinking alcohol can overwhelm and damage your liver, so it's best to cut down. NSAIDs can enhance the action of diabetes medicines and lead to low blood sugar, so diabetics need extra attention. In large doses, these drugs (except for aspirin) can also worsen high blood pressure over time.

New warnings were recently issued warnings about naproxen (Aleve), a nonsteroidal anti-inflammatory drug sold over the counter. Researchers at the National Institutes of Health were conducting a study to determine whether the drug could be used to treat Alzheimer's disease, but the study was halted after findings showed that patients who took naproxen were 50 percent more likely to have heart attacks or strokes. The Food and Drug Administration has advised people who take the drug to contact their doctors.

Examples: celecoxib (Celebrex), valdecoxib (Bextra)

Doctors had high hopes for this class of drugs for their patients who needed long-term pain relief. This drug is a type of NSAID called a COX-2 inhibitor because it targets that particular component of the inflammation process. (Other NSAIDs target both COX-1, which is found everywhere in the body, and COX-2, which is concentrated in inflamed areas.) Though doctors initially believed the drug's narrowed focus would reduce side effects, serious problems have recently been associated with this class of drugs.

Possible side effects: In April 2005, the FDA asked the manufacturer of Bextra (valdecoxib) to withdraw the drug from the market. After reviewing available data, the agency concluded that the risk of taking the drug outweighed its benefits. Risks of the drug include an increased potential for cardiovascular problems when the drug is used for pain relief in patients who have had coronary artery bypass operations, and a potentially life-threatening skin reaction in which large sections of skin blister and peel off.

In June 2005, the FDA asked the manufacturers of COX-2 inhibitors to add a boxed warning label advising users of an increased risk of cardiovascular problems and gastrointestinal bleeding associated with the drugs. The Celebrex label must also include information about a study that found an increased risk of heart problems in some participants. In the study, the manufacturer of Celebrex halted studies of the drug's effectiveness against cancer when participants in one of the studies experienced in increased risk of heart problems. Participants in the cancer studies were given 400 to 800 milligrams of Celebrex, while arthritis patients are usually prescribed anywhere from 100 to 400 milligrams.

The FDA is encouraging doctors to prescribe the lowest effective dosage of Celebrex possible for the shortest duration possible to help prevent side effects. The agency has also urged the manufacturer of Celebrex to conduct a long-term study of the drug’s safety.

In September 2004, the manufacturer of Vioxx, a popular COX-2 inhibitor, voluntarily removed the drug from the market after reports that it caused increased risk of stroke and heart attack in some people. A study by researchers at Vanderbilt University found that people on higher doses (50 mg) of Vioxx, were almost twice as likely to develop heart disease or suffer heart attacks when compared to those taking other NSAIDs or 25 mg doses of Vioxx. According to the US Food and Drug Administration, further studies bore out the evidence of increased cardiovascular risks.

If you are currently taking a COX-2 inhibitor, call your doctor for more information and advice.

There are a variety of other NSAIDs available by prescription, including nabumetone (Relafen), salsalate (Disalcid), meloxicam (Mobic), meclofenamate sodium (Meclomen), indomethacin (Indocin), and diclofenac sodium/misoprostol (Arthrotec). Many of these are gentler on the stomach than aspirin, but each has its own set of side effects, often serious. Their prices range between the over-the-counter NSAIDs and the COX-2 inhibitors.

These are usually slow-acting and work by interrupting the complex immune response that damages your joints in rheumatoid arthritis and other rheumatic conditions. Each works a little differently and side effects vary slightly, but all interfere with your immune system. The idea is that improving your rheumatoid arthritis will be worth the toll on your body -- weakened immunity against infection and other side effects. These drugs often take one to six months to take full effect, so they are also called slow-acting anti-rheumatic drugs. Many rheumatologists start their patients off on one of the first three drugs listed below. Finding the right drug (or combination) for a person can be a long process of trial and error.

Antimalarial drugs have recently been used to treat immune disorders, and the most commonly prescribed one is hydroxychloroquine (Plaquenil). It helps 30 to 40 percent of all rheumatoid arthritis patients who try it, but takes a long time to show improvement -- one to six months. Hydroxychloroquine is a common first choice because it doesn't usually cause side effects.

Possible side effects: Side effects are uncommon, but include gastrointestinal symptoms. In rare cases, it can cause inflammation of the nervous system and heart muscles. At higher doses it can sometimes cause retinal damage over time, so regular eye exams are important.

This drug suppresses the immune reaction in rheumatoid arthritis and is also an anti-inflammatory. About 60 percent of people with rheumatoid arthritis respond to this drug, but it often causes side effects. It takes at least one month to see improvement while on this drug.

Possible side effects: Patients are usually monitored closely for the first three months because of side effects, which include skin rash, headache, nausea, vomiting, stomach problems, and reduced sperm count. Some less common side effects are anemia, reduced white blood cell counts, fever, itching, and skin problems.

First used to treat various kinds of cancers, methotrexate is now commonly prescribed -- usually in combination with NSAIDs -- to treat rheumatoid arthritis. For active rheumatoid arthritis that doesn't respond to NSAIDs, methotrexate is often the next treatment of choice. It can start to work within a month, which is much sooner than some other options such as antimalarials or gold salts. A recent study found that the sooner methotrexate treatment is started, the more it helps. This finding may be true for other drugs as well, so rheumatologists are likely to treat rheumatoid arthritis more aggressively early.

Like most drugs used to treat rheumatoid arthritis, methotrexate works by mildly weakening the immune system. Patients who don't respond to methotrexate alone may be prescribed the drug in combination with other drugs such as cyclosporine. Taking folic acid can protect against the side effects of methotrexate. While you're on this drug, your doctor will monitor your liver function and possibly your blood cell counts, too.

Possible side effects: Methotrexate can cause an upset stomach, nausea, diarrhea, fatigue, unusual bleeding, and bruising. It can cause liver problems, so you should tell your doctor if you have a history of liver disease or alcoholism. Rarely, it can also cause lung problems. Because methotrexate weakens immunity and can lower white blood cell counts, you're more at risk for infections and will have a harder time fighting them off. Be sure to tell your doctor if you have an infection or a weakened immune system. Also, talk to your doctor if you're planning to have a child. Methotrexate can impair fertility in both men and women, and has the potential to cause birth defects.

This is one of the newer drugs for treating rheumatoid arthritis, and it helps about 40 percent of those who try it. Leflunomide is an option for people who can't take methotrexate or who don't respond to it, and improvement takes one to two months.

Possible side effects: This drug causes liver enzymes to be higher than normal in 5 percent of users (60 percent of those on combination methotrexate and leflunomide) indicating possible liver damage. Leflunomide can cause diarrhea, skin rashes, and hair loss, and may affect fertility in men and women. This drug causes birth defects; If you're a woman on this drug and you want to have a baby, you'll need to take gold salts to "wash" the drug from your system before you try to conceive. Otherwise, leflunomide can stay in the body for up to two years.

Example: etanercept (Enbrel), infliximab (Remicade), (anakinra) Kineret

These high-tech drugs -- products of genetic engineering -- work by targeting particular parts of the inflammation reaction. The first two drugs target tumor necrosis factor-alpha (TNF-alpha), a naturally occurring protein that plays a key role in checking tumor growth, and is also involved in joint inflammation. Recently approved to treat rheumatoid arthritis, anakinra is another genetically engineered drug. It blocks a different agent in the synovial inflammation process. It's an IL-1 receptor agonist, which means it blocks the receptor for IL-1 on certain immune cells, sort of like jamming a lock. This keeps unwanted immune proteins from doing their inflammatory work.

Biologic response modifiers are especially helpful for people with mild to moderate rheumatoid arthritis who aren't responding to other drugs. However, they can dampen the immune system significantly, and if you suffer from chronic infections, have a history of exposure to tuberculosis, or are otherwise at risk for infections, you should probably not take this drug.

Both TNF-alpha blockers are often prescribed in combination with methotrexate. Infliximab is taken intravenously and etanercept is an injectable drug, so both are fairly inconvenient -- and very expensive. On the bright side, they usually take effect within two weeks, and work for more than half of all people who try them. These drugs can also slow the damage of rheumatoid arthritis better than methotrexate alone.

Possible side effects: All can raise the risk of serious infections because they suppress your immune system in a specific way. Your doctor should know if you have an active infection or have been exposed to tuberculosis in the past. If you notice any signs of an infection, see your doctor right away. Etanercept and anakinra can commonly cause reactions at the injection site. Infliximab may aggravate heart disease and increase the likelihood of congestive heart failure. Because these drugs interfere with the way your body fights cancer they pose a potential cancer risk. In fact, the FDA mentioned a seven-fold increase in lymphoma among some patients taking Remicade in controlled studies, leading the agency to order manufacturers to cite the risk in their warning labels. Patients with asthma or chronic obstructive pulmonary disease have higher rates of lung infections on anakinra.

Examples: prednisone (Deltasone, Orasone), methylprednisolone (Medrol)

These powerful medications -- either taken orally or sometimes injected into a joint -- ease inflammation and put the brakes on the immune system. They offer rapid, dramatic relief of rheumatoid arthritis, but are not a good choice for long-term therapy because of their wide range of serious side effects. Corticosteroids are often prescribed during severe flare-ups or when other drugs aren't working. Your doctor will start lowering your dosage as soon as the disease seems to be under control. You'll need regular checkups to make sure the benefits of the drugs outweigh the risks.

Possible side effects: Corticosteroids can be very hard on the body, especially when taken at high doses for long periods of time. Side effects can include weakened immunity (and increased risk of infection), mood changes, weight gain, ulcers, and gastrointestinal bleeding. Skin becomes sensitive to sunlight and can also become fragile, resulting in easy bruising and stretch marks. Acne, increased body hair, and "moon face" are other cosmetic problems with corticosteroids. Potential long-term complications include osteoporosis, diabetes, cataracts, and hypertension (which increases the risk of heart disease, kidney damage, and stroke). People on these drugs are monitored for a variety of complications.

Among patients who are unable to take NSAIDs or methotrexate, gold salts can work up to 60 percent of the time. The salts are injected or taken as pills, though injections work better. It takes about three to six months before gold salts show a benefit, which is longer than average.

Possible side effects: Inflammation of the skin and mouth, protein in the urine, and lowered white blood cell counts. These are more common when on injections. Other side effects of the injections include dizziness, nausea, and pain within an hour of the shot. Taking the pill form often causes diarrhea.

Examples: azathioprine (Imuran), cyclosporine (Neoral), cyclophosphamide (Cytoxan), penicillamine (Cuprimine)

Often used to prevent rejection after organ transplant, azathioprine (Imuran) and cyclosporine (Neoral) are immune suppressants that are sometimes used to treat arthritis when other drugs have failed. They're not a first choice treatment because of their side effects, and because broadly suppressing the immune system also leaves you prone to infections. Cyclophosphamide (Cytoxan) is an anticancer drug with a wide range of serious side effects, so it is rarely used for rheumatoid arthritis.

Penicillamine is an older drug derived from the antibiotic penicillin. Once commonly used for treating rheumatoid arthritis, now it's rarely used because the dose needs to be increased slowly each month, and it takes four to six months to start working. Researchers are also studying minocycline (a tetracycline antibiotic) because it may be useful in combination with methotrexate at a lower cost than some of the new biologic drugs.

Possible side effects: These vary by drug. Immune-suppressing drugs can increase your risk of infections. Imuran can cause digestive system problems including nausea and vomiting. Cyclosporine is highly toxic and can cause high blood pressure and kidney damage, but its more common side effects include headache, swollen or bleeding gums, sensitivity to sunlight, and tremors. Cyclophosphamide can cause nausea, vomiting, rash, fatigue, dizziness, ringing in the ears, hair loss, temporary sterility (in men), and bladder inflammation (rarely). Side effects from penicillamine include nausea, upset stomach, and kidney damage.

-- Chris Woolston, MS, is a health and medical writer with a master's degree in biology. He is a contributing editor at Consumer Health Interactive, and was a staff writer at Hippocrates, a magazine for physicians. His reporting on occupational health earned him an award from the Northern California Society of Professional Journalists. Deepi Brar is the multimedia editor at Consumer Health Interactive and a former researcher in gene cancer therapy at the City of Hope hospital.

References

First published September 26, 2002
Last updated January 25, 2007
Copyright © 2002 Consumer Health Interactive

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