Arthritis medication

by Nathan Wei, MD, FACP, FACR

Nathan Wei is a nationally known board-certified rheumatologist and author of the Second Opinion Arthritis Treatment Kit. It's available exclusively at this website... not available in stores.

Click here: Second Opinion Arthritis Treatment Kit

The medications used to treat arthritis depend mostly on the type of arthritis being treated. That’s why diagnosis is important.

However, regardless of diagnosis, there are only three main categories.

• Analgesics
• Anti-inflammatory drugs
• Disease-modifying drugs

Analgesics are pain relievers. They have no anti-inflammatory effect. Analgesics may be non-narcotic or narcotic. Most patients with mild arthritis will get relief with over-the-counter analgesics such as acetaminophen (Tylenol).

There are a variety of strong pain relievers that often contain narcotic drugs, that a physician may prescribe to help relieve severe arthritis pain.

Often, these pain relievers are combined with acetaminophen (Tylenol). They include:

• Tylenol with Codeine (acetaminophen with codeine)
• Lorcet, Lortab, Vicodin. (Hydrocodone with acetaminophen)
• Morphine
• OxyContin (oxycodone)
• Ultram (tramadol)
• Ultracet (tramadol with acetaminophen)

Alcohol and drugs containing acetaminophen or Tylenol don't mix. The combination can increases the risk of severe liver damage.

Narcotics increase the risk of developing dependence. Also, narcotic drugs can cause constipation, drowsiness, dry mouth, and difficulty with urination.

Unlike non-steroidal anti-inflammatory drugs which will be discussed below, narcotic pain relievers do not decrease inflammation. Narcotic drugs work on pain receptors in the central nervous system to relieve pain.

For people who have more pain or in whom acetaminophen just doesn’t “cut it”, the next category of medicines is the non-steroidal anti-inflammatory drug group (NSAIDS).

(Pain that isn't relieved by a narcotic drug or NSAID alone, can sometimes respond to combining the two. In some cases, an NSAID/analgesic combination may relieve pain better than either alone.)

NSAIDS, both over the counter and prescription, can be used to relieve the symptoms of arthritis. Most patients with arthritis have tried one of these drugs.

Non-steroidal anti-inflammatory drugs have analgesic (pain-killing), anti-inflammatory, and antipyretic (fever-reducing) properties. The mechanism of action of NSAIDs is to block the formation of prostaglandins. The long and short of it is that prostaglandins are responsible for the start of the inflammatory response. So, by blocking their production, NSAIDS reduce inflammation.

Prostaglandins also have other properties. They function to protect the stomach lining, promote clotting of the blood, regulate salt and fluid balance, and maintain blood flow to the kidneys when kidney function is reduced. By decreasing prostaglandin production, NSAIDs can cause stomach damage, bleeding, fluid retention, and diminished kidney function.

NSAIDs are 95% albumin (protein) bound. The unbound part of the NSAID is increased in patients with low albumin concentrations such as in active rheumatoid arthritis and the elderly. That's why toxicity is such an issue in this type of situation.

Since NSAIDs bind to plasma proteins they can be displaced by or may displace other plasma protein bound drugs such as coumadin, methotrexate, digoxin, cyclosporine, oral antidiabetic agents, and sulfa drugs. This interaction can increase either therapeutic or toxic effects of either drug. Sometimes this effect is significant and sometimes it is not. The bottom line: keep an eye on the patient.

There seems to be a variation in patient response with NSAIDs. One may work better in a given patient than another.

A trial period of two weeks should be given for anti-inflammatory effectiveness to be observed.

Fever-lowering and anti-inflammatory effects of NSAIDs can mask the signs and symptoms of infection.

Adverse effects of NSAIDs which can occur at any time include renal (kidney) failure, hepatic (liver) damage, bleeding, and gastric (stomach) ulceration.

NSAIDs can interfere with blood pressure medicines such as beta-adrenergic antagonists, angiotensin-converting enzyme inhibitors, or diuretics.

Long-term use of NSAIDs may have a damaging effect on chondrocyte (cartilage) function.

COX-2 NSAIDS like Celebrex block one type of prostaglandin that is responsible for inflammation without affecting the prostaglandins that protect the stomach. This is supposed to make the COX-2's safer from an ulcer perspective. And they are. But...

There is evidence that the COX-2 inhibitors Celebrex as well as all other NSAIDS increase the risk of heart attack and stroke, especially at higher doses and when used over long periods of time

Glucocorticoids (steroids, corticosteroids) are powerful anti-inflammatory drugs that are used to treat many forms of arthritis including rheumatoid arthritis, plus lupus and other forms of inflammation such as vasculitis.

Although effective, steroids have many side effects. Glucocorticoids are synthetic drugs that mimic a naturally occurring steroid called cortisol. Steroids work by decreasing inflammation and reducing immune system function.

Glucocorticoids are catabolic. They are different from anabolic steroids, which some athletes use to build bigger muscles. Examples of glucocorticoids include cortisone, prednisone and methylprednisolone.

Steroids can be given topically, by mouth (orally) or by injection. When injected, they can be given into a vein or directly into a joint or bursa or into tendon sheaths.

In certain diseases, however, the immune system doesn't function properly. This may cause inflammation to work against the body's own tissues and cause damage.

When inflammation threatens to damage critical organs, steroids can be life-saving. They may prevent the progression of kidney inflammation, which can lead to kidney failure in people who have lupus or vasculitis. For these people, steroid therapy may save the patient from kidney dialysis or transplantation.

Low doses of steroids provide relief from pain and stiffness for people with rheumatoid arthritis. Temporary "bursts" of higher doses of steroids may help a person recover from a flare of arthritis.

Steroids often are injected directly into joints to treat conditions such as rheumatoid arthritis, gout, or other inflammatory diseases.

Steroids should not be injected when there is infection in or near the area to be targeted or even elsewhere in the body. Also, if a joint is "end-stage", injections are not likely to provide any benefit.

If someone has a potential bleeding problem or is taking anticoagulants (often referred to as blood thinners), steroid injections may cause bleeding at the site. For these people, injections should be given with great caution.

Steroid injections more often than every three or four months, are not recommended because they weaken tissue.

The following side effects might occur:

• Infection
• Allergic reactions
• Bleeding into the joint
• Rupture of a tendon
• Skin discoloration
• Weakening of bone, ligaments and tendons (from excessively frequent, repeated injections into the same area)

Not everyone will develop side effects and side effects vary.

Side effect occurrence depends on the dose, type of steroid and length of treatment. Common side effects of steroids include:

• Acne
• Blurred vision
• Cataracts or glaucoma
• Easy bruising
• Difficulty sleeping
• High blood pressure
• Increased appetite, weight gain
• Increased growth of body hair
• Lower resistance to infection
• Muscle weakness
• Anxiety, nervousness, restlessness
• Osteoporosis • Sudden mood swings or psychosis
• Swollen, puffy face
• Water retention, swelling
• Worsening of diabetes

The side effects listed generally do not occur when occasional steroid injections are given for arthritis, tendonitis or bursitis.

However, if steroid use involves high doses and is prolonged (for a few months to several years), an increase in the number of side effects will occur.

To minimize the side effects of steroids:

•Use the minimal dose required to gain control of the disease.
•Reduce the dose gradually as the disease remains under control.

People with the following conditions should use steroids cautiously:

•Uncontrolled diabetes
•Uncontrolled hypertension (high blood pressure) or congestive heart failure
•Peptic ulcer disease
•Osteoporosis (bone thinning)

Disease modifying anti-rheumatic drugs (DMARDS) can alter the course of some forms of inflammatory arthritis such as rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis.

DMARDs work by suppressing immune system function. In inflammatory forms of arthritis the immune system is overactive and attacks the joints and internal organs.

Although effective, DMARDS are slow acting and often take a few months to "kick in." Therefore, they are often combined with a faster working drug such as an NSAID or steroids to help relieve arthritis symptoms.

Examples of DMARDS include:

•Leflunomide or Arava

Over the past several years, researchers have developed newer DMARDs that more specifically target the immune system and have fewer side effects. These are called biologics.

Arava is a pill that is taken in a dose of 10 or 20 mg once a day. Arava can be taken on an empty stomach or with meals.

The current studies on Arava suggest these possible side effects: rash, reversible hair loss, irritation of the liver, nausea, diarrhea, and abdominal pain. When taking Arava, it is necessary to have periodic blood tests.

Arava is not recommended for people who have liver disease, pregnant or nursing women, or people with immune systems weakened by an immune deficiency or disorder.

Since Arava might cause birth defects, both men and women should use a reliable method of birth control while being treated with this medication.

Plaquenil is a drug used to treat malaria. It was discovered that it worked for arthritis when people taking the drug for malaria reported improvements in their arthritis. The drug affects the immune system, although doctors do not know exactly how it works.

It can be given along with steroid treatment to reduce the amount of steroid needed. It is also given to treat lupus.

Plaquenil is given by mouth daily. Side effects include low white blood cell counts, blood or protein in the urine, nausea, and skin rashes. It can rarely cause injury to the retina of the eye; therefore, patients on this drug should see an eye doctor every six to 12 months. It is the mildest of the DMARDS.

Gold has been used as a medical treatment for centuries and was a mainstay of RA treatment from the 1920s to the early 1980's.

Possible side effects include skin rash, anemia, low white blood cell count, or liver and kidney problems. Gold is rarely used anymore.

Azulfidine is a sulfa-based product that is used extensively in Europe. This drug is not widely used for treatment of arthritis in the United States with the exception of the pediatric group where it is still a mainstay of disease modification.

Biologics are the newest and most exciting treatments for arthritis. Currently approved to treat certain forms of inflammatory arthritis such as psoriatic arthritis or rheumatoid arthritis, they work by altering the function of the immune system with laser-like precision.

These drugs are given by intravenous (by vein) infusion or by a subcutaneous injection.

Biologics are designed to either inhibit or increase the effect of a component of the immune system called cytokines. These cytokines are protein messengers that play a pivotal role in either enhancing or suppressing inflammation (a key problem in several forms of arthritis such as rheumatoid arthritis and psoriatic arthritis).

What makes these drugs so different from other drugs used to treat RA that modify the immune system is that biologics affect a specific component of the immune system, not the entire immune system. Thus, these drugs theoretically have fewer side effects.

Biologic therapy poses some risks, since they make the patient more vulnerable to infections and diseases. Biologics may also cause some chronic diseases in remission, like tuberculosis, for example, to flare up, and they are not recommended for people with multiple sclerosis and other autoimmune conditions.

Some of the long-term effects of using these medications aren't known. For instance, do they increase the risk of malignancy? And if so, how much?

Biologic response modifiers have been studied for osteoarthritis as well. These drugs are called disease modifying osteoarthritis drugs (DMOADS).It is felt by many that osteoarthritis is more than just “wear and tear” and that a prominent inflammatory component exists as well. So far, the experience has been disappointing

The final pathway that remains to be explored with arthritis medications are treatments that can heal the damage that has already occurred. One exciting area of research is stem cell therapy.

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Click here Second Opinion Arthritis Treatment Kit

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