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Arthritis Overview
Rheumatoid Arthritis
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Rheumatoid Arthritis Medication

Most people who have rheumatoid arthritis take medications. Some medications are used only for pain relief; others are used to reduce inflammation. Still others, often called disease-modifying antirheumatic drugs (DMARDs), are used to try to slow the course of the disease.

The person's general condition, the current and predicted severity of the illness, the length of time he or she will take the drug, and the drug's effectiveness and potential side effects are important considerations in prescribing drugs for rheumatoid arthritis. The “Drug Table” section shows currently used rheumatoid arthritis medications, along with their uses and effects, side effects, and monitoring requirements.

Biologic response modifiers are new drugs used for the treatment of rheumatoid arthritis. They can help reduce inflammation and structural damage to the joints by blocking the action of cytokines, proteins of the body's immune system that trigger inflammation during normal immune responses. Three of these drugs, etanercept (Enbrel*), infliximab (Remicade), and adalimumab (Humira), reduce inflammation by blocking the reaction of TNF-α molecules. Another drug, called anakinra (Kineret), works by blocking a protein called interleukin 1 (IL-1) that is seen in excess in patients with rheumatoid arthritis.

For many years, doctors initially prescribed aspirin or other pain-relieving drugs for rheumatoid arthritis, as well as rest and physical therapy. They usually prescribed more powerful drugs later only if the disease worsened. Today, however, many doctors have changed their approach, especially for patients with severe, rapidly progressing rheumatoid arthritis. Studies show that early treatment with more powerful drugs, and the use of drug combinations instead of one medication alone, may be more effective in reducing or preventing joint damage. Once the disease improves or is in remission, the doctor may gradually reduce the dosage or prescribe a milder medication.

Summary of Common Rheumatoid Arthritis Medications

  1. Analgesics and Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
  2. Corticosteroids
  3. Disease-modifying antirheumatic drugs (DMARDs)
  4. Biologic Response Modifiers

A. NSAIDS

Medications

Uses/Effects

Side Effects

Monitoring

Analgesics and Nonsteroidal Anti-inflammatory Drugs (NSAIDs)

Analgesics relieve pain; NSAIDs relieve pain and reduce inflammation.

Upset stomach, peptic ulcer, bleeding, renal failure. Use of NSAIDs may increase rate of miscarriage for pregnant women.

For all traditional NSAIDs: Before taking these drugs, let your doctor know if you drink alcohol or use blood thinners or if you have any of the following: sensitivity or allergy to aspirin or similar drugs, kidney or liver disease, heart disease, high blood pressure, asthma, or peptic ulcers.

Acetaminophen

Nonprescription medications used to relieve pain. Examples are aspirin-free Anacin*, Excedrin caplets, Panadol, Tylenol, and Tylenol Arthritis.

Usually no side effects when taken as directed.

Not to be taken with alcohol or with other products containing acetaminophen. Not to be used for more than 10 days unless directed by a physician.

Aspirin
      Buffered
      Plain

Aspirin is used to reduce pain, swelling, and inflammation, allowing patients to move more easily and carry out normal activities. It is generally part of early and ongoing therapy.

Upset stomach; tendency to bruise easily; ulcers, pain, or discomfort; diarrhea; headache; heartburn or indigestion; nausea or vomiting.

Doctor monitoring is needed.

Traditional NSAIDs
      Ibuprofen
      Ketoprofen
      Naproxen

NSAIDs help relieve pain within hours of admin-istration in dosages available over-the-counter (available for all three medications). They relieve pain and inflammation in dosages available in prescription form (ibu-profen and ketoprofen). It may take several days to reduce inflammation.

For all traditional NSAIDs: Abdominal or stomach cramps, pain, or discomfort; diarrhea; dizziness; drowsiness or light-headedness; headache; heartburn or indigestion; peptic ulcers; nausea or vomiting; possible kidney and liver damage (rare).

For all traditional NSAIDs: Before taking these drugs, let your doctor know if you drink alcohol or use blood thinners or if you have or have had any of the following: sensitivity or allergy to aspirin or similar drugs, kidney or liver disease, heart disease, high blood pressure, asthma, or peptic ulcers.

COX-2 Inhibitor NSAIDs

COX-2 inhibitors, like traditional NSAIDs, block COX-2, an enzyme in the body that stimulates an inflammatory response. Unlike traditional NSAIDs, however, they do not block the action of COX-1, an enzyme that protects the stomach lining. This results in reduced risk of gastro-intestinal ulceration and bleeding. Reduces joint pain and inflammation.

Stomach irritation, ulceration, and bleeding may occur. Caution is advisable for patients with a history of bleeding or ulcers, de-creased renal function, hepatic disease, hyper-tension, or asthma.

Use of COX-2s with low-dose aspirin is permitted but may slightly increase ulcer risk. Doctor monitoring is recommended before taking a COX-2 inhibitor, especially if you have had a heart attack, stroke, angina, blood clot, hypertension, or sensitivity to aspirin or other NSAIDs. Doctor monitoring for possible allergic responses to COX-2s is important.

B. Corticosteroids

Medications

Uses/Effects

Side Effects

Monitoring

Corticosteroids

These are steroids given by mouth or injection. They are used to relieve inflammation and reduce swelling, redness, itching, and allergic reactions.

Increased appetite, indigestion, nervousness, or restlessness.

For all corticosteroids, let your doctor know if you have one of the following: fungal infection, history of tuberculosis, underactive thyroid, herpes simplex of the eye, high blood pressure, osteoporosis, or stomach ulcer.

Methylprednisolone
Prednisone

These steroids are available in pill form or as an injection into a joint. Improvements are seen in several hours up to 24 hours after administration. There is potential for serious side effects, especially at high doses. They are used for severe flares and when the disease does not respond to NSAIDs and DMARDs.

Osteoporosis, mood changes, fragile skin, easy bruising, fluid retention, weight gain, muscle weakness, onset or worsening of diabetes, cataracts, increased risk of infection, hyper-tension (high blood pressure).

Doctor monitoring for continued effectiveness of medication and for side effects is needed.


 

C. Disease-modifying antirheumatic drugs (DMARDs)

Medications

Uses/Effects

Side Effects

Monitoring

Disease-modifying antirheumatic drugs (DMARDs)

These are common arthritis medications. They relieve painful, swollen joints and slow joint damage, and several DMARDs may be used over the disease course. They take a few weeks or months to have an effect, and may produce significant improvements for many patients. Exactly how they work is still unknown.

Side effects vary with each medicine. DMARDs may increase risk of infection, hair loss, and kidney or liver damage.

Doctor monitoring allows the risk of toxicities to be weighed against the potential benefits of individual medications.

Azathioprine

This drug was first used in higher doses in cancer chemotherapy and organ transplantation. It is used in patients who have not responded to other drugs, and in combination therapy.

Cough or hoarseness, fever or chills, loss of appetite, lower back or side pain, nausea or vomiting, painful or difficult urination, unusual tiredness or weakness.

Before taking this drug, tell your doctor if you use allopurinol or have kidney or liver disease. This drug can reduce your ability to fight infection, so call your doctor immediately if you develop chills, fever, or a cough. Regular blood and liver function tests are needed.

Cyclosporine

This medication was first used in organ transplantation to prevent rejection. It is used in patients who have not responded to other drugs.

Bleeding, tender, or enlarged gums; high blood pressure; increase in hair growth; kidney problems; trembling and shaking of hands.

Before taking this drug, tell your doctor if you have one of the following: sensitivity to castor oil (if receiving the drug by injection), liver or kidney disease, active infection, or high blood pressure. Using this drug may make you more susceptible to infection and certain cancers. Do not take live vaccines while on this drug.

Hydroxychloroquine

It may take several months to notice the benefits of this drug, which include reducing the signs and symptoms of rheumatoid arthritis.

Diarrhea, eye problems (rare), headache, loss of appetite, nausea or vomiting, stomach cramps or pain.

Doctor monitoring is important, particularly if you have an allergy to any antimalarial drug or a retinal abnormality.

Gold sodium thiomalate

This was one of the first DMARDs used to treat rheumatoid arthritis.

Redness or soreness of tongue; swelling or bleeding gums; skin rash or itching; ulcers or sores on lips, mouth, or throat; irritation on tongue. Joint pain may occur for one or two days after injection.

Before taking this drug, tell your doctor if you have any of the following: lupus, skin rash, kidney disease, or colitis. Periodic urine and blood tests are needed to check for side effects.

Leflunomide

This drug reduces signs and symptoms and slows structural damage to joints caused by arthritis.

Bloody or cloudy urine; congestion in chest; cough; diarrhea; difficult, burning, or painful urination or breathing; fever; hair loss; headache; heartburn; loss of appetite; nausea and/or vomiting; skin rash; stomach pain; sneezing; and sore throat.

Before taking this medication, let your doctor know if you have one of the following: active infection, liver disease, known immune deficiency, renal insufficiency, or underlying malignancy. You will need regular blood tests, including liver function tests. Leflunomide must not be taken during pregnancy because it may cause birth defects in humans.

Methotrexate

This drug can be taken by mouth or by injection and results in rapid improvement (it usually takes 3-6 weeks to begin working). It appears to be very effective, especially in combination with infliximab or etanercept. In general, it produces more favorable long-term responses compared with other DMARDs such as sulfasalazine, gold sodium thiomalate, and hydroxychloroquine.

Abdominal discomfort, chest pain, chills, nausea, mouth sores, painful urination, sore throat, unusual tiredness or weakness.

Doctor monitoring is important, particularly if you have an abnormal blood count, liver or lung disease, alcoholism, immune-system deficiency, or active infection. Methotrexate must not be taken during pregnancy because it may cause birth defects in humans.

Sulfasalazine

This drug works to reduce the signs and symptoms of rheumatoid arthritis by suppressing the immune system.

Abdominal pain, aching joints, diarrhea, headache, sensitivity to sunlight, loss of appetite, nausea or vomiting, skin rash.

Doctor monitoring is important, particularly if you are allergic to sulfa drugs or aspirin, or if you have a kidney, liver, or blood disease.

D. Biologic Response Modifiers

Medications

Uses/Effects

Side Effects

Monitoring

Biologic Response Modifiers

These drugs selectively block parts of the immune system called cytokines. Cytokines play a role in inflammation. Long-term efficacy and safety are uncertain.

Increased risk of infection, especially tuberculosis. Increased risk of pneumonia, and listeriosis (a foodborne illness caused by the bacterium Listeria monocytogenes).

It is important to avoid eating undercooked foods (including unpasteurized cheeses, cold cuts, and hot dogs) because undercooked food can cause listeriosis for patients taking biologic response modifiers.

Tumor Necrosis Factor Inhibitors
      Etanercept
      Infliximab
      Adalimumab

These medications are highly effective for treating patients with an inadequate response to DMARDs. They may be prescribed in combination with some DMARDs, particularly methotrexate. Etanercept requires subcutaneous (beneath the skin) injections two times per week. Infliximab is taken intravenously (IV) during a 2-hour procedure. It is administered with methotrexate. Adalimumab requires injections every 2 weeks. Long-term efficacy and safety are uncertain.

Etanercept: Pain or burning in throat; redness, itching, pain, and/or swelling at injection site; runny or stuffy nose.
Infliximab: Abdominal pain, cough, dizziness, fainting, headache, muscle pain, runny nose, shortness of breath, sore throat, vomiting, wheezing.
Adalimumab: Redness, rash, swelling, itching, bruising, sinus infection, headache, nausea.

Long-term efficacy and safety are uncertain. Doctor monitoring is important, particularly if you have an active infection, exposure to tuberculosis, or a central nervous system disorder. Evaluation for tuberculosis is necessary before treatment begins.

Interleukin1 Inhibitor
      Anakinra

This medication requires daily injections. Long-term efficacy and safety are uncertain.

Redness, swelling, bruising, or pain at the site of injection; head-ache; upset stomach; diarrhea; runny nose; and stomach pain.

Doctor monitoring is required.

 

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