Rheumatoid Arthritis Drugs
Rheumatoid arthritis drugs include the following groups
- Non Steroidal Anti-inflammatory Drugs also called NSAID's
- Disease Modifying Anti-Rheumatic Drugs also called DMARDs
- Biological Agents
- Immunosuppressive Drugs
- Diet Supplements
NSAIDs are a group of rheumatoid arthritis drugs that reduce the symptoms but do not stop the damage of cartilage and bone. They include the following drugs
- Aspirin. It is acetyl-salicylic acid. In the body it is converted to salicylic acid, which is responsible for its effects. High doses of 3 to 6 gm per day are required for anti-inflammatory effect. Hence it is not preferred in rheumatoid arthritis.
Propionic acid derivatives
- Indomethacin. A strong anti-inflammatory drug. Can cause gastro-intestinal irritation and bleeding along with headache and mental confusion. Dosage are 75 to 150mg per day in divided doses.
- Sulindac. It is weaker than indomethacin.
Aryl-acetic acid derivatives
- Ibuprofen. Can cause gastric irritation. But less than most other NSAIDs. Rarely cause gastric bleeding. One of the safest NSAIDs. Can be used in children. Dose is 400 to 800mg three times a day.
- Diclofenac. Gastric ulceration and bleeding are low. Dose is 75 to 100mg twice daily.
- Aceclofenac. It is a new drug. As effective as diclofenac. Dose is 100mg twice daily.
- Piroxicam. A potent anti-inflammatory. Effective in synovial fluid. Reduces migration of white blood cells. Dose is 20mg once or twice daily. It is a good rheumatoid arthritis drug for mild disease.
- Meloxicam. Less gastric side effects
- Nimesulide. Weak inhibitor of enzyme cyclo-oxygenase. Reduces TNF release. Better tolerated by asthamatics that are sensitive to other NSAIDs. Can cause gastric irritation. Dose is 100 to 200mg twice daily.
Coxibs. They cause a increase in the coagulation of blood, leading to increased chances of a heart attack.
- Nabumetone. Low incidence of gastric irritation and bleeding. Dose is 500mg once a day.
- Rofecoxib,valdecoxib (no longer marketed)
- celcoxib. As effective as diclofenac and naproxen. Dose is 100 to 200mg twice daily.
- Etoricoxib. Low gastro-intestinal side effects. Dose is 60, 90 or 120mg daily.
NSAIDs fuction by blocking the enzyme cyclo-oxygenase. The function of this enzyme is to convert Arachidonic acid into prostaglandins and thromboxane. These two compounds are required by the body for a variety of normal functions.
Enzyme cyclo-oxygenase is present in two forms cyclo-oxygenase 1 and cyclo-oxygenase 2. Normally the body only contains the enzyme cyclo-oxygenase 1 and is defecient in enzyme cyclo-oxygenase 2.
Enzyme cyclo-oxygenase 2 is produced at the sites of inflammation. It leads to the production of cytokines and chemokines which enhance the inflammation.
Most NSAIDs block enzyme cyclo-oxygenase 1 and 2, where as the coxibs block only cyclo-oxygenase 2. Most of the side effects of NSAIDs are caused by the inhibition of cyclo-oxygenase 1. So coxibs have the lowest incidence of gastro-intestinal ulceration and bleeding.
Coxibs have earned a bad name because they have been associated with a increase in the risk of heart attacks. So they should be only used in patients that have a low risk of heart attack (young, lean and thin, no diabetes, no hypertension, no smoking).
Next group of rheumatoid arthritis drugs are steroids. They suppress the inflammation by preventing the movement of white blood cells to the local site and by preventing the release of cytokines and chemokines that increase inflammation. The main steroids used as rheumatoid arthritis drugs include the following
- Prednisolone. Can cause fluid retention with high doses. Usual dose is 5 to 40mg per day in divided doses or as a single dose.
- Methylprednisolone. More effective than prednisolone. Dose is 4 to 32mg per day in divided doses.
- Triamcinolone. More effective than prednisolone. Dose is 5 to 30mg per day in divided doses.
- Dexamethasone. Very effective steroid. Does not cause fluid retention and increase in blood pressure. Dose is 0.5 to 5mg pre day.
- Betamethasone is similar to dexamethasone.
Ulcers can be prevented by the use of drugs that reduce the gastric secretion such as
- H2 histamine blockers which include ranitidine (150 to 300mg twice daily) and famotidine (20 to 40mg twice daily)
- Proton pump blockers which include omeprazole (20 to 40mg twice daily) and rabeprazole (10 to 20mg daily)
Osteoporosis can be prevented and treated by the use of a group of drugs called bisphosphonates. They reduce the number of bone absorbing cells in the body. They include the drugs Alendronate (35 to 70mg weekly) and Risedronate (35mg weekly). They should be given empty stomach early in the morning and one should remain standing or sitting for 30 minutes there after. Because these drugs too can cause gastric irritation.
Next group of rheumatoid arthritis drugs includes Disease Modifying Anti-Rheumatic Drugs or DMARDs. They reduce the destruction of bone and cartilage. They include the following drugs
- Methotrexate. This is a anti-cancer drug that causes the inhibition of the enzyme dihydrofolate reductase. This causes a reduction in the production of cytokines. It is given in a dose of 7.5 to 15mg per week. The drug begins to show its effect in 1 to 2 months. It can lead to ulcers in the mouth, gastro-intestinal disturbances and impairment in the liver. It is to be absolutely avoided in pregnancy, liver disease, infections and gastric ulcers.
- Hydroxychloroquine. This is a drug used for the treatment of malaria. It has been found to be effective in rheumatoid arthritis. It induces remission in up to 50% patients. It can be given for a long period. Main side effect is damage to the retina of the eye and whitening of the cornea. Dose is 400mg per day. It is not effective in preventing cartilage damage.
- Leflunomide. It reduces the symptoms and progression of the disease. It stops the action of the activated lymphocytes. Its effect comes on within 4 weeks. For the first three days it is given in the dose of 100mg per day. After three days 20mg is given daily.
- Gold salts are one of the best rheumatoid arthritis drugs but also very toxic. The injectable form of gold is more toxic. Oral form is less toxic but also less effective. It causes remission in more than 50% of patients. It reduces the migration and activation of white blood cells.It can cause damage to the kidney and liver and suppression of the bone marrow. Oral gold causes diarrhoea and abdominal pain. Oral gold is known as Auranofin. Its dose is 6mg per day in two divided doses.
- D-penicillamine is a drug that is used for Wilson's disease because of its copper chelating effect. It has the same effect and toxicity as gold. Dose is 250 to 500mg per day.
All Biological drugs reduce symptoms and prevents bone and cartilage damage. These rheumatoid arthritis drugs are of the following types
- block the activity of cytokine Tumor Necrosis Factor (TNF), this group includes
Anakinra functions by blocking the receptor on which Interleukin 1 acts. It thereby prevents the release of cytokines that enhance the inflammation. It is less effective than Tumor Necrosis factor blockers, and ineffective in those patients in whom TNF blockers have failed. Its main side effect is pain and burning at the injection site. It is given as a daily injection of 100mg.Abatacept is protein that inhibits the T cells. It can be used with methotrexate. It is used in patients that have failed TNF blocking treatment. Its combination with TNF blocking agents does not enhance the efficacy and can lead to severe infections. It is given by a IV infusion over 30 minutes. The dose is repeated after 15 days then at monthly intervals.Rituximab is a antibody that causes a decrease in the number of mature B cells. It is given as a transfusion. The major complications are blood reactions. These can be managed by steroids. Treatment can be repeated when B cell level returns.
- Infliximab which is given by an intra-venous (IV or through the veins) route slowly over a period of about 2 hours. Dose of this drug is about 3mg for every kilogram of body weight. The second dose is repeated after 2 to 3 weeks. There after it is given every 8 weekly.
- Adalimumab which is given by an injection under the skin either every week or fortnight. Each pre-filled syringe has 40 mg of the drug.
- Etanercept binds to TNF and prevents it from attaching to its receptor. of bone and cartilage. It is given in the dose of 50mg every week by injection in the fat below your skin.
Combination of rheumatoid arthritis drugs is also used.TNF blockers given along with DMARDs provides the maximum benefit. TNF blockers have the potential to cause serious infections and can result in the re-activation of tuberculosis. Lymphomas and other cancers have also been seen with these agents. Their use should be monitored by a doctor well versed and experienced in their use.
Immunosupressents used as rheumatoid arthritis drugs include the following
- Cyclosporine. It is a drug that is used in organ transplantation and autoimmune disorders. It acts by inhibiting the T cells and decreasing the production of cytokines. It damages the liver and the kidney. In rheumatoid arthritis it is used in lower doses and so the side effects are not usually mild. Dose is 2 to 5mg per kilogram of body weight per day.
- Azathioprine. It suppresses the T cells. Side effect is bone marrow depression. Dose is 1 to 2mg per kilogram of body weight per day.
- Cyclophosphamide. It suppresses the B cells. Used in extra-articular rheumatoid arthritis.
Newer rheumatoid arthritis drugs are being developed. This page will be upgraded when they are approved for use in patients.
I hope the information provided about rheumatoid arthritis drugs was helpful. If you have any query you can ask me at the contact me page.
This page was last updated on 31st March 2009.
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