April 19, 2014
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Arthritis (Rheumatoid)

 Health Home >> Arthritis (Rheumatoid) >> Treating RA and taking control 


Disease-modifying anti-rheumatic drugs (DMARDs)

Disease-modifying anti-rheumatic drugs (DMARDs) slow or suppress the immune system from attacking the joints in the treatment of rheumatoid arthritis (RA). DMARDs are often combined with each other or with other medications, such as biologics.

The way DMARDs work to suppress the immune system is not completely understood. It is believed that they block the action of white blood cells (which destroy foreign substances in the body). Some DMARDs may also block other substances in the body involved in triggering inflammation (such as prostaglandins).

DMARDs used in Canada for RA include:

  • azathioprine (Imuran®, generics)
  • cyclosporine (Neoral®, generics)
  • gold therapy or sodium aurothiomalate (Myochrysine®, generics)
  • hydroxychloroquine (Plaquenil®, generics)
  • leflunomide (Arava®, generics)
  • methotrexate (Methotrexate®, generics)
  • penicillamine (Cuprimine®)
  • sulfasalazine (Salazopyrin®, generics)
  • tacrolimus (Prograf®)
Azathioprine (Imuran®, generics)
  • What does it do? Azathioprine suppresses the immune system and is used to treat severe RA in people who have not responded to other therapies.
  • How do I use it? Azathioprine tablets are taken once or twice a day. The injection is given intravenously (into a vein).
  • What are some known side effects? Azathioprine can cause infection, nausea, vomiting, diarrhea, fever, malaise, and muscle pain. It may also increase the risk of cancer, particularly skin cancer and lymphoma (cancer that affects white blood cells in the lymph system), and can cause an abnormal decrease in the number of white blood cells and/or platelets. Azathioprine can cause harm to an unborn baby, so pregnant women should not take this medication.
Cyclosporine (Neoral®, generics)
  • What does it do? Cyclosporine suppresses the immune system and is used to treat severe RA when other therapies are not appropriate or cannot be tolerated.
  • How do I use it? Cyclosporine is taken orally (by mouth), usually twice a day.
  • What are some known side effects? Cyclosporine can cause infection, high blood pressure, tremor, headache, numbing or tingling sensation, nausea, vomiting, abdominal pain, diarrhea, enlarged gums, muscle cramps or aches, and fatigue. It may also increase the risk of cancer.
Gold salts or sodium aurothiomalate (Myochrysine®)
  • What does it do? Gold salt is believed to work by interrupting processes in the body that cause inflammation, thereby reducing inflammation associated with RA.
  • How do I use it? Gold salt is injected into a muscle (intramuscular (IM) injection) once weekly by a health care provider until the full benefits are seen, then every 2 to 4 weeks thereafter.
  • What are some known side effects? Gold salt can cause injection site reactions (e.g., irritation, pain), skin rash, skin ulcers, increased protein in the urine, a fall in the number of white blood cells, and unexpected bleeding or bruising.
Hydroxychloroquine (Plaquenil®, generics)
  • What does it do? The way hydroxychloroquine works in RA symptoms is not exactly clear, but it is believed to reduce inflammation of the joints. It is used to treat RA for people who have not responded to other therapies.
  • How do I use it? Hydroxychloroquine is taken orally, usually once a day.
  • What are some known side effects? Hydroxychloroquine can cause skin rash, skin changes, hair loss, nausea, diarrhea, loss of appetite, abdominal pain, and changes to the cornea that can cause vision problems (e.g., blurred vision, night blindness).
Leflunomide (Arava®, generics)
  • What does it do? Leflunomide is believed to work by interrupting processes in the body that cause inflammation, thereby reducing inflammation associated with RA.
  • How do I use it? Leflunomide is taken orally, usually once a day.
  • What are some known side effects? Leflunomide can cause high blood pressure, stomach problems (e.g., nausea, vomiting, diarrhea), weight loss, headache, dizziness, weakness, hair loss, eczema, dry skin, tingling feeling on the skin, skin rash, mouth ulcers, and abdominal pain. It may also cause liver damage and increase the risk of serious infections, including sepsis (a bacterial infection that spreads throughout the body). Pregnancy should be avoided if either partner is using leflunomide, as this medication can cause birth defects or death of the fetus. Appropriate contraception should be used while taking this medication. Pregnancy should also be avoided for a minimum of 2 years after finishing treatment with leflunomide. Men should continue to use reliable contraception for 2 years after finishing treatment with leflunomide.
Methotrexate (Methotrexate®, generics)
  • What does it do? The way methotrexate works in RA symptoms is not exactly clear, but it is believed to reduce inflammation and suppress the immune system.
  • How do I use it? Methotrexate usually taken orally once weekly. Methotrexate can also be given by injection on a schedule determined by your doctor.
  • What are some known side effects? Methotrexate can cause mouth ulcers, nausea, abdominal pain or discomfort, dizziness, fatigue, malaise, fever, chills, nausea or vomiting, rash, and infection. Pregnancy should be avoided if either partner is using methotrexate, as this medication can cause birth defects. Pregnancy should also be avoided for a minimum of 3 months after finishing treatment with methotrexate. This medication can also lead to an increase in liver enzymes, which is a concern if the situation is persistent. Your doctor will test the function of your liver regularly while you are on methotrexate.
Penicillamine (Cuprimine®)
  • What does it do? The way penicillamine works in RA symptoms is not exactly clear. Penicillamine is used to treat severe RA for people who have not responded to other therapies.
  • How do I use it? Penicillamine is taken orally, usually once a day.
  • What are some known side effects? Penicillamine can cause skin rash, loss of appetite, upper abdominal pain, nausea, vomiting, diarrhea, taste perception changes, a decrease in while blood cells, unexpected bleeding or bruising, and increased protein in the urine. It may also cause mouth ulcers, decrease in blood cell counts, ringing in the ear, vision problems (due to inflammation of the optic nerve), and nerve damage. Some people using this medication may also experience an effect known as a drug fever, which usually occurs 2 to 3 weeks after starting the medication. Pregnant women should not use this medication.
Sulfasalazine (Salazopyrin®, generics)
  • What does it do? The way sulfasalazine works in RA symptoms is not exactly clear, but it is believed to reduce inflammation and suppress the immune system. Sulfasalazine is used to treat RA for people who have not responded to other therapies.
  • How do I use it? Sulfasalazine is taken orally, usually twice a day.
  • What are some known side effects? Sulfasalazine can cause nausea, vomiting, stomach upset, loss of appetite, headache, bluish skin caused by decreased hemoglobin in the blood, and infection.
Tacrolimus (Prograf®)
  • What does it do? Tacrolimus suppresses the immune system and is used to treat RA when other DMARD agents are not appropriate or when people have not responded to other therapies.
  • How do I use it? Tacrolimus is taken orally once a day.
  • What are some known side effects? Tacrolimus can cause infection, tremor, constipation, diarrhea, headache, abdominal pain, high blood pressure, difficulty sleeping, and nausea. Tacrolimus may also increase the risk of lymphoma (cancer that affects white blood cells in the lymph system), damage to the nervous system, and kidney damage.

DMARDs can cause some rare but serious side effects, including allergic reactions, a reduced ability to fight off infections, blood clotting problems, increased risk of developing cancer, and damage to the kidneys, liver, or bone marrow.

During the course of your RA therapy, your doctor may recommend regular blood tests and checkups. Ask your doctor what side effects you should watch out for and which ones need to be reported to your doctor.

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