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Reviewed by: HU Medical Review Board | Last reviewed: June 2023

Immunosuppressants are a group of drugs that stop or slow the immune system from working the way it normally does. These drugs were first developed in the 1960s to prevent the body from attacking the newly transplanted organs or to treat cancer (chemotherapy). Doctors later realized that these medicines would also control inflammation and an overactive immune system in people with autoimmune diseases like lupus.

Other names for immunosuppressants are immunosuppressives, immune modulators, or antirejection drugs.

How do immunosuppressants help people with lupus?

Immunosuppressants generally are prescribed when an antimalarial is not controlling lupus symptoms or to help reduce the use of steroids. Steroids are usually given at first to quickly control symptoms and then replaced with immunosuppressants. This is because immunosuppressants take longer to work but have fewer long term risks than even low-dose steroids.1,2

The choice of medication depends on the type of symptoms, their severity, patient age, childbearing potential, safety concerns, and cost.1,3,4

  • Methotrexate (Rheumatrex™) and azathioprine (Imuran®) are generally given to people with moderate lupus that have significant but non-organ threatening symptoms. These drugs are particularly useful as steroid-sparing agents.
  • Mycophenolate mofetil (Cellcept®) works well to suppress lupus from attacking the kidneys in moderate to severe lupus but generally does not help with neuropsychiatric symptoms.
  • Cyclophosphamide (Cytoxan®) may be useful when severe lupus is threatening the health of the kidneys, or cardiovascular, lung, or central nervous system.
  • Cyclosporine (Neoral®, Sandimmune®) and rituximab (Rituxan®) are generally only prescribed to people with quite severe lupus symptoms to control organ damage.
  • Tacrolimus may be used for lupus nephritis, a serious complication of the kidneys that affects some people with lupus.

Most people with lupus will take immunosuppressants for only as long as it takes to get their symptoms under control and prevent permanent organ damage. They will then go back to taking antimalarials to manage their lupus.

What are the possible side effects of immunosuppressants?

Immunosuppressants come with many side effects, so you and your doctor will have to weigh the potential benefits of using one of these drugs versus the potential dangers. Here are some of the most common side effects of taking immunosuppressives:1-4,6

  • Infections. Because your immune system is suppressed, your body is less able to fight off infections. This means you will be more likely to get sick if you are exposed to a virus such as the cold, flu, herpes zoster (shingles or chickenpox), or measles. You must also monitor your skin for any cut or scrape, and let your doctor know right away if you see any swelling, redness, soreness, or pain.
  • Methotrexate (Rheumatrex™) is the most frequently used immunosuppressant but it may cause nausea, mouth sores, headaches, sun-sensitivity, liver damage, and leave you more likely to get lung infections. It is also used in people with rheumatoid arthritis. You cannot drink excessive alcohol while taking methotrexate, or use NSAIDs or aspirin when on high doses.
  • Cyclophosphamide (Cytoxan®) is given intravenously, or through an IV, and may cause menstrual problems, bladder problems, hair loss, and sterility.
  • Azathioprine (Imuran®) may cause pancreatitis and a type of hepatitis (liver disease). Your doctor may order regular liver function tests and blood counts

If you take immunosuppressants, your doctor will monitor you closely for signs of infection, and order regular tests to watch your liver function, kidney function, and other signs of overall health. Immune modulators may also increase your risk for developing certain types of cancer, including lymphoma and cervical cancer, so your doctor will also encourage you to get regular cancer screenings.4,6 These are not all the possible side effects of immunosuppressants. People taking them should talk to their doctor about what to expect with treatment.

Can you take immunosuppressants while trying to conceive or while pregnant?

Many immunosuppressives are not recommended during pregnancy or while trying to conceive. For example, mycophenolate mofetil (Cellcept®) should be discontinued at least six weeks before trying to conceive. Because of its toxic effects on the reproductive organs in both men and women, cyclophosphamide (Cytoxan®) is also generally not prescribed to anyone of reproductive age unless the symptoms of lupus are life-threatening.2,6 This is not a complete list. Please check with your doctor for all of the potential medication risks during pregnancy.

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