Immunosuppressive medications for lupus

Examples

Generic Name Brand Name
azathioprine Imuran
cyclophosphamide Cytoxan
cyclosporine (cyclosporin A) Neoral, Sandimmune
methotrexate sodium MTX, Rheumatrex
mycophenolate mofetil CellCept

Depending on the drug, an immunosuppressive medication may be given in pill form, weekly injections, or by intravenous (IV) pulse therapy (injection given monthly).

Azathioprine, cyclophosphamide, and methotrexate sodium are also referred to as cytotoxic medications.

How It Works

Lupus (systemic lupus erythematosus, or SLE) is an autoimmune disease, in which the immune system attacks the body's own tissues as though they were foreign substances. Immunosuppressive medications, including cytotoxics, reduce inflammation and suppress the immune system. In higher doses, cytotoxic medications are also used to treat certain forms of cancer.

Why It Is Used

Azathioprine, mycophenolate, and cyclophosphamide are the most common immunosuppressive medications used to treat severe kidney disease associated with lupus.

Cyclosporine is sometimes used to treat a certain type of kidney problem called membranous disease. Its use is limited as a lupus treatment because of its tendency to cause kidney toxicity.

Methotrexate is used to control skin rash and joint pain caused by lupus. It may be tried when other drugs such as NSAIDs, antimalarials, or low-dose corticosteroids have not brought relief.1 Methotrexate is more commonly used to treat rheumatoid arthritis.

Immunosuppressive medications can be used with corticosteroids for severe, extensive skin rashes or other severe symptoms that do not respond to other therapy. Corticosteroids are often gradually reduced as symptoms are controlled.

Pregnancy and immunosuppressants: Immunosuppressants can cause birth defects. Do not take immunosuppressants if you are pregnant. If you wish to become pregnant or father a child, talk with your doctor. Men or women taking immunosuppressants should stop taking them before trying to conceive a baby.

How Well It Works

Azathioprine

Long-term studies suggest that people with severe lupus treated with azathioprine (Imuran) in addition to corticosteroids have:1

  • Less kidney damage and better long-term kidney function.
  • Fewer lupus flares.
  • Less need for corticosteroids.

You may gradually be able to use this medication to reduce your dose of corticosteroids (as directed by your health professional).

Azathioprine works slowly, and may take 3 to 6 months to reach full effectiveness. After symptoms are well controlled and the dose of corticosteroids has been reduced, it may be possible to gradually reduce the dose of azathioprine and to stop the medication completely.

Cyclophosphamide

Cyclophosphamide (Cytoxan):1

  • Is more effective yet more toxic than azathioprine.
  • Reduces inflammation of kidneys and other affected organs.
  • Controls lupus-related problems such as central nervous system disease and thrombopenia in some people when given intravenously.
  • May not control symptoms by itself, so corticosteroids or other drugs may need to be taken with it.

Methotrexate

Methotrexate can control skin rashes and joint pain. There also are reported benefits for controlling more severe lupus symptoms, such as inflammatory conditions of the kidneys and tissues around the heart and lungs, but there has been little research in these areas.1

Mycophenolate mofetil

Studies report that mycophenolate mofetil is effective in suppressing the immune system's action, and may be effective in relieving chronic skin lupus that has been resistant to other medications. It is also being studied for treating lupus kidney disease.2 Some doctors use mycophenolate instead of or after treatment with cyclophosphamide.

Side Effects

The most serious side effects of immunosuppressants are lowered white blood cell counts and increased risk of infection. Immunosuppressants lower your immunity, making your body less able to defend against viral, bacterial, and fungal infections, such as a common herpes-type virus (cytomegalovirus [CMV]), shingles, staphylococcus, and yeast. Side effects may include temporary hair thinning, nausea, and diarrhea.

Azathioprine: Side effects include liver damage.3 If you take azathioprine, you should have regular liver blood tests. Because of an increased risk of precancerous cervical cell changes, women taking azathioprine are advised to have regular Pap tests. Some studies suggest that azathioprine may slightly increase the risk of future non-Hodgkin's lymphoma.3 Further research is necessary to confirm these findings.

Cyclosporine: This medication increases the risk of kidney problems and is used infrequently for lupus treatment. However, cyclosporine can be effective when used to treat membranous disease, a kidney condition sometimes associated with lupus. Side effects include a mild tremor (shaking), increased hair growth, high blood pressure, numbness, and decreased appetite. Uncommon side effects are fatigue, fever, painful urination, and, rarely, seizures. While taking cyclosporine, blood pressure and kidney function should be checked regularly.

Cyclophosphamide: Side effects include a slightly increased risk of future skin, bladder, bowel, or blood cancer; ovarian failure, resulting in menopause and permanent infertility; and bleeding in the bladder. Side effects that go away after treatment include hair thinning, nausea, and increased risk of infection. A monthly intravenous dose (instead of a daily oral dose) reduces the risks of bladder bleeding, allows for more accurate dosing, and may reduce the risk of infertility if given during menstruation. Intravenous cyclophosphamide may reduce the risk of some cancers, especially bladder cancer, linked to more frequent oral dosing.

Methotrexate: Side effects, reversible after the medication is stopped, include skin rash, nausea, fatigue, and hair thinning. Other side effects, also reversible, include mild liver inflammation (elevation of liver enzyme blood test) and low blood counts. Rare, serious, irreversible side effects include permanent liver damage (cirrhosis) and inflammation of the lung. Regular blood and liver tests may help detect lung or liver damage early.

See Drug Reference for a full list of side effects. (Drug Reference is not available in all systems.)

What To Think About

Taking strong drugs such as azathioprine and cyclophosphamide along with corticosteroids is more effective than taking corticosteroids alone in controlling severe lupus kidney disease, reducing tissue damage, and reducing the maintenance dose of corticosteroids.1

Combinations of both immunosuppressants and corticosteroids can be very effective but also increase the risk of side effects, so regular follow-up and monitoring by your health professional is essential.

Methotrexate is well documented as a treatment for other diseases and conditions involving abnormal cell growth, such as cancer. While methotrexate's effectiveness for lupus treatment is not well researched, it is becoming more commonly used for milder lupus inflammation and symptoms.1

Immunosuppressants can cause birth defects.3 Do not use take immunosuppressants if you are pregnant or wish to become pregnant. Do not father a child while you are taking it.

Immunosuppressive and cytotoxic medications have been associated with a small increase in the risk of developing certain cancers. But if you have severe, possibly life-threatening lupus, you may decide that a medication's risk is outweighed by its potential benefits.

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References

Citations

  1. Hahn BH (2005). Management of systemic lupus erythematosus. In ED Harris et al., eds., Kelley's Textbook of Rheumatology, 7th ed., vol. 2, pp. 1225–1247. Philadelphia: Elsevier Saunders.
  2. Wallace DJ (2002). Management of lupus erythematosus: Recent insights. Current Opinion in Rheumatology, 14(3): 212–219.
  3. Wofsy D (2005). Therapy of systemic lupus erythematosus. In WJ Koopman, LW Moreland, eds., Arthritis and Allied Conditions: A Textbook of Rheumatology, 15th ed., vol. 2, pp. 1561–1574. Philadelphia: Lippincott Williams and Wilkins.

Last Updated: May 13, 2008

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