Depending on the drug, an immunosuppressive medicine may
be given in pill form, weekly injections, or by
intravenous (IV) pulse therapy (injection given
Azathioprine, cyclophosphamide, and methotrexate sodium
are also referred to as cytotoxic medications.
How It Works
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 medicines, including
inflammation and suppress the immune system. In higher
doses, cytotoxic medicines are also used to treat certain forms of
Why It Is Used
Azathioprine, mycophenolate, and
cyclophosphamide are the most common immunosuppressive medicines used to
kidney disease associated with lupus.
Methotrexate is used to
control skin rash and joint pain caused by lupus. It may be tried to allow less corticosteroid medicine to be used.1 Methotrexate is more commonly used to
medicines 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
How Well It Works
Methotrexate may help control skin rashes
and joint pain.2 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
Other immunosuppressive medicines are used for more severe lupus. Most studies have been done using one of the immunosuppressives, along with corticosteroids, for lupus that is causing serious kidney problems (lupus nephritis). But they are also used to try to control other serious symptoms of lupus, such as inflammation around the heart and lungs. Azathioprine, cyclophosphamide, and mycophenolate mofetil are the most commonly used medicines. They can take several weeks to reach full effectiveness, but they generally help decrease serious symptoms. As the immunosuppressive takes effect, the amount of corticosteroids can usually be decreased.2
Side effects of immunomodulator medicines include:
Rare side effects include:
Suppression of blood cell production (bone marrow suppression), which may increase the risk of infection or serious bleeding. Return to normal blood cell production may take several weeks after the medicine is stopped.
- Inflammation of the pancreas (pancreatitis). This may occur with AZA.
Extremely rare side effects of azathioprine include a possible increased risk of cancer. Mycophenolate mofetil may increase the risk of cancer of the lymph system (lymphoma) and other types of cancer.
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 seems to be more effective
than taking corticosteroids alone in controlling severe lupus kidney disease,
reducing tissue damage, and reducing the maintenance dose of
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.
Immunosuppressants can cause birth defects. Do not
use take immunosuppressants if you are pregnant or wish to become pregnant. Do
not father a child while you are taking it.
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
Complete the new medication information form (PDF)(What is a PDF document?) to help you understand this medication.
Tassiulas IO, Boumpas DT (2009). Clinical features and treatment of systemic lupus erythematosus. In GS Firestein et al., eds., Kelley's Textbook of Rheumatology, 8th ed., vol. 2, pp. 1263-1300. Philadelphia: Saunders Elsevier.
Hahn BH (2008). Systemic lupus erythematosus. In AS Fauci et al., eds., Harrison's Principles of Internal Medicine, 17th ed., vol. 2, pp. 2075-2083. New York: McGraw-Hill Medical.