Which medications in the drug class DMARDs, Immunomodulators are used in the treatment of Rheumatoid Arthritis (RA)?

Updated: Feb 07, 2020
  • Author: Howard R Smith, MD; Chief Editor: Herbert S Diamond, MD  more...
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DMARDs, Immunomodulators

DMARDs represent the most important measure in the successful treatment of RA.

Methotrexate (Rheumatrex, Trexall, Otrexup)

MTX is a folic acid antagonist that is approved for the management of severe active RA in patients who have had an insufficient therapeutic response to or are intolerant of an adequate trial of first-line therapy, including full-dose NSAIDs. It inhibits dihydrofolic acid reductase, which ultimately interferes with DNA synthesis, repair, and cellular replication.

Tocilizumab (Actemra)

Tocilizumab is an IL-6 receptor inhibitor. It is indicated for moderate to severe active RA in adults who have had an inadequate response to 1 or more TNF-antagonist therapies. It has been approved as an IV infusion or SC injection that may be used alone or in combination with MTX or other DMARDs. 

Sarilumab (Kevzara)

Human monoclonal antibody that binds to both soluble and membrane-bound IL-6 receptors (sIL-6R and mIL-6R). It is administered as a SC injection. May be prescribed as monotherapy or with methotrexate or other conventional DMARDs.

Azathioprine (Imuran)

Although azathioprine is not a first-line agent, it is sometimes used in the treatment of active RA to reduce signs and symptoms, particularly in patients who may have coinciding connective tissue diseases, such as systemic lupus erythematosus. Aspirin, NSAIDs, or low-dose glucocorticoids may be continued during treatment with azathioprine. The mechanism whereby azathioprine affects autoimmune diseases is unknown; however, it works primarily on T cells.

The initial dosage is 1 mg/kg/day (50-100 mg/day) given as a single dose or in divided doses twice daily. The dosage may be increased by 0.5 mg/kg/day at 6-8 weeks and thereafter at 4-week intervals, up to a maximum dosage of 2.5 mg/kg/day. Azathioprine is available in tablet form for oral administration or in 100-mg vials for IV injection.

Cyclosporine (Gengraf, Neoral)

Although cyclosporine is approved for the treatment of patients with severe active RA in which the disease has not adequately responded to MTX, it is not commonly used to treat RA, because of its nephrotoxicity. When cyclosporine is used, patients' renal function must be closely monitored.

Cyclosporine can be used in combination with MTX in RA patients who do not have an adequate response to MTX alone.

Anakinra (Kineret)

Anakinra is a recombinant, nonglycosylated form of the human interleukin (IL)-1 receptor antagonist (IL-1Ra) that is indicated for reducing signs and symptoms and slowing the progression of structural damage of moderately to severely active RA that has failed treatment with 1 or more DMARDs. Anakinra can be used alone or in combination with DMARDs other than TNF-blocking agents.

Abatacept (Orencia)

Abatacept is a selective costimulation modulator that inhibits T-cell activation by binding to CD80 and CD86, thereby blocking their interaction with CD28. CD28 interaction provides a signal needed for the full T-cell activation that is implicated in RA pathogenesis.

This agent is approved for reducing signs and symptoms, inducing major clinical response, inhibiting the progression of structural damage, and improving physical function in adult patients with moderately to severely active RA. Abatacept can be used as monotherapy or concomitantly with DMARDs other than TNF antagonists.

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