Discoid Lupus Erythematosus Medication

Updated: Aug 21, 2018
  • Author: Elizabeth Tkachenko; Chief Editor: William D James, MD  more...
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Medication

Medication Summary

Hydroxychloroquine and chloroquine phosphate have shown beneficial effects in treating discoid lupus erythematosus (DLE). Additionally, The antimalarial drugs may prevent the development of systemic lupus erythematosus (SLE) in patients with DLE, and they might decrease the risk of cardiovascular disease. [23]  Alternative therapies, anecdotal reports, and small, open-label trials (as reported by Callen [55] ) suggest that the following agents may be useful in some patients:

  • Dapsone
  • Thalidomide [28, 29, 56, 57]
  • Isotretinoin [58]
  • Acitretin
  • Azathioprine [44]
  • Mycophenolate mofetil [45]
  • Methotrexate [43]
  • Auranofin
  • Phenytoin
  • Fumaric acid esters [59]
  • Photodynamic therapy [60]
  • Imiquimod cream 5% [61]
  • Lenalidomide [49, 50]
  • Intravenous immunoglobulin [53]
  • Belimumab [47, 48]
  • Tofacitinib [6, 51]
  • Apremilast [52]
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Antimalarial agents

Class Summary

Antimalarial agents may have immunomodulatory properties. Hydroxychloroquine is the drug of choice when a systemic agent is needed for discoid lupus erythematosus (DLE). Chloroquine is second-line antimalarial therapy. Chloroquine and hydroxychloroquine should not be used in combination due to the increased risk of ocular toxicity. The antimalarial drugs may prevent the development of systemic lupus erythematosus (SLE) in patients with DLE, and they might decrease the risk of cardiovascular disease.

Hydroxychloroquine (Plaquenil)

Hydroxychloroquine is used for the treatment of DLE and SLE. It inhibits chemotaxis of eosinophils and locomotion of neutrophils and impairs complement-dependent antigen-antibody reactions. Hydroxychloroquine sulfate 200 mg is equivalent to 155 mg hydroxychloroquine base and 250 mg chloroquine phosphate.

Chloroquine (Aralen)

Chloroquine inhibits chemotaxis of eosinophils and locomotion of neutrophils and impairs complement-dependent antigen-antibody reactions.

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Leprostatic agents

Class Summary

Leprostatic agents may modulate the immune system.

Dapsone

Dapsone's mechanism of action is similar to that of sulfonamides, in which competitive antagonists of para-aminobenzoic acid (PABA) prevent the formation of folic acid, inhibiting bacterial growth. The anti-inflammatory action may relate to suppression of neutrophil function by inhibition of the halide-myeloperoxidase system.

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Gold compounds

Class Summary

Gold compounds have proven effective in the treatment of inflammation with autoimmune etiology.

Auranofin (Ridaura)

Gold is taken up by macrophages, which, in turn, inhibit phagocytosis and lysosomal membrane stabilization. Gold alters immunoglobulins, decreasing prostaglandin synthesis and lysosomal enzyme activity.

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Immunomodulators

Class Summary

Immunomodulators affect factors that regulate the immune system.

Methotrexate (Rheumatrex, Trexall)

Methotrexate reversibly inhibits dihydrofolate reductase; it limits the availability of 1-carbon fragments necessary for the synthesis of purines and the conversion of deoxyuridylate to thymidylate in the synthesis of DNA and cell reproduction. Methotrexate is extensively used to treat cancer, rheumatoid arthritis, and psoriasis and is used as a steroid-sparing agent in various autoimmune conditions.

Thalidomide (Thalomid)

Thalidomide is an immunomodulatory agent that may suppress excessive production of tumor necrosis factor (TNF)-alpha and may down-regulate selected cell-surface adhesion molecules involved in leukocyte migration. If the patient weighs less than 50 kg (110 lb), start the individual at the low end of the dose regimen.

Azathioprine (Imuran, Azasan)

Azathioprine antagonizes purine metabolism and inhibits the synthesis of DNA, ribonucleic acid (RNA), and proteins. It may decrease the proliferation of immune cells, which results in lower autoimmune activity.

Mycophenolate (CellCept, Myfortic)

Mycophenolate inhibits inosine monophosphate dehydrogenase and suppresses de novo purine synthesis by lymphocytes, thereby inhibiting their proliferation. It inhibits antibody production.

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Corticosteroids

Class Summary

Corticosteroids are anti-inflammatory agents that suppress the immune system at several levels, including through the inhibition of inflammatory cells and the production of antibodies.

Triamcinolone (Kenalog-10)

Triamcinolone can be administered intralesionally in a concentration of 3-5 mg/mL. The amounts injected should be recorded. Systemic adverse effects are uncommon with low doses. Atrophy is possible and is dose dependent.

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Retinoids

Class Summary

Retinoids have the ability to regulate cell proliferation and the immune system.

Acitretin (Soriatane)

Acitretin is a retinoic acid analog similar to etretinate and isotretinoin. Etretinate is the main metabolite, and acitretin has demonstrated clinical effects close to those seen with etretinate. The mechanism of action is unknown.

Isotretinoin (Claravis, Sotret, Amnesteem)

Isotretinoin is a synthetic 13-cis isomer of naturally occurring tretinoin (trans -retinoic acid). Both agents are structurally related to vitamin A. Isotretinoin decreases sebaceous gland size and sebum production. It may inhibit sebaceous gland differentiation and abnormal keratinization.

A US Food and Drug Administration (FDA)–mandated registry is now in place for all individuals prescribing, dispensing, or taking isotretinoin. For more information on this registry, see iPLEDGE. This registry aims to decrease the risk of pregnancy and unwanted and potentially dangerous adverse effects during a course of isotretinoin therapy.

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