Chloroquine and hydroxychloroquine are 4-aminoquinoline compounds commonly employed as anti-malarial
drugs. Chloroquine and its synthetic analogue, hydroxychloroquine also belong to the disease-modifying anti-rheumatic
drug class because these drugs are immunosuppressive. The immunosuppressive activity of chloroquine and hydroxychloroquine
is likely to account for their capacity to reduce T-cell and B-cell hyperactivity as well as pro-inflammatory
cytokine gene expression. This review evaluated experimental and clinical trials results as well as clinical response data
relative to the use of chloroquine and/or hydroxychloroquine as first-line medical therapies in systemic lupus erythematosus,
rheumatoid arthritis, primary Sjogren’s syndrome, the anti-phospholipid syndrome and in the treatment of sarcoidosis.
A primary outcomes measure in these clinical trials was the extent to which chloroquine and/or hydroxychloroquine
reduced disease progression or exacerbations and/or the use and dosage of corticosteroids. The relative efficacy of chloroquine
and hydroxychloroquine in modifying the clinical course of these autoimmune disorders is balanced against evidence
that these drugs induce adverse effects which may reduce their use and effectiveness in the therapy of autoimmune
Keywords: Anti-phospholipid syndrome, chloroquine, hydroxychloroquine, immunosuppression, sarcoidosis, Sjogren’s syndrome,
systemic lupus erythematosus, rheumatoid arthritis.
Rights & PermissionsPrintExport