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Antimalarial drugs in the treatment of rheumatic disease

Daniel J Wallace, MD
Section Editor
Daniel E Furst, MD
Deputy Editor
Monica Ramirez Curtis, MD, MPH


A variety of antimalarial medications have been shown to be effective for connective tissue diseases since quinine was first used to treat systemic lupus erythematosus (SLE) more than 100 years ago. Three of these drugs are now primarily used due to their safety profile.

Chloroquine and hydroxychloroquine (HCQ) are 4-aminoquinoline derivatives. They are structurally similar, differing only by replacement of an ethyl group in chloroquine with a hydroxyethyl group in HCQ. HCQ comprises 95 percent of all rheumatic disease antimalarial prescriptions.

Quinacrine is used much less frequently than the others because it requires compounding and causes a yellowish skin color with long-term treatment. It incorporates the chloroquine structure but is a 9-aminoacridine compound.


There are several problems in analysis of the pharmacokinetics of antimalarials:

Variation from individual to individual is wide


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Literature review current through: Sep 2016. | This topic last updated: Sep 19, 2016.
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