Antimalarials are drugs known for more than 300 years. Most widely used antimalarials are chloroquine, hydroxychloroquine, and less commonly quinacrine. The mechanisms of action are various and incompletely defined in the present moment. Antimalarials are used in numerous autoimmune diseases, the most frequent of which are rheumatoid arthritis and lupus erythematous. These drugs benefit especially cutaneous and articular disease, and moreover they are helpful for improvement blood glucose, lipids, and platelet aggregation. We discuss the dose and the most common adverse effects, especially those related to retina. Attention is especially directed to the treatment of pregnant women. Antimalarials favorable effectiveness-toxicity proportion advises consider them in the management of autoimmune diseases.