Home Anti-Malarials in the Treatment of Lupus
Oscar Gluck, M.D.
Anti-Malarials in the Treatment of Lupus

Anti-malarials were first developed during World War II to treat parasitic infections like malaria. As early as the 1960’s, it was found that these medications could also be used to treat the joint pain that occurs with rheumatoid arthritis. Soon thereafter, anti-malarials were found to have similar beneficial effects in the treatment of joint pain associated with systemic lupus erythematosus (SLE) and some physicians use it for the treatment of Sjogren’s syndrome.

Anti-malarials are particularly effective in treating skin and joint symptoms that may occur in SLE. They have been demonstrated to improve muscle and joint pain, inflammation of the lining of the heart (pericarditis) and lung (pleuritis), and other symptoms of lupus such as fatigue and fever. However, anti-malarials alone are not appropriate treatment for more severe manifestations of systemic lupus such as kidney disease.

Anti-malarials are very effective in the treatment of discoid lupus erythematosus (DLE): 60-90% of patients with DLE went into remission or showed major improvement after being treated with anti-malarials. Skin lesions of DLE which have not responded to treatment with topical therapy (e.g., creams, ointments) may improve with the use of anti-malarial drugs.

Anti-malarials are useful in subacute cutaneous lupus, and in overlap syndromes in which patients have acute symptoms of lupus and other auto-immune disorders.

The anti-malarials which are utilized in North America for the management of systemic lupus include hydroxychloroquine (Plaquenil) and chloroquine (Aralen). These medications are not equivalent in their side effects. In the United States, hydroxychloroquine (Plaquenil) is the most popular because it is felt to be less likely to cause eye side effects. Quinacrine (Atabrine) is available from compounding pharmacists and will be available again in 1994.

How do Anti-Malarials Control Systemic Lupus Erythematosus?

The specific mechanisms by which anti-malarials control systemic lupus are unclear. It is known that anti-malarials protect against the damaging effects of ultraviolet light and improve skin lesions. Some researchers suggest that they combine with certain chemicals or groups of proteins and interfere with enzyme groups that play a role in inflammation. Other researchers believe that more complex mechanisms are involved, such as the inhibition of antibody response of the direct inhibition of the lupus erythematosus (LE) cell reaction.

Can Anti-Malarials be Taken with other Medications?

Anti-malarials can be taken with other medications used for the treatment of systemic lupus such as corticosteroids (Prednisone), cytotoxics and anti-inflammatory medications including aspirin. In fact, anti-malarials are sometimes given in combination with Prednisone to reduce the amount of steroid that is needed to improve symptoms. Obviously, any combination of medications should always be prescribed by a physician.

Is it Safe to Take Anti-Malarials During Pregnancy?

The manufacturer recommends that anti-malarials not be given during pregnancy because of the potential for congenital malformations in the baby. However, anti-malarials are apparently safe when used to prevent malaria in pregnant women (lower doses than this are used in the treatment of SLE). Dr. Ann Parke of the University of Connecticut has treated 11 lupus patients who were pregnant with anti-malarials without adverse effects to the fetus. Clearly, more research is needed on this topic. Patients should discuss the pros and cons of continuing treatment with anti-malarials during pregnancy or if they are planning to become pregnant.

What are the Side Effects of Anti-Malarials?

The side effects of anti-malarials include skin rashes and pigmentary changes. Atabrine specifically, can cause yellow pigmentation of the skin. Hair loss and dryness of the skin have also been described. Stomach upset, loss of appetite, abdominal bloating, cramps, nausea, vomiting and diarrhea may also occur with the use of anti-malarials. These side effects usually go away after the patient adjusts to the medication. However, if they continue, a physician should be consulted.

Some patients may experience headaches, muscle aching and weakness as a result of taking anti-malarials. Nervousness, irritability or dizziness can occur, but these side effects are uncommon. Major neurological side effects such as confusion or seizures are quite rare. However, if any of these side effects occurs, they should be reported immediately to a physician.

A major potential side effect of anti-malarial use is the possible damage to the retina (back of the eye) that these medications can produce. It is important to note that retinal damage due to the use of anti-malarials is dose-related, and that the low doses currently used in the treatment of lupus are rarely associated with retinal damage. Most cases of eye disease occur in patients receiving more than 400 mg of Plaquenil or more than 250 mg of Aralen daily. Atabrine is not known to cause retinal damage.

Retinal damage due to the use of Plaquenil is sometimes reversible, if it is treated early. However, damage due to the use of chloroquine (Aralen) is irreversible. Thus, it is necessary to have the patient see an eye doctor or ophthalmologist prior to beginning treatment with anti-malarials for a baseline examination and to receive follow-up eye examinations every three to six months thereafter.