Lupus Site - a guide for lupus patients and their families





What are antimalarials?

Introduced during World War II as an antimalarial drug, chloroquine (brand name - Aralen) was later followed by synthesis of the chemically-related compound, hydroxychloroquine (Plaquenil). As early as the 1960's it was noted that these medications produced a beneficial side effect. With chronic use they could ease the joint discomfort occurring with rheumatoid arthritis. Additionally, it was later observed that they have similar beneficial effects in the management of these same symptoms in Systemic Lupus Erythematosus (SLE). Skin lesions of Discoid Lupus Erythematosus (DLE) which have not responded to topical therapy (medicated creams, lotions, etc.) may improve with the use of these "antimalarial drugs".

How do antimalarials work?

Antimalarials block UV light from damaging skin; have an anti-inflammatory effect; lower cholesterol levels; inhibit clotting; block cytokines, which promote inflammation; & most importantly, alter the acid-base of the cells, which limits their ability to process antigens. (If antigens were processed, this would lead to the creation of unnecessary antibodies.)  Antimalarials do not lower blood counts, or make patients more susceptible to infection.

What antimalarials are used in the treatment of lupus?

Hydroxychloroquine (Plaquenil) is available as a 200 mg tablet and is generally prescribed to be taken as one or two tablets once or twice daily.

Chloroquine (Aralen) is marketed as a 250 mg tablet which is usually taken once daily.

Some physicians prefer to prescribe hydroxychloroquine, referring to some studies which describe evidence that it may have a lower potential for damage to the retina of the eye. Other clinicians maintain that the low doses of these agents in common use do not make this choice critical. Preference for either of these drugs may be regional, or may reflect training, product familiarity and personal conviction.

When are antimalarials used?

Patients with Lupus who may be advised to begin treatment with these medications include:

Patients who have already been treated with anti-inflammatory drugs but have experienced inadequate symptom relief or troublesome side effects.

Patients who may be able to be controlled with lower doses of prednisone if they also receive an antimalarial drug (thus avoiding side effects associated with higher doses of prednisone).

Patients with medical conditions which make it undesirable for them to be maintained on prednisone or other anti-inflammatory drugs.

What lupus symptoms can antimalarials help?

Discoid lesions, redness, mouth ulcers & hair loss improve in 90% of patients.  Joint pain & swelling decrease.  Over time, inflammation of the pleura & pericardium lessens, as do symptoms of fatigue & cognitive dysfunction.  Antimalarials are not effective in the treatment of organ-threatening SLE.

How long does it take for antimalarials to start working?

It can take anything from 3 weeks to a few months for them to start working.  You may not notice any improvement at first, but if you stop taking the antimalarials you will often find the symptoms worsen, therefore the drugs have been working but at a slow rate.

What are the side effects of antimalarials?

Side effects which can occur in patients taking hydroxychloroquine (Plaquenil) or chloroquine (Aralen) include:

More common - diarrhoea, headache, loss of appetite, nausea or vomiting, stomach cramping or pain.

Less common - bleaching of hair or increased hair loss, blue-black\ discoloration of skin, finger nails, or inside of mouth, dizziness or light headedness, itching (more common in blacks), nervousness or restlessness, skin rash.

These side effects may go away after the patient's system adjusts to the medicine. It is important to check back with the doctor, however, if they are continuous and bothersome.

Other side effects are more rare and should be reported immediately to the physician:

- convulsions (seizures)

- increased muscle weakness mood or other mental changes ringing or buzzing in the ears, or any

- loss of hearing

- sore throat and fever

- unusual bleeding or bruising


Blurred vision or any other change in vision after prolonged treatment are symptoms which should always be reported immediately to your doctor. They may represent early signs of toxicity to the retina of the eye which is generally preventable if reported early. Low doses, used at present (as noted above), are rarely associated with retinal toxicity. As a precautionary measure it is recommended that patients commencing treatment with the antimalarial drugs receive a baseline ophthalmic evaluation. This examination should be repeated every six months while taking the medication and for a further period of time if treatment was discontinued due to visual symptoms. Periodic routine blood testing (hemoglobin and white blood cell count with differential) has also been recommended for early detection of other adverse effects.




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