Guest guest Posted October 17, 2003 Report Share Posted October 17, 2003 Anti-Malarials in the Treatment of Lupus Gluck, M.D. History of Anti-Malarials Use in the Treatment of Lupus Types of Anti-Malarials How Do Anti-Malarials Control Systemic Lupus Erythematosus? Can Anti-Malarials Be Taken With Other Medications? Is It Safe To Take Anti-Malarials During Pregnancy? What Are Some Side Effects of Anti-Malarials? Vision The Lupus Foundation of America Related Information History of Anti-Malarials Anti-malarial medications, which are also anti-rheumatic drugs, are derived from the bark of the Peruvian cinchona tree. The active agents, quinine and cinchona, were isolated by Pelltier in 1820. Anti-malarials were first used during World War II to treat parasitic infections like malaria. As early as the 1960s 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). Some physicians also used it for the treatment of Sjogren's syndrome. < Back to the Top Use in the Treatment of Lupus 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) inflammation of the lining of the lung (pleuritis) other symptoms of lupus such as fatigue and fever. However, anti-malarials alone are not appropriate treatment for more severe manifestations of systemic lupus as kidney disease. Anti-malarials are very effective in the treatment of discoid lupus erythematosus (DLE): 60-90 percent of those with DLE went into remission or showed major improvements 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 also useful in subacute cutaneous lupus, and in overlap syndromes which have acute symptoms of lupus and other autoimmune disorders. < Back to the Top Types of Anti-Malarials The anti-malarials used in North America for the management of systemic lupus include: hydroxychloroquine (Plaquenil) chloroquine (Aralen) quinacrine (Atabrine). 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 is only available from compounding pharmacists. < Back to the Top How Do Anti-Malarials Control Systemic Lupus Erythematosus? Anti-malarials appear to interfere with immune cellular function. The antimalarials are weak bases and can alter the pH inside the cell, thus interfering with intracellular enzyme activity that depends on a more acidic micro environment. When this occurs, there is an anti-inflammatory effect. Many chemicals that participate in the inflammatory cascade are altered, and blood is thinned due to alterations in platelet aggregation. It is also known that anti-malarials protect against the damaging effects of ultraviolet light and can improve skin lesions. In addition, anti-malarials combine with certain chemicals or groups of proteins that play a role in the immune response. Anti-malarials have an effect on immune mediators, such as cytokines: They decrease auto-antibody production, inhibit the proliferative response of lymphocytes that are activated, and may have a direct effect on DNA. In these ways anti-malarials have the potential to put the disease into remission. < Back to the Top 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. < Back to the Top Is It Safe To Take Anti-Malarials During Pregnancy? The manufacturer still recommends that anti-malarials should not be given during pregnancy unless the rheumatologist or physician determines that the benefits outweigh the possible adverse effects. Fetal Eyes: There has been some evidence that chloroquine administered intravenously to pregnant animals crossed the placenta rapidly and accumulated selectively in the fetal eyes. Studies show that the drug remained in the ocular tissue for up to five months even though it was eliminated from the rest of the body. Pregnancy: Thorough studies on the use of anti-malarials in pregnant women have not been done. Anti-malarials seem to be safe when used to prevent malaria in pregnant women, but at lower doses than are used in the treatment of systemic lupus. Physicians at the University of Kentucky, at the University of Connecticut, and in London have treated many pregnant women who have lupus with anti-malarials without adverse effects on the fetus. More research is needed on this topic. Women with lupus who are planning to become pregnant should talk to their doctor about the pros and cons of continuing anti-malarial drug treatment. < Back to the Top What Are Some Side Effects of Anti-Malarials? The side effects of anti-malarials include skin rashes and pigment (skin color) changes. Atabrine specifically can cause yellow pigmentation of the skin. Other side effects can include: hair loss dry skin loss of appetite abdominal bloating upset stomach stomach cramps nausea, vomiting, and diarrhea These side effects usually go away after the patient adjusts to the medication. If they continue, however, a physician should be consulted. Individuals who take generic hydroxychloroquine might try the brand Plaquenil before switching to a different anti-inflammatory drug. Some people may experience headaches, muscle aches, 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 and seizures, are quite rare. However, if any of these side effects occur, they should be reported immediately to a physician. < Back to the Top Vision A major potential side effect of anti-malarial use is the possible damage to the retina at the back of the eye. It is important to note that retinal damage due to the use of anti-malarials is dose-related, and the low doses currently used in the treatment of lupus are rarely associated with this condition. Most cases of eye disease occur in people receiving more than 400 mg of Plaquenil or more than 250 mg of Aralen daily. Atabrine is not known to cause retinal damage. Recent evidence shows that there is no irreversible eye damage with Plaquenil in doses of 5 mg/kg (2.3 mg/lb) per day. For the average-weight person, this is less than 400 mg per day, if used for less than 10 years. Retinal damage that is caused by Plaquenil is sometimes reversible if it is detected early. However, damage due to the use of Chloroquine (Aralen) is irreversible. It is necessary to see an eye doctor or ophthalmologist prior to beginning treatment with anti-malarials in order to have a baseline examination. A follow-up examination every three to six months thereafter is also necessary. Eye exams of the macula to rule out fine pigmentary disturbances should be performed at least every year. On many occasions, an ophthalmologist can see mild changes in the retinal pigment that indicate early damage. In addition to regular eye check-ups to test visual acuity and eye pressure, tests for color vision and visual field might be necessary. New computer-assisted machines for testing the visual field are very sensitive to small changes that might be due to anti-malarials. People with lupus can also monitor themselves between visits with a black and white or red and black Amsler grid, which can be requested from an ophthalmologist. If visual symptoms do occur (blurred vision or any other changes in vision), these should be reported immediately to a doctor. In summary, anti-malarials can contribute substantially to the relief of some symptoms associated with lupus, especially those affecting the skin and joints. Other potential benefits of Plaquenil have included decreased levels of cholesterol in individuals who are steroid-dependent, and decreased thrombosis in individuals with positive cardiolipin antibodies. The side effects mentioned are not common, and anti-malarials are generally regarded as safe to use in the treatment of lupus. < Back to the Top The Lupus Foundation of America The Lupus Foundation of America (LFA) was established in 1977 to educate and support those affected by lupus and find the cure. The LFA supports research, education, awareness, patient services, and advocacy. The Lupus Foundation of America is the only nationwide organization exclusively serving individuals, families and friends affected by lupus. The LFA has hundreds of local chapters and support groups throughout the United States, as well as international affiliates around the world. The LFA is a grassroots, volunteer-driven organization. Contact the LFA or the chapter that serves your area to find out how you can become involved in our mission. Become a Lupus E-Advocate and help pass federal legislation that will benefit people with lupus. Send an e-mail message to advocacy@... and enter SUBSCRIBE in the subject line. You'll receive periodic advocacy updates and other breaking lupus news and information. For information about lupus or to locate the chapter nearest you, visit our website at www.lupus.org or call our information request line toll-free at 1- (en Español, ). Approved by the Lupus Foundation of America's Patient Education Committee © 2000 Lupus Foundation of America, Inc. < Back to the Top Related Information On this web site Brochures: Cardiopulmonary Disease and Lupus Joint and Muscle Pain in Lupus Pregnancy and Lupus Skin Disease in Lupus On the Internet MEDLINE plus: About Your Medicines FDA: Pharmacy Compounding - Customizing Prescription Drugs International Academy of Compounding Pharmacists Much Love, Deanna LUPUS Serenity Prayer... Lord, grant me the serenity to accept the things I cannot change, the courage to change the things I can, and the wisdom to hide the bodies of doctors I shot when they said, You're perfectly healthy, it's all in your head " Quote Link to comment Share on other sites More sharing options...
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