In SLE, antimalarials can be used for early or mild cases without organ involvement or as a steroid-sparing agent. In cases of systemic involvement, antimalarial mono-therapy is not indicated.
However, antimalarials can induce remissions and prevent exacerbations of chronic SLE ([No authors listed] 1995, Tsakonas et al. 1998). In a placebo-controlled randomized trial, chloroquine (250 mg) kept mild lupus in remission without serious side effects. The risk of an exacerbation of the disease was 4.6 times higher with placebo than with chloroquine (Meinao et al. 1996). Compared with nonsteroidal anti-inflammatory drugs, these compounds have the advantage of a lower risk for cutaneous, liver, and nephrotoxic reactions. In contrast to immunosuppressants, there is no risk of either bone marrow suppression or opportunistic infections. Therefore, chloroquine and hydroxychloroquine can be regarded as basic therapy for uncomplicated SLE (Barthel et al. 1996, D'Cruz 2001, Molad et al. 2002, Ruiz-Irastorza et al. 2000). In a recent survey, 70% of patients with SLE had received antimalarials (Wang et al. 1999). The average duration of therapy was 6.9 years per patient. Reasons for withdrawal of therapy were remission (42%), side effects (29%, see above), noncompliance (15%), and miscellaneous reasons, such as pregnancy (6%). Only in 8% was a lack of efficacy the reason for stopping therapy.
In SLE, the cutaneous symptoms, weariness, myalgias, and joint symptoms generally improve with antimalarial therapy (Williams et al. 1994). Also, mucosal lesions respond favorably (Orteu et al. 2001). If the heart, lungs, or kidneys are involved or if hematologic or vasculitic central nervous system manifestations occur, antimalarials should never be used alone (Barthel et al. 1996).
Whereas in SLE no exact data are available, a synergistic effect of the combination of methotrexate, sulfadiazine, and hydroxychloroquine was reported in rheumatoid arthritis. In addition, the hepatotoxicity of methotrexate was reduced (O'Dell et al.
1996, 2002). Exacerbations also were rare with continuation of hydroxychloroquine use (Clegg et al. 1997).
In SCLE, effectiveness of antimalarials of 50% to 80% was reported (Versapuech et al. 2000). Keep in mind that 90% of nonsmokers but only 40% of smokers with DLE/SCLE responded to antimalarials (Jewell and McCauliffe 2000). Therefore, smoking has to be regarded as a confounding factor impairing the therapeutic efficacy of antimalarials.
Quinacrine was also reported to add beneficial, steroid-sparing effects to a hydroxychloroquine therapy in SLE (Toubi et al. 2000) and SCLE (von Schmiedeberg et al. 2000). It can improve fever, adenopathy, sun sensitivity, mucous membrane lesions, alopecia, arthritis, headache, fatigue, and serositis. Quinacrine has no activity against nephritis, myocarditis, central nervous system involvement, or hematologic, hepatitis, or lung parenchymal involvement of lupus (Wallace 1989).
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