Systemic lupus erythematosus (SLE) is a multisystem autoimmune disease that affects various organs. Lupus nephritis is one of the most common, and most important, serious manifestations of SLE. Antimalarial agents are part of the immunomodulatory regimen used to treat patients with SLE; however, their role in the treatment of patients with lupus nephritis in particular is less well recognized, especially by nephrologists. Not all antimalarial agents have been used in the treatment of lupus; this Review will focus on studies using chloroquine and hydroxychloroquine. In addition, this Review will briefly describe the history of antimalarial drug use in patients with SLE, the theorized mechanisms of action of the agents chloroquine and hydroxychloroquine, their efficacy in patients with SLE and those with lupus nephritis, their use in pregnancy, and potential adverse effects. The Review will also cover the latest recommendations regarding monitoring for hydroxychloroquine-associated or chloroquine-associated retinopathy. Overall, antimalarial drugs have numerous beneficial effects in patients with SLE and lupus nephritis, and have a good safety profile.
Antimalarial therapy for patients with systemic lupus erythematosus (SLE) is associated with improved survival and reduced disease activity, as well as cardioprotective and anticancer effects
In lupus nephritis, antimalarial therapy is associated with reduced corticosteroid use, reduced disease activity, extended time to end-stage renal disease, and, with adjunctive immunomodulatory treatment, improved duration of renal remission
Treatment with antimalarial agents should be continued in pregnant women with SLE; the beneficial effects may include a reduction in the risk of cardiac manifestations of neonatal SLE
Antimalarial drugs have a good safety profile; gastrointestinal symptoms are the most common adverse effect
Baseline monitoring for retinopathy is required, but regular monitoring is recommended by the American Academy of Ophthalmology guidelines only for patients who have taken antimalarial agents for >5 years
In patients with impaired renal function, caution with dosing of antimalarial agents is recommended and careful monitoring for adverse events should be undertaken
This is a preview of subscription content, access via your institution
Open Access articles citing this article.
Efficacy and safety of artesunate for patients with IgA nephropathy: a study protocol for a multicenter, double-blind, randomized, placebo-controlled trial
Trials Open Access 25 May 2022
C-type lectin receptor Dectin3 deficiency balances the accumulation and function of FoxO1-mediated LOX-1+ M-MDSCs in relieving lupus-like symptoms
Cell Death & Disease Open Access 03 September 2021
Emerging roles of Toll-like receptor 9 in cardiometabolic disorders
Inflammation and Regeneration Open Access 21 July 2020
Subscribe to this journal
Receive 12 print issues and online access
$189.00 per year
only $15.75 per issue
Rent or buy this article
Get just this article for as long as you need it
Prices may be subject to local taxes which are calculated during checkout
Schmajuk, G., Yazdany, J., Trupin, L. & Yelin, E. Hydroxychloroquine treatment in a community-based cohort of patients with systemic lupus erythematosus. Arthritis Care Res. (Hoboken) 62, 386–392 (2010).
Ruiz-Irastorza, G., Ramos-Casals, M., Brito-Zeron, P. & Khamashta, M. A. Clinical efficacy and side effects of antimalarials in systemic lupus erythematosus: a systematic review. Ann. Rheum. Dis. 69, 20–28 (2010).
Wallace, D. J. The history of antimalarials. Lupus 5 (Suppl. 1), S2–S3 (1996).
Tett, S. E., Cutler, D. J., Day, R. O. & Brown, K. F. Bioavailability of hydroxychloroquine tablets in healthy volunteers. Br. J. Clin. Pharmacol. 27, 771–779 (1989).
Furst, D. E. Pharmacokinetics of hydroxychloroquine and chloroquine during treatment of rheumatic diseases. Lupus 5 (Suppl. 1), S11–S15 (1996).
Kalia, S. & Dutz, J. P. New concepts in antimalarial use and mode of action in dermatology. Dermatol. Ther. 20, 160–174 (2007).
McChesney, E. W. Animal toxicity and pharmacokinetics of hydroxychloroquine sulfate. Am. J. Med. 75, 11–18 (1983).
Leecharoen, S., Wangkaew, S. & Louthrenoo, W. Ocular side effects of chloroquine in patients with rheumatoid arthritis, systemic lupus erythematosus and scleroderma. J. Med. Assoc. Thai. 90, 52–58 (2007).
Barré, P. E., Gascon-Barré, M., Meakins, J. L. & Goltzman, D. Hydroxychloroquine treatment of hypercalcemia in a patient with sarcoidosis undergoing hemodialysis. Am. J. Med. 82, 1259–1262 (1987).
Fox, R. Anti-malarial drugs: possible mechanisms of action in autoimmune disease and prospects for drug development. Lupus 5 (Suppl. 1), S4–S10 (1996).
Ermann, J. & Bermas, B. L. The biology behind the new therapies for SLE. Int. J. Clin. Pract. 61, 2113–2119 (2007).
van den Borne, B. E., Dijkmans, B. A., de Rooij, H. H., le Cessie, S. & Verweij, C. L. Chloroquine and hydroxychloroquine equally affect tumor necrosis factor-alpha, interleukin 6, and interferon-gamma production by peripheral blood mononuclear cells. J. Rheumatol. 24, 55–60 (1997).
Karres, I. et al. Chloroquine inhibits proinflammatory cytokine release into human whole blood. Am. J. Physiol. 274, R1058–R1064 (1998).
Wozniacka, A., Lesiak, A., Narbutt, J., McCauliffe, D. P. & Sysa-Jedrzejowska, A. Chloroquine treatment influences proinflammatory cytokine levels in systemic lupus erythematosus patients. Lupus 15, 268–275 (2006).
Jang, C. H., Choi, J. H., Byun, M. S. & Jue, D. M. Chloroquine inhibits production of TNF-alpha, IL-1beta and IL-6 from lipopolysaccharide-stimulated human monocytes/macrophages by different modes. Rheumatology (Oxford) 45, 703–710 (2006).
Jeong, J. Y. & Jue, D. M. Chloroquine inhibits processing of tumor necrosis factor in lipopolysaccharide-stimulated RAW 264.7 macrophages. J. Immunol. 158, 4901–4907 (1997).
Sperber, K. et al. Selective regulation of cytokine secretion by hydroxychloroquine: inhibition of interleukin 1 alpha (IL-1-alpha) and IL-6 in human monocytes and T cells. J. Rheumatol. 20, 803–808 (1993).
Weber, S. M., Chen, J. M. & Levitz, S. M. Inhibition of mitogen-activated protein kinase signaling by chloroquine. J. Immunol. 168, 5303–5309 (2002).
Löffler, B. M., Bohn, E., Hesse, B. & Kunze, H. Effects of antimalarial drugs on phospholipase A and lysophospholipase activities in plasma membrane, mitochondrial, microsomal and cytosolic subcellular fractions of rat liver. Biochim. Biophys. Acta 835, 448–455 (1985).
Kim, W. U. et al. Hydroxychloroquine potentiates Fas-mediated apoptosis of rheumatoid synoviocytes. Clin. Exp. Immunol. 144, 503–511 (2006).
Potvin, F., Petitclerc, E., Marceau, F. & Poubelle, P. E. Mechanisms of action of antimalarials in inflammation: induction of apoptosis in human endothelial cells. J. Immunol. 158, 1872–1879 (1997).
Wozniacka, A. et al. The influence of antimalarial treatment on IL-1beta, IL-6 and TNF-alpha mRNA expression on UVB-irradiated skin in systemic lupus erythematosus. Br. J. Dermatol. 159, 1124–1130 (2008).
Hurst, N. P., French, J. K., Gorjatschko, L. & Betts, W. H. Studies on the mechanism of inhibition of chemotactic tripeptide stimulated human neutrophil polymorphonuclear leucocyte superoxide production by chloroquine and hydroxychloroquine. Ann. Rheum. Dis. 46, 750–756 (1987).
Nguyen, T. Q., Capra, J. D. & Sontheimer, R. D. 4-Aminoquinoline antimalarials enhance UV-B induced c-jun transcriptional activation. Lupus 7, 148–153 (1998).
Lesiak, A. et al. Effect of chloroquine phosphate treatment on serum MMP-9 and TIMP-1 levels in patients with systemic lupus erythematosus. Lupus 19, 683–688 (2010).
Lim, E. J. et al. Toll-like receptor 9 dependent activation of MAPK and NF-kB is required for the CpG ODN-induced matrix metalloproteinase-9 expression. Exp. Mol. Med. 39, 239–245 (2007).
Wallace, D. J., Linker-Israeli, M., Metzger, A. L. & Stecher, V. J. The relevance of antimalarial therapy with regard to thrombosis, hypercholesterolemia and cytokines in SLE. Lupus 2 (Suppl. 1), S13–S15 (1993).
Toubi, E. et al. The reduction of serum B-lymphocyte activating factor levels following quinacrine add-on therapy in systemic lupus erythematosus. Scand. J. Immunol. 63, 299–303 (2006).
Dubois, E. L. Antimalarials in the management of discoid and systemic lupus erythematosus. Semin. Arthritis Rheum. 8, 33–51 (1978).
Dubois, E. L. Quinacrine (atabrine) in treatment of systemic and discoid lupus erythematosus. AMA Arch. Intern. Med. 94, 131–141 (1954).
Rudnicki, R. D., Gresham, G. E. & Rothfield, N. F. The efficacy of antimalarials in systemic lupus erythematosus. J. Rheumatol. 2, 323–330 (1975).
[No authors listed] A randomized study of the effect of withdrawing hydroxychloroquine sulfate in systemic lupus erythematosus. The Canadian Hydroxychloroquine Study Group. N. Engl. J. Med. 324, 150–154 (1991).
Meinão, I. M., Sato, E. I., Andrade, L. E., Ferraz, M. B. & Atra, E. Controlled trial with chloroquine diphosphate in systemic lupus erythematosus. Lupus 5, 237–241 (1996).
Alarcón, G. S. et al. Effect of hydroxychloroquine on the survival of patients with systemic lupus erythematosus: data from LUMINA, a multiethnic US cohort (LUMINA L). Ann. Rheum. Dis. 66, 1168–1172 (2007).
Fessler, B. J. et al. Systemic lupus erythematosus in three ethnic groups: XVI. Association of hydroxychloroquine use with reduced risk of damage accrual. Arthritis Rheum. 52, 1473–1480 (2005).
Molad, Y. et al. Protective effect of hydroxychloroquine in systemic lupus erythematosus. Prospective long-term study of an Israeli cohort. Lupus 11, 356–361 (2002).
Shinjo, S. K. et al. Antimalarial treatment may have a time-dependent effect on lupus survival: data from a multinational Latin American inception cohort. Arthritis Rheum. 62, 855–862 (2010).
Westlake, S. L. & Edwards C. J. Anti-malarials and lupus in West Africa use and lupus in Africans. Lupus 18, 193–195 (2009).
Hodis, H. N., Quismorio, F. P. Jr, Wickham, E. & Blankenhorn, D. H. The lipid, lipoprotein, and apolipoprotein effects of hydroxychloroquine in patients with systemic lupus erythematosus. J. Rheumatol. 20, 661–665 (1993).
Petri, M., Lakatta, C., Magder, L. & Goldman, D. Effect of prednisone and hydroxychloroquine on coronary artery disease risk factors in systemic lupus erythematosus: a longitudinal data analysis. Am. J. Med. 96, 254–259 (1994).
Tam, L. S., Gladman, D. D., Hallett, D. C., Rahman, P. & Urowitz, M. B. Effect of antimalarial agents on the fasting lipid profile in systemic lupus erythematosus. J. Rheumatol. 27, 2142–2145 (2000).
Borba, E. F. & Bonfá, E. Longterm beneficial effect of chloroquine diphosphate on lipoprotein profile in lupus patients with and without steroid therapy. J. Rheumatol. 28, 780–785 (2001).
Sachet, J. C. et al. Chloroquine increases low-density lipoprotein removal from plasma in systemic lupus patients. Lupus 16, 273–278 (2007).
Cardoso, C. R., Signorelli, F. V., Papi, J. A. & Salles, G. F. Prevalence and factors associated with dyslipoproteinemias in Brazilian systemic lupus erythematosus patients. Rheumatol. Int. 28, 323–327 (2008).
Bevan, A. P., Christensen, J. R., Tikerpae, J. & Smith, G. D. Chloroquine augments the binding of insulin to its receptor. Biochem. J. 311, 787–795 (1995).
Petri, M. Hydroxychloroquine use in the Baltimore Lupus Cohort: effects on lipids, glucose and thrombosis. Lupus 5 (Suppl. 1), S16–S22 (1996).
Rekedal, L. R. et al. Changes in glycosylated hemoglobin after initiation of hydroxychloroquine or methotrexate treatment in diabetes patients with rheumatic diseases. Arthritis Rheum. 62, 3569–3573 (2010).
Penn, S. K. et al. Hydroxychloroquine and glycemia in women with rheumatoid arthritis and systemic lupus erythematosus. J. Rheumatol. 37, 1136–1142 (2010).
Gerstein, H. C., Thorpe, K. E., Taylor, D. W. & Haynes, R. B. The effectiveness of hydroxychloroquine in patients with type 2 diabetes mellitus who are refractory to sulfonylureas—a randomzed trial. Diabetes Res. Clin. Pract. 55, 209–219 (2002).
Bellomio, V. et al. Metabolic syndrome in Argentinean patients with systemic lupus erythematosus. Lupus 18, 1019–1025 (2009).
Razani, B., Feng, C. & Semenkovich, C. F. p53 is required for chloroquine-induced atheroprotection but not insulin sensitization. J. Lipid Res. 51, 1738–1746 (2010).
Roman, M. J. et al. Prevalence and correlates of accelerated atherosclerosis in systemic lupus erythematosus. N. Engl. J. Med. 349, 2399–2406 (2003).
Zhang, C. Y. et al. Evaluation of risk factors that contribute to high prevalence of premature atherosclerosis in Chinese premenopausal systemic lupus erythematosus patients. J. Clin. Rheumatol. 15, 111–116 (2009).
Souza, A. W., Hatta, F. S., Miranda, F. Jr & Sato, E. I. Atherosclerotic plaque in carotid arteries in systemic lupus erythematosus: frequency and associated risk factors. Sao Paulo Med. J. 123, 137–142 (2005).
Von Feldt, J. M. et al. Homocysteine levels and disease duration independently correlate with coronary artery calcification in patients with systemic lupus erythematosus. Arthritis Rheum. 54, 2220–2227 (2006).
Selzer, F. et al. Comparison of risk factors for vascular disease in the carotid artery and aorta in women with systemic lupus erythematosus. Arthritis Rheum. 50, 151–159 (2004).
Selzer, F. et al. Vascular stiffness in women with systemic lupus erythematosus. Hypertension 37, 1075–1082 (2001).
Tanay, A. et al. Vascular elasticity of systemic lupus erythematosus patients is associated with steroids and hydroxychloroquine treatment. Ann. NY Acad. Sci. 1108, 24–34 (2007).
Bessant, R. et al. Prevalence of conventional and lupus-specific risk factors for cardiovascular disease in patients with systemic lupus erythematosus: a case-control study. Arthritis Rheum. 55, 892–899 (2006).
Urowitz, M. B. et al. Atherosclerotic vascular events in a multinational inception cohort of systemic lupus erythematosus. Arthritis Care Res. (Hoboken) 62, 881–887 (2010).
Ruiz-Irastorza, G. et al. Antimalarials may influence the risk of malignancy in systemic lupus erythematosus. Ann. Rheum. Dis. 66, 815–817 (2007).
Sisó, A. et al. Previous antimalarial therapy in patients diagnosed with lupus nephritis: Influence on outcomes and survival. Lupus 17, 281–288 (2008).
Ruiz-Irastorza, G. et al. Effect of antimalarials on thrombosis and survival in patients with systemic lupus erythematosus. Lupus 15, 577–583 (2006).
Jung, H. et al. The protective effect of antimalarial drugs on thrombovascular events in systemic lupus erythematosus. Arthritis Rheum. 62, 863–868 (2010).
Tsakonas, E. et al. A long-term study of hydroxychloroquine withdrawal on exacerbations in systemic lupus erythematosus. The Canadian Hydroxychloroquine Study Group. Lupus 7, 80–85 (1998).
Pons-Estel, G. J. et al. Protective effect of hydroxychloroquine on renal damage in patients with lupus nephritis: LXV, data from a multiethnic US cohort. Arthritis Rheum. 61, 830–839 (2009).
Vlad, S. C. Protective effect of hydroxychloroquine on renal damage may be biased: comment on the article by Pons-Estel et al. Arthritis Rheum. 61, 1614 (2009).
Vinet, E., Bernatsky, S. & Suissa, S. Have some beneficial effects of hydroxychloroquine been overestimated? Potential biases in observational studies of drug effects: comment on the article by Pons-Estel et al. Arthritis Rheum. 61, 1614–1615 (2009).
Kasitanon, N., Fine, D. M., Haas, M., Magder, L. S. & Petri, M. Hydroxychloroquine use predicts complete renal remission within 12 months among patients treated with mycophenolate mofetil therapy for membranous lupus nephritis. Lupus 15, 366–370 (2006).
Parke, A. Antimalarial drugs and pregnancy. Am. J. Med. 85, 30–3 (1988).
Parke, A. & West, B. Hydroxychloroquine in pregnant patients with systemic lupus erythematosus. J. Rheumatol. 23, 1715–1718 (1996).
Costedoat-Chalumeau, N., Amoura, Z., Huong, D. L., Lechat, P. & Piette, J. C. Safety of hydroxychloroquine in pregnant patients with connective tissue diseases. Review of the literature. Autoimmun. Rev. 4, 111–115 (2005).
Germain, S. & Nelson-Piercy, C. Lupus nephritis and renal disease in pregnancy. Lupus 15, 148–155 (2006).
Clowse, M. E., Magder, L., Witter, F. & Petri, M. Hydroxychloroquine in lupus pregnancy. Arthritis Rheum. 54, 3640–3647 (2006).
Levy, R. A. et al. Hydroxychloroquine (HCQ) in lupus pregnancy: double-blind and placebo-controlled study. Lupus 10, 401–404 (2001).
Izmirly, P. M. et al. Evaluation of the risk of anti-SSA/Ro-SSB/La antibody-associated cardiac manifestations of neonatal lupus in fetuses of mothers with systemic lupus erythematosus exposed to hydroxychloroquine. Ann. Rheum. Dis. 69, 1827–1830 (2010).
Wang, C. et al. Discontinuation of antimalarial drugs in systemic lupus erythematosus. J. Rheumatol. 26, 808–815 (1999).
Sundelin, S. P. & Terman, A. Different effects of chloroquine and hydroxychloroquine on lysosomal function in cultured retinal pigment epithelial cells. APMIS 110, 481–489 (2002).
Marmor, M. F., Kellner, U., Lai, T. Y., Lyons, J. S. & Meiler, W. F. Revised recommendations on screening for chloroquine and hydroxychloroquine retinopathy. Ophthalmology 118, 415–422 (2011).
Rynes, R. I. Ophthalmologic considerations in using antimalarials in the United States. Lupus 5 (Suppl. 1), S73–S74 (1996).
Spalton, D. J. Retinopathy and antimalarial drugs—the British experience. Lupus 5 (Suppl. 1), S70–S72 (1996).
Marmor, M. F., Carr, R. E., Easterbrook, M., Farjo, A. A. & Mieler, W. F. Recommendations on screening for chloroquine and hydroxychloroquine retinopathy: a report by the American Academy of Ophthalmology. Ophthalmology 109, 1377–1382 (2002).
Mavrikakis, I. et al. The incidence of irreversible retinal toxicity in patients treated with hydroxychloroquine: a reappraisal. Ophthalmology 110, 1321–1326 (2003).
Lyons, J. S. & Severns, M. L. Using multifocal ERG ring ratios to detect and follow Plaquenil retinal toxicity: a review: review of mfERG ring ratios in Plaqunil toxicity. Doc. Ophthal. 118, 29–36 (2008).
Wolfe, F. & Marmor, M. F. Rates and predictors of hydroxychloroquine retinal toxicity in patients with rheumatoid arthritis and systemic lupus erythematosus. Arthritis Care Res. (Hoboken) 62, 775–784 (2010).
Levy, G. D. et al. Incidence of hydroxychloroquine retinopathy in 1,207 patients in a large multicenter outpatient practice. Arthritis Rheum. 40, 1482–1486 (1997).
The Royal College of Ophthalmologists. Hydroxychloroquine and Ocular Toxicity Recommendations on Screening [online], (2009).
Nord, J. E., Shah, P. K., Rinaldi, R. Z. & Weisman, M. H. Hydroxychloroquine cardiotoxicity in systemic lupus erythematosus: a report of 2 cases and review of the literature. Semin. Arthritis Rheum. 33, 336–351 (2004).
Puri, P. K., Lountzis, N. I., Tyler, W. & Ferringer, T. Hydroxychloroquine-induced hyperpigmentation: the staining pattern. J. Cutan. Pathol. 35, 1134–1137 (2008).
Herman, S. M., Shin, M. H., Holbrook, A. & Rosenthal, D. The role of antimalarials in the exacerbation of psoriasis: a systematic review. Am. J. Clin. Dermatol. 7, 249–257 (2006).
Bracamonte, E. R., Kowalewska, J., Starr, J., Gitomer, J. & Alpers, C. E. Iatrogenic phospholipidosis mimicking Fabry disease. Am. J. Kidney Dis. 48, 844–850 (2006).
Costedoat-Chalumeau, N. et al. Very low blood hydroxychloroquine concentration as an objective marker of poor adherence to treatment of systemic lupus erythematosus. Ann. Rheum. Dis. 66, 821–824 (2007).
Costedoat-Chalumeau, N. et al. Low blood concentration of hydroxychloroquine is a marker for and predictor of disease exacerbations in patients with systemic lupus erythematosus. Arthritis Rheum. 54, 3284–3290 (2006).
Calvo-Alén, J. et al. Systemic lupus erythematosus in a multiethnic US cohort (LUMINA): XXIV. Cytotoxic treatment is an additional risk factor for the development of symptomatic osteonecrosis in lupus patients: results of a nested matched case-control study. Ann. Rheum. Dis. 65, 785–790 (2006).
James, J. A. et al. Hydroxychloroquine sulfate treatment is associated with later onset of systemic lupus erythematosus. Lupus 16, 401–409 (2007).
Ruiz-Irastorza, G. et al. Predictors of major infections in systemic lupus erythematosus. Arthritis Res. Ther. 11, R109 (2009).
Shinjo, S. K. Systemic lupus erythematosus in the elderly: antimalarials in disease remission. Rheumatol. Int. 29, 1087–1090 (2009).
Pons-Estel, G. J. et al. Possible protective effect of hydroxychloroquine on delaying the occurrence of integument damage in lupus: LXXI, data from a multiethnic cohort. Arthritis Care Res. (Hoboken) 62, 393–400 (2010).
de Leeuw, K. et al. Traditional and non-traditional risk factors contribute to the development of accelerated atherosclerosis in patients with systemic lupus erythematosus. Lupus 15, 675–682 (2006).
Choojitarom, K. et al. Lupus nephritis and Raynaud's phenomenon are significant risk factors for vascular thrombosis in SLE patients with positive antiphospholipid antibodies. Clin. Rheumatol. 27, 345–351 (2008).
Kaiser, R., Cleveland, C. M. & Criswell, L. A. Risk and protective factors for thrombosis in systemic lupus erythematosus: results from a large, multi-ethnic cohort. Ann. Rheum. Dis. 68, 238–241 (2009).
Tektonidou, M. G., Laskari, K., Panagiotakos, D. B. & Moutsopoulos, H. M. Risk factors for thrombosis and primary thrombosis prevention in patients with systemic lupus erythematosus with or without antiphospholipid antibodies. Arthritis Rheum. 61, 29–36 (2009).
Barber, C. E., Geldenhuys, L. & Hanly, J. G. Sustained remission of lupus nephritis. Lupus 15, 94–101 (2006).
Buchanan, N. M. et al. Hydroxychloroquine and lupus pregnancy: review of a series of 36 cases. Ann. Rheum. Dis. 55, 486–488 (1996).
Costedoat-Chalumeau, N. et al. Safety of hydroxychloroquine in pregnant patients with connective tissue diseases: a study of one hundred thirty-three cases compared with a control group. Arthritis Rheum. 48, 3207–3211 (2003).
Carvalheiras, G. et al. Pregnancy and systemic lupus erythematosus: review of clinical features and outcome of 51 pregnancies at a single institution. Clin. Rev. Allergy Immunol. 38, 302–306 (2010).
Aviña-Zubieta, J. A., Galindo-Rodriguez, G., Newman, S., Suarez-Almazor, M. E. & Russell, A. S. Long-term effectiveness of antimalarial drugs in rheumatic diseases. Ann. Rheum. Dis. 57, 582–587 (1998).
Finbloom, D. S., Silver, K., Newsome, D. A. & Gunkel, R. Comparison of hydroxychloroquine and chloroquine use and the development of retinal toxicity. J. Rheumatol. 12, 692–694 (1985).
Spalton, D. J., Verdon Roe, G. M. & Hughes, G. R. Hydroxychloroquine, dosage parameters and retinopathy. Lupus 2, 355–358 (1993).
Morand, E. F., McCloud, P. I. & Littlejohn, G. O. Continuation of long term treatment with hydroxychloroquine in systemic lupus erythematosus and rheumatoid arthritis. Ann. Rheum. Dis. 51, 1318–1321 (1992).
Costedoat-Chalumeau, N. et al. Cardiomyopathy related to antimalarial therapy with illustrative case report. Cardiology 107, 73–80 (2007).
Costedoat-Chalumeau, N. et al. Heart conduction disorders related to antimalarials toxicity: an analysis of electrocardiograms in 85 patients treated with hydroxychloroquine for connective tissue diseases. Rheumatology (Oxford) 46, 808–810 (2007).
Wozniacka, A., Cygankiewicz, I., Chudzik, M., Sysa-Jedrzejowska, A. & Wranicz, J. K. The cardiac safety of chloroquine phosphate treatment in patients with systemic lupus erythematosus: the influence on arrhythmia, heart rate variability and repolarization parameters. Lupus 15, 521–525 (2006).
Cervera, A., Espinosa, G., Font, J. & Ingelmo, M. Cardiac toxicity secondary to long term treatment with chloroquine. Ann. Rheum. Dis. 60, 301 (2001).
Di Giacomo, T. B., Valente, N. Y. & Nico, M. M. Chloroquine -induced hair depigmentation. Lupus 18, 264–266 (2009).
Bezerra, E. L., Vilar, M. J., da Trindade Neto, P. B. & Sato, E. L. Double-blind, randomized, controlled clinical trial of clofazimine compared with chloroquine in patients with systemic lupus erythematosus. Arthritis Rheum. 52, 3073–3078 (2005).
Van Beek, M. J. & Piette, W. W. Antimalarials. Dermatol. Clin. 19, 147–160 (2001).
Casado, E. et al. Antimalarial myopathy: an underdiagnosed complication? Prospective longitudinal study of 119 patients. Ann. Rheum. Dis. 65, 385–390 (2006).
Collins, G. B. & McAllister, M. S. Chloroquine psychosis masquerading as PCP: a case report. J. Psychoactive Drugs 40, 211–214 (2008).
The authors declare no competing financial interests.
Rights and permissions
About this article
Cite this article
Lee, SJ., Silverman, E. & Bargman, J. The role of antimalarial agents in the treatment of SLE and lupus nephritis. Nat Rev Nephrol 7, 718–729 (2011). https://doi.org/10.1038/nrneph.2011.150
This article is cited by
Lupusnephritis – von der Diagnose zur Therapie
Die Innere Medizin (2023)
Efficacy and safety of artesunate for patients with IgA nephropathy: a study protocol for a multicenter, double-blind, randomized, placebo-controlled trial
Klassifikation der Lupusnephritis
Die Nephrologie (2022)
Impact of gamma-irradiation on the degradation and mineralization of hydroxychloroquine aqueous solutions
International Journal of Environmental Science and Technology (2022)
MERCI: a machine learning approach to identifying hydroxychloroquine retinopathy using mfERG
Documenta Ophthalmologica (2022)