Antimalarials – are they effective and safe in rheumatic diseases?

Antimalarial drugs (AD) are a group of widespread therapeutic agents in multiple rheumatic indications. Although the effect of AD is mild and extended in time, low toxicity is their appreciated value. This paper describes the current state of knowledge on the mechanism of action, use, toxicity and pleiotropic effects of AD in the pharmacotherapy of autoimmune diseases.

REFERENCES (42)

Woodward R, Doering W. The total synthesis of quinine. J Am Chem Soc 1944; 66: 849.

Google Scholar

Iredale J, Fieger H, Wainer IW. Determination of the stereoisomers of hydroxychloroquine and its major metabolites in plasma and urine following a single oral administration of racemic hydroxychloroquine. Semin Arthritis Rheum 1993; 23 (Suppl. 1): 74-81.

Google Scholar

Furst DE. Pharmacokinetics of hydroxychloroquine and chloroquine during treatment of rheumatic diseases. Lupus 1996; 5 (Suppl. 1): S11-S15.

Google Scholar

McLachlan AJ, Tett SE, Cutler DJ, et al. Bioavailability of hydroxychloroquine tablets in patients with rheumatoid arthritis. Br J Rheumatol 1994; 33: 235-239.

Google Scholar

Ono C, Yamada M, Tanaka M. Absorption, distribution and excretion of 14C-chloroquine after single oral administration in albino and pigmented rats: binding characteristics of chloroquine-related radioactivity to melanin in vivo. J Pharm Pharmacol 2003; 55: 1647-1654.

Google Scholar

Tanaka E, Taniguchi A, Urano W, et al. Pharmacogenetics of disease-modifying anti-rheumatic drugs. Best Pract Res Clin Rheumatol 2004; 18: 233-247.

Google Scholar

Furst DE, Lindsley H, Baethge B, et al. Dose-loading with hydroxychloroquine improves the rate of response in early, active rheumatoid arthritis: a randomized, double-blind six-week.

Google Scholar

trial with eighteen-week extension. Arthritis Rheum 1999; 42: 357-365.

Google Scholar

Costedoat-Chalumeau N, Hulot JS, Amoura Z, 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) 2007; 46: 808-810.

Google Scholar

10.

Götestam Skorpen C, Hoeltzenbein M, Tincani A, et al. The EULAR points to consider for use of antirheumatic drugs before pregnancy, and during pregnancy and lactation. Ann Rheum Dis 2016; 75: 795-810.

Google Scholar

11.

Willis R, Seif AM, McGwin G Jr, et al. Effect of hydroxychloroquine treatment on pro-inflammatory cytokines and disease activity in SLE patients: data from LUMINA (LXXV), a multiethnic US cohort. Lupus 2012; 21: 830-835.

Google Scholar

12.

Ruiz-Irastorza G, Ramos-Casals M, Brito-Zeron P, et al. Clinical efficacy and side effects of antimalarials in systemic lupus erythematosus: a systematic review. Ann Rheum Dis 2010; 69: 20-28.

Google Scholar

13.

James JA, Kim-Howard XR, Bruner BF, et al. Hydroxychloroquine sulfate treatment is associated with later onset of systemic lupus erythematosus. Lupus 2007; 16: 401-409.

Google Scholar

14.

Hahn BH, McMahon MA, Wilkinson A, et al. American College of Rheumatology guidelines for screening, treatment, and management of lupus nephritis. Arthritis Care Res (Hoboken) 2012; 64: 797-808.

Google Scholar

15.

Gaujoux-Viala C, Smolen JS, Landewé R, et al. Current evidence for the management of rheumatoid arthritis with synthetic disease-modifying antirheumatic drugs: a systematic literature review informing the EULAR recommendations for the management of rheumatoid arthritis. Ann Rheum Dis 2010; 69: 1004-1009.

Google Scholar

16.

Penn SK, Kao AH, Schott LL, et al.Hydroxychloroquine and glycemia in women with rheumatoid arthritis and systemic lupus erythematosus. J Rheumatol 2010; 37: 1136-1142.

Google Scholar

17.

Ramos-Casals M, Brito-Zerón P, Sisó-Almirall A, et al. Topical and systemic medications for the treatment of primary Sjögren’s syndrome. Nat Rev Rheumatol 2012; 8: 399-411.

Google Scholar

18.

Solomon DH, Massarotti E, Garg R, et al. Association between disease-modifying antirheumatic drugs and diabetes risk in patients with rheumatoid arthritis and psoriasis. JAMA 2011; 305: 2525-2531.

Google Scholar

19.

Mok CC, Mak A, Ma KM. Bone mineral density in postmenopausal Chinese patients with systemic lupus erythematosus. Lupus 2005; 14: 106-112.

Google Scholar

20.

Voronov I, Ochotny N, Jaumouillé V, et al. The R740S mutation in the V-ATPase a3 subunit increases lysosomal pH, impairs NFATc1 translocation, and decreases in vitro osteoclastogenesis. J Bone Miner Res 2013; 28: 108-118.

Google Scholar

21.

Cairoli E, Rebella M, Danese N, et al. Hydroxychloroquine reduces low-density lipoprotein cholesterol levels in systemic lupus erythematosus: a longitudinal evaluation of the lipid-lowering effect. Lupus 2012; 21: 1178-1182.

Google Scholar

22.

Tektonidou MG, Laskari K, Panagiotakos DB, et al. Risk factors for thrombosis and primary thrombosis prevention in patients with systemic lupus erythematosus with or without antiphospholipid antibodies. Arthritis Rheum 2009; 61: 29-36.

Google Scholar

23.

Jung H, Bobba R, Su J, et al. The protective effect of antimalarial drugs on thrombovascular events in systemic lupus erythematosus. Arthritis Rheum 2010; 62: 863-868.

Google Scholar

24.

Tanay A, Leibovitz E, Frayman A, et al. Vascular elasticity of systemic lupus erythematosus patients is associated with steroids and hydroxychloroquine treatment. Ann N Y Acad Sci 2007; 1108: 24-34.

Google Scholar

25.

Bengtsson C, Andersson SE, Edvinsson L, et al. Effect of medication on microvascular vasodilatation in patients with systemic lupus erythematosus. Basic Clin Pharmacol Toxicol 2010; 107: 919-924.

Google Scholar

26.

Selzer F, Sutton-Tyrrell K, Fitzgerald S, et al. Vascular stiffness in women with systemic lupus erythematosus. Hypertension 2001; 37: 1075-1082.

Google Scholar

27.

Sisó A, Ramos-Casals M, Bové A, et al. Previous antimalarial therapy in patients diagnosed with lupus nephritis: influence on outcomes and survival. Lupus 2008; 17: 281-288.

Google Scholar

28.

Ruiz-Irastorza G, Olivares N, Ruiz-Arruza I, et al. Predictors of major infections in systemic lupus erythematosus. Arthritis Res Ther 2009; 11: R109.

Google Scholar

29.

Rahim R, Strobl JS. Hydroxychloroquine, chloroquine, and all-trans retinoic acid regulate growth, survival, an histone acetylation in breast cancer cells. Anticancer Drugs 2009; 20: 736-745.

Google Scholar

30.

Savarino A, Gennero L, Chen HC, et al. Anti-HIV effects of chloroquine: mechanisms of inhibition and spectrum of activity. AIDS 2001; 15: 2221-2229.

Google Scholar

31.

Kim WU, Yoo SA, Min SY, et al. Hydroxychlor- oquine potentiates Fas-mediated apoptosis of rheumatoid synoviocytes. Clin Exp Immunol 2006; 144: 503-511.

Google Scholar

32.

Ruiz-Irastorza G, Ugarte A, Egurbide MV, et al. Antimalarials may influence the risk of malignancy in systemic lupus erythematosus. Ann Rheum Dis 2007; 66: 815-817.

Google Scholar

33.

Kalia S, Dutz JP. New concepts in antimalarial use and mode of action in dermatology. Dermatol Ther 2007; 20: 160-174.

Google Scholar

34.

Van Beek MJ, Piette WW. Antimalarials. Dermatol Clin 2001; 19: 147-160.

Google Scholar

35.

Pelle MT, Callen JP. Adverse cutaneous reactions to hydroxychloroquine are more common in patients with dermatomyositis than in patients with cutaneous lupus erythematosus. Arch Dermatol 2002; 138: 1231-1233.

Google Scholar

36.

Rynes RI. Antimalarial drugs in the treatment of rheumatological diseases. Br J Rheumatol 1997; 36: 799-805.

Google Scholar

37.

Tang C, Godfrey T, Stawell R, et al. Hydroxychloroquine in lupus: emerging evidence supporting multiple beneficial effects. Intern Med J 2012; 42: 968-978.

Google Scholar

38.

Wolfe F, Marmor MF. Rates and predictors of hydroxychloroquine retinal toxicity in patients with rheumatoid arthritis and systemic lupus erythematosus. Arthritis Care Res 2010; 62: 775-784.

Google Scholar

39.

Missner S, Kellner U. Comparison of different screening methods for chloroquine/hydroxychloroquine retinopathy: multifocal electroretinography, color vision, perimetry, ophthalmoscopy, and fluorescein angiography. Graefes Arch Clin Exp Ophthalmol 2012; 250: 319-325.

Google Scholar

40.

Casado E, Gratacós J, Tolosa C, et al. Antimalarial myopathy: an underdiagnosed complication? Prospective longitudinal study of 119 patients. Ann Rheum Dis 2006; 65: 385-390.

Google Scholar

41.

Clowse ME, Magder L, Witter F. Hydroxychloroquine in lupus pregnancy. Arthritis Rheum 2006; 54: 3640-3647.

Google Scholar

42.

Avińa-Zubieta JA, Galindo-Rodriguez G, et al. Long-term effectiveness of antimalarial drugs in rheumatic diseases. Ann Rheum Dis 1998; 57: 582-587.

Google Scholar

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