Hydroxychloroquine is used by 35% of SLE patients enrolled in the Baltimore Lupus Cohort. Eighty per cent of patients who took hydroxychloroquine at cohort entry remain on it six years later. In addition to its role for disease manifestations of lupus, hydroxychloroquine may be indicated for the prevention of disease or treatment-induced complications, including hyperlipidemia, diabetes mellitus, liver function test elevation and thrombosis.
PetriM, HowardD, GoldmanDW.Side-effects of medications prescribed for systemic lupus erythematosus (abstract).Arthritis Rheum1992; 35: S358.
2.
PetriM, Perez-GutthannS, SpenceD, HochbergMC.Risk factors for coronary artery disease in patients with systemic lupus erythematosus.Am J Med1992; 93: 513–519.
3.
PetriM, SpenceD, BoneLR, HochbergMC.Coronary artery disease risk factors in the Hopkins Lupus Cohort: prevalence, patient recognition and preventive practices.Medicine1992; 71: 291–302.
4.
PetriM. Arterial thrombotic events (TE) in SLE: the Baltimore Lupus Cohort study (Abstract).Arthritis Rheum1994; 37(Suppl. 9): S297.
5.
ChenHW, LeonardDA.Chloroquine inhibits cyclization of squalene oxide to lanosterol in mammalian cells.J Biol Chem1984; 259: 8156–8162.
6.
GoldsteinJL, BrownMS.The LDL pathway in human fibroblasts: a receptor-mediated mechanism for the regulation of cholesterol metabolism.Curr Top Cell Regul1976; 11: 147–181.
7.
FaustJR, GoldsteinJL, BrownMS.Receptor-mediated uptake of low density lipoprotein and utilization of its cholesterol for steroid synthesis in cultured mouse adrenal cells.J Biol Chem1977; 252: 4861–4871.
8.
OramJF, AlbersJJ, CheungMC, BiermanEL.The effects of subfractions of high density lipoprotein on cholesterol efflux from cultured fibroblasts. Regulation of low density lipoprotein receptor activity.J Biol Chem1981; 256: 8348–8356.
9.
MatsuzawaY, HostetlerKY.Studies on drug-induced lipidosis: subcellular localization of phospholipid and cholesterol in the liver of rats treated with chloroquine of 4,4′-bis(diethylaminoethoxy) α,β-diehyldiphenylethane.J Lipid Res1980; 21: 202–214.
10.
SewellRB, BarhamSS, LaRussoNF.Effect of chloroquine on the form and function of hepatocyte lysosomes. Morphologic modifications and physiologic alterations related to the biliary excretion of lipids and proteins.Gastroenterology1983; 85: 1146–1153.
11.
LaFontH. Influence of acute injection of chloroquine on the biliary secretion of lipids and lysosomal enzyme in rats.Lipids1984; 19: 195–201.
12.
LorberM. Hypocholesterolaemia and abnormal high-density lipoprotein in rheumatoid arthritis.Br J Rheumatol1985; 24(3): 250–255.
13.
WallaceDJ. Cholesterol-lowering effect of hydroxychloroquine in patients with rheumatic disease: reversal of deleterious effects of steroids on lipids.Am J Med1990; 89: 322–326.
14.
HodisHN, QuismorioFPJr, WickhamE, BlankenhornDH.The lipid, lipoprotein and apolipoprotein effects of hydroxychloroquine in patients with systemic lupus erythematosusJ Rheumatol1993; 20: 661–665.
15.
PetriM, LakattaC, MagderL, GoldmanDW.Effect of prednisone and hydroxychloroquine on coronary artery disease risk factors in systemic lupus erythematosus: a longitudinal data analysis.Am J Med1994; 96: 254–259.
16.
PetriM. Dietary intervention for hypercholesterolemia in systemic lupus erythematosus (Abstract).Arthritis Rheum1993; 36(9, Suppl.): S186.
17.
PhillipsRE. Hypoglycaemia and antimalarial drugs: quinidine and release of insulin.Br Med J (Clin Res Ed)1986; 292(6531): 1319–1321.
18.
Abu-ShakraM, LeeP.Hypoglycemia: an unusual adverse reaction to chloroquine (Letter).Clin Exp Rheumatol1994; 12: 95.
19.
BamberMG, RedapthA.Chloroquine and hypoglycaemia (Letter).Lancet1987; 1: 1211.
20.
SmithGD, AmosTAS, MahlerR, PetersTJ.Effect of chloroquine on insulin and glucose homoeostasis in normal subjects and patients with non-insulin-dependent diabetes mellitus.Br Med J1987; 294: 465–467.
21.
BlazerBR. In vivo chloroquine-induced inhibition of insulin degradation in a diabetic patient with severe insulin resistance.Diabetes1984; 33: 1133–1136.
22.
KhanMN. Insulin and insulin receptor uptake into rat liver. Chloroquine action on receptor recycling.Diabetes1985; 34: 1025–1030.
23.
DuckworthWC, KitabchiAE.Insulin metabolism and degradation.Endocrine Rev1981; 2: 210–233.
24.
NealGW, KitabchiAE.Insulin degradation by human skeletal muscle.Biochim Biophys Acta1982; 719: 259–266.
25.
DennisPA, AronsonNNJrThe effects of low temperature and chloroquine on 125I-insulin degradation by the perfused rat liver.Arch Biochem Biophys1981; 212: 170–176.
26.
FylesJM, CawthorneMA, HowellSL.The effect of chloroquine on receptor internalization in pancreatic islets.Diabetic Med1986; 3: P57, 373A.
27.
OparaE, van HaeftenT.Use of chloroquine in adipocyte insulin binding experiments: improved estimation of insulin internalization and receptor bound insulin with linearization of the Scatchard plot (Abstract).Diabetes1987; 26(Suppl. 1): 160A.
28.
CynoberL. Modulation of insulin action on 2-deoxyglucose uptake by chloroquine in chick embryo fibroblasts.Diabetes1987; 36: 27–32.
29.
FleigWE, HossG, Nother-FleigG, DitschuneitH.Insulin binding to cultured adult hepatocytes. Effects of bacitracin and chloroquine on the nature of cell-associated radioactivity.Biochem J1986; 237: 99–104.
30.
SorimachiK, OkayasuT, YasumuraY.Increase in insulin binding affinity by chloroquine in cultured rat hepatoma cells.Endocr Res1987; 13: 49–60.
31.
QuatraroA. Hydroxychloroquine in decompensated, treatment-refractory noninsulin-dependent diabetes mellitus. A new job for an old drug?Ann Intern Med1990; 112(9): 678–681.
32.
PetriM, YooS-S.Predictors of glucose intolerance in systemic lupus erythematosus (Abstract).Arthritis Rheum1994; 37: S323.
33.
GrafiaJ. Prospective study of 20 episodes of fever in 13 patients with systemic lupus erythematosus (Abstract).Arthritis Rheum1994; 37(9, Suppl): S322.
34.
FriesJF, SinghG, LenertL, FurstDE.Aspirin, hydroxychloroquine and hepatic enzyme abnormalities with methotrexate in rheumatoid arthritis.Arthritis Rheum1990; 33: 1611–1619.
35.
SeidemanP. Chloroquine reduces the bioavailability of methotrexate in patients with rheumatoid arthritis. A possible mechanism of reduced hepatotoxicity.Arthritis Rheum1994; 37(6): 830–833.
36.
PetriM, BakerC, GoldmanD.Liver function test (LFT) abnormalities in systemic lupus erythematosus (SLE) (Abstract).Arthritis Rheum1992; 35: S239.
37.
LoudonJR.Hydroxychloroquine and postoperative thromboembolism after total hip replacement.Am J Med1988; 85(Suppl. 4A): 57–61.
38.
JohnsonR, LoudonJR.Hydroxychloroquine sulfate prophylaxis for pulmonary embolism for patients with low-friction arthroplasty.Clin Orthop1986; 211: 151–153.
39.
JohnsonR, CharnleyJ.Hydroxychloroquine in prophylaxis of pulmonary embolism following hip arthroplasty.Clin Orthoped1979; 144: 174–177.
40.
CarterAE, EbanR, PerrettRD.Prevention of post-operative deep venous thrombosis and pulmonary embolism.Br Med J1971; 1: 312–314.
41.
CarterAE, EbanR.Prevention of postoperative deep venous thrombosis in legs by orally administered hydroxychloroquine sulfate.Br Med J1974; 3: 94–95.
42.
PilcherDB.Hydroxychloroquine sulfate in prevention of thromboembolic phenomena in surgical patients.Am Surgeon1975; 41: 761–766.
43.
HansenEH. Hydroxychloroquine sulphate in prevention of deep venous thrombosis following fracture of the hip, pelvis or thoracolumbar spine.J Bone Jt Surg1976; 58A: 1089–1093.
44.
ChrismanDO, SnookGA, WilsonTC, ShortJY.Prevention of venous thromboembolism by administration of hydroxychloroquine.J Bone Jt Surg1976; 58A: 918–920.
45.
CookED. Failure of orally administered hydroxychloroquine sulphate to prevent venous thromboembolism following elective hip operations.J Bone Jt Surg1977; 59A: 496–500.
46.
JohanssonE, ForsbergK, JohnssonH.Clinical and experimental evaluation of the thromboprophylactic effect of hydroxychloroquine sulfate after total hip replacement.Haemostasis1981; 10: 89–96.
47.
WuTK, TsapogasMJ, JordanFR.Prophylaxis of deep venous thrombosis by hydroxychloroquine sulfate and heparin.Surg Gynecol Obstet1977; 145: 714–718.
48.
WinocourPD, Kinlough-RathboneRL, MustardJF.The effect of the phospholipase inhibitor mepacrine on platelet aggregation, the platelet release reaction and fibrinogen binding to the platelet surface.Thrombosis Haemostasis1981; 45: 257–262.
49.
SeuterF.Inhibition of platelet aggregation by acetylsalicylic acid and other inhibitors.Haemostatis1976; 5: 85–95.
50.
RosenbergFJ. Acetylsalicylic acid: inhibition of platelet aggregation in the rabbit.J Pharm Exp Ther1971; 179: 410–418.
51.
MadowBP.Use of anti-malarial drugs as ‘desludging’ agents in vascular disease processes.JAMA1960; 172: 1630–1633.
CecchiE, FerrarisD.Desludging action of hydroxychloroquine in rheumatoid arthritis.Acta Rheumatol Scand1962; 8: 214–221.
54.
ErnstE, RoseM, LeeR.Modification of trans-operative changes in blood fluidity by hydroxychloroquine. A possible explanation for the drugs anti-thrombotic effect.Pharmatherapeutica1984; 4: 48–52.
55.
BirdHA, HarknessJ, WrightV.Some rheological properties of blood during anti-rheumatoid therapy.Pharmatherapeutica1981; 3: 36–39.
56.
RosenbergFJ, PhillipsPG, DruzbaPG.Platelets and thrombosis. Use of a rabbit extracarporeal shunt in the assay of antithrombotic and thrombotic drugs. Baltimore: University Park Press1974: 233–234.
Canadian Hydroxychloroquine Study Group.A randomized study of the effect of withdrawing hydroxychloroquine sulfate in systemic lupus erythematosus.N Engl J Med1991; 324: 150–154.
59.
KruizeAA. Hydroxychloroquine treatment for primary Sjogren's syndrome: a two year double blind crossover trial.Ann Rheum Dis1993; 52(5): 360–364.
