The presumable combined effects of hydroxychloroquine and its metabolites on the blood lipids and glucose in the treatment of rheumatoid arthritis.

OBJECTIVE

To explore the potential combined effects of hydroxycholoroquine (HCQ) and its metabolites on blood lipids and glucose in the treatment of rheumatoid arthritis (RA).

METHODS

In the HCQ group, the concentrations of HCQ and its metabolites, including desethylhydroxychloroquine (DHCQ), esethylchloroquine (DCQ) and bisdesethylchloroquine (BDCQ), were detected by high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). The relationships between the levels of blood lipid and glucose and concentrations of HCQ and its metabolites were also analysed. Further, a multiple regression model was employed to evaluate the actual roles of HCQ and its metabolites in various factors affecting blood lipids and glucose.

RESULTS

Significant higher high-density lipoprotein cholesterol (HDL) and lower low-density lipoprotein cholesterol (LDL) are found in the HCQ group than in the control group [1.63 ± 0.39 mmol/l vs. 1.39 ± 0.35 mmol/l, p < 0.001; 2.15 (1.80, 2.81) mmol/l vs. 2.54 (2.24, 3.10) mmol/l, p = 0.017, respectively]. Multivariate regression analysis indicates only HCQ concentration might act as an independent factor influencing the levels of HDL, VLDL, and TG in RA patients.

CONCLUSION

HCQ might increase HDL level and reduce LDL, VLDL, TC, and TG levels in RA treatment. These beneficial effects on modifying lipid profile might be counteracted to various degrees by some of its metabolites (DHCQ and BDCQ). Therefore, for RA patients with HCQ in their treatment regime, it might facilitate the improvement of lipids profile by promoting the excretion of HCQ metabolites. This study did not demonstrate the significant hypoglycemic effect of HCQ and its metabolites.