Table 4.
The anti-hyperlipidaemic effects of CQ and HCQ in human studies
| Study population | Treatment, dose and duration | Research outcomes | Mechanism of action | Reference |
|---|---|---|---|---|
| Patients with T2DM (n=10; aged 43-61 years) | CQ (250 mg, four times daily, 3 days) | TC: ↓, LDL-C: ↓, apoB: ↓, apoB/apoA-1 ratio: ↓, NEFA: ↔ | - | 37 |
| Patients with T2DM (n=135; aged 18-65 years) | HCQ (400 mg/day, 24 weeks) | TC: ↓, TG: ↓, LDL-C: ↓, HDL-C: ↔ | - | 39 |
| Sulfonylurea-refractory patients with poorly controlled T2DM (n=69; aged 35-80 years) | HCQ (300 mg/day, 6 months) | LDL-C: ↓ | - | 40 |
| Patients with T2DM failing metformin and sulfonylurea (n=15; aged 18-75 years) | HCQ (400 mg/day, 4 months) | TC: ↓, non-HDL-C: ↓, TG: ↔, LDL-C: ↔, HDL-C: ↔ | - | 41 |
| Patients with primary dyslipidaemia (n=127; aged 49.21 ± 9.58 years) | HCQ (200 mg/day) + atorvastatin (10 mg/day), 24 weeks | TC: ↓, TG: ↓, LDL-C: ↓, non-HDL-C: ↓, HDL-C: ↔ | hs-CRP: ↓ | 44 |
| Patients with MetS (n=25; aged 18-60 years) | Placebo (3 weeks) → CQ (80 mg/week, 3 weeks) → CQ (80 mg/day, 3 weeks) → CQ (250 mg/day, 3 weeks) | TC: ↓, non-HDL-C: ↓, LDL-C: ↓, TG: ↔, HDL-C: ↔, NEFA: ↔ | TNF-α: ↓, CRP: ↔, leptin: ↔, adiponectin: ↔ | 45 |
| Patients with MetS (n=56; aged 18-70 years) | CQ (80 mg/day, 1 year) | TC; ↓, non-HDL-C: ↓, LDL-C: ↓ | p-JNK: ↓ | |
| Obese, non-diabetic subjects (n=13; aged 24-71 years) | HCQ (6.5 mg/kg/day, 6 weeks) | TC: ↔, TG: ↔, HDL-C: ↔, LDL-C: ↔ | CRP: ↔, IL-6: ↔ | 42 |
| Patients with SLE (n=51; aged ≥18 years) | HCQ (dose and duration not mentioned) | Dyslipidaemia: ↓ | - | 53 |
| Patients with SLE (n=24; aged 37.2 ± 16.0 years) | HCQ (200 mg/day) - 3 months | TC: ↓, LDL-C: ↓, frequency of dyslipidaemia: ↓ | - | 54 |
| Female patients with SLE (n=17) | HCQ (400 or 800 mg/day) - 3 months | TC: ↓, TG: ↓, VLDL-C: ↓, LDL-C: ↔, HDL-C: ↔, non-HDL-C: ↓, TC/HDL-C ratio: ↓, LDL-C/HDL-C ratio: ↓ | - | 55 |
| Patients with SLE (n=34; aged 48.7 ± 13.3 years) | HCQ (standard dose) | TC: ↔, HDL-C: ↔ | - | 56 |
| Chinese patients with mild or inactive SLE (n=44; aged 38.9 ± 7.9 years) | HCQ (244 ± 86 mg/day, duration not mentioned) | TG: ↔, TC: ↔, HDL-C: ↔, LDL-C: ↔ | apoA-1: ↔, apoB: ↔, lipoprotein A: ↔ | 57 |
| Patients with rheumatoid arthritis without diabetes (n= 23; aged 56 ± 11.4 years) | HCQ (6.5 mg/kg/day, 8 weeks) | TC: ↓, LDL-C: ↓, TG: ↔, HDL-C: ↔ | - | 48 |
| Male and female patients with rheumatoid arthritis (n=150; aged 65.8 ± 10.0 years) | HCQ (dose not mentioned, >3 months) | TG: ↓, TC: ↓, LDL-C: ↓, HDL-C: ↔, HDL-C/LDL-C: ↑, TC/HDL-C: ↓ | - | 58 |
| Patients with rheumatoid arthritis (n=256; aged 54-72 years) | HCQ (6.5 mg/kg/day, median exposure time: 1.98 years) | TG: ↓, TC: ↓, LDL-C: ↓, HDL-C: ↑, LDL-C/HDL-C: ↓, TC/HDL-C: ↓ | - | 59 |
| Patients with rheumatoid arthritis (n=254; aged 57.2 ± 11.1 years) | HCQ (dose and duration not mentioned) | TG: ↓, TC: ↓, LDL-C: ↓, HDL-C: ↑, TC/HDL-C: ↓, LDL-C/HDL-C: ↓ | - | 60 |
| Patients with early rheumatoid arthritis (n=6130; aged 45.45 ± 12.12 years) | HCQ (dose and duration not mentioned) | TC: ↓, LDL-C: ↓, HDL-C: ↑ | - | 61 |
| Patients with early rheumatoid arthritis (n=119; aged 48.66 ± 11.98 years) | Methotrexate + sulfasalazine + HCQ - 24, 48 and 102 weeks | TC: ↓, LDL-C: ↓, HDL-C: ↑ | - | 62 |
| Patients with early rheumatoid arthritis (n=103; aged 49.3 ± 12.5 years) | Methotrexate + sulfasalazine + HCQ - 24, 48 and 102 weeks | - | PON-1 activity: ↑, apoA-1: ↑, HDL inflammatory index: ↓, MPO: ↓ | 73 |
| Patients with SLE or rheumatoid arthritis (n=26; aged 46 ± 16 years) | HCQ (mean daily dose: 284.6 ± 67.5 mg, 5 - 6 months) | TG: ↓, HDL-C: ↔, LDL-C: ↓, non-HDL-C: ↓ | - | 47 |
| Female patients with Sjögren syndrome (n=71; aged >18 years) | HCQ | TC: ↓, HDL-C: ↑, atherogenic index: ↓ | - | 64 |
Abbreviations: apoA-1, apolipoprotein A-1; apoB, apolipoprotein B; CQ, chloroquine; CRP, C-reactive protein; HCQ, hydroxychloroquine; HDL-C, high-density lipoprotein cholesterol; hs-CRP, high sensitivity C-reactive protein; IL-6, interleukin-6; LDL-C, low-density lipoprotein cholesterol; MetS, metabolic syndrome; MPO, myeloperoxidase; NEFA, non-esterified fatty acids; p-JNK, phosphorylated c-Jun N-terminal kinase; PON-1, paraoxonase 1; SBP, systolic blood pressure; SLE, systemic lupus erythematosus; TC, total cholesterol; TG, triglyceride; TNF-α, tumour necrosis factor-alpha; T2DM, type 2 diabetes mellitus; VLDL-C, very low-density lipoprotein cholesterol; ↑, increase/stimulate; ↓, decrease/inhibit; ↔, no change.