Hydroxychloroquine

Information about Hydroxychloroquine

Hydroxychloroquine is a derivative of chloroquine that has both antimalarial and antiinflammatory activities and is now most often used as an antirheumatologic agent in systemic lupus erythematosis and rheumatoid arthritis.

Liver safety of Hydroxychloroquine

Hydroxychloroquine therapy has not been associated with liver function abnormalities and is an extremely rare cause of clinically apparent acute liver injury.

Mechanism of action of Hydroxychloroquine

Hydroxychloroquine (hye drox" ee klor' oh kwin) is a hydroxylated derivative of chloroquine and has similar antimalarial activity but is less toxic, allowing for use in higher doses for longer periods. Originally used as an antimalarial agent, hydroxychloroquine was later found to have antiinflammatory activity. Its mechanism of action is not well known, but it is concentrated in lysosomes and appears to stabilize lysosomal membranes inhibiting phagocytosis and release of proinflammatory lysosomal enzymes and cytokines.

FDA approval information for Hydroxychloroquine

Hydroxychloroquine was approved for use in the United States in 1994, and indications were later broadened and now include rheumatoid and psoriatic arthritis, discoid and systemic lupus erythematosus and prevention and treatment of malaria. Hydroxychloroquine has also been used as therapy of porphyria cutanea tarda where it seems to act by increasing excretion of porphyrins.

Dosage and administration for Hydroxychloroquine

Hydroxychloroquine is available in generic forms and under the brand names of Plaquenil in tablets of 200 mg. The usual dose is 400 mg daily in one or two divided doses.

Side effects of Hydroxychloroquine

Common side effects include headaches, dizziness, gastrointestinal upset and rash. Retinopathy is a serious side effect of hydroxychloroquine and regular ophthalmologic monitoring is recommended for patients on long term therapy.

Antirheumatic Agents

• Gold Preparations

• • Auranofin, Gold salts, Gold sodium thiomalate

• Interleukin receptor antagonists

• • Anakinira, Canakinumab, Rilonacept, Sarilumab, Tocilizumab

• Major immunosuppressive agents

• • Cyclosporine, Mycophenylate, Sirolimus, Tacrolimus

• Monoclonal antibodies

• • Adalimumab, Canakinumab, Certolizumab, Golimumab, Infliximab, Rituximab, Sarilumab, Tocilizumab, Ustekinumab

• Thiopurines

• • Azathioprine, Mercaptopurine, Thioguanine

• Tumor necrosis factor antagonists

• • Adalimumab, Certolizumab, Etanercept, Golimumab, Infliximab

• Tyrosine kinase inhibitors

• • Baricitinib, Tofacitinib

• Miscellaneous

• • Abatacept, Flavocoxid, Hydroxychloroquine, Leflunomide, Methotrexate, Penicillamine

• Dailymed label info on Hydroxychloroquine
• FDA Hydroxychloroquine