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hydroxychloroquine : ウィキペディア英語版
hydroxychloroquine

Hydroxychloroquine is an antimalarial drug, sold under the trade names ''Plaquenil'', ''Axemal'' (in India), ''Dolquine'' and ''Quensyl'', also used to reduce inflammation in the treatment of rheumatoid arthritis (see disease-modifying antirheumatic drugs) and lupus. Hydroxychloroquine differs from chloroquine by the presence of a hydroxyl group at the end of the side chain: The N-ethyl substituent is beta-hydroxylated. It is available for
oral administration as hydroxychloroquine sulfate (plaquenil) of which 200 mg contains 155 mg base
in chiral form. Hydroxychloroquine has similar pharmacokinetics to chloroquine, with quick gastrointestinal absorption and elimination by the kidney. Cytochrome P450 enzymes (CYP 2D6, 2C8, 3A4 and 3A5) metabolize hydroxychloroquine to N-desethylhydroxychloroquine.

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.
==Medical use==
Hydroxychloroquine has been used for many years to treat malaria. It is also used to treat systemic lupus erythematosus, rheumatic disorders like rheumatoid arthritis and Sjögren's syndrome, and porphyria cutanea tarda. Its efficacy to treat Sjögren's syndrome has recently been called into question in a double-blind study involving 120 patients over a 48 week period.〔 Effects of Hydroxychloroquine on Symptomatic Improvement in Primary Sjögren Syndrome, Gottenberg, et al. (2014) http://jama.jamanetwork.com/article.aspx?articleID=1887760〕 Hydroxychloroquine increases lysosomal pH in antigen presenting cells. In inflammatory conditions, it blocks toll-like receptors on plasmacytoid dendritic cells (PDCs). Toll-like receptor 9 (TLR 9), which recognizes DNA-containing immune complexes, leads to the production of interferon and causes the dendritic cells to mature and present antigen to T cells. Hydroxychloroquine, by decreasing TLR signaling, reduces the activation of dendritic cells and the inflammatory process.
Hydroxychloroquine is also widely used in the treatment of post-Lyme arthritis following Lyme disease. It may have both an anti-spirochaete activity and an anti-inflammatory activity, similar to the treatment of rheumatoid arthritis.
Anti-diabetic activity of hydroxychloroquine has been demonstrated in a recently conducted systematic, randomized, active-controlled, multicentric study in type 2 diabetes patients uncontrolled on sulfonylurea and metformin combination. These patients were randomized to additionally receive either hydroxychloroquine or pioglitazone tablets. After 6 months of treatment, reduction in HbA1c and blood glucose was comparable between 2 treatment groups. Besides, patients treated with hydroxychloroquine showed a significant reduction in total cholesterol, triglycerides and LDL levels.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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