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Hydroxychloroquine

羥氯喹

Mechanism of action:

Hydroxychloroquine 是一種 4-胺基喹啉類（4-aminoquinoline）衍生物。Hydroxychloroquine 為弱鹼性分子，可在溶酶體（lysosome）與胞內體（endosome）中累積，提高其內部酸鹼值，進而抑制依賴酸性環境的酵素活性。這會使抗原胜肽的加工與 MHC class II 呈現效率下降，導致 T 細胞活化減弱；也可抑制 Toll-like receptors（TLR7、TLR9），減少干擾素與多種促發炎細胞激素的釋放，降低慢性發炎反應。Hydroxychloroquine 也被認為可在瘧原蟲食物液泡中干擾血基質（heme）解毒相關過程（包含影響血基質聚合/結晶化），導致有毒血基質累積，進而殺死躲在紅血球內部的瘧原蟲。

​Reference(s):

1. Lim HS et al. (2009). Pharmacokinetics of hydroxychloroquine and its clinical implications in chemoprophylaxis against malaria caused by Plasmodium vivax. Antimicrob Agents Chemother. 


2. Furst DE et al. (1996). Pharmacokinetics of hydroxychloroquine and chloroquine during treatment of rheumatic diseases. Lupus. 


3. Collins KP et al. (2018). Hydroxychloroquine: a physiologically-based pharmacokinetic model in the context of cancer-related autophagy modulation. J Pharmacol Exp Ther.

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