Aix Marseille Université, Marseille, France.
Rheumatol Int. 2021 Jul;41(7):1189-1202. doi: 10.1007/s00296-021-04868-6. Epub 2021 Apr 24.
Chloroquine (CQ) and its hydroxylated analog, hydroxychloroquine (HCQ), are 4-aminoquinoline initially used as an antimalarial treatment. CQ and HCQ (4-aminoquinoline, 4-AQ) are today used in rheumatology, especially to treat rheumatoid arthritis and systemic lupus erythematosus. Their mechanism of action revolves around a singular triptych: 4-AQ acts as alkalizing agents, ionized amphiphilic molecules, and by binding to numerous targets. 4-AQ have so pleiotropic and original mechanisms of action, providing them an effect at the heart of the regulation of several physiological functions. However, this broad spectrum of action is also at the origin of various and original side effects, notably a remarkable chronic systemic toxicity. We describe here the 4-AQ-induced lesions on the eye, the heart, muscle, the nerves, the inner ear, and the kidney. We also describe their prevalence, their pathophysiological mechanisms, their risk factors, their potential severity, and the means to detect them early. Most of these side effects are reversible if treatment is stopped promptly. This 4-AQ-induced toxicity must be known to prescribing physicians, to closely monitor its appearance and stop treatment in time if necessary.
氯喹（CQ）及其羟化类似物羟氯喹（HCQ）最初是作为抗疟药物使用的 4-氨基喹啉。CQ 和 HCQ（4-氨基喹啉，4-AQ）如今在风湿病学中使用，特别是用于治疗类风湿关节炎和系统性红斑狼疮。它们的作用机制围绕着一个独特的三联体：4-AQ 作为碱化剂、离子化两亲分子，并与许多靶标结合。4-AQ 的作用机制如此多样且独特，为其提供了对多种生理功能调节的作用。然而，这种广泛的作用机制也是各种独特副作用的根源，尤其是显著的慢性全身毒性。我们在这里描述了 4-AQ 引起的眼部、心脏、肌肉、神经、内耳和肾脏损伤。我们还描述了它们的流行程度、病理生理机制、危险因素、潜在严重程度以及早期检测它们的方法。如果及时停止治疗，大多数这些副作用都是可逆的。开具处方的医生必须了解这种 4-AQ 诱导的毒性，密切监测其出现情况，并在必要时及时停止治疗。
