Ochsendorf F R, Runne U
Zentrum der Dermatologie und Venerologie, J.W. Goethe-Universität, Frankfurt/M.
Hautarzt. 1991 Mar;42(3):140-6.
Precise knowledge of the undesirable effects of chloroquine and hydroxychloroquine allows better exploitation of their therapeutic effects. Retinopathy can be avoided by observing a maximum daily dosage of 3.5-4 mg/kg ideal body weight for chloroquine and 6-6.5 mg/kg for hydroxychloroquine. In this way, both can be used for long-term therapy. The pharmacokinetics of chloroquine (storage in deep compartments with long plasma half-life) means that it can cumulate, especially with higher dosages and in the presence of renal or hepatic insufficiency. A high plasma concentration reinforces the side-effects without reinforcing the therapeutic effects. Besides subjective symptoms (e.g. anorexia, diarrhoea, nausea), the following undesirable reactions are significant. On the skin exanthema, hyperpigmentation and photodynamic reactions can develop. The hair can become white in blonde and red-haired men. In the eye, chloroquine deposits in the cornea and disturbances of accommodation can occur, besides retinopathy. Neuromyopathy and central nervous system disturbances (e.g. psychosis) are rare, as is impairment of auditory function or blood cells. During pregnancy there is a risk of potential fetal damage (hearing loss, abortion). An acute overdose is extremely dangerous: the lethal dose is 1 g for children and 4 g for adults. As death occurs rapidly, chloroquine has to be stored where it is absolutely inaccessible to children.
准确了解氯喹和羟氯喹的不良反应有助于更好地发挥它们的治疗作用。通过观察氯喹每日最大剂量为理想体重3.5 - 4毫克/千克，羟氯喹为6 - 6.5毫克/千克，可避免视网膜病变。这样，两者都可用于长期治疗。氯喹的药代动力学（储存在深部隔室，血浆半衰期长）意味着它会蓄积，尤其是在剂量较高以及存在肾或肝功能不全时。高血浆浓度会增强副作用，但不会增强治疗效果。除了主观症状（如厌食、腹泻、恶心）外，以下不良反应较为显著。在皮肤上可出现皮疹、色素沉着和光动力反应。金发和红发男性的头发可能变白。在眼部，除视网膜病变外，氯喹还可沉积在角膜并出现调节障碍。神经肌肉病变和中枢神经系统紊乱（如精神病）较为罕见，听觉功能或血细胞受损也很少见。怀孕期间存在潜在胎儿损伤（听力丧失、流产）的风险。急性过量极其危险：儿童致死剂量为1克，成人为4克。由于死亡迅速发生，氯喹必须储存在儿童绝对无法触及的地方。
