Chou An-Kuo, Chiu Chong-Chi, Wang Jhi-Joung, Chen Yu-Wen, Hung Ching-Hsia
Department of Anesthesiology, China Medical University Hospital, Taichung, Taiwan.
School of Medicine, College of Medicine, China Medical University, Taichung, Taiwan.
J Pharm Pharmacol. 2021 Oct 7;73(11):1513-1519. doi: 10.1093/jpp/rgab054.
The purpose of the experiment was to estimate whether intrathecal antimalarial drugs could provoke spinal block, and their comparison with lidocaine.
Rats were intrathecally administrated with antimalarial agents (primaquine, chloroquine, hydroxychloroquine and amodiaquine) and lidocaine, and neurobehavioural examinations (nociception, proprioception and motor function) were assessed; n = 8 per group. One-way and two-way analysis of variance were designed to analyse data.
At a concentration of 20 mM, primaquine (0.46 mg/rat) exhibited the longest duration and the most potent effect of nociceptive, proprioceptive and motor blockade (P < 0.01) among five drugs, whereas the other antimalarial drugs displayed a lesser or similar potency of spinal blockade compared with lidocaine (0.29 mg/rat). In dose-dependent studies, primaquine was more potent (P < 0.01) than lidocaine for spinal block. At ED25, ED50 and ED75 equipotent doses, primaquine produced a greater duration of spinal motor, proprioceptive and nociceptive blockade when compared with lidocaine (P < 0.01).
Primaquine, chloroquine, hydroxychloroquine and amodiaquine produced spinal blockade. Primaquine was more potent and displayed a prolonged life of local anaesthetic effect compared with lidocaine, whereas the other antimalarial drugs displayed a lesser or similar potency compared with lidocaine.
本实验旨在评估鞘内注射抗疟药物是否会引发脊髓阻滞，并将其与利多卡因进行比较。
给大鼠鞘内注射抗疟药物（伯氨喹、氯喹、羟氯喹和阿莫地喹）及利多卡因，评估神经行为学检查（痛觉、本体感觉和运动功能）；每组n = 8只。采用单向和双向方差分析设计来分析数据。
在浓度为20 mM时，伯氨喹（0.46 mg/只大鼠）在五种药物中表现出最长的持续时间以及最强的痛觉、本体感觉和运动阻滞作用（P < 0.01），而其他抗疟药物与利多卡因（0.29 mg/只大鼠）相比，脊髓阻滞作用较弱或相似。在剂量依赖性研究中，伯氨喹对脊髓阻滞的作用比利多卡因更强（P < 0.01）。在ED25、ED50和ED75等效剂量下，与利多卡因相比，伯氨喹产生的脊髓运动、本体感觉和痛觉阻滞持续时间更长（P < 0.01）。
伯氨喹、氯喹、羟氯喹和阿莫地喹可产生脊髓阻滞。与利多卡因相比，伯氨喹作用更强且局部麻醉效果持续时间更长，而其他抗疟药物与利多卡因相比作用较弱或相似。
