Department of Anesthesiology, Chi Mei Medical Center, Tainan, Taiwan.
Department of Pharmacy, Chia Nan University of Pharmacy and Science, Tainan, Taiwan.
Neurosci Lett. 2020 Sep 14;735:135233. doi: 10.1016/j.neulet.2020.135233. Epub 2020 Jul 2.
The purpose of this study was to investigate the ability of chloroquine and chloroquine in combination with vasoconstrictor epinephrine to act as a local anesthetic in skin analgesia. After subcutaneous injection of drugs in rats, the inhibition of the cutaneous trunci muscle reflex (CTMR) is designed for evaluation of the cutaneous analgesic effect. The analgesic effect of chloroquine was compared with that of bupivacaine or coadministration of chloroquine and epinephrine. Chloroquine produced exactly the same local anesthesia as bupivacaine did in a dose-dependent manner. On the ED (50 % effective dose) basis, the analgesic potency was chloroquine (4.81 [4.45-5.20] μmol) < bupivacaine (0.46 [0.40‒0.52] μmol) (p < 0.01). At every equipotent dose tested (ED, ED and ED), chloroquine had a longer duration of cutaneous analgesia than bupivacaine (p < 0.01). Epinephrine enhanced the potency and duration of chloroquine-induced cutaneous analgesia. We found that chloroquine and bupivacaine elicit dose-dependent cutaneous analgesia. Chloroquine is not as potent as bupivacaine, but acts as an infiltrative anesthetic for a longer duration of time and is more potent and effective when used in combination with epinephrine.
本研究旨在探讨氯喹和氯喹联合血管收缩剂肾上腺素作为皮肤镇痛局部麻醉剂的能力。在大鼠皮下注射药物后，设计评估皮肤镇痛效果的皮肤横断肌反射（CTMR）抑制。将氯喹的镇痛效果与布比卡因或氯喹和肾上腺素联合用药进行比较。氯喹以剂量依赖性方式产生与布比卡因完全相同的局部麻醉作用。基于 ED（50%有效剂量），镇痛效力为氯喹（4.81[4.45-5.20]μmol）<布比卡因（0.46[0.40-0.52]μmol）（p<0.01）。在测试的每个等效剂量（ED、ED 和 ED）下，氯喹的皮肤镇痛持续时间均长于布比卡因（p<0.01）。肾上腺素增强了氯喹诱导的皮肤镇痛的效力和持续时间。我们发现氯喹和布比卡因引起剂量依赖性皮肤镇痛。氯喹的效力不如布比卡因，但作用时间更长，与肾上腺素联合使用时更有效。
