TY - JOUR
T1 - Antimalarial primaquine for spinal sensory and motor blockade in rats
AU - Chou, An Kuo
AU - Chiu, Chong Chi
AU - Wang, Jhi Joung
AU - Chen, Yu Wen
AU - Hung, Ching Hsia
N1 - Funding Information:
This research grant (CMU108-MF-56) was supported by China Medical University, Taiwan.
Publisher Copyright:
© The Author(s) 2021. Published by Oxford University Press on behalf of the Royal Pharmaceutical Society. All rights reserved.
PY - 2021/11/1
Y1 - 2021/11/1
N2 - Objectives The purpose of the experiment was to estimate whether intrathecal antimalarial drugs could provoke spinal block, and their comparison with lidocaine. Methods 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. Key findings 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). Conclusions 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.
AB - Objectives The purpose of the experiment was to estimate whether intrathecal antimalarial drugs could provoke spinal block, and their comparison with lidocaine. Methods 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. Key findings 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). Conclusions 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.
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U2 - 10.1093/jpp/rgab054
DO - 10.1093/jpp/rgab054
M3 - Article
C2 - 34370863
AN - SCOPUS:85118283451
SN - 0022-3573
VL - 73
SP - 1513
EP - 1519
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
IS - 11
ER -