TY - JOUR
T1 - Antimalarial primaquine for skin infiltration analgesia in rats
AU - Chang, Ying Jen
AU - Liu, Kuo Sheng
AU - Wang, Jhi Joung
AU - Chen, Yu Wen
AU - Hung, Ching Hsia
N1 - Funding Information:
The authors gratefully acknowledge the financial support provided by the grant (CMNCKU10716) from Chi Mei Medical Center, Taiwan and the grant (CMU108-S-41) from China Medical University, Taiwan.
Publisher Copyright:
© 2021 The Author(s) 2021. Published by Oxford University Press on behalf of Royal Pharmaceutical Society. All rights reserved. For permissions, please e-mail: [email protected].
PY - 2021/2/1
Y1 - 2021/2/1
N2 - Objectives: The purpose of this study was to estimate the ability of antimalarial medications to induce local infiltration analgesia. Methods: Using a rat model of skin infiltration anaesthesia, the effects of antimalarial medications (primaquine, chloroquine, hydroxychloroquine and amodiaquine) were compared with the application of lidocaine. Key findings: At a dose of 3 μmol, primaquine and chloroquine displayed better potency (all P < 0.05) and greater duration (all P < 0.01) of cutaneous analgesia than lidocaine, whereas the other antimalarial medications showed a similar potency and duration of cutaneous analgesia when compared with lidocaine. When a dose of 3 μmol antimalarial medication was used, primaquine was the most potent and had the longest duration of action among four antimalarial medications. The relative potency ranking (ED50, 50% effective dose) has been found to be primaquine [2.10 (1.87-2.37) μmol] > lidocaine [6.27 (5.32-7.39) μmol] (P < 0.01). Infiltration analgesia of skin with primaquine had a greater duration of action than did lidocaine on the equipotent (ED25, ED50, ED75) basis (P < 0.01). Conclusions: Primaquine and chloroquine have greater potency and longer lasting skin analgesia when compared with lidocaine, while the other antimalarials display a similar potency in comparison with lidocaine.
AB - Objectives: The purpose of this study was to estimate the ability of antimalarial medications to induce local infiltration analgesia. Methods: Using a rat model of skin infiltration anaesthesia, the effects of antimalarial medications (primaquine, chloroquine, hydroxychloroquine and amodiaquine) were compared with the application of lidocaine. Key findings: At a dose of 3 μmol, primaquine and chloroquine displayed better potency (all P < 0.05) and greater duration (all P < 0.01) of cutaneous analgesia than lidocaine, whereas the other antimalarial medications showed a similar potency and duration of cutaneous analgesia when compared with lidocaine. When a dose of 3 μmol antimalarial medication was used, primaquine was the most potent and had the longest duration of action among four antimalarial medications. The relative potency ranking (ED50, 50% effective dose) has been found to be primaquine [2.10 (1.87-2.37) μmol] > lidocaine [6.27 (5.32-7.39) μmol] (P < 0.01). Infiltration analgesia of skin with primaquine had a greater duration of action than did lidocaine on the equipotent (ED25, ED50, ED75) basis (P < 0.01). Conclusions: Primaquine and chloroquine have greater potency and longer lasting skin analgesia when compared with lidocaine, while the other antimalarials display a similar potency in comparison with lidocaine.
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U2 - 10.1093/jpp/rgaa021
DO - 10.1093/jpp/rgaa021
M3 - Article
C2 - 33793809
AN - SCOPUS:85103807143
SN - 0022-3573
VL - 73
SP - 206
EP - 211
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
IS - 2
ER -