TY - JOUR
T1 - Intrathecal pramoxine causes long-lasting spinal sensory and motor block in rats
AU - Chou, An Kuo
AU - Chiu, Chong Chi
AU - Han, Ming Ming
AU - Chen, Yu Wen
AU - Wang, Jhi Joung
AU - Hung, Ching Hsia
N1 - Funding Information:
The authors gratefully acknowledge the financial support provided by the grant (MOST 104-2314-B-039-017-MY3) from the Ministry of Science and Technology in Taiwan.
Publisher Copyright:
© 2018 Royal Pharmaceutical Society
PY - 2018/4
Y1 - 2018/4
N2 - Objectives: The objective of this experiment was to investigate spinal anaesthetic effects of pramoxine and its comparison with bupivacaine, a long-lasting local anaesthetic. Methods: After intrathecal injection, three neurobehavioural assessments, which consisted of nociceptive, proprioceptive and motor block, were constructed in rats. The effects of bupivacaine and pramoxine (four doses of each drug) in a dose-related manner were conducted to obtain the ED50 (50% effective dose). Pramoxine potency and duration at provoking spinal nociceptive, proprioceptive and motor block were compared with those of bupivacaine. Key findings: We manifested that pramoxine provoked dose-relatedly spinal blockades of nociception, proprioception and motor function. Based on the ED50, the rank potency at producing spinal nociceptive, proprioceptive and motor block was bupivacaine (0.90 (0.82–1.02), 1.00 (0.92–1.08) and 1.16 (1.02–1.34) μmol/kg) greater (P < 0.01 for the differences) than pramoxine (15.47 (14.04–17.05), 16.46 (15.06–17.99), and 17.77 (16.48–19.15) μmol/kg). The spinal block duration created by bupivacaine was not predominantly different (P > 0.05 for the differences) from that created by pramoxine at the equipotent doses (ED75, ED50 and ED25). Conclusions: Our preclinical experiment indicated that pramoxine elicited a dose-related spinal block, was less potent than bupivacaine and had a similar duration of spinal block compared with bupivacaine.
AB - Objectives: The objective of this experiment was to investigate spinal anaesthetic effects of pramoxine and its comparison with bupivacaine, a long-lasting local anaesthetic. Methods: After intrathecal injection, three neurobehavioural assessments, which consisted of nociceptive, proprioceptive and motor block, were constructed in rats. The effects of bupivacaine and pramoxine (four doses of each drug) in a dose-related manner were conducted to obtain the ED50 (50% effective dose). Pramoxine potency and duration at provoking spinal nociceptive, proprioceptive and motor block were compared with those of bupivacaine. Key findings: We manifested that pramoxine provoked dose-relatedly spinal blockades of nociception, proprioception and motor function. Based on the ED50, the rank potency at producing spinal nociceptive, proprioceptive and motor block was bupivacaine (0.90 (0.82–1.02), 1.00 (0.92–1.08) and 1.16 (1.02–1.34) μmol/kg) greater (P < 0.01 for the differences) than pramoxine (15.47 (14.04–17.05), 16.46 (15.06–17.99), and 17.77 (16.48–19.15) μmol/kg). The spinal block duration created by bupivacaine was not predominantly different (P > 0.05 for the differences) from that created by pramoxine at the equipotent doses (ED75, ED50 and ED25). Conclusions: Our preclinical experiment indicated that pramoxine elicited a dose-related spinal block, was less potent than bupivacaine and had a similar duration of spinal block compared with bupivacaine.
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U2 - 10.1111/jphp.12894
DO - 10.1111/jphp.12894
M3 - Article
C2 - 29441574
AN - SCOPUS:85042086700
SN - 0022-3573
VL - 70
SP - 543
EP - 549
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
IS - 4
ER -