Tetrodotoxin-bupivacaine-epinephrine combinations for prolonged local anesthesia.
Tetrodotoxin-bupivacaine-epinephrine combinations for prolonged local anesthesia.
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DOI：
10.3390/md9122717
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发表时间：
2011-12
期刊：
影响因子：
5.4
通讯作者：
Bognet C
中科院分区：
文献类型：
--
作者：
Berde CB;Athiraman U;Yahalom B;Zurakowski D;Corfas G;Bognet C
目前可用的局部麻醉剂在人体中的镇痛持续时间通常小于12小时。持续时间较长的局麻药将有助于术后镇痛。先前的研究表明，在大鼠中，河豚毒素（TTX）与布比卡因的组合对坐骨神经阻滞持续时间具有超累加效应。在这些研究中，肾上腺素联合TTX延长阻滞时间超过10倍，同时降低全身毒性。TTX，配制成Tectin，作为慢性癌症疼痛的注射全身镇痛药，正在进行III期临床试验。在这里，我们检查了大鼠局部神经阻滞后的剂量-持续时间关系和坐骨神经组织学，其中Tectin与0.25%（2.5 mg/mL）布比卡因溶液组合，有或没有肾上腺素5 µg/mL（1：200，000）。在Sprague-Dawley大鼠中进行经皮坐骨神经阻滞，并用不同的Tectin-布比卡因-肾上腺素组合盲法测试感觉阻滞的强度和持续时间。使用ANOVA和事后Sidak检验分析组间比较。对神经进行盲法检查，以确定是否有损伤迹象。含0.25%布比卡因和10 µM Tectin和5 µg/mL肾上腺素的阻滞时间比含0.25%布比卡因普通（P < 0.001）或含0.25%布比卡因和5 µg/mL肾上腺素（P < 0.001）的阻滞时间延长约3倍。所有组的神经组织学均为良性。Tectin 0.25%布比卡因与肾上腺素5 µg/mL的组合似乎有望延长局部麻醉持续时间。
Currently available local anesthetics have analgesic durations in humans generally less than 12 hours. Prolonged-duration local anesthetics will be useful for postoperative analgesia. Previous studies showed that in rats, combinations of tetrodotoxin (TTX) with bupivacaine had supra-additive effects on sciatic block durations. In those studies, epinephrine combined with TTX prolonged blocks more than 10-fold, while reducing systemic toxicity. TTX, formulated as Tectin, is in phase III clinical trials as an injectable systemic analgesic for chronic cancer pain. Here, we examine dose-duration relationships and sciatic nerve histology following local nerve blocks with combinations of Tectin with bupivacaine 0.25% (2.5 mg/mL) solutions, with or without epinephrine 5 µg/mL (1:200,000) in rats. Percutaneous sciatic blockade was performed in Sprague-Dawley rats, and intensity and duration of sensory blockade was tested blindly with different Tectin-bupivacaine-epinephrine combinations. Between-group comparisons were analyzed using ANOVA and post-hoc Sidak tests. Nerves were examined blindly for signs of injury. Blocks containing bupivacaine 0.25% with Tectin 10 µM and epinephrine 5 µg/mL were prolonged by roughly 3-fold compared to blocks with bupivacaine 0.25% plain (P < 0.001) or bupivacaine 0.25% with epinephrine 5 µg/mL (P < 0.001). Nerve histology was benign for all groups. Combinations of Tectin in bupivacaine 0.25% with epinephrine 5 µg/mL appear promising for prolonged duration of local anesthesia.
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影响因子：
8.8
作者：
Kohane, DS;Yieh, J;Berde, CB
通讯作者：
Berde, CB
影响因子：
5.7
作者：
Fanelli, G;Casati, A;Torri, G
通讯作者：
Torri, G
DOI：
10.1111/j.2517-6161.1995.tb02031.x
发表时间：
1995-01-01
影响因子：
5.8
作者：
BENJAMINI, Y;HOCHBERG, Y
通讯作者：
HOCHBERG, Y
影响因子：
4.7
作者：
Hagen, Neil A.;du Souich, Patrick;Ngoc, Anh Ho
通讯作者：
Ngoc, Anh Ho
影响因子：
4.7
作者：
Hagen, Neil A.;Fisher, Kim M.;Ngoc, Anh Ho
通讯作者：
Ngoc, Anh Ho