Amitriptyline for prolonged cutaneous analgesia in the rat
Amitriptyline for prolonged cutaneous analgesia in the rat
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DOI：
10.1097/00000542-200201000-00023
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发表时间：
2002-01-01
期刊：
影响因子：
8.8
通讯作者：
Wang, GK
中科院分区：
文献类型：
--
作者：
Khan, MA;Gerner, P;Wang, GK
背景：据报道，阿米替林是比布比卡因更有效的局部麻醉剂。为了与确定长期皮肤镇痛药物的目标保持一致，作者比较了阿米替林和布比卡因对大鼠的皮肤镇痛效果。方法：对大鼠剃毛的背部皮肤进行皮下注射。注射0.6ml不同浓度的阿米替林或布比卡因（含或不含肾上腺素）（1:200,000）后，对皮肤上的小麦进行标记。通过与对照反应相比，对标记区域施加总共六次针刺未能引起伤害性运动反应的次数分数来定量评估对皮肤干肌反射的抑制。六次针刺无反应被定义为 100% 最大可能效果。结果：0.05% 和 0.5 阿米替林与 0.05 和 0.5% 布比卡因引起的皮肤镇痛完全恢复分别发生在 9.9+/-0.2 和 19.3+/-0.4 小时以及 2.2+/-0.1 和 16.1+/-0.2 小时。 （平均值+/-SE）。添加肾上腺素使该持续时间分别增加至 14.1+/-0.1 和 21.4+/-0.2 小时，而 3.2+/-0.1 和 17.0+/-0.3 小时。共注射 0.25% 阿米替林、0.25% 布比卡因和肾上腺素后，完全伤害性阻断持续 24+/-0.5 小时，完全恢复需要 33+/-0.5 小时。对于 0.5% 阿米替林和布比卡因与肾上腺素，最大可能效果百分比与时间曲线下的面积分别为 1,770+/-24 和 1,471+/-50% h，而对于共同注射的 0.25% 阿米替林、0.25% 布比卡因和肾上腺素，该值为 2,836+/-62% h 结论：与布比卡因相比，阿米替林是一种长效的皮肤浸润局部麻醉药。肾上腺素可显着增强其镇痛效果。阿米替林和布比卡因与肾上腺素联合注射可延长两种药物的镇痛持续时间。
Background: Amitriptyline has been reported to be a more potent local anesthetic than bupivacaine. in keeping with the objective of identifying drugs for prolonged cutaneous analgesia, the authors compared the cutaneous analgesic effectiveness of amitriptyline and bupivacaine in rats.Methods: Rats were subcutaneously injected on shaved dorsal skin. The skin wheat raised after injection of 0.6 ml of various concentrations of either amitriptyline or bupivacaine with and without epinephrine (1:200,000) was marked. Inhibition of the cutaneous trunci muscle reflex was evaluated quantitatively by the fraction of times a total of six pinpricks applied to the marked area failed to elicit a nocifensive motor response compared with control responses. No responses out of six pinpricks was defined as 100% maximum possible effect.Results: Complete recovery from the cutaneous analgesia elicited by 0.05% and 0.5 amitriptyline versus 0.05 and 0.5% bupivacaine occurred in 9.9+/-0.2 and 19.3+/-0.4 h versus 2.2+/-0.1 and 16.1+/-0.2 h, respectively (mean+/-SE). Addition of epinephrine Increased this duration to 14.1+/-0.1 and 21.4+/-0.2 h versus 3.2+/-0.1 and 17.0+/-0.3 h, respectively. Complete nociceptive blockade after coinjection of 0.25% amitriptyline, 0.25% bupivacaine, and epinephrine lasted 24+/-0.5 h, and complete recovery from this block took 33+/-0.5 h. Areas under the percent maximum possible effect versus time curve were 1,770+/-24 and 1,471+/-50% h for 0.5% amitriptyline and bupivacaine with epinephrine, respectively, whereas this value was 2,836+/-62% h for the coinjected 0.25% amitriptyline, 0.25% bupivacaine, and epinephrine admixture.Conclusion: Amitriptyline is a longer-acting local anesthetic compared with bupivacaine for cutaneous infiltration. Its analgesic effectiveness is significantly enhanced by epinephrine. Coinjection of amitriptyline and bupivacaine with epinephrine enhances the analgesic duration of both drugs.