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布比卡因、依替卡因、利多卡因和罗哌卡因在正庚烷、大鼠坐骨神经以及人体硬膜外和皮下脂肪中的吸收情况。

Absorption of bupivacaine, etidocaine, lignocaine and ropivacaine into n-heptane, rat sciatic nerve, and human extradural and subcutaneous fat.

作者信息

Rosenberg P H, Kyttä J, Alila A

出版信息

Br J Anaesth. 1986 Mar;58(3):310-4. doi: 10.1093/bja/58.3.310.

Abstract

Absorption of four amide local anaesthetics, including a new experimental agent, ropivacaine, in n-heptane, rat sciatic nerve and human extradural and subcutaneous fat was studied in vitro. The relative n-heptane/buffer (37 degrees C) partitioning of bupivacaine:etidocaine:lignocaine:ropivacaine was 10:39:1:2.9. The absorption of bupivacaine and etidocaine into nerve tissue was identified at steady state, but in extradural and subcutaneous fat etidocaine was taken up significantly more than bupivacaine. The lowest uptake was with lignocaine, and at steady state its mean concentrations were similar in all three tissues. There was a significantly higher concentration of ropivacaine than lignocaine in all tissues. Mean tissue concentrations of bupivacaine in sciatic nerve and subcutaneous fat, on the other hand, were significantly higher than those of ropivacaine. The ratios of relative mean uptake (mg g-1), at steady state, of bupivacaine, etidocaine, lignocaine and ropivacaine were: sciatic nerve 3.3:4:1:1.8, extradural fat 4.1:8.3:1:2.3 and subcutaneous fat 3.8:10.6:1:1.9, all of which were clearly lower than the theoretical n-heptane/buffer partitioning ratios.

摘要

在体外研究了四种酰胺类局部麻醉药,包括一种新的实验药物罗哌卡因,在正庚烷、大鼠坐骨神经以及人体硬膜外和皮下脂肪中的吸收情况。布比卡因:依替卡因:利多卡因:罗哌卡因在正庚烷/缓冲液(37℃)中的相对分配系数为10:39:1:2.9。在稳态时可确定布比卡因和依替卡因向神经组织中的吸收,但在硬膜外和皮下脂肪中,依替卡因的摄取量明显多于布比卡因。利多卡因的摄取量最低,在稳态时其在所有三种组织中的平均浓度相似。在所有组织中,罗哌卡因的浓度均显著高于利多卡因。另一方面,坐骨神经和皮下脂肪中布比卡因的平均组织浓度显著高于罗哌卡因。在稳态时,布比卡因、依替卡因、利多卡因和罗哌卡因的相对平均摄取量(mg g-1)之比为:坐骨神经3.3:4:1:1.8,硬膜外脂肪4.1:8.3:1:2.3,皮下脂肪3.8:10.6:1:1.9,所有这些均明显低于理论上的正庚烷/缓冲液分配系数。

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