Hassan H G, Renck H, Lindberg B, Akerman B, Hellquist R
Acta Anaesthesiol Scand. 1985 May;29(4):375-9. doi: 10.1111/j.1399-6576.1985.tb02218.x.
Local anaesthetics of the amide type were studied in a modified rat infraorbital nerve block model, with which it was possible to determine varying degrees of sensory block. Of the agents investigated, 0.5% bupivacaine tended to give a longer duration of block than 2% prilocaine or 2% lidocaine, while 0.5% etidocaine had the shortest duration. The duration of prilocaine was prolonged by addition of adrenaline, 5 micrograms/ml, more than that of the other agents. Addition of dextrans of Mw 40-110 X 10(3) did not cause any prolongation of block induced by bupivacaine. When mixed with dextrans over a wide range of Mw (40-4900 X 10(3), prilocaine exhibited significant prolongations of its action by up to 200%. The extent of prolongation was dependent on the degree of block, the concentration of dextrans in the local anaesthetic solution, and the Mw of the dextran although in a less uniform way. An increase in the relative viscosity of the solutions might be a factor of importance for the prolonging effect of addition of dextran to local anaesthetics. Since a formulation providing analgesia of a long duration would be of clinical value, further studies on combinations of the comparatively low-toxicity agent prilocaine and macromolecular substances are of interest.
在改良的大鼠眶下神经阻滞模型中对酰胺类局部麻醉药进行了研究,利用该模型能够确定不同程度的感觉阻滞。在所研究的药物中,0.5%布比卡因产生的阻滞持续时间往往比2%丙胺卡因或2%利多卡因更长,而0.5%依替卡因的阻滞持续时间最短。加入5微克/毫升肾上腺素后,丙胺卡因的阻滞持续时间比其他药物延长得更多。加入分子量为40 - 110×10³的右旋糖酐不会导致布比卡因引起的阻滞时间延长。当与广泛分子量范围(40 - 4900×10³)的右旋糖酐混合时,丙胺卡因的作用时间显著延长,延长幅度高达200%。延长程度取决于阻滞程度、局部麻醉溶液中右旋糖酐的浓度以及右旋糖酐的分子量,尽管方式不太一致。溶液相对粘度的增加可能是右旋糖酐添加到局部麻醉药中产生延长作用的一个重要因素。由于提供长效镇痛的制剂具有临床价值,因此对低毒性药物丙胺卡因与大分子物质组合的进一步研究具有重要意义。