Xylocain(利多卡因,利多卡因),它的发现和Gordh对其临床应用的贡献。

M H Holmdahl
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引用次数: 44

摘要

欧拉(Hans v. Euler)在研究大麦某些氯基缺陷突变体中基因和酶的化学关系时,分离出了一种吲哚——谷氨酰胺。厄德特曼合成了异葛胺,发现它有微弱的麻醉性质。随后他与Löfgren合成了其他氨基酰胺,但没有一种能与现有的酯类局部麻醉剂,对氨基苯甲酸的衍生物,如普鲁卡因竞争。后来Löfgren和Lundqvist跟进了这些研究,发现了一种中间化合物利多卡因(2-二甲氨基乙酰- 2,6 -二甲醚)。在T. Gordh进行的临床试验中,利多卡因比普鲁卡因表现出如此显著的进步,因此利多卡因被引入临床使用。半个世纪以来,它一直是标准的局部麻醉药物。所有的局部麻醉剂在足够大的剂量下都是神经毒性的。然而,Xylocain有着良好的安全记录。仅在最近几年才有关于木locain用于脊髓麻醉可能引起毒性刺激和损伤的报道。病因尚不清楚。本文讨论了Gordh及其同事的两个早期观察结果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Xylocain (lidocaine, lignocaine), its discovery and Gordh's contribution to its clinical use.

Hans v. Euler, while investigating how genes and enzymes were chemically related in some chlorofylldefective mutants of barley, isolated gramine, an indole. Erdtman synthetized isogramine and found it to have weak anesthetic properties. He then together with Löfgren synthetized other amino-amides, but no one of them could compete with the existing local anesthetics of the ester-type, derivatives of para-aminobenzoic acid, e.g. procaine. Later Löfgren and Lundqvist followed up these studies and found an amid compound lidocaine (2-dimethylaminoacet-2, 6-xylidide). Lidocaine represented such a significant advance over procaine in clinical tests preformed by T. Gordh that it was introduced for clinical use. It has now during a half century been the standard local anesthetic drug. All local anesthetics are neurotoxic in high enough doses. Xylocain, however, has had an excellent record of safety. Only during the last years have there been reports on possible toxic irritation and damage by Xylocain used for spinal anesthesia. The aetiology is still not clear In this connection two early observations by Gordh and his coworkers are discussed.

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