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赛罗卡因(利多卡因),其发现及戈德对其临床应用的贡献。

Xylocain (lidocaine, lignocaine), its discovery and Gordh's contribution to its clinical use.

作者信息

Holmdahl M H

机构信息

Department of Anesthesia and Intensive Care, University Hospital, Uppsala, Sweden.

出版信息

Acta Anaesthesiol Scand Suppl. 1998;113:8-12. doi: 10.1111/j.1399-6576.1998.tb04979.x.

Abstract

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.

摘要

汉斯·冯·欧拉在研究大麦某些叶绿素缺陷型突变体中基因与酶的化学关系时,分离出了禾胺,一种吲哚。厄特曼合成了异禾胺,并发现它具有微弱的麻醉特性。然后他与勒夫格伦一起合成了其他氨基酰胺,但它们中没有一种能与现有的酯类局部麻醉药,即对氨基苯甲酸的衍生物,如普鲁卡因相竞争。后来勒夫格伦和伦德奎斯特继续进行这些研究,发现了一种酰胺化合物利多卡因(2 - 二甲基氨基乙酰 - 2,6 - 二甲基苯胺)。在T. 戈德进行的临床试验中,利多卡因相对于普鲁卡因有如此显著的进步,以至于它被引入临床使用。在半个世纪以来,它一直是标准的局部麻醉药。所有局部麻醉药在足够高的剂量下都具有神经毒性。然而,利多卡因有着出色的安全记录。只是在最近几年才有关于用于脊髓麻醉的利多卡因可能产生毒性刺激和损伤的报道。病因仍不清楚。在此方面,讨论了戈德及其同事的两项早期观察结果。

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