Xylocain (Lidocaine, Lignocaine), its discovery and Gordh's contribution to its clinical use

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