The history of lidocaine began with its synthesis from cocaine. Cocaine is a naturally occurring compound indigenous to the Andes Mountains, West Indies, and Java. It was the first anesthetic to be discovered and is the only naturally occurring local anesthetic; all others are synthetically derived. Cocaine was introduced into Europe in the 1800s following its isolation from coca beans. Sigmund Freud, the noted Austrian psychoanalyst, used cocaine on his patients and became addicted through self-experimentation.
In the latter half of the 1800s, interest in the drug became widespread, and many of cocaine’s pharmacologic actions and adverse effects were elucidated during this time. In the 1880s, Koller introduced cocaine to the field of ophthalmology, and Hall introduced it to dentistry. Halsted was the first to report the use of cocaine for nerve blocks in the United States in 1885 and also became addicted to the drug through self-experimentation.
Lidocaine, the first amino amide–type local anesthetic, was first synthesized under the name ‘xylocaine’ by Swedish chemist Nils Löfgren in 1943. His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself. It was first marketed in 1949.
The history of lidocaine includes the development of procaine, the first synthetic derivative of cocaine, which was developed in 1904. Lofgren later developed lidocaine, the most widely used cocaine derivative, during World War II in 1943. The history of lidocaine continues with the subsequent development of the ester class, benzocaine, tetracaine, among others as well as additional amides, prilocaine, bupivacaine and others.
The history of lidocaine includes its uses in nerve block injections, topical anesthetics and as an anti arrhythmic agent. It is supplied in liquid injection forms which can also include epinephrine as well as in topical creams and gels. Lidocaine is now widely used in medicine, tattoo procedures, piercings, and much more.