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Cocaine is a naturally occurring compound. It was the first anesthetic to be discovered and is the only naturally occurring local anesthetic; all others are synthetically derived. Cocaine was introduced in Europe in 1860 after its isolation from coca leaves by German chemist Albert Niemann (1834–1861). Sigmund Freud (1856–1939), the noted Austrian psychoanalyst, was an early proponent of its medicinal uses. He encouraged a physician colleague, Dr. Carl Koller (1857–1944) to experiment with its analgesic properties.

The origins of local anesthesia date back to 1884 when Koller introduced cocaine to the field of ophthalmology in Vienna. He discovered that cocaine instilled into his conjunctival fornix produced localized insensitivity to touch and pain.1 The news quickly spread around the world and to the United States after publication of Koller's paper on September 18, 1887. William Stewart Halsted (1852–1922) and his colleague Richard John Hall (1856–1897) were the first to report the use of cocaine for nerve blocks in the United States in 1884.2 Halsted injected cocaine into the lower jaw of a patient and extracted a tooth with no pain or sensation reported by the patient. Halsted and Hall developed various nerve and regional blocking techniques.

On August 16 1898, August Bier performed the first surgery under spinal anesthesia at the Royal Surgical Hospital by injection of 15 mg of cocaine intrathecally. In 1908, Bier pioneered the technique for intravenous regional anesthesia (IVRA)3 commonly known as “Bier block” (Fig. 86-1).

After the adverse effects of cocaine (toxicity, addiction, and others) became more widely known, new anesthetic drugs were sought to replace it (Fig. 86-2).

FIGURE 86-2.

Timeline for local anesthetic discovery and introduction.

The first successful attempt came on November 27, 1904, when German chemist Alfred Einhorn (1856–1917) patented 18 para-aminobenzoic derivatives that were developed in Hesse, Germany.4 One of the compounds was given the name novocaine, from the Latin nov,-new + caine, a common ending for alkaloids used as anesthetics. In 1905, in an article by Heinrich Braun, novocaine was compared with other local anesthetics being developed.5 Novocaine was found to be safe and quickly became the standard for local anesthesia; it then was renamed procaine in the United States during World War I. The drug needed to be combined with high concentrations of adrenaline for optimal affect. In addition, some patients were highly allergic to it. These drawbacks prompted searches for stronger anesthetic agents with fewer allergic side effects.

Lidocaine, the first amino amide-type local anesthetic was synthesized under the name xylocaine by Swedish chemist Nils Lofgren in 1943. His colleague Bengt Lundquist self-administered the first local ...

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