Cocaine
Although the ineffectual attempts at local anesthesia indicated
a growing awareness of local anesthetic methods, the origins of neural blockade as
we know it today had already been established in a rudimentary form on the eastern
slopes of the Andes in South America for more than 350 years. When the invading
Spaniards arrived in Peru in the 16th century (1532–1549), they found an advanced
culture, with Cusco as the capital city and people with highly developed engineering
and artistic skills. Few historians dispute that the Inca civilization was one of
the highest developed cultures in America at the time, and the Spanish invaders were
the means by which the powerful pharmacologic effects of the coca leaf ultimately
were revealed to the European community.
Inca priests chewed the dried leaves of a plant, Erythroxylon
coca (see Fig. 1-9B
),
as a stimulant and used it as an integral part of religious ceremonies. Cultivation
and use of the coca leaves by the Andean Indians date back thousands of years. Coca
is an indigenous Indian (Aymaran) word meaning "food for the traveler." There is
controversy about whether the Incas used the plant as a local anesthetic. Because
they had no written language, much of what is known about their civilization is derived
from the Spanish chroniclers, whose mention of coca was scanty, perhaps because use
of the plant was limited to the priests before the fall of the Incan civilization.
There was also no pictorial evidence from Incan pottery or weavings that coca was
applied to surgical wounds. The priests did perform painful surgical procedures
such as trepanations, and from several sources we learn that the patient chewed coca
leaves as well as other native plants, but there is no firm evidence to support the
claim that saliva enriched by coca juice was applied to the wound.[131]
The first written account of the coca plant being used as a local
anesthetic was by the Spanish Jesuit Bernabe Cobo (1582–1657), who chewed the
plant to relieve a toothache and wrote about it in 1544.[208]
Albert Niemann (1834–1861) of Göttingen, Germany, who isolated the alkaloid
from the dried leaves in 1856, gave the name cocaine
to the active drug.[209]
[210]
Interest in cocaine in Europe and America was directed initially toward the central
effects of the drug when taken systemically. Vasili von Anrep[211]
(1852–1918) was the first to remark on its local anesthetic properties, and
after animal experiments, he suggested its use as a local anesthetic during surgery.
This suggestion went unnoticed, and the drug remained a curiosity. A comprehensive
pharmacology textbook from 1883 does not mention cocaine or the plant E.
coca.[212]
Sigmund Freud (1856–1939), a young house officer at the
prestigious Allgemeines Krankenhaus in Vienna, had a unique interest in cocaine and
tested the drug as a substitute for opioids on a colleague who was addicted to morphine.
Although this research met with little success, he also had noticed its ability
to produce numbness of the tongue and provided a small sample to his junior colleague,
Carl Koller[213]
(1858–1944), an intern who
was interested in producing local anesthesia for operations on the eye.
Koller had anticipated a career as a scientist in Vienna. He
had taken up this question for his research project because the anesthetic methods
of the time were highly unsatisfactory for ophthalmic surgery. General anesthetics
presented numerous difficulties for the surgeon, and refrigeration anesthesia, although
marginally successful for surgery on the extremities, was clearly inappropriate for
the eye. Koller observed that after topical cocaine application, he was able to
pinch and prick the cornea of dogs without discomfort to the animals. Self-experimentation
confirmed complete analgesia of the corneal surface, and he proceeded to use the
agent for superficial surgery on the eye.
Koller arranged to demonstrate the use of topical cocaine analgesia
at the Ophthalmologic Congress in Heidelberg, Germany on September 15, 1884. As
the time
for this presentation approached, he was unable to afford the travel expenses from
Vienna, and a colleague from Trieste, Josef Brettauer (1835–1905), presented
the three-page manuscript in his absence.[214]
[215]
The presentation and demonstration were followed by an enthusiastically favorable
response. Priority for the discovery was briefly confounded by a report on topical
cocaine analgesia at an ophthalmologic meeting in October 1884 by Leopold Koenigstein,
who did not mention Koller's prior paper, and by other comments that Sigmund Freud
had actually originated the idea of cocaine analgesia. Koenigstein later conceded
full credit for the discovery to Koller, and Freud eventually rejected all claims
to the idea of topical analgesia with cocaine, although many concede that, with his
earlier publication on the subject,[216]
he was
instrumental in reviving interest in a drug that before 1884 was of no interest to
pharmacologists.
Koller's career in Vienna seemed secure, but a disagreement arose
with another house officer in January 1885. The altercation escalated into a duel
with sabers, an activity that was banned in Austria at that time. Koller emerged
unscathed from the duel, but the offending party suffered two saber cuts to the face.
After this episode, Koller became depressed and ultimately decided to leave Austria.
He first immigrated to Holland, and then settled in New York City in 1886. There
he built a successful private practice while continuing to contribute occasional
clinical articles to the ophthalmologic literature. He died in New York City in
1944, after modestly receiving several awards for his seminal role in the development
of local and regional anesthesia.[213]
