The comedian Robin Williams once quipped that cocaine is
God’s way of telling you that you’re making too much money.
The United States must indeed be a wealthy country, considering that 3 million of our fellow citizens abuse this drug; this is
six times the number of heroin addicts in our nation. It is estimated that 50% of Americans between the ages of 25 and
30 years has tried cocaine.
What does cocaine do in the brain? First, it binds to sodium
ion channels and blocks them from functioning. This action
stops the fl ow of action potentials and prevents neurons from
communicating with each other. Cocaine also blocks the conduction of pain signals, which explains why, after it was isolated
from the coca plant (Erythroxylon coca) in 1855, it was used as a
local anesthetic, including for the eye and for toothaches. But
ultimately, its anesthetic actions would be discovered to have
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nothing to do with the reason for its later illegal street use: its
ability to produce euphoria.
Cocaine acts similarly to amphetamine with regard to its
ability to enhance the effects of the catecholamines and serotonin at the synapse. The actions of cocaine on the brain lead
to increased alertness, reduced hunger, increased physical and
mental endurance, increased motor activity, and an intensifi cation of most normal pleasures. This last feature may explain
why so many claim that cocaine enhances emotional and sexual
feelings. Cocaine abusers usually co-administer other drugs that
are brain depressants (e.g., alcohol, heroin, or marijuana) to
decrease the unpleasant hyperstimulant aspects of cocaine.
Approximately 16 to 32 milligrams of cocaine is an effective
street dosage that is usually without immediate negative side
effects. An increase in heart rate usually occurs within about
8 minutes after administration and dissipates 30 to 40 minutes
later. The half-life, or the time it takes for half of the drug to
exit the blood and body, is about 40 to 50 minutes. Cocaine will
actually degrade spontaneously in the body to produce an inactive compound with a tongue-twister name, benzoylecgonine.
The physiological effects of cocaine are therefore much shorter
than those of amphetamine. Partly for this reason, most users
claim that it does not “wear out” the body in the same way that
amphetamine does.
Getting cocaine to its site of action within the brain fi rst
requires getting adequate amounts of the drug into the blood.
Snuffi ng cocaine by applying it to mucous membranes inside
E U P H O R I A , D E P R E S S I O N , & M A D N E S S s 6 7
the nose is much more effective than either oral administration
or intravenous use because the drug enters the blood and brain
more quickly and is therefore more immediately euphoragenic.
Unfortunately, there is a problem with this approach to getting
cocaine into the blood. Cocaine constricts the blood vessels
feeding the cartilage in the bridge of the nose and, with repeated
nasal application, leads to the ischemic (lack of blood) death of
the tissues supporting the end of the nose. Initially, the irritation to the tissue causes a runny nose; ultimately, the irritation
leads to a true necrosis, or cell death, and the end of the nose
either collapses or becomes quite distorted.
Orally administered cocaine is not well-absorbed from
gastrointestinal tract, and its effects on the brain thus tend to be
far less reinforcing when taken in this fashion. However, oral
administration does have a long history. Many years before
cocaine extracts were applied to mucous membranes, ancient
peoples simply ate the leaves of the coca plant. Indeed, although
cocaine use peaked in the 1880s and the 1980s, chewing coca
leaves for their psychoactive effects — they contain up to 1% of
cocaine by weight — was certainly a popular practice long before
these eras. The leaves have been found in 5000-year-old graves.
Approximately 800 years ago in South America, people started
chewing the leaves wrapped around a piece of limestone to
increase the pH in their mouths and to augment the release of
cocaine from the leaves. By improving the extraction of cocaine
from the leaves, the experience became far more pleasurable.
The Incas introduced religious ritual to its use and invented the
6 8 S Y O U R B R A I N O N F O O D
word “cocata” to describe the distance a person could walk on
one chew of coca leaf before the benefi cial effects wore off. The
tribal chiefs gave coca leaves to runners in the Andes Mountains
to help them tolerate the altitude and to increase their endurance; the runners were also paid in coca leaves, thus maintaining
their addiction and continued service until they died of exhaustion and malnutrition. The conquering Spanish subsequently
recognized the cost-saving wisdom in this approach and paid
their Incan servants with coca leaves, enabling them to work
harder and eat less food. Amerigo Vespucci, who gave his name
to the newly “discovered” land, wrote about the use of coca
leaves by the local tribes.
Fast-forward a number of centuries, and we see the oral use
of coca plant extracts taking a new form. In 1862, Angelo
Mariani, a Corsican chemist, combined a Bordeaux wine with
coca plant extracts to produce and sell Vin Mariani. The labels
displayed testimonials from Pope Leo XIII, who gave it the
Vatican’s gold medal of appreciation, as well as from President
Ulysses S. Grant and from Thomas Edison, who claimed that it
helped him stay awake longer to complete his experiments. Vin
was such a commercial success that many other alcoholbased tonics containing coca leaf extracts were introduced in
the late 1880s. One quite successful tonic was introduced
by John S. Pemberton in 1884. Pemberton called his drink
“A French wine of coca, ideal tonic.” Later, in 1886, he removed
the alcohol, replaced cocaine with an extract from the kola nut,
and called it Coca-Cola. But why combine coca leaf extracts with
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wine in the fi rst place? The reason is that the combined effect of
these two drugs on the brain is far more euphoragenic, and
therefore more addicting, than either compound alone. When
combined with alcohol, as in Vin Mariani, the mixture forms a
powerful psychoactive compound called coca-ethylene, which is
more lipid-soluble than cocaine and thus enters the brain faster;
by now you know what that implies in terms of the enhanced
pleasure it will produce.
Drug designers are never far behind the chemists in discovering new ways to make drugs enter the brain faster. After all,
greater addiction of one’s customers leads to higher profi ts!
Thus, in the 1960s free-base cocaine was produced and people
discovered that it very quickly entered the blood and brain and
produced an ever greater euphoria. The natural product that
had been obtained from the coca leaf for so many centuries
exists as cocaine hydrochloride; this is an acidic compound that
can be volatilized — that is, turned into a vapor. However, at a
high temperature, the cocaine is destroyed. This is why naturally
occurring cocaine was never smoked; the active ingredient is
completely lost. I would predict that someone somewhere at
some time must have tried smoking coca leaves and found that
it was a disappointing failure. To be effective when smoked, cocaine must be reconverted chemically to its alkaloid or base
form. The process of converting and then isolating the product
is called free-basing.

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