Cocaine: A Once-Promising Drug

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Chapter 1
Cocaine: A Once-Promising Drug

At the beginning of the twentieth century, the medicine cabinets and pantries in many American homes held a variety of pills and foods containing cocaine as an ingredient. At the time, cocaine was considered to offer considerable benefits as an energy booster and as a topical remedy to relieve minor pain such as toothache. For example, in 1900, Sears, Roebuck, and Company advertised a product called Coca Wine. The advertisement for the wine boasted that it "sustains and refreshes both the body and brain. . . . It may be taken at any time with perfect safety . . . it has been effectually proven that in the same space of time more than double the amount of work could be undergone when Peruvian Wine of Coca was used, and positively no fatigue experienced."1

At the turn of the last century, both the medical profession and the pharmaceutical industry believed the claims that cocaine was useful and safe as an energy booster and for pain relief. Doses of the ingredient in foods and medicines were quite small, and most consumers did not experience problems from occasional use of such products. The few people who studied and wrote about cocaine during this era also believed that it had the potential to become a panacea—a wonder drug for the new century.

South American Origins

Although Americans in the early twentieth century saw cocaine as a modern miracle, Indian tribes living in the Andes ranges of South America had known about this drug for five thousand years. People living at high altitudes where the air is thin discovered that chewing the leaves of the indigenous coca plant increased their energy levels. This plant, known to modern-day botanists as Erythroxylon coca, not only boosted energy but seemed to impart a sense of well-being.

Unbeknownst to the Indians, the boost in energy they experienced came from a chemical agent in the leaves called cocaine alkaloid. This chemical also contributes to the coca plant's abundance—it acts as an insecticide, killing insects that try to feed on the plant.

Cocaine alkaloid occurs in low concentrations in the coca leaf, between .01 and .08 percent. As a result, chewing the leaves delivers a relatively low dose of the drug. At these low doses, people could partake of cocaine and still function normally. Furthermore, because the drug was never ingested in large quantities, its addictive qualities were less pronounced.

Indians noticed other beneficial effects besides the energy boost and euphoria. They discovered that chewing the coca leaf reduced the pain of tooth decay. They also found that chewing coca leaves relieved the physical discomfort that was part of long journeys on foot in the Andes. In fact, the use of coca was so common among mountain travelers that they measured the length of a journey by the number of wads of coca leaves chewed rather than by time or distance.

Introduction to Europe and America

The use of coca changed somewhat when the Spanish conquistadors first came to South America during the mid–sixteenth century. After the Spanish conquered the mountain tribes they forcibly converted them to Catholicism; Catholic priests, wishing to stamp out what they saw as a pagan practice, forbade the chewing of coca leaves. The Spanish, however, also forced the Indians to labor in the mines and fields and quickly observed that the workers tired more quickly when deprived of their coca leaves. To remedy this situation, the Spanish overseers distributed leaves to workers three to four times a day to increase their energy levels and productivity. The overseers began chewing the leaves as well and noted the same pleasant effects that the Indians experienced.

The Spanish sent shipments of the leaves back to Europe, where they became quite popular among the wealthy. The chewing of coca leaves did not, however, become widespread because shipping large quantities of leaves was not economically feasible and attempts to grow coca in Europe failed because the climate there was not suitable.

For nearly two hundred years, interest in coca leaves and their effect on the mind and body languished; for the most part the coca plant was merely a curiosity, of concern only to botanists such as Sir William Hooker, who in 1835 made the first accurate drawing of Erythroxylon coca for the magazine Companion to the Botanical Magazine. Cocaine's potential for medical use remained known to a few doctors, however, and in 1850 small amounts of diluted cocaine were used experimentally for the first time as an anesthetic during throat surgery. By 1855, scientists had accomplished a major breakthrough when they learned how to extract pure cocaine from the coca leaves in large volumes.

Although the medical community in Europe was just beginning to investigate the medical benefits of cocaine, soldiers had the most direct experience with the drug. Military leaders, learning of cocaine's effectiveness both as a painkiller and as an energy booster, tested cocaine on troops and found that these soldiers were able to endure longer marches and to fight more vigorously than soldiers who did not take the drug. Tests also indicated a distinct increase in soldiers' willingness to engage in fierce battles under the drug.

As the amount and availability of cocaine increased in Europe, some of it got into the hands of the public, which quickly discovered its ability to boost a person's energy level. Office workers found that cocaine seemed to make their day pass more swiftly, and athletes soon recognized that cocaine might have value in sports that required endurance. Several English long-distance runners, for example, attributed their success to chewing the coca leaves during races.

Medical Applications

Meanwhile, researchers continued to investigate the new drug's potential as a topical anesthetic. Doctors performing delicate operations on eyes discovered that cocaine numbed tissues, allowing them to perform surgery with only minor discomfort to the conscious patient, who could continue to move the eye as directed. The use of cocaine soon spread to surgery of other body parts, including the ears, nose, and mouth. Not only did cocaine numb the targeted area, but the patient remained awake. This allowed the doctors to converse with their patients during surgery, which helped the doctors to monitor their progress. Several pharmaceutical companies noted the success of cocaine as an anesthetic and during the 1880s began selling large amounts of the drug to hospitals.

Other physicians saw cocaine as possibly benefiting mental patients. In 1884, for example, the Austrian psychiatrist Sigmund Freud performed his own study of cocaine. Based on that study, Freud published a paper, Über Coca, in which he recommended the use of cocaine to treat a variety of conditions, including depression, morphine addiction, digestive disorders, and asthma. Freud tried taking cocaine himself and noted cocaine's effects as a mental stimulant and as an appetite depressant.

As cocaine became more commonly used, pharmaceutical companies perfected its manufacture and refinement. By the end of the nineteenth century, companies were producing thousands of pounds of the drug each year. Cocaine, it appeared, was a drug with unlimited potential.

Freud on Cocaine

In 1883 Austrian psychoanalyst Sigmund Freud read a study in a German medical journal about the beneficial effects of cocaine on German soldiers. He was fascinated by the elevating effects of the drug on soldiers' energy levels and decided to perform his own experiments, with himself as subject. At the website of BLTC Research, David Pierce reports that Freud wrote in his personal journal, "I take very small doses of it regularly and against depression and against indigestion, and with the most brilliant success." In 1884 Freud wrote Über Coca, in which he describes the effects from injection of cocaine in research animals as "the most gorgeous excitement."

When describing the effects of cocaine on humans in Über Coca, Freud reported that humans experience

exhilaration and lasting euphoria, which in no way differs from the normal euphoria of the healthy person. . . . You perceive an increase of self-control and possess more vitality and capacity for work. . . . In other words, you are simply normal, and it is soon hard to believe you are under the influence of any drug. . . . Long intensive physical work is performed without any fatigue. . . . This result is enjoyed without any of the unpleasant after-effects that follow exhilaration brought about by alcohol. . . . Absolutely no craving for the further use of cocaine appears after the first, or even after repeated taking of, the drug.

Commercial Value

Beneficial though cocaine seemed to the medical profession, its real growth was among people who were simply looking for an antidote to fatigue. Since no one in the medical profession had raised any serious reservations about possible harmful effects of cocaine, it appeared to be ideal as an energy booster. The earliest and most popular use of cocaine in a commercial product was the drink Vin Mariani, a mixture of wine and cocaine introduced in England in 1863. The beverage's popularity was widespread, perhaps due to the fact that Vin Mariani claimed it was endorsed by such luminaries as the American inventor Thomas Edison, British writer Sir Arthur Conan Doyle, England's Queen Victoria, and even the pope.

Following the success of Vin Mariani, the Coca-Cola Company, in 1886, added 60 milligrams of cocaine to each bottle of its product and advertised it as a beverage that would invigorate the drinker. At about this same time, drug companies also saw the commercial value of cocaine and added it to products designed to relieve sore throats and toothaches.

By 1910 commercialization of products with cocaine was rampant as elixirs sold as magical potions guaranteed to make people happier and more energetic. Claims that these potions could cure everything from backaches to heart problems to difficulties in a person's love life caused congressional leaders to become alarmed at the widespread and uncontrolled use of cocaine in the nation's food and drugs.

The elevated moods and energy surges that cocaine induced in its users became widely known. Its effects on the body, however, remained a mystery. Although no ill effects had been observed, many doctors called for research to determine exactly what effects cocaine had on the body and whether any of these effects might have long-term adverse consequences.

Short-Term Physiological Effects

In the decades since research began, doctors have come to recognize that of the body's many systems, the cardiovascular system experiences the most noticeable short-term effects of cocaine use. The first of these is a rapid increase in the user's heart rate, which results in the heart pumping a greater volume of blood through the body. This is essentially the same effect that results from strenuous physical activity except that when cocaine is the cause, blood vessels narrow, forcing the heart to work not just faster but harder. Occasionally, cocaine also causes temporary rapid or erratic heart rhythms, increased blood pressure, and increased body temperature.

The central nervous system also experiences temporary physiological changes. As the cocaine carried by the bloodstream enters the brain, the electrical activity of the brain is temporarily altered as the cocaine is absorbed by cells called neurons. The absorption of cocaine alters the chemistry of the brain to increase production of the chemical dopamine. This change in brain chemistry is responsible for the sense of euphoria, sometimes referred to as a "rush" that is usually described in pleasurable terms as a sudden sense of excitement.

Dopamine Research

Although the neurotransmitter dopamine has been linked to the euphoric effects of cocaine for several years, recent research suggests that dopamine may only be part of the puzzle, and researchers now suspect that other neurotransmitters may also play a role.

In 1999 researchers at the University of North Carolina at Chapel Hill wrote a summary of dopamine research titled "Breakthrough? Study Finds Dopamine Cannot Be Source of Pleasure in Brain." University researchers implanted a tiny carbon fiber electrode in laboratory rats to stimulate the animals' brains' pleasure centers in the same way cocaine does. According to Dr. R. Mark Wightman, "We discovered that when we applied the electric shock to a pleasure sensor in the brain of untrained rats, we clearly saw dopamine, but when the animals themselves applied the shock, little or no dopamine appeared."

Wightman and his staff conclude that although dopamine may be involved in initial learning or anticipation of reward, it clearly is not responsible for continuous pleasure. Wightman suspects that cocaine stimulates production of other neurotransmitters such as serotonin, and that these may be responsible for continued pleasure.

In most healthy people, most of these symptoms disappear within thirty to sixty minutes as the liver chemically decomposes the cocaine, which is then removed from the system by the kidneys.

Long-Term Physiological Effects

Researchers found little, if any, lingering effects from occasional use of cocaine. The long-term physiological effects for persistent cocaine use over many years are dramatic, however. Although the kidneys filter out cocaine after each use, the cumulative effect of hundreds of cocaine doses eventually alters the body's physiology and leads to physical damage. The organ that suffers the most damage is the brain. The more frequently cocaine users ingest the drug, the more frequently the blood vessels in the brain are narrowed and fail to adequately provide needed oxygen. Deprived of oxygen, brain cells die, so frequent cocaine use eventually compromises the brain's function. Furthermore, as the blood pressure in the millions of tiny constricted blood vessels and capillaries that supply the brain builds, they gradually break, causing hemorrhage. Dr. Thomas Kosten described this phenomenon during congressional testimony in 1999:

If these vessels are blocked for even a few minutes, brain cells die and thinking, feeling, moving and life itself can cease. Cocaine blocks these blood vessels by constricting them and filling them with abnormal clotting cells called platelets. A large blockage like this leads to strokes in some cocaine abusers, and in most abusers the blockages are smaller, but occur in multiple places in the brain. These multiple blockages leave the cocaine abuser's brain shrunken, discolored and often poorly functioning.2

The restriction of blood supply to the brains of long-term cocaine users appears to be permanent. Scientists have recently been able to observe the restricted blood flow in the brains of such individuals. Using an imaging technique called positron emission tomography (PET), scientists can document the flow of blood in the brain tissue. When the researchers compared PET scans of long-term cocaine abusers with PET scans of normal non–cocaine abusers, they found that the abusers had less blood flow in several areas of the brain. When the researchers performed PET scans again ten days after cocaine use had been discontinued, the blood flow deficits remained even though the subjects in the study had stopped using cocaine.

Not only does the cocaine-related brain damage appear permanent, but the constricted arteries are vulnerable to strokes, which in turn can cause paralysis of parts of the body, the complete loss of speech, loss of memory, and even death. The overall effect is similar to greatly accelerating the aging process. Dr. R. I. Herning, a researcher working on the effects of long-term cocaine use, says, "Our data suggest that cocaine abusers in their thirties have arteries that are as constricted as those of normal subjects in their sixties."3

The cardiovascular system can also suffer damage from long-term cocaine use. The heart, in response to blood vessel constrictions, pumps faster and with greater force in order to meet the oxygen requirements of the body. When the heart is forced to sustain these elevated rates and pressures, it is vulnerable to serious, even deadly problems. For example, the heart can begin to beat erratically, which is called ventricular fibrillation. During an attack of fibrillation, little blood is pumped and without immediate treatment, the victim can die. The heart can also race at rates three to four times normal, a condition called tachycardia. Persistent tachycardia can lead to death.

Medical researchers have proven that long-term cocaine use can cause permanent and massive damage to the brain and heart. Understanding the physical damage inflicted on the body by cocaine, however, has been far easier for researchers than understanding the psychological effects of cocaine. Central to this understanding is the question of whether cocaine is addictive or not.

Is Cocaine Addictive?

The debate over whether or not cocaine is addictive is ongoing and complicated. The majority of mental health professionals take the view that regular cocaine users cannot voluntarily stop taking the drug. In this sense, cocaine meets the definition of an addictive drug. Moreover, these experts believe that cocaine use leads to physical changes in the brain that encourage continued use. Journalist Norbert R. Myslinski reports:

According to Prof. Karen Bolla of Johns Hopkins University, cocaine impairs memory, manual dexterity, and decision making for at least a month. Her study suggests damage to the brain's prefrontal cortex, leading to loss of control over consumption of the drug. A deadly spiral is set up, making it more and more difficult for the addict to quit. Continued drug abuse becomes increasingly a matter of brain damage and less a matter of weak character.4

Another study performed by researchers at Rockefeller University in New York City confirms Bolla's conclusions and provides a detailed explanation of the brain chemistry of a chronic cocaine user. The Rockefeller University investigators found that repeated exposure to cocaine causes a change at the molecular level that alters a brain protein called cyclin-dependent kinase 5. The researchers believe that altering this protein leads to cocaine addiction. Dr. Alan I. Leshner, director of the National Institute on Drug Abuse (NIDA), says, "This research provides a valuable insight into the step-by-step molecular adaptations that the brain makes in response to drugs. These adaptations result in long-term changes at the cellular level that are involved in the development of addiction."5

The medical view that cocaine is addictive is generally shared by long-term cocaine users themselves. One self-confessed addict, when asked how cocaine use—particularly in the form known as crack—could be stopped, says, "You can't . . . period. It will be on this earth as long as there is people. As long as there is people, there will be people smoking crack cocaine." When asked what he would say to anyone thinking about trying cocaine, he says, "Don't ever do it, don't even try it once. You do it once, I don't [care] who you are, you will be hooked for the rest of your life."6 The urge to keep using the drug is strong enough to motivate some addicts to resort to extreme measures. Gilda Berger quotes a crack user in her book Crack: The New Drug Epidemic, who claims, "I'd kill for it!"7

Cocaine Comparisons

Commonly used addictive drugs have many different characteristics. The following table, provided by Dr. Jack E. Henningfield in the New York Times article "Is Nicotine Addictive? It Depends on Whose Criteria You Use," compares cocaine with five other drugs and ranks them according to five addictive characteristics. A rank of 1 indicates least effect; a rank of 6 indicates highest potency.

Dependence: How difficult it is for the user to quit; the relapse rate; the percentage of people who eventually become dependent; the rating users give their own need for the substance; and the degree to which the substance will be used in the face of evidence that it causes harm.

Withdrawal: Presence and severity of characteristic withdrawal symptoms.

Tolerance: How much of the substance is needed to satisfy increasing cravings for it, and the level of stable need that is eventually reached.

Reinforcement: A measure of the substance's ability, in human and animal tests, to get users to take it again and again, and in preference to other substances.

Intoxication: Though not usually counted as a measure of addiction in itself, the level of intoxication is associated with addiction and increases the personal and social damage a substance may do.

DrugDependenceWithdrawalToleranceReinforcementIntoxication
Nicotine64532
Heroin55655
Cocaine43364
Alcohol36446
Caffeine22211
Marijuana11123

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Powerful as the evidence is that cocaine is addictive, some medical researchers disagree over just how addictive the drug is. One of the most compelling arguments against strong addictive properties is the fact that a relatively small percentage of people who use cocaine actually become addicted. Various national agencies report an average cocaine addiction rate of about 1 percent of individuals who have tried the drug—lower than the addiction rate for nicotine among those who have tried tobacco. If cocaine is so addictive, they argue, why is the addiction rate so low?

As the debate over its addictive potential continues, the reality of nearly epidemic cocaine use in America remains, despite the fact that the drug is illegal in every state.