A Brief History of Stimulants

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Chapter 1
A Brief History of Stimulants

Today's world is fast paced and demanding. Advertisers send messages that being thin is fashionable. Parents prod their children to study hard and earn good grades. Supervisors urge employees to be more productive. The drive to be the best one can be—thinner, smarter, or faster—seems to be part of the American psyche.

For those who always feel pressured to achieve more, chemical stimulants may be appealing. This diverse group of drugs, containing dozens of stimulants, has one common denominator: All of them speed up the functions of the body, making people feel more alert. However, stimulants vary widely in how much they accelerate body activities, the manner in which they are used, and their legal status.

The most commonly used legal stimulants are caffeine and nicotine, both of which are derived from plants. The best-known restricted stimulants are cocaine, which also comes from a plant, and amphetamines, which are synthesized in a lab.

Inside the Body

Although stimulants are derived from several sources, they all alter the body's functions in about the same way. They change the way information is carried along nerves.

Throughout the body, nerve cells line up end-to-end to create living superhighways for the transmission of information. Data zips down the length of a nerve in the form of an electrical impulse. However, an electrical impulse cannot travel directly from one nerve cell to the next because there is a small gap, a synapse, located between cells. To get across the gap, the impulse must be ferried by special chemicals called neurotransmitters. So, when an electrical impulse reaches the end of a cell, it stimulates the release of neurotransmitters. These chemicals flow across the synapse, carrying the impulse and stimulating the next cell. In this way, the impulse moves along the chain of nerve cells.

Stimulants do their work at the synapses, where they cause a buildup of neurotransmitters. High levels of neurotransmitters in synapses create several changes in the body. They activate the release of adrenaline, setting off the "fight or flight" response, a system that

prepares the body for emergencies. Adrenaline increases heart rate, the flow of blood to muscles, and the speed at which impulses are transmitted along nerves. As a result, stimulants make a person feel stronger, more alert, and energized. Some stimulants, like caffeine, only mildly excite the nervous system. Others, like amphetamine, cause very noticeable changes. An adrenaline surge, along with the energy it produces, may not sound harmful. But Andrew Weil and Winifred Rosen, authorities on mind-altering drugs, point out the downside to artificial spikes in adrenaline levels:

One of life's basic rules is You Never Get Something for Nothing (or, There's No Such Thing as a Free Lunch), and stimulants are no exception to this rule…. Instead of miraculously delivering free gifts of cosmic en ergy, stimulants merely force the body to give up some of its own energy reserves. So when the stimulant wears off, the person feels especially tired, with less than normal energy. This may be perceived as feeling "down," sleepy, or depressed.1

The buildup of neurotransmitters at synapses causes another change in the body: It excites a complex brain mechanism called the reward pathway. This pathway is designed to help teach the body to perform tasks required for survival, such as eating, through positive reinforcement.

Nicotine, cocaine, and amphetamines are able to trigger the reward pathway, but they do so in an abnormal way. When consumed, these stimulants do not just switch on the reward system; they overexcite it, causing intense feelings of happiness. The brain quickly learns to associate these feelings with the drugs. Thus, the drugs "teach" the brain that they are essential for survival and that the body cannot manage without them.

The Most Popular Stimulant

Caffeine is the most commonly used stimulant in the world. Because its effects are mild, it does not interact with the reward pathway, but it does speed up the body. About 90 percent of Americans depend on caffeine to jump-start their mornings. This stimulant is found in more than sixty different species of plants

that are used to prepare foods and beverages. Caffeine has played a big part in the development of cultures around the world.

One of the oldest caffeine-containing plants is the coffee tree. Historians believe that the shrubby coffee tree originated in the fourth century b.c. in the area that makes up present-day Ethiopia. From there, traders brought coffee to Venice. By the 1600s, coffeehouses had become popular meeting places where businessmen, scholars, and politicians got together to exchange ideas over a cup of coffee. According to drug historians Cynthia Kuhn, Scott Swartzwelder, and Wilkie Wilson, "The environment created in coffee houses turned out to be one that gave rise to creative thinking in the entrepreneurial and business realms."2 Coffeehouses spread across Europe and eventually to the young United States.

Even though most people welcomed the spread of coffee across both the Old and New Worlds, some medical experts feared that it was a dangerous brew. In the United States and Europe, doctors hotly debated coffee's safety. A typical cautionary word came from Dr. T.D. Crothers, professor of nervous and mental diseases at the New York School of Clinical Medicine. He taught that coffee was as addicting and dangerous as morphine or alcohol. Describing the downside of coffee addiction, he said, "In some extreme cases, delusional states of a grandiose character appear; rarely violent or destructive, but usually of a reckless, unthinking variety. Associated with these are suspicions of wrong and injustice from others; also extravagant credulity and skepticism."3 Even today, the medical community has continued to issue occasional warnings to limit coffee's use. Despite these, coffee has remained popular.

Drinking coffee is just one of several ways to consume caffeine. Tea, cola, and chocolate also contain caffeine. Chocolate, the caffeine-containing extract made from the seeds of the cacao plant, has been popular for centuries. About two thousand years ago, the Mayans made a warm, bitter drink from it that they called chocolatl; it was so thick that it was eaten with a spoon. Today, most cultures prefer to mix chocolate with sugar to curb the bitter taste.

The Science Behind the Brew

Even though people have been consuming food containing caffeine for centuries, the pure chemical was not identified and isolated until 1821. It is now known that caffeine speeds up the activity of neurons in the brain and causes the release of adrenaline, like other stimulants do. However, caffeine has another action that is less known, one that explains why caffeinated beverages keep people awake at night.

As it works, the brain makes a chemical by-product called adenosine. By the end of the day, adenosine levels in the brain are high. High levels signal to certain cells in the brain that it is time to feel fatigued. Thus, the accumulation of adenosine helps slow the body at the end of the day, preparing it for sleep. Caffeine interferes with this process by blocking the action of adenosine. As a result, cells do not get the signal that it is time to slow down and rest, so they keep working at their normal pace.

Adenosine buildup also signals blood vessels in the brain to dilate. Researchers believe that this dilation helps ensure that plenty of food and oxygen will be delivered to cells during sleep. However, when caffeine is present, the command to dilate does not get sent, so the vessels remain small and constricted.

Caffeine's ability to prevent the dilation of blood vessels in the brain makes it a useful treatment for vascular headaches. Painful vascular headaches are caused by enlarged blood vessels in the brain. Some people who suffer with this condition take prescription caffeine pills when their headaches begin, a strategy that reduces the size of the vessels and prevents the headaches from worsening.

Caffeine also mildly stimulates the nerves that regulate the size of bronchial tubes in the lungs. The stimulation causes these tubes to widen slightly, making it easier to breathe. Researchers are examining this property to see if it may give caffeine some value in treating the sick. For example, in the Harvard Commentary Health News, Dr. Robert Shmerling says, "Newborns, especially those who are premature or have undergone surgery just after birth, may be treated with caffeine to stimulate their breathing."4

The Leaf of Gold

Following caffeine, nicotine ranks as the second most widely used stimulant. Unlike caffeine, nicotine comes primarily from one source, the leaves of the tobacco plant, Nicotiana tabacum. This plant has been tended and harvested for thousands of years.

Tobacco is native to the Americas, and historians have found evidence that it was used as far back as 6000 b.c. When explorer Christopher Columbus and his crew landed on San Salvador island in 1492, the locals offered him gifts of tobacco leaves. In his journal, Columbus wrote, "The natives brought fruit, wooden spears, and certain dried leaves which gave off a distinct fragrance."5 Imitating the natives, Columbus and his crew smoked and chewed the leaves. Finding tobacco to their liking, they took samples back to Europe to share.

By the 1600s tobacco was cultivated in several parts of the United States. In every sense, tobacco was a cash crop that soon became a pillar of American society. According to a nineteenth-century historian,

So prominent is the place that tobacco occupies in the early records of the middle Southern States, that its cultivation and commercial associations may be said to form the basis of their history. It was the direct source of their wealth, and became for a while the representative of gold and silver; the standard value of other merchantable products; and this tradition was further preserved by the stamping of a tobacco-leaf upon the old continental money used in the Revolution.6

Other Uses of Nicotine

While caffeine is usually consumed in food or beverages, nicotine can be introduced into the body by several different routes: through the skin, the membranes lining the mouth and nose, the lungs, or the digestive system. Once nicotine reaches the bloodstream, it travels to the brain within just a few seconds. There, it has many of the same effects as other stimulants: It increases heart rate and blood pressure and activates the reward center of the brain, sending the body the false message that nicotine is necessary for survival.

Examining these properties, scientists think that nicotine may have a role in the treatment of diseases of the brain. Colleen McBride, director of cancer prevention at Duke University, believes that nicotine may have value in treating some of the symptoms of depression, as well as Parkinson's and Alzheimer's diseases, conditions that hamper memory and thinking. According to McBride, "We might put some of these people on nicotine patches or some type of nicotine replacement therapy for life…. There's growing evidence that it may be useful in treating Parkinson's disease, Alzheimer's—their level of concentration, their ability to focus."7

Amphetamine Arrives

Whereas caffeine and nicotine have been widely used in the Western Hemisphere for centuries, amphetamines are relatively new. Amphetamine was accidentally made in a lab in 1887 by a German scientist working on a treatment for asthma.

Not realizing the potential of his discovery, the scientist put the amphetamine aside and stopped experimentation on it. The drug sat on the shelf for forty years. In 1927 UCLA researcher Gordon Alles decided to explore amphetamine further to see if it had any therapeutic value.

Through experimentation, Alles found that amphetamine is a powerful bronchodilator, which means that it opens the breathing tubes in the lungs. To his surprise, patients who tested the drug told him that it also gave them energy and made them feel good. Hoping that those stimulating properties were merely unimportant side effects, drug companies put Alles's drug on the market to treat colds and asthma. In the late 1920s, over-the-counter amphetamine inhalers called Benzedrine reached drugstores everywhere. In a short time, the word was out that Benzedrine inhalers not only cleared congestion but delivered a powerful burst of energy. During Prohibition and the depression, periods when very few recreational drugs were available, Benzedrine inhalers were a hit with anyone who wanted a quick buzz. By 1929 drug companies were encouraged by the success of their first amphetamine product and decided to market the drug as a tablet. During World War II, soldiers on both sides of the conflict were given amphetamine tablets to reduce fatigue.

The Birth of Methamphetamine

In the meantime, scientists in Japan were experimenting with the amphetamine molecule to see if it might generate any other potential medicines. One of their experiments yielded methamphetamine, a more potent form of amphetamine. Like its parent drug, methamphetamine could be taken orally. However, because it was a water-soluble powder, it could also be dissolved and injected, providing a more potent way to administer the chemical.

Regardless of how they are consumed, once in the bloodstream, amphetamines travel to the brain in just a few seconds. In the brain tissue, they dramatically increase nerve cell activity, which in turn decreases appetite and causes feelings of energy and excitement. Amphetamines also stimulate the reward center of the brain, delivering strong feelings of pleasure.

With these effects in mind, drug companies enthusiastically marketed amphetamine and its derivatives as treatments for depression and as dieting aids. People in every walk of life found a use for the drugs and a reason to purchase them: Truck drivers who needed to stay awake on long trips, athletes who wanted extra energy, housewives yearning to lose a few pounds, and students cramming for exams sought out the drugs. During each year of the 1950s, manufacturers in the United States produced enough

Candy-Flavored Cigarettes

They come in strawberry, chocolate, vanilla, and grape. Hand rolled and beautifully packaged, flavored cigarettes from India called bidis appeal to many teens. Although they are sometimes marketed as a safe alternative to cigarettes, bidis contain more nicotine than American cigarettes and are loaded with more of the undesirable, cancer-causing ingredient, like tar and other toxins, than traditional cigarettes.

In an interview with the Ventura County Star, Dr. Terry Pechacek of the Centers for Disease Control and Prevention's Office of Smoking and Health warns that "These things [bidis] are unregulated, highly available and kids think they're safe…. Studies in India find that the lung cancer risk among bidi smokers is higher than people smoking Western style cigarettes."

One state, Illinois, has already taken steps to protect smokers by banning the sale of bidis. "It's a deceptive product," said Senator Kathleen Parker to the Jefferson City News Tribune. "It is something they're claiming is going to help a person stop smoking. Actually it's more addictive."

amphetamines to supply each man, woman, and child with fifty doses. Most people used them under the recommendation of their physicians.

By 1965 physicians were seeing undeniable signs of addiction in some amphetamine users. Doctors reported these adverse effects to the Food and Drug Administration (FDA) the organization in charge of assuring the safety of foods and drugs used by Americans. As a result, amphetamines were soon placed under federal restrictions to protect consumers.

A Role in Medicine

Today there are very few conditions for which physicians prescribe amphetamines. Medical use is restricted to the treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) and narcolepsy. ADD and ADHD are characterized by impulsive behavior and disorganized thinking patterns. The most commonly prescribed form of amphetamine for these disorders is Ritalin, chemically known as methylphenidate. Ritalin activates the part of the brain that helps to focus thinking and calm behavior. Narcolepsy is a disorder characterized by an uncontrollable desire for sleep. Narcoleptics may suddenly fall asleep several times during the day, even while talking or driving. The ability of amphetamines to arouse their brains helps them stay awake.

An Interest in Cocaine

Unlike amphetamines, which are made in the lab, cocaine is derived from a natural source. Cocaine is the active ingredient in the leaves of Erythroxylon coca, a native plant of South America. Coca cultivation and use by South American cultures dates back to 2500 b.c. when leaves were chewed by the working class to increase their stamina and give them the energy needed to perform physically demanding tasks.

The first Europeans to learn about coca were explorers to the New World. In 1499 Amerigo Vespucci wrote in his journal about the unusual habit of leaf chewing among the South American natives:

Their cheeks bulged with the leaves of a certain green herb which they chewed like cattle, so that they could hardly speak…. When I asked … why they carried these leaves in their mouth, which they did not eat, … they replied it prevents them from feeling hungry, and gives them great vigor and strength.8

Physicians did not seriously consider the drug as a possible medication until 1883. One of the first physicians to do so was an army doctor. According to Edward Brecher, editor of The Consumers Union Report on Licit and Illicit Drugs, "German army physician, Dr. Theodor Aschenbrandt, secured a supply of pure cocaine from the pharmaceutical firm of Merck and issued it to Bavarian soldiers during their autumn maneuvers. He reported beneficial effects on their ability to endure fatigue."9 These results piqued interest among other physicians and scientists.

The Miracle Cure

Viennese doctor Sigmund Freud, a pioneer in the field of psychology, was intrigued by Aschenbrandt's findings. Edward Brecher explains:

Young Freud at the time was suffering from depression, chronic fatigue, and other neurotic symptoms. "I have been reading about cocaine," Freud wrote to his fiancée in 1884. "I am procuring some myself and will try it with cases of heart disease and also of nervous exhaustion."10

Following the standard medical protocol of the day, Freud experimented with the drug on himself. He found that a tiny quantity, only one-twentieth of a gram, gave him boundless energy and relieved his depression. Impressed by these positive results, Freud tried cocaine on several patients, his sisters, and his fiancée. He was pleased to find that it seemed to help everyone, no matter what their condition.

One of Freud's colleagues, German surgeon Carl Koller, was fascinated by cocaine's ability to act as a local anesthetic, or numb the skin to which it was applied. As part of his practice, Koller performed eye surgery, an experience that was extremely painful to his patients. Experimenting with a solution of the white powder dissolved in water, Koller found that he could deaden the cornea of a patient's eye. For the first time in history, it was possible to perform eye surgery without the usual pain. By 1885, Koller's landmark discovery, along with Freud's continued support and enthusiasm, generated so much interest in cocaine that doctors, surgeons, and dentists around the world ordered the drug to try on their own patients.

In the late 1800s, the medical industry began incorporating cocaine into hundreds of new elixirs. To sell these products, advertisements promised that the remedies could cure almost every known disease. The cocaine-laced Ryno's Hay Fever and Catarrh Remedy, "for when the nose is stuffed up, red and sore," was also promoted as a tonic that "could make the coward brave, the so-lent [shy] eloquent, and render the sufferer insensitive to pain."11 Even Sears, Roebuck, and Company got in the act, offering a Peruvian wine of coca that "sustains and refreshes both the body and brain."12

As the world celebrated the many uses of cocaine, a few doctors began to see the drug's ugly side when some patients began to display classic symptoms of addiction. To protect consumers, the federal government ultimately passed the Pure Food and Drug Act which prohibited the use or sale of cocaine without a prescription, in 1906.

Legal Uses Today

As with amphetamines, cocaine's addicting qualities brought it under medical and governmental scrutiny. Working in the same manner as its chemical cousins, cocaine triggers the reward center, creating sensations of intense pleasure. Its mechanism of action, however, is slightly different from the one used by amphetamines, which cause an overproduction of neurotransmitters. Neil Swan, writing for the National Institute on Drug Abuse, explains that cocaine blocks the normal cleanup of neurotransmitters after they are released: "When cocaine is present, it prevents the reabsorption of dopamine [a neurotransmitter]. As a result, the neurotransmitter is left in the synapse of cells in the pleasure center, artificially extending sensations of pleasure."13

Today the sale and use of cocaine are even more restricted than they were a century ago, yet cocaine remains an important drug in the operating room. Cocaine is unrivaled as a local anesthetic, used to numb the eyes, ears, nose, and throat during surgery. There are very few other medical uses of the drug. Cocaine is an ingredient in a remedy called Brompton's mixture, which is still sold in Great Britain to alleviate the chronic pain of terminally ill patients. At one time, cocaine was used as a treatment for depression, but substitute medications have been developed that have proved more beneficial.

In the Rhythm

One of the appeals of stimulants is their ability to change the natural rhythms of life, creating energy and alertness on demand. Generally, people are most alert in the mornings, and their energy wanes as the day proceeds. A cola during the afternoon slump can combat drowsiness and fatigue. Used in this way, stimulants are generally safe. However, the use of stronger stimulants is a huge concern for public health and welfare.

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A Brief History of Stimulants

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