Chapter 5  Stimulants

Cocaine Amphetamines Methcathinone Methylphenidate Anorectic Drugs Khat   Stimulants Identification

Coca plants.

Stimulants, sometimes referred to as "uppers," reverse the effects of fatigue on both mental and physical tasks. Two commonly used stimulants are nicotine, which is found in tobacco products, and caffeine, an active ingredient in coffee, tea, some soft drinks, and many non-prescription medicines. Used in moderation, these substances tend to relieve malaise and increase alertness. Although the use of these products has been an accepted part of U.S. culture, the recognition of their adverse effects has resulted in a proliferation of caffeine-free products and efforts to discourage cigarette smoking.

A number of stimulants, however, are under the regulatory control of the CSA. Some of these controlled substances are available by prescription for legitimate medical use in the treatment of obesity, narcolepsy, and attention deficit disorders. As drugs of abuse, stimulants are frequently taken to produce a sense of exhilaration, enhance self esteem, improve mental and physical performance, increase activity, reduce appetite, produce prolonged wakefulness, and to "get high." They are among the most potent agents of reward and reinforcement that underlie the problem of dependence.

Stimulants are diverted from legitimate channels and clandestinely manufactured exclusively for the illicit market. They are taken orally, sniffed, smoked, and injected. Smoking, snorting, or injecting stimulants produce a sudden sensation known as a "rush" or a "flash." Abuse is often associated with a pattern of binge use--sporadically consuming large doses of stimulants over a short period of time. Heavy users may inject themselves every few hours, continuing until they have depleted their drug supply or reached a point of delirium, psychosis, and physical exhaustion. During this period of heavy use, all other interests become secondary to recreating the initial euphoric rush. Tolerance can develop rapidly, and both physical and psychological dependence occur. Abrupt cessation, even after a brief two- or three-day binge, is commonly followed by depression, anxiety, drug craving, and extreme fatigue known as a "crash."

Therapeutic levels of stimulants can produce exhilaration, extended wakefulness, and loss of appetite. These effects are greatly intensified when large doses of stimulants are taken. Physical side effects, including dizziness, tremor, headache, flushed skin, chest pain with palpitations, excessive sweating, vomiting, and abdominal cramps, may occur as a result of taking too large a dose at one time or taking large doses over an extended period of time. Psychological effects include agitation, hostility, panic, aggression, and suicidal or homicidal tendencies. Paranoia, sometimes accompanied by both auditory and visual hallucinations, may also occur. Overdose is often associated with high fever, convulsions, and cardiovascular collapse. Because accidental death is partially due to the effects of stimulants on the body's cardiovascular and temperature-regulating systems, physical exertion increases the hazards of stimulant use.

Cocaine

Cocaine, the most potent stimulant of natural origin, is extracted from the leaves of the coca plant (Erythroxylum coca), which is indigenous to the Andean highlands of South America. Natives in this region chew or brew coca leaves into a tea for refreshment and to relieve fatigue, similar to the customs of chewing tobacco and drinking tea or coffee.

Pure cocaine was first isolated in the 1880s and used as a local anesthetic in eye surgery. It was particularly useful in surgery of the nose and throat because of its ability to provide anesthesia, as well as to constrict blood vessels and limit bleeding. Many of its therapeutic applications are now obsolete due to the development of safer drugs.

Illicit cocaine is usually distributed as a white crystalline powder or as an off-white chunky material. The powder, usually cocaine hydrochloride, is often diluted with a variety of substances, the most common being sugars such as lactose, inositol, and mannitol, and local anesthetics such as lidocaine. The adulteration increases the volume and thus multiplies profits. Cocaine hydrochloride is generally snorted or dissolved in water and injected. It is rarely smoked because it is heat labile (destroyed by high temperatures).

"Crack," the chunk or "rock" form of cocaine, is a ready-to-use freebase. On the illicit market, it is sold in small, inexpensive dosage units that are smoked. Smoking delivers large quantities of cocaine to the lungs, producing effects comparable to intravenous injection. Drug effects are felt almost immediately, are very intense, and are quickly over. Once introduced in the mid-1980s, crack abuse spread rapidly and made the cocaine experience available to anyone with $10 and access to a dealer. In addition to other toxicities associated with cocaine abuse, cocaine smokers suffer from acute respiratory problems including cough, shortness of breath, and severe chest pains with lung trauma and bleeding. It is noteworthy that the emergence of crack was accompanied by a dramatic increase in drug abuse problems and drug-related violence.

The intensity of the psychological effects of cocaine, as with most psychoactive drugs, depends on the dose and rate of entry to the brain. Cocaine reaches the brain through the snorting method in three to five minutes. Intravenous injection of cocaine produces a rush in 15 to 30 seconds, and smoking produces an almost immediate intense experience. The euphoric effects of cocaine are almost indistinguishable from those of amphetamine, although they do not last as long. These intense effects can be followed by a dysphoric crash. To avoid the fatigue and the depression of coming down, frequent repeated doses are taken. Excessive doses of cocaine may lead to seizures and death from respiratory failure, stroke, or heart failure. There is no specific antidote for cocaine overdose.

Cocaine is the second most commonly used illicit drug (following marijuana) in the United States. According to the 2003 National Survey on Drug Use and Health, more than 34 million Americans (14.7%) age 12 or older had used cocaine at least once in their lifetime. There are no drugs approved for replacement-pharmacotherapy (drugs taken on a chronic basis as a substitute for the abused drug, like methadone for heroin addiction). Cocaine addiction treatment relies heavily on psychotherapy and drugs like antidepressants to relieve some of the effects of cocaine abuse.

	1. Coca farmers, known as "campesinos," cultivate plants throughout the Andean region of South America.
	2. Depending on the method and variety of coca used, coca plants may take up to two years to mature fully.
	3. Once harvested, coca leaves are sometimes allowed to dry in the sun to keep the leaves from rotting.
	4. Cocaine base processors stomp the coca leaves to macerate the leaves and help extract desired alkaloids.
	5. The solution is transferred by bucket to a second plastic lined pit, where lime or cement is added.
	6. Gasoline is then added to the basic solution and mixed.
	7. Cocaine hydrochloride (HCl) is produced through further refining and processing the cocaine base.
	8. Cocaine HCl is the final product exported from South America.
	9. Crack cocaine is made in the U.S. from several basic household products and cocaine HCl.

Amphetamines

Amphetamine, dextroamphetamine, methamphetamine, and their various salts, are collectively referred to as amphetamines. In fact, their chemical properties and actions are so similar that even experienced users have difficulty knowing which drug they have taken.

Amphetamine was first marketed in the 1930s as Benzedrine® in an over-the-counter inhaler to treat nasal congestion. By 1937, amphetamine was available by prescription in tablet form and was used in the treatment of the sleeping disorder, narcolepsy, and the behavioral syndrome called minimal brain dysfunction, which today is called attention deficit hyperactivity disorder (ADHD). During World War II, amphetamine was widely used to keep the fighting men going and both dextroamphetamine (Dexedrine®) and methamphetamine (Methedrine®) were readily available.

DEA Special Agents and chemists conduct a raid on a clandestine methamphetamine lab.

As use of amphetamines spread, so did their abuse. In the 1960s, amphetamines became a perceived remedy for helping truckers to complete their long routes without falling asleep, for weight control, for helping athletes to perform better and train longer, and for treating mild depression. Intravenous amphetamines, primarily methamphetamine, were abused by a subculture known as "speed freaks." With experience, it became evident that the dangers of abuse of these drugs outweighed most of their therapeutic uses.

Increased control measures were initiated in 1965 with amendments to the federal food and drug laws to curb the black market in amphetamines. Many pharmaceutical amphetamine products were removed from the market including all injectable formulations, and doctors prescribed those that remained less freely. Recent increases in medical use of these drugs can be attributed to their use in the treatment of ADHD. Amphetamine products presently marketed include generic and brand name amphetamine (Adderall®, Dexedrine®, Dextrostat®) and brand name methamphetamine (Desoxyn®). Amphetamines are all controlled in Schedule II of the CSA.

To meet the ever-increasing black market demand for amphetamines, clandestine laboratory production has mushroomed. Today, most amphetamines distributed to the black market are produced in clandestine laboratories. Methamphetamine laboratories are, by far, the most frequently encountered clandestine laboratories in the United States. The ease of clandestine synthesis, combined with tremendous profits, has resulted in significant availability of illicit methamphetamine, especially on the West Coast, where abuse of this drug has increased dramatically in recent years. Large amounts of methamphetamine are also illicitly smuggled into the United States from Mexico.

Amphetamines are generally taken orally or injected. However, the addition of "ice," the slang name for crystallized methamphetamine hydrochloride, has promoted smoking as another mode of administration. Just as "crack" is smokable cocaine, "ice" is smokable methamphetamine. Methamphetamine, in all its forms, is highly addictive and toxic.

The effects of amphetamines, especially methamphetamine, are similar to cocaine, but their onset is slower and their duration is longer. In contrast to cocaine, which is quickly removed from the brain and is almost completely metabolized, methamphetamine remains in the central nervous system longer, and a larger percentage of the drug remains unchanged in the body, producing prolonged stimulant effects. Chronic abuse produces a psychosis that resembles schizophrenia and is characterized by paranoia, picking at the skin, preoccupation with one's own thoughts, and auditory and visual hallucinations. These psychotic symptoms can persist for months and even years after use of these drugs has ceased and may be related to their neurotoxic effects. Violent and erratic behavior is frequently seen among chronic abusers of amphetamines, especially methamphetamine.

Methcathinone

Methcathinone, known on the streets as "Cat," is a structural analogue of methamphetamine and cathinone. Clandestinely manufactured, methcathinone is almost exclusively sold in the stable and highly water soluble hydrochloride salt form. It is most commonly snorted, although it can be taken orally by mixing it with a beverage or diluted in water and injected intravenously. Methcathinone has an abuse potential equivalent to methamphetamine and produces amphetamine-like effects. It was placed in Schedule I of the CSA in 1993.

Methylphenidate

Methylphenidate, a Schedule II substance, has a high potential for abuse and produces many of the same effects as cocaine and the amphetamines. The abuse of this substance has been documented among narcotic addicts who dissolve the tablets in water and inject the mixture. Complications arising from this practice are common due to the insoluble fillers used in the tablets. When injected, these materials block small blood vessels, causing serious damage to the lungs and retina of the eye. Binge use, psychotic episodes, cardiovascular complications, and severe psychological addiction have all been associated with methylphenidate abuse.

Methylphenidate is used legitimately in the treatment of excessive daytime sleepiness associated with narcolepsy, as is the newly marketed Schedule IV stimulant, modafinil (Provigil®). However, the primary legitimate medical use of methylphenidate (Ritalin®, Methylin®, Concerta®) is to treat attention deficit hyperactivity disorder (ADHD) in children. The increased use of this substance for the treatment of ADHD has paralleled an increase in its abuse among adolescents and young adults who crush these tablets and snort the powder to get high. Abusers have little difficulty obtaining methylphenidate from classmates or friends who have been prescribed it.

Anorectic Drugs

A number of drugs have been developed and marketed to replace amphetamines as appetite suppressants. These anorectic drugs include benzphetamine (Didrex®), diethylproprion (Tenuate®, Tepanil®), mazindol (Sanorex®, Mazanor®), phendimetrazine (Bontril®, Prelu-27®), and phentermine (Lonamin®, Fastin®, Adipex®). These substances are in Schedule III or IV of the CSA and produce some amphetamine-like effects. Of these diet pills, phentermine is the most widely prescribed and most frequently encountered on the illicit  market. Two Schedule IV anorectics often used in combination with phentermine, fenfluramine and dexfenfluramine, were removed from the U.S. market because they were associated with heart valve problems.

Khat

For centuries, khat, the fresh young leaves of the Catha edulis shrub, has been consumed where the plant is cultivated, primarily East Africa and the Arabian Peninsula. There, chewing khat predates the use of coffee and is used in a similar social context. Chewed in moderation, khat alleviates fatigue and reduces appetite. Compulsive use may result in manic behavior with grandiose delusions or in a paranoid type of illness, sometimes accompanied by hallucinations. Khat has been smuggled into the United States and other countries from the source countries for use by emigrants. It contains a number of chemicals, among which are two controlled substances, cathinone (Schedule I) and cathine (Schedule IV). As the leaves mature or dry, cathinone is converted to cathine, which significantly reduces its stimulatory properties.

Stimulants Identification