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Handle with Care: Popular Stimulants

Stimulants have been around the block a few times. Since prehistory, people have used a variety of substances to energize, motivate, and inspire. Native North Americans smoked tobacco, the natives of the Andes chewed coca leaves, and Indians and Chinese drank tea. And then there are our Western offerings: sugar, tea, coffee, cigarettes, and stimulant drugs. Even some medications for the relief of headaches, such as Anacin, contain caffeine. Other caffeine tablets, such as Dexatrine, are sold outright as stimulants. In this section we will explore the effects of these substances, as well as their caffeine-containing cousins: chocolate, guarana, maté, and kola nut. We'll also look at ephedra (ma huang) and yohimbe.

They may be popular, but stimulants are also problematic. All stimulants work by mimicking or triggering the release of the three primary neurotransmitters: dopamine, adrenaline, and noradrenaline. That's what makes you feel motivated and high. We learned earlier how downregulation in the brain eventually puts a stop to the fun of getting high. The exact same thing happens with stimulants: overstimulation leads to downregulation, causing the receptor sites to shut down. You keep needing more of the product for the same effect. But how much is too much? And are there some stimulants we can take safely in moderation?

While a substance can make us feel good in the moment, in the long term it can actually be harmful. In one short-term experiment, coffee was shown to heighten alertness (as if we didn't know!), but the researchers weren't looking at the memory impairment or increased blood pressure in habitual coffee drinkers. Also, researchers are not always without bias and may interpret results to fit their preconceptions or desired outcome.

We'll deal with these issues as we discuss each substance in detail. But for now, we can say that some stimulants are never recommended, while others can be acceptable in moderation, depending on the situation.

Popular Stimulants
Sugar: Toxic Treat
Sugar is a fairly recent entry into the stimulant game. Of course, it's always been available in natural sources such as fruit, with its slow-releasing fructose, balanced by the fiber content. Refined sugar, however, only came in with the Industrial Revolution. Today, we can hardly picture a celebration without sweet treats – birthday and wedding cakes, Halloween candy, and Christmas candy canes. Every religion and culture have their celebratory sweets.

How can such a delicious and seemingly harmless treat be so damaging? Stripped of its fiber and nutrients, highly refined sugar is rapidly absorbed and broken down into molecules of glucose that quickly reach the brain to produce feelings of "comfort" or "energy." Sugar binging looks a lot like any other addiction – tolerance develops, and you need more to get the same effect. How serious is that?

Downside of Sugar Excess sugar is bad for you. While sugar is valuable fuel for our cells, it can be toxic when consumed in excess, often causing damage to the arteries, kidneys, eyes, and nerves. The body tries to get it out of the blood and into storage as quickly as possible, but this can then cause a "rebound" low blood-sugar effect with its own set of problems. Some people feel stimulated immediately after eating it, then become cranky and finally go into a low blood-sugar slump.

Caffeine: Brewing Up Trouble
Found in more than one hundred plants throughout the world, caffeine is consumed primarily in beverages. A half-dozen caffeine-containing plants are more widely used than all other herbal materials combined!

More than a thousand years ago, Muslims used coffee for religious rituals. Finally reaching Europe in the seventeenth century, it was seen by the authorities as a dangerous drug. Nonetheless, coffeehouses spread, as did dependence on this new drug. The rest is history. Together with tea, it comprises 97 percent of worldwide caffeine consumption. Some parts of the world use other forms of caffeine – guarana, maté, and kola nut – which are now becoming more popular in the West.

Caffeine was first isolated from coffee in 1821. The effects of coffee are more potent than those of caffeine alone, since it contains two other stimulants – theophylline and theobromine. These weaker versions of caffeine are also found in decaffeinated coffee. All three are xanthines, alkaloid compounds that occur in both plants and animals.

The main reason we drink caffeine is that it boosts mood and energy. It does this by blocking the receptors for a brain chemical called adenosine, whose function is to stop dopamine release. With less adenosine activity, then, you increase dopamine and adrenaline. You feel alert, motivated, and stimulated, though some people will feel uncomfortable and jittery. Caffeine reaches its peak concentration in 30-60 minutes, after which it is inactivated by the liver, with only half its peak level left after 4-6 hours.

So where's the danger? Caffeine is addictive. Research shows that consuming as little as 100 mg a day can lead to withdrawal symptoms when you stop, including headache, fatigue, difficulty concentrating, and drowsiness. It's worth knowing that, while a small cup of instant coffee may contain less than 100 mg of caffeine, a large cup of "designer" coffee can contain as much as 500 mg – five times the "addictive" dose. Even more chemicals are used in manufacturing decaffeinated coffee, and, in the end, it still contains traces of caffeine – about 0.5 mg per 8-ounce cup.

Downside of Caffeine

At best, we can say that coffee has minor short-term mental and emotional benefits but that these are not sustained. A study published in the American Journal of Psychiatry observed 1,500 psychology students divided into four categories depending on their coffee intake: abstainers; low consumers (1 cup or equivalent a day); moderate (1-5 cups a day); and high (5 cups or more a day). On psychological testing, the moderate and high consumers had higher levels of anxiety and depression than the abstainers, and the high consumers had higher incidence of stress-related medical problems coupled with lower academic performance.

The bottom line? Drink coffee in moderation, if at all.

Tea: Not So Refreshing
Tea (Camellia sinensis) has been a favorite stimulant in many countries for centuries. Black tea is prepared by the initial slow drying of the fresh leaves, which allows them to begin to ferment, while for green tea, the leaves are dried quickly. Both contain caffeine.

The drinking of tea began in ancient Asia, and by the seventeenth century, the beverage had been adopted as Britain's standard refresher. By the early nineteenth century, as we've seen, tea had become a highly sought-after stimulant in the newly industrializing society, providing energy to goad the workers into faster production. And as tea required lots of sugar to enhance its bitter taste, the economy got another boost from sugar sales.

Tea continues to be a significant pick-me-up and social ritual in Britain, where tea consumption is four times that of coffee. In the United States, the figures are reversed. You can guess why by recalling the historic Boston Tea Party, which preceded the American Revolution. Rather than pay a tea tax to their oppressors across the sea, the colonists dumped boxes of imported tea from British trade ships into the harbor – and haven't had much taste for it since.

Tea's stimulating effects come from the same compounds as in coffee – caffeine, theobromine, and theophylline. Because of different methods of preparation and the many varieties of the cultivated plant, the average caffeine content of tea ranges widely from about 1 percent to more than 4 percent. The downsides of drinking tea are mentioned below. However, green tea does have some redeeming features.

Downside of Tea A strong cup of tea contains as much caffeine as a weak cup of coffee. Also, the tannin content of tea interferes with the absorption of minerals.

The Cola Generation
Cola drinks contain about one-quarter to one-half of the caffeine found in a weak cup of coffee. One cola drink even contained small amounts of coca (cocaine) in its original formula, hence the name, Coca-Cola. We also have non-cola caffeinated soft drinks such as Mountain Dew. Today's drinks generally contain sugar and colorings, which are also stimulants. Maybe worse, diet drinks contain the artificial sweetener aspartame (Nutrasweet), which can be toxically overstimulating to the brain. We have seen people who thought they were "going crazy" with jitters, insomnia, and disordered thinking magically recover when they stopped drinking diet sodas. Ironically, although touted as a diet product, these drinks can actually cause weight gain. See http://www.dorway.com/blayenn.html for scientific information on aspartame.

More recently, new soft drinks have been introduced that push up the levels of caffeine they contain, boosting both their kick and addictiveness. Shades of the tobacco industry! With names such as Jolt or Red Bull, their caffeine content can equal or even surpass that of a cup of coffee. Children and young people are drinking large amounts of caffeinated soft drinks, especially relative to their weight, exposing their developing brains and bodies to a hazardous substance. Never mind illicit drugs – junk food and caffeinated drinks can lead to serious health problems and addictions in children.

Downside of Colas

Caffeine Buzzometer (Caffeine Levels of Common Products)
Product Caffeine Content (per serving)
Coca-Cola Classic 350 ml (12 fl oz) 45 mg
Diet Coke 350 ml (12 floz) 45 mg
Red Bull 250 ml (8.3 fl oz) 80 mg
Hot cocoa 150 ml (5 fl oz) 10 mg
Coffee, instant 150 ml (5 fl oz) 40-105 mg
Espresso, cappuccino, or latte (single) 30-50 mg
Coffee, filter 150 ml (5 fl oz) 110-150 mg
Coffee, Starbucks grande 500 mg
Coffee, decaffeinated 150 ml (5 fl oz) 0.3 mg
Tea 150 ml (5 fl oz) 20-100 mg
Green tea 150ml (5 fl oz) 15-30 mg
Chocolate cake (1 slice) 20-30 mg
Bittersweet chocolate (1 oz) 5-35 mg
Excedrin (2 tablets) 130 mg
NoDoz (2 capsules) 200 mg
Dexatrim (1 500-mg capsule) 80 mg

Death by Chocolate?
Chocolate's major active ingredient is cocoa, a significant source of the stimulant theobromine. Research by British psychologist, Dr. David Benton at the University of Wales in Swansea, found chocolate to be an excellent mood elevator. When he played sad music to a group of students, their moods sank. He then offered them the choice of milk chocolate or carob, a natural chocolate substitute that is similar in taste. Without their knowing which product they were eating, the participants found that the chocolate raised their moods, while the carob didn't. Moreover, as their moods fell, their cravings for chocolate increased.

In addition to theobromine – which is also found in tea and coffee – chocolate also contains the mood-enhancing stimulant phenethylamine. Both theobromine and phenethylamine stimulate dopamine production. Even experimental alcohol-loving rats, when given the choice, will replace some of their alcohol intake with chocolate.

A recent study of mice and rats shows that dopamine kick-starts a brain messenger chemical called DARP-32, which in turn activates hormones that make females more interested in sex. Without even knowing about DARP-32, generations of lonely, frustrated men and women have binged on chocolate, with sometimes surprising results. Valentine's Day chocolates say it all.

The bad news? Too much chocolate, especially the highly sweetened kind, causes all the problems of going overboard on sugar, including weight gain. Chocolate is often high in fats, too. The addictive nature of chocolate suggests the development of tolerance, and "just one piece of chocolate" becomes, instead, "just one more." In addition, like coffee, cocoa beans are often grown in countries where pesticide use is unregulated, exposing the consumer to cancer-causing compounds.

If you are going to eat chocolate, eat the pure, dark, preferably organic type, not cheap bars full of fat and sugar. But, as with any stimulant, if you eat chocolate every day, or find yourself craving it, you've gone too far. Keep chocolate as a special treat, not a daily ritual.

Downside of Chocolate

Guarana, Maté, Kola Nut: Caffeine by Any Other Name
The name guarana conjures up exotic images of tribal people in the Amazonian rain forests, living in harmony with nature. And if it's "natural," it must be good for you. Right? Well, not exactly. The seeds and leaves of the guarana plant, a climbing shrub native to Brazil and Uruguay, are high in caffeine.

Once a traditional social drink, appetite suppressant, and aphrodisiac, guarana is used extensively in South America today in soft drinks. Because it contains saponins – compounds found in ginseng – native preparations may possess tonic or balancing properties. They are less irritating to the gastrointestinal tract than say, coffee, and also have a mild and long-lasting effect. This is probably due to the presence of fats and oils in the seeds, which prolong absorption. On the other hand, most commercially prepared products are absorbed and used up in the body as quickly as a cup of coffee. Once again, the closer we stick to the natural form of a product, the healthier it is for us.

A dried paste made chiefly from the crushed seed of guarana has a relatively high caffeine content, ranging from 2.5 to 5 percent, and averaging about 3.5 percent. To determine how much caffeine is in any product, you must do your math: multiply the total weight of the capsule or powder by the percentage of caffeine or guarana to get the number of milligrams of caffeine per dose.

The conclusion regarding its use? Like tea or coffee, guarana can be overstimulating and have the same ill effects. In a dilute, milder form, guarana can be used as an occasional pick-me-up for those whose adrenal status is healthy – that is, not suffering from stress or burnout.

Another traditional South American stimulant is the jungle tea maté (pronounced "ma-tay"). The dried leaves of this low-growing bush are brewed into a hot drink. Besides low concentrations of caffeine, maté contains theophylline (0.05 percent), theobromine (0.1 to 2 percent), tannins, vitamins, and minerals. At 15-25 mg of caffeine per cup, as in green tea, maté is used for enhancing alertness and concentration. It can be useful on occasion, certainly better than most stimulants mentioned here. As with any stimulant, excessive use can tax the adrenal glands.

Kola nut is used as an aphrodisiac, probably working the same way as chocolate. The nut (Cola nitida) is a seed kernel related to the cacao tree, and is native to the rain forests of West Africa. It is also cultivated in the West Indies and other tropical areas. Containing up to 3 percent caffeine, its stimulant properties were originally derived from chewing on the seeds. Kola nut is now available as tea made of ground seeds. Kola nut was the "cola" part of coke, which, as we mentioned earlier, also originally contained coca extract. Cola drinks now get their kick from synthesized or extracted caffeine plus sugar.

Downsides of Guarana, Maté, and Kola Nut

Ephedra (Ma Huang): Life in the Fast Lane
Though a traditional remedy with a long history of medical use, ephedra has recently become a controversial herb – within both the natural products industry and government regulatory agencies – because of its misuse. Called ma huang (Ephedra sinica), this ancient Chinese remedy triggers the release of adrenaline, the hormone that mediates the stress response. Since the stress response also causes an initial surge in energy, as well as suppression of appetite, ephedra is often used for both quick energy and weight loss. One study found that it worked better than Redux, a weight loss drug that was later withdrawn from the market because of its toxic effects. A 1996 study found that a combination of 30 mg of ephedra, 100 mg of caffeine, and 300 mg of aspirin promoted fat-burning. Ephedra is also used as a decongestant, most commonly as ephedrine, a more potent and longer-lasting synthetic version of ephedra.

Ephedra is also used by some for recreation. Advertised as "herbal Ecstasy," ephedra actually has little in common with the entheogen Ecstasy, or MDMA. Rather, what's marketed as herbal Ecstasy is generally a combination of ephedra and caffeine – both in high doses – which causes a "rush" that is stimulating and energizing. The high-dose combination can be dangerous, however, producing a rapid heart rate and a rise in blood pressure with accompanying headache, dizziness, and, on rare occasions, even death.

Having the right information will help you choose whether or not to use ephedra. Doses of ephedra should not exceed 8 mg per dose or 24 mg per day. If used at all, ephedra should be taken for short periods of time – days, not weeks or months. Athletes often use ephedra as a stimulant, and while it may increase exercise tolerance, the risk of heart problems is certainly not worth it. We have already seen young athletes, perhaps with undiagnosed preexisting heart problems, have a sudden heart arrhythmia, some fatal, in association with taking ephedra-containing supplements. Nor is it advised for people with diabetes, heart conditions, or those who are energy depleted, recovering from any illness, suffering from a weak constitution, or just hypersensitive to it.

Downside of Ephedra Below are some of the negative side effects associated with ephedra at higher than the recommended doses:

Contraindications Ephedra should not be taken by children, pregnant or breast-feeding women, or people with diabetes, high blood pressure, heart problems, thyroid problems, or psychiatric disorders. Consult with a health-care practitioner prior to use if you have difficulty urinating, prostate enlargement, or glaucoma, or are using any prescription drug. It should not be taken in combination with the so-called "MAOI" antidepressant drugs, or cold medication containing ephedrine pseudoephedrine, or phenylpropanolamine. Discontinue if sleepiness, dizziness, loss of appetite, or nausea occurs.

The natural products industry has taken action to educate the public and to provide quality, safe products. Such organizations include the Ephedra Committee of the American Herbal Products Association and the American Botanical Council. Many countries restrict the use of ephedra. The Canadian health agency recently recalled all ephedra products that make weight-loss or stimulant claims, that are manufactured in combination with stimulants (e.g., caffeine and caffeine-containing herbs), or that exceed the federal dosage levels (i.e., more than 8 mg of ephedrine per dose, 25 mg per day, and recommended for longer than a seven-day period). Ephedra/ephedrine products that are marketed as traditional medicines or are sold as nasal decongestants continue to be available, provided that they comply with the federal dosage levels and do not contain caffeine.

In the U.K., ephedra is available only by prescription by registered herbalists and pharmacists. In the United States, ephedra is currently available without prescription. Due to adverse events reports, the F.D.A. has proposed dosage limits and is considering other restrictions including an outright ban of the herb. In the summer of 2001, the New England Journal of Medicine released a study of the effects of ephedra six months early because the Journal considered the findings sufficiently negative and important.

Yohimbe: The Sexy Herb
The traditional African herb yohimbe is as controversial a stimulant as ephedra. In its extracted alkaloid form, yohimbine, it is used not only as a mood enhancer and weight-loss product but also as a male aphrodisiac. In fact, yohimbine hydrochloride in 5.4-mg tablets is prescribed by doctors to treat impotence.

Yohimbe enhances the stimulant neurotransmitters, dopamine and nor- adrenaline. As with other stimulants, it affects people differently. For some, there is a pleasant enhancement of the senses, an increase in empathy and communication, and enhanced sexual arousal. Men can have longer-lasting erections and powerful ejaculations. But others feel uncomfortably stimulated, with rapid heart rate, headache, anxiety, and insomnia. Yohimbe can also cause a dangerous rise in blood pressure.

The bottom line? Yohimbe appears safe for occasional use, with the proper precautions. It should not be taken by those with any cardiovascular condition.

Downside of Yohimbe
In susceptible individuals, it can cause uncomfortable overstimulation – rapid heart rate, headache, anxiety, insomnia, and a dangerous rise in blood pressure. Avoid liver, cheeses, red wine, nasal decongestants, and diet aids.

Contraindications
Yohimbe should not be taken by people suffering from any cardiovascular condition, diabetes, or heart, liver, or kidney disease.

Definite No's: From Smoking To Speed
The Tobacco High
Together with caffeine and alcohol, nicotine is one of the three most widely used psychoactive drugs in our society. With no redeeming value, "smoking will continue as the leading cause of preventable, premature mortality for many years to come," according to the U.S. Surgeon General. In 1997, smoking killed 435,000 people in the United States alone.

Nicotine, the primary stimulant in cigarettes, has a significant effect, even in small doses. In fact, nicotine is such a powerful toxin that one cigar contains enough to kill several people (and not just from the smell)!

If you have ever smoked, can you recall the sensation of your first cigarette? It probably tasted terrible, burned your mouth and lungs (if you even inhaled), and made you feel nauseated and dizzy. Those are some of its toxic effects in action. After a few more smokes, your body no longer rebels. In fact, you rather like it. In short – you're hooked.

Nicotine has a complex series of actions, both stimulating and relaxing. It is more addictive than heroin – and is often the hardest addiction to break. Nicotine stimulates the adrenals to release adrenaline, raising blood pressure and heart rate, and increases gastrointestinal activity. Nicotine also acts as a muscle relaxant.

In the brain, nicotine activates the release of dopamine, exhibiting a stimulant effect similar to that of caffeine. It also has a short-term antidepressant effect, though this is most often followed by a rebound depression. In larger amounts, nicotine acts as a sedative, probably because of its effect on serotonin. People trying to kick the tobacco habit describe the accompanying tension and irritability as "feeling like you want to jump out of your skin." They also often experience low blood-sugar problems, which leads them to overeat and gain weight.

Cocaine: Ups and Downs
Cocaine is probably the best-known – and most powerful – illegal stimulant. The active ingredient of the coca plant, cocaine was first isolated in the West around 1860. The father of psychoanalysis, Sigmund Freud, personally experimented with the refined powdered drug and described cocaine as "magical." While the coca leaf typically contains between 0.1 and 0.9 percent cocaine, concentrated coca paste contains up to 60 to 80 percent pure cocaine. The drug works by blocking the reabsorption of dopamine, which leaves more in the synapse to interact with the receptors.

The coca leaf, as found in nature, is safely used by field laborers in the Andes to maintain energy. The concentrated drug, however, leads to an intense "rush," with enhanced mood, sensory awareness, self-confidence, and sexual interest. Unfortunately, this is generally followed by a crash into anxiety, depression, irritability, and exhaustion. If the vicious cycle of addiction ensues, there is an intense craving for the next hit, and users follow a downhill course of deteriorating physical and mental health – often emerging as severe depression, agitation, and even paranoia.

Amphetamines: Mother's Little Uppers
Popularly known as "speed," amphetamines have been used for years by long-distance truck drivers, students cramming for finals, and harried housewives needing a lift. Like cocaine, amphetamine blocks neurons' reabsorption of the neurotransmitters noradrenaline and dopamine, but it also triggers their release, doubling its potency.

Amphetamines were discovered in the 1930s and commonly prescribed by the 1960s. In contrast with little "happy pills," these were stimulating ones that allowed users to do more, focus better, and feel more energized – until the pill wore off and they needed another fix. These drugs were later used as diet pills and as a treatment for attention deficit disorder (ADD). We have seen how women with food cravings, weight problems, depression, and even ADD were given the perfect happy pill for their condition – until the prescription ran out.

Doctors thought they were helping these women but actually turned them into addicts. Legislation then became more rigorous, and in the 1980s, the number of these prescriptions fell. The 1990s brought a resurgence, with the mushrooming of medical diet centers, dispensing stimulants such as Fen-Phen and Redux, later found to be dangerous and subsequently removed from the market.

Chronic stimulant users find it difficult to relax, and so they use relaxants such as alcohol, sleeping pills, tranquilizers, and marijuana to bring them down. This addictive cycle impairs performance, promotes stress, and depletes energy.

Amphetamines such as dexedrine and its relative, Ritalin, continue to be prescribed for children with ADD. While stimulants may work for ADD in the short term, we have found that we can prescribe natural nutrients (including amino acids) that not only work just as well in many cases but also provide the missing elements, rather than just covering the symptoms. Children show marked improvements in both behavior and grades after strategic foods such as sugar (from breakfast cereals to doughnuts) and caffeine (in the form of cola drinks) are removed from their diet. A good resource on the subject is Marcia Zimmerman's The ADD Nutrition Solution (www.thenutritionsolution.com).

If you are well nourished and your chemistry is well balanced, there is simply no need – or, generally, no desire – to use any of these stimulants. Then, on the odd occasion when you really need an extra lift, a small amount will have a big effect. However, in the next section, we introduce natural alternatives without the costly downsides.

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From NATURAL HIGHS: Supplements, Nutrition, and Mind/Body Techniques to Help You Feel Good by Hyla Cass and Patrick Holford. Copyright © Hyla Cass, M.D., and Patrick Holford. Used by arrangement with Avery, a member of Penguin Group (USA) Inc.

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