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17.6: Drugs, Athletic Performance, and the Brain

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    Learning Objectives
    • Know the different supplements and drugs that are used to maintain or enhance athletic performance.
    • List the use and abuse of anabolic steroids.

    Protein

    Bodybuilders may supplement their diets with protein for reasons of convenience, lower cost (relative to meat and fish products) and to avoid the concurrent consumption of carbohydrates and fats. In addition, some argue that bodybuilders, by virtue of their unique training and goals, require higher-than-average quantities of protein to support maximal muscle growth; however there is no compelling evidence and no scientific consensus for bodybuilders to consume more protein than the recommended dietary allowance.

    19A14.jpg
    Figure \(\PageIndex{1}\): Protein milkshakes, made from protein powder (center) and milk (left), are a common bodybuilding supplement. (CC BY-SA 3.0; Sandstein).

    Protein supplements are sold in ready-to-drink shakes, bars, meal replacement products (see below), bites, oats, gels and powders. Protein powders are the most popular and may have flavoring added for palatability. The powder is usually mixed with water, milk or juice and is generally consumed immediately before and after exercising, or in place of a meal. The sources of protein are as follows, and differ in protein quality depending on their amino acid profile and digestibility:

    • Whey protein contains high levels of all the essential amino acids and branched-chain amino acids. It also has the highest content of the amino acid cysteine, which aids in the biosynthesis of glutathione. For bodybuilders whey protein provides amino acids used to aid in muscle recovery. Whey protein is derived from the process of making cheese from milk. There are three types of whey protein: whey concentrate, whey isolate, and whey hydrolysate. Whey concentrate is 29–89% protein by weight whereas whey isolate is 90%+ protein by weight. Whey hydrolysate is enzymatically predigested and therefore has the highest rate of digestion of all protein types. Whey protein is usually taken immediately before and after a workout
    • Casein protein (or milk protein) has glutamine, and casomorphin. Casein is usually taken before going to bed.
    • Soy protein from soybeans contain isoflavones, a type of phytoestrogen.
    • Egg-white protein is a lactose- and dairy-free protein.
    • Hemp protein from hemp seed, contains highly-digestible protein, and hemp oil is high in essential fatty acids.
    • Rice protein, when made from the whole grain, is a protein source that is highly digestible and allergen free. Since rice protein is low in the amino acid lysine, it is often combined with pea protein powder to achieve a superior amino acid profile.
    • Pea protein is a hypoallergenic protein with a lighter texture than most other protein powders. Pea protein has an amino acid profile similar to that of soy, but pea protein does not elicit concerns about unknown effects of phytoestrogens. Pea protein is also less allergenic than soy. Pea protein has high fiber content and has no allergic ingredients and therefore is easy for digestion as compared to whey protein. Pea protein is a slow digesting protein and is able to keep you full longer.

    Some nutritionists claim that osteoporosis may occur from excessive protein intake because protein can put pressure on the kidneys and lead to bone loss due to calcium leaching. However, some have suggested that higher calcium excretion may be due to a corresponding increase in protein-induced calcium absorption in the intestines. In addition to complete proteins, some supplements will contain protein fragments such as branched-chain amino acids or individual amino acids (such as glutamine). Amino acids are considered to be inferior to whole protein and have been used by some companies to artificially inflate and falsify protein values in their product (protein spiking). Many protein supplements explicitly indicate on the label that no protein spiking has occurred.

    Branched-chain amino acids

    Amino acids are the building blocks of protein; the body breaks consumed protein into amino acids in the stomach and intestines. Amino acids are classified as essential, conditionally essential and non-essential. There are three branched-chain amino acids (BCAAs): leucine, isoleucine, and valine. All three branched-chain amino acids are essential amino acids. Each has numerous benefits on various biological processes in the body. Unlike other amino acids, BCAAs are metabolized in the muscle and have an anabolic/anti-catabolic effect on it. There is some evidence that BCAA's may enhance muscle recovery after intense physical activity and no side effects have been reported at this time.

    Glutamine

    Glutamine is the most abundant amino acid found in human muscle and is commonly found in supplements or as a micronized, instantly soluble powder because supplement manufacturers claim the body's natural glutamine stores are depleted during anaerobic exercise. Some studies have shown there to be no significant effect of glutamine on bench press strength, knee-extension torque or lean muscle mass when compared to controls taking a placebo, though another study found that glutamine is beneficial in raising T-helper/suppressor cell ratio in long-distance runners.

    Essential fatty acids

    The essential fatty acids (alpha-linolenic acid and linoleic acid) may be important to supplement while bodybuilding; these cannot readily be made in the body, but are required for various functions within the body to take place. Fatty fish, such as fresh salmon and trout are rich in essential fatty acids and fish oils can also be taken in supplement form. Flaxseed oil, often sold as a supplement on its own, is an ideal source of alpha-Linolenic acid, which can also be found in walnuts and pumpkin seeds.

    Prohormone

    Prohormones are precursors to hormones and are most typically sold to bodybuilders as a precursor to the natural hormone testosterone. This conversion requires naturally occurring enzymes in the body. Side effects are not uncommon, as prohormones can also convert further into DHT and estrogen. To deal with this, many supplements also have aromatase inhibitors and DHT blockers such as chrysin and 4-androstene-3,6,17-trione. To date most prohormone products have not been thoroughly studied, and the health effects of prolonged use are unknown. Although initially available over the counter, their purchase was made illegal without a prescription in the US in 2004, and they hold similar status in many other countries. They remain legal, however, in the United Kingdom and the wider European Union. Their use is prohibited by most sporting bodies.

    Creatine

    Creatine is an organic acid naturally occurring in the body that supplies energy to muscle cells for short bursts of energy (as required in lifting weights) via creatine phosphate replenishment of ATP. A number of scientific studies have shown that creatine can improve strength, energy, muscle mass, and recovery times. In addition, recent studies have also shown that creatine improves brain function. and reduces mental fatigue.Unlike steroids or other performance-enhancing drugs, creatine can be found naturally in many common foods such as herring, tuna, salmon, and beef.

    19A15.jpg
    Figure \(\PageIndex{2}\): Skeletal formula of creatine

    Creatine increases what is known as cell volumization by drawing water into muscle cells, making them larger. This intracellular retention should not be confused with the common myth that creatine causes bloating (or intercellular water retention). Creatine is sold in a variety of forms, including creatine monohydrate and creatine ethyl ester, amongst others. Though all types of creatine are sold for the same purposes, there are subtle differences between them, such as price and necessary dosage. Some studies have suggested that consumption of creatine with protein and carbohydrates can have a greater effect than creatine combined with either protein or carbohydrates alone.

    β-Hydroxy β-methylbutyrate

    When combined with an appropriate exercise program, dietary supplementation with β-hydroxy β-methylbutyrate (HMB) has been shown to dose-dependently augment gains in muscle hypertrophy (i.e., the size of a muscle), muscle strength, and lean body mass, reduce exercise-induced skeletal muscle damage, and expedite recovery from high-intensity exercise. HMB is believed to produce these effects by increasing muscle protein synthesis and decreasing muscle protein breakdown by various mechanisms, including activation of the mechanistic target of rapamycin (mTOR) and inhibition of the proteasome in skeletal muscles. The inhibition of exercise-induced skeletal muscle damage by HMB is affected by the time that it is used relative to exercise. The greatest reduction in skeletal muscle damage from a single bout of exercise appears to occur when calcium HMB is ingested 1–2 hours prior to exercise.

    Thermogenic products

    A thermogenic is a broad term for any supplement that the manufacturer claims will cause thermogenesis, resulting in increased body temperature, increased metabolic rate, and consequently an increased rate in the burning of body fat and weight loss. Until 2004 almost every product found in this supplement category comprised the "ECA stack": ephedrine, caffeine and aspirin. However, on February 6, 2004 the Food and Drug Administration (FDA) banned the sale of ephedra and its alkaloid, ephedrine, for use in weight loss formulas. Several manufacturers replaced the ephedra component of the "ECA" stack with bitter orange or citrus aurantium (containing synephrine) instead of the ephedrine.

    Controversies of Fitness Supplements

    Mislabeling: According to University of Helsinki food safety professor Marina Heinonen, more than 90% of dietary supplement health claims are incorrect. While many of the claims are based on scientifically based physiological or biochemical processes, their use in bodybuilding parlance is often heavily colored by bodybuilding lore and industry marketing and as such may deviate considerably from traditional scientific usages of the terms. In addition, ingredients listed have been found at times to be different from the contents. In 2015, Consumer Reports reported unsafe levels of arsenic, cadmium, lead and mercury in several of the protein powders that were tested. Other studies in 2013 showed that one-third of the supplements tested contained unlisted steroids. In 2015 a CBC investigative report found that protein spiking (the addition of amino acid filler to manipulate analysis) was not uncommon, however many of the companies involved challenged these claims.

    Health problems: The US FDA reports 50,000 health problems a year due to dietary supplements and these often involve bodybuilding supplements. For example, the "natural" best-seller Craze, 2012's "New Supplement of the Year" by bodybuilding.com, sold in Walmart, Amazon etc., was found to contain undisclosed amphetamine-like compounds. Also other products by Matt Cahill have contained dangerous substances causing blindness or liver damages, and experts say that Cahill is emblematic for the whole industry.

    Liver damage: The incidence of liver damage from dietary supplements has tripled in a decade, the majority of these involved bodybuilding supplements. This resulted in liver transplants and, in some cases, death to the patient. Some have argued that the liver damage is more often caused by prescription drugs rather than supplements.

    Lack of effectiveness: In addition to being potentially harmful, some have argued that there is little evidence to indicate any benefit to using bodybuilding supplements. For example, according to the IOC, no consensus had been reached in determining whether an individual in exercise training benefits from protein and amino acid supplements. "In view of the lack of compelling evidence to the contrary, no additional dietary protein is suggested for healthy adults undertaking resistance or endurance exercise".

    Caffeine and Athletic Performance

    Caffeine is a proven ergogenic aid in humans. Caffeine improves athletic performance in aerobic (especially endurance sports) and anaerobic conditions. Moderate doses of caffeine (around 5 mg/kg) can improve sprint performance, cycling and running time trial performance, endurance (i.e., it delays the onset of muscle fatigue and central fatigue), and cycling power output. Caffeine increases basal metabolic rate in adults. Caffeine ingestion prior to aerobic exercise increases fat oxidation, particularly in persons with low physical fitness.

    Caffeine improves muscular strength and power, and may enhance muscular endurance. Caffeine also enhances performance on anaerobic tests. Caffeine consumption before constant load exercise is associated with reduced perceived exertion. While this effect is not present during exercise-to-exhaustion exercise, performance is significantly enhanced. This is congruent with caffeine reducing perceived exertion, because exercise-to-exhaustion should end at the same point of fatigue. Caffeine also improves power output and reduces time to completion in aerobic time trials, an effect positively (but not exclusively) associated with longer duration exercise.

    Anabolic Steroids

    Anabolic steroids are synthetic, or human-made, variations of the male sex hormone testosterone. The proper term for these compounds is anabolic-androgenic steroids. "Anabolic" refers to muscle building, and "androgenic" refers to increased male sex characteristics. Some common names for anabolic steroids are Gear, Juice, Roids, and Stackers. Health care providers can prescribe steroids to treat hormonal issues, such as delayed puberty. Steroids can also treat diseases that cause muscle loss, such as cancer and AIDS. But some athletes and bodybuilders misuse these drugs in an attempt to boost performance or improve their physical appearance.

    The majority of people who misuse steroids are male weightlifters in their 20s or 30s. Anabolic steroid misuse is much less common in women. It is difficult to measure steroid misuse in the United States because many national surveys do not measure it. However, use among teens is generally minimal. The 2016 NIDA-funded Monitoring the Future study has shown that past-year misuse of steroids has declined among 8th and 10th graders in recent years, while holding steady for 12th graders.

    People who misuse anabolic steroids usually take them orally, inject them into muscles, or apply them to the skin as a gel or cream. These doses may be 10 to 100 times higher than doses prescribed to treat medical conditions.

    Commons patterns for misusing steroids include:

    • cycling—taking multiple doses for a period of time, stopping for a time, and then restarting
    • stacking—combining two or more different steroids and mixing oral and/or injectable types
    • pyramiding—slowly increasing the dose or frequency of steroid misuse, reaching a peak amount, and then gradually tapering off to zero
    • plateauing—alternating, overlapping, or substituting with another steroid to avoid developing a tolerance

    There is no scientific evidence that any of these practices reduce the harmful medical consequences of these drugs.

    How Anabolic Steroids Work

    Anabolic steroids work differently from other drugs of abuse; they do not have the same short-term effects on the brain. The most important difference is that steroids do not directly activate the reward system to cause a “high”; they also do not trigger rapid increases in the brain chemical dopamine, which reinforces most other types of drug taking behavior. Misuse of anabolic steroids might lead to negative mental effects, such as: paranoid (extreme, unreasonable) jealousy, extreme irritability and aggression (“roid rage”), delusions—false beliefs or ideas, impaired judgment, and mania. Aside from mental effects, steroid use commonly causes severe acne. It also causes the body to swell, especially in the hands and feet.

    Anabolic steroid misuse might lead to serious, even permanent, health problems such as kidney problems or failure, liver damage and tumors, enlarged heart, high blood pressure, and changes in blood cholesterol, all of which increase the risk of stroke and heart attack, even in young people, and increased risk of blood clots. Several other effects are gender- and age-specific:

    • In men: shrinking testicles, decreased sperm count, baldness, development of breasts, increased risk for prostate cancer
    • In women: growth of facial hair or excess body hair, decreased breast size, male-pattern baldness, changes in or stop in the menstrual cycle, enlarged clitoris, deepened voice
    • In teens: stunted growth (when high hormone levels from steroids signal to the body to stop bone growth too early) and stunted height (if teens use steroids before their growth spurt)

    Some of these physical changes, such as shrinking sex organs in men, can add to mental side effects such as mood disorders.

    Anabolic Steroids Addiction

    Even though anabolic steroids do not cause the same high as other drugs, they can lead to a substance use disorder. A substance use disorder occurs when a person continues to misuse steroids, even though there are serious consequences for doing so. The most severe form of a substance use disorder is addiction. People might continue to misuse steroids despite physical problems, high costs to buy the drugs, and negative effects on their relationships. These behaviors reflect steroids' addictive potential.

    Research has further found that some steroid users turn to other drugs, such as opioids, to reduce sleep problems and irritability caused by steroids. People who misuse steroids might experience withdrawal symptoms when they stop use, including:fatigue, restlessness, loss of appetite, sleep problems, decreased sex drive and steroid cravings.

    One of the more serious withdrawal symptoms is depression, which can sometimes lead to suicide attempts. Some people seeking treatment for anabolic steroid addiction have found a combination of behavioral therapy and medications to be helpful. In certain cases of addiction, patients have taken medicines to help treat symptoms of withdrawal. For example, health care providers have prescribed antidepressants to treat depression and pain medicines for headaches and muscle and joint pain. Other medicines have been used to help restore the patient's hormonal system.

    Drugs, Athletic Performance, and Drug Screening

    In competitive sports, doping is the use of banned athletic performance-enhancing drugs by athletic competitors. The term doping is widely used by organizations that regulate sporting competitions. The use of drugs to enhance performance is considered unethical, and therefore prohibited, by most international sports organizations, including the International Olympic Committee. Furthermore, athletes (or athletic programs) taking explicit measures to evade detection exacerbate the ethical violation with overt deception and cheating.

    The origins of doping in sports go back to the very creation of sport itself. From ancient usage of substances in chariot racing to more recent controversies in baseball and cycling, popular views among athletes have varied widely from country to country over the years. The general trend among authorities and sporting organizations over the past several decades has been to strictly regulate the use of drugs in sport. The reasons for the ban are mainly the health risks of performance-enhancing drugs, the equality of opportunity for athletes, and the exemplary effect of drug-free sport for the public. Anti-doping authorities state that using performance-enhancing drugs goes against the "spirit of sport".

    Many sports organizations have banned the use of performance-enhancing drugs and have very strict rules and penalties for people who are caught using them. The International Amateur Athletic Federation, now World Athletics, was the first international governing body of sport to take the situation seriously. In 1928 they banned participants from doping, but with little in the way of testing available they had to rely on the word of the athlete that they were clean. It was not until 1966 that FIFA and Union Cycliste Internationale (cycling) joined the IAAF in the fight against drugs, followed by the International Olympic Committee the following year. Progression in pharmacology has always outstripped the ability of sports federations to implement rigorous testing procedures but since the creation of the World Anti-Doping Agency in 1999, it has become more effective to catch athletes who use drugs. The first tests for athletes were at the 1966 European Championships and two years later the IOC implemented their first drug tests at both the Summer and Winter Olympics. Anabolic steroids became prevalent during the 1970s and after a method of detection was found they were added to the IOC's prohibited substances list in 1975, after which the 1976 Summer Olympics in Montreal were the first Olympic games which tested for them.

    Exercise and the Brain

    The neurobiological effects of physical exercise are numerous and involve a wide range of interrelated effects on brain structure, brain function, and cognition.[1][2][3][4]A large body of research in humans has demonstrated that consistent aerobic exercise (e.g., 30 minutes every day) induces persistent improvements in certain cognitive functions, healthy alterations in gene expression in the brain, and beneficial forms of neuroplasticity and behavioral plasticity; some of these long-term effects include: increased neuron growth, increased neurological activity (e.g., c-Fos and BDNF signaling), improved stress coping, enhanced cognitive control of behavior, improved declarative, spatial, and working memory, and structural and functional improvements in brain structures and pathways associated with cognitive control and memory.[1][2][3][4][5][6][7][8][9][10] The effects of exercise on cognition have important implications for improving academic performance in children and college students, improving adult productivity, preserving cognitive function in old age, preventing or treating certain neurological disorders, and improving overall quality of life.[1][11][12]

    In healthy adults, aerobic exercise has been shown to induce transient effects on cognition after a single exercise session and persistent effects on cognition following regular exercise over the course of several months.[1][10][13] People who regularly perform aerobic exercise (e.g., running, jogging, brisk walking, swimming, and cycling) have greater scores on neuropsychological function and performance tests that measure certain cognitive functions, such as attentional control, inhibitory control, cognitive flexibility, working memory updating and capacity, declarative memory, spatial memory, and information processing speed.[1][5][7][9][10][13] The transient effects of exercise on cognition include improvements in most executive functions (e.g., attention, working memory, cognitive flexibility, inhibitory control, problem solving, and decision making) and information processing speed for a period of up to 2 hours after exercising.[13]

    Aerobic exercise induces short- and long-term effects on mood and emotional states by promoting positive affect, inhibiting negative affect, and decreasing the biological response to acute psychological stress.[13] Over the short-term, aerobic exercise functions as both an antidepressant and euphoriant,[14][15][16][17] whereas consistent exercise produces general improvements in mood and self-esteem.

    Regular aerobic exercise improves symptoms associated with a variety of central nervous system disorders and may be used as an adjunct therapy for these disorders. There is clear evidence of exercise treatment efficacy for major depressive disorder and attention deficit hyperactivity disorder.[11][16][20][21][22][23] The American Academy of Neurology's clinical practice guideline for mild cognitive impairment indicates that clinicians should recommend regular exercise (two times per week) to individuals who have been diagnosed with this condition.[24] Reviews of clinical evidence also support the use of exercise as an adjunct therapy for certain neurodegenerative disorders, particularly Alzheimer’s disease and Parkinson's disease. Regular exercise is also associated with a lower risk of developing neurodegenerative disorders.[28][31] A large body of preclinical evidence and emerging clinical evidence supports the use of exercise as an adjunct therapy for the treatment and prevention of drug addictions. Regular exercise has also been proposed as an adjunct therapy for brain cancers.[37]

    Endorphins play a major role in the body's inhibitory response to pain. Endorphin production can be triggered by vigorous aerobic exercise. The release of β-endorphin has been postulated to contribute to the phenomenon known as a "runner's high." Endorphins may contribute to the positive effect of exercise on anxiety and depression. The same phenomenon may also play a role in exercise addiction. Regular intense exercise may cause the brain to downregulate the production of endorphins in periods of rest to maintain homeostasis, causing a person to exercise more intensely in order to receive the same feeling. However, several studies have supported the hypothesis that the runner's high is due to the release of endocannabinoids rather than that of endorphins.

    Summary

    • Anabolic steroids are synthetic variations of the male sex hormone testosterone. Health care providers can prescribe steroids to treat various medical conditions. But some athletes and bodybuilders misuse these drugs to boost performance or improve their physical appearance.
    • People who abuse anabolic steroids usually take them orally, inject them into the muscles, or apply them to the skin with a cream or gel.
    • People misuse steroids in a variety of doses and schedules. Misuse of anabolic steroids might lead to short-term effects, including paranoid jealousy, extreme irritability and aggression, delusions, impaired judgment, and mania. Continued steroid misuse can act on some of the same brain pathways and chemicals that are affected by other drugs, including dopamine, serotonin, and opioid systems.
    • Caffeine improves athletic performance in aerobic (especially endurance sports) and anaerobic conditions.
    • Anabolic steroid misuse might lead to serious long-term, even permanent, health problems. Several other effects are gender- and age-specific.
    • Even though anabolic steroids do not cause the same high as other drugs, they can lead to addiction. Some people seeking treatment for anabolic steroid addiction have found behavioral therapy and medications to be helpful. Medicines can help treat symptoms of withdrawal in some cases.
    • The use of drugs to enhance performance is considered unethical, and therefore prohibited, by most international sports organizations, including the International Olympic Committee.
    • Endorphin production can be triggered by vigorous aerobic exercise.

    Contributors and Attributions

    • Wikipedia
    • National Institute on Drug Abuse; National Institutes of Health; U.S. Department of Health and Human Services.

    17.6: Drugs, Athletic Performance, and the Brain is shared under a not declared license and was authored, remixed, and/or curated by LibreTexts.

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