Chapter 11 Performance-Enhancing Substances and Methods

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B. Anabolic Agents testosterone DHEA, etc...

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D. Diuretics (water pills) and other masking agents bumetanide chlorothiazide furosemide hydrochlorothiazide probenecid spironolactone triameterene trichlormethiazide etc...

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E. Street drugs heroin marijuana TCH sythetic cannabinoids

Preworkout energy drinks

Efficacy -Effective for increasing resistance training volume performance -Other types of anaerobic exercise (including Wingate tests and speed/agility performance) not as responsive to energy drink consumption Adverse effects -Due to the presence of caffeine, the same potential adverse effects that exist for caffeine also exist for energy drinks.

2013-2014 National Collegiate Athletic Association Banned Drug Classes cont..

F. Peptide Hormones and Analogues growth hormone (hGH) human chorionic honadotropin (hCG) erythropoietin (EPO)

The branched chain amino acid _______ is a key regulator in stimulating muscle protein synthesis.

Leucine. **Leucine directly activates the Akt/mTOR pathway in skeletal muscle which is a key pathway in skeletal muscle protein synthesis

Hormones

Testosterone - interacts with skeletal muscle tissue Erythropoietin - stimulates red cell production for increased aerobic endurance Catecholamines - has metabolic and nervous system effects and enhance weight loss and provide greater arousal for performance.

World Anti-Doping Agency (WADA)

The agency responsible for promoting, coordinating and monitoring at international level the fight against the use of drugs in sport. Establishes banned substances list for Olympics

Examples of banned prohormone supplements

androstanediol androstanedione bolasterone methyltestosterone norandrostenediol norandrostenedione 19-nor-4-androstenediol 19-nor-5-androstenediol 1-testosterone precursors to other hormones like testosterone. Little evidence that it produces much effect.

1. Which of the following dietary supplements are considered a stimulant? I. creatine II. caffeine III. HMB IV. citrus aurantium a. I and II b. II and IV c. III and IV d. I and III

b. II and IV

3. Which of the following is the BEST reason for aerobic endurance athletes to avoid erythropoietin use? a. hematocrit and hemoglobin levels may decrease. b. It may cause an unregulated increase in red blood cell production c. resistance to infectious disease may be impaired d. it may reduce the ability of the blood to carry oxygen

b. it may cause an unregulated increase in red blood cell production

FDA regulates

both finished dietary supplement products and dietary ingredients. *Dietary Supplement Health and Education Act (DSHEA) - manufacturers and distributors of dietary supplements are prohibited from marketing products that are adulterated or misbranded. This means that these firms are responsible for evaluating the safety and labeling of their products before marketing to ensure that they meet all the requirements of DSHEA and FDA regulations. *Companies can however make claims about effects on the body's structure and function as long as the manufacturers can show that the statements are truthful and not misleading.

2. Which of the following is NOT part of caffeine's role in improving athletic performance? a. increased power production b. decreased glycogen depletion c. increased fat oxidation d. decreased urine production

d. decreased urine production

The FDA's definition of a drug

encompasses substances that change the body's structure or function. This includes substances that stimulate hormone secretion. Also if a compound is administered differently from the way in which foods would be consumed it may be classified as a drug.

Dietary supplements

highly refined products that would not be confused with a food. May not have any positive nutritional value so not referred to as nutritional supplement. I.e.: tablet of amino acids.

Dietary supplements

products that supply one or more nutrients as a supplement to, not a substitute for, healthful foods

B-Blockers

-Class of drugs that block the B-adrenergic receptors, preventing the catecholamines from binding. -Have an ability to reduce anxiety and tremors during performance Adverse effects -ergolytic effect (reduce performance) -impairs cardiovascular response to exercise by reducing max HR, VO2 max and athletic performance -bronchospasm, heart failure, prolonged hypoglycemia, bradycardia, heart block and intermittent claudication

Nutritional Buffers - b-alanine

-Nonessential amino acid -rate-limiting substrate for carnosine synthesis -carnosine is found primarily in fast-twitch Type II skeletal muscle -carnosine estimated to contribute up to 40% of skeletal MBC of H+ produced during intense anaerobic exercise --> encouraging a drop in pH **Theory is increasing carnosine levels through chronic training or b-alanine supplementation or both would improve MBC and most likely improve anaerobic performance. Efficacy:High-intensity exercises performed with a lower level of acidosis are unlikely to benefit from b-alanine supplementation. Adverse Effects: paresthesia (tingling or numbness of skin) in high and acute doses and disappear within about 1 hour

Nutritional Muscle Buffers - Sodium Bicarbonate

-alkalinizing agent - counteracts or neutralizes acid (low pH). -naturally formed in the body and is also found in baking soda. -supplementation has been shown to increase the pH of blood by a pH difference between inside and outside of muscle cells that causes accelerated movement of H+ out of the contracting muscle helping to regulate intramuscular pH. -supplementation improves MBC and in turn high-intensity performance Efficacy: shown to improve total work capacity, peak power, peak torque and strength. Ingested about 60-90 min before exercise. Adverse effects: dosage should be 0.3 g/kg body mass about 60-90 min before exercise. More than that causes diarrhea, cramping, nausea and vomiting.

Citrus Aurantium is from fruit commonly known as bitter orange

-appetite suppressant -increases metabolic rate and lipolysis contains synephrine - a sympathomimetic agent which some suggest stimulates specific beta adrenergic receptoors that stimulate fat metabolism without any negative side effects associated with other things that stimulate adrenergic recptors. Adverse effects: causes vasoconstriction and elevates BP **currently on banned list of performance-enhancing drugs.

Dietary supplements (Arginine)

-conditionally essential amino acid -crucial role in nutrition and metabolism -required for synthesis of protein and creatine and its metabolism results in the production of nitric oxide Claims: elevate nitric oxide levels which causes..., increase muscle blood flow by vasodilation, and improve exercise performance ***does not increase blood flow in healthy athletes Adverse effects: GI distress, nausea, cramps, diarrhea ****Due to its inability to increase nitric oxide production, enhance muscle blood flow or improve endurance exercise performance, oral arginine supplementation is not recommended for healthy athletes.

Importance of creatine to exercise

-creatine phosphate (CP) has essential role in energy metabolism and a substrate for the formation of ATP by rephosphorylating ADP especially during short duration high intensity exercise. -The ability to rapidly rephosphorylate ADP is dependent on the enzyme creatine kinase and the availability of CP within the muscle. -As CP stores become depleted the ability to perform high intensity exercise declines. **depletion of muscle CP during high-intensity exercise is the PRIMARY MECHANISM LEADING TO FATIGUE in such events

Nutritional Buffers

-during high-intensity anaerobic exercise a lot of hydrogen ions (H+) are produced along with reduction if pH in skeletal muscle. This adversely effects performance. -MUSCLE BUFFERING CAPACITY (MBC) is the ability to regulate H+ concentration in skeletal muscle during high-intensity exercise. -Strong positive relationship between MBC and exercise performance -Theory is improving MBC by training or nutritional means (b-alanine, sodium bicarbonate or citrate) would improve performance in sports that may be limited by H+ buildup.

Dietary supplements (essential amino acids, branched-chain amino acids)

-high levels are found in any number of animal-based proteins, leucine is found in plants such as spinach and broccoli but minimal compared to animal-based sources. -branched-chain amino acids (isoleucine, leucine and valine) are responsible for increasing muscle protein synthesis. **leucine content may be the rate-limiting factor in terms of maximizing muscle protein synthesis. Adverse effects: no known adverse effects

Erythropoietin (EPO)

-hormone secreted by the kidney to stimulate the production of red blood cells by bone marrow -it is also a protein hormone that can be produced by recombinant DNA techniques -effective ergogenic aid to increase hemoglobin concentrations getting more oxygen-carrying capacity of the blood which increases aerobic capacity Adverse Effects -increases hematocrit which -increases red blood cell number and increases blood viscosity -increased risk of blood clotting -elevations in systolic BP -increased risk of stroke and cerebral or pulmonary embolism

Nutritional Muscle Buffers - Sodium Citrate

-increases blood pH without GI distress and commonly seen with sodium bicarbonate supplementation. -once in the blood sodium citrate actually breaks down into bicarbonate thus increasing extracellular pH. Resulting in helping to regulate intramuscular pH during high-intensity exercise Efficacy: has shown some benefit but more research needed Adverse effects: could possibly cause some GI upset

HCG (Hman Chorianic Gonadotropin)

-made in the placenta of pregnant women -closely related in structure and function to luteinizing hormone -used in pregnancy kits to test of pregnant because only made in body when pregnant -used by athletes in finishing a cycle of anabolic steroids and looking to activate their own endogenous testosterone production

Creatine

-nitrogenous organic compound that is synthesized naturally in the body, primarily in the liver (smaller amount in kidneys and pancreas) and helps to supply energy to all cells in the body. -arginine, glycine and methionine are the precursors for synthesis in those organs. -found in both meat and fish -98% of creatine is stored within skeletal muscle in either its free form or its phosphorylated form

Caffeine

-possibly increases fat oxidation through mobilization of free fatty acids from adipose tissue or intramuscular fat stores. -this would slow glycogen depletion and delay fatigue -during short-duration high-intesity exercise primary ergogenic effect is enhanced power production cause by enhanced excitation-contraction coupling, affecting neuromuscular transmission and mobilization of intracellular calcium ions from the sarcoplasmic reticulum. -Also thought to enhance the kinetics of glycolytic regulatory enzymes such as phosphorylase. **In doses of 3-9 mg/kg body wt consumed 60 min before exercise or during prolonged exercise, caffeine is ergogenic. There is no further benefit when it is consumed at higher doses >9 mg/kg. It can decrease feelings of perceived exertion, improve work capacity, and increase mental alertness. The research doesn't support caffeine-induced diuresis during exercise or any harmful change in fluid balance that would negatively affect performance. Adverse effects: anxiety, GI disturbances, restlessness, insomnia, tremors, heart arrhythmias, physically addicting with withdrawal symptoms

Ephedrine

-relief from bronchial asthma, bronchitis, allergies, shortness of breath, cold and flu symptoms -strong thermogenic quality by elevating basal metabolic rate and increasing energy expenditure and resulting in fat loss -effective when taken with caffeine to improve aerobic performance Adverse effects: ephedra banned by FDA -ephedra containing dietary supplements or ephedrine plus caffeine caused increase of nausea, vomiting, psychiatric symptoms such as anxiety and change in mood, autonomic hyperactivity, palpitations and few cases of death.

B-adrenergic agonists

-substances chemically related to epinephrine, a hormone produced in the adrenal medulla that regulates physiological effects such as lipoloysis (breakdown of fat) and thermogenesis (increased energy expenditure resulting in production of heat) -designed to treat asthma -increases lean mass and decreases body fat -most popular adrenergic agonist is Clenbuterol -bronchodilator -transient tachycardia, hyperthermia, tremors, dizziness, palpitations and insomnia but actual documented events are limited.

L-Carnitine Supplementation

-synthesized from amino acids lysine and methionine -responsible for transport of fatty acids from cytosol into the mitochondria to be oxidized for energy -Theory is increases fat utilization and spares muscle glycogen. **supplementation has not been proven effective -may enhance recovery *shown decreases in pain and muscle damage, decreases in markers of metabolic stress, enhanced recovery *upregulates androgen receptors and increases IGF binding proteins that preserve IGF-I concentrations. These endocrine adaptations from the supplement may have an important role in enhanced recovery seen after high-intensity exercise. Adverse effects: seems to be well-tolerated

Anabolic Steroids

-synthetic variants of the male hormone testosterone -elevates testosterone concentrations stimulates protein synthesis increasing strength, muscle mass and body mass and athletic performance (changes depend on the training status of the individual) -also causes: increased body hair, masculine voice, male pattern baldness, libido, sperm production and aggressiveness.

Definition of products that can be sold as dietary supplements

1. A product other than tobacco intended to supplement the diet that contains one or more of the following dietary ingredients: a. a vitamin b. a mineral c. an herb or other botanical d. an amino acid e. a dietary substance for use by humans to supplement the diet by increasing the total dietary intake f. a concentrate, metabolite, constituent, extract, or combination of any ingredient identified in a through e. 2. The product must also be intended for ingestion and cannot be advertised for use as a conventional food or as the sole item within a meal or diet.

2 types of performance-enhancing substances

1. hormones and the drugs that mimic their effects 2. dietary supplements

Insulin

A protein hormone secreted by the pancreas that is essential for the metabolism of carbohydrates and the regulation of glucose levels in the blood. -rumored to to potentiate effects of growth hormone and insulin-like growth factors.

2013-2014 National Collegiate Athletic Association Banned Drug Classes

A. Stimulants amphetimine (adderall) caffeine (guarana) cocaine ephedrine fenfluramine (Fen) methamphetamine methylphenidate (Ritalin) phentermine (Phen) synephrine (bitter orange) methylhexaneamine "bath salts" mephedrone etc...

Dosing

Athletes typically use anabolic steroids in a "stacking" regimen where they administer several different drugs simultaneously to increase potency -alternate cycles and steps down to reduce likelihood of negative side effects.

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C. Alcohol and Beta-Blockers (banned for Rifle only) alcohol atenolol metoprolol nadolol pindolol propranolol timolol etc...

4. Creatine supplementation improves all of the following EXCEPT A. lean body mass B. maximal strength C. endurance performance D. Power

C. endurance performance

Signs and symptoms of ergogenic aid abuse

Cardiovascular -lipid profile changes -elevated BP -decreased myocardial function Endocrine -gynecomastia -decreased sperm count -testicular atrophy -impotence and transient infertility Genitourinary -Males: decreased sperm count and decreased testicular size -Women: Menstrual cycle irregularities, clitoromegaly, deepening voice, masculinization -Both: gynecomastia, libido changes Dermatological -acne -male pattern baldness Hepatic -increased risk of liver tumors and liver damage Musculoskeletal -premature epiphyseal plate closure -increased risk of tendon tears -intramuscular abscess Psychological -mania -depression -aggression -hostility -mood swings

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G. Anti-Estrogens anastrozole tamoxifen formestane ATD etc...

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H. Beta-2 agonists bambuterol formoterol salbutamol salmeterol etc...

Dietary supplements (B-Hydroxy-BMethylbutyrate) (HMB)

HMB is a derivative of EAA leucine and its metabolite a-ketoisocaproic acid. -HMB stimulates protein synthesis and decreases protein breakdown by inhibiting the ubiquitin-proteasome pathway. -Due to HMB's role in the regulation of protein breakdown, it may be an effective supplement for minimizing losses of lean muscle mass in situations that promote a catabolic state. Efficacy: HMB is most effective when an adequate training stimulus is provided. For untrained individuals, this does not likely require high-volume training. For trained individuals, a high-intensity, high-volume resistance training program is likely needed in order for benefits to be realized with HMB supplementation. **no adverse effects

Creatine Supplementation

What does it do? bulks up stores of creatine phosphate in muscles by 20% (but there is a saturation limit, more is not better) and boosts lean body mass. Proposed benefits: Increases maximal strength and power output and lean body mass **must supplement for an extended amount of time **Creatine supplementation has been shown to increase maximal strength, power and lean body mass in both trained and untrained populations. Additionally, creatine supplementation is safe and relatively inexpensive. **creatine has shown no evidence to cause dehydration and cramping

5. Which of the following performance-enhancing substances is most likely to increase lean body mass? a. anabolic steroids b. arginine c. ephedrine d. B-alanine

a. anabolic steroids

The distinction between a drug and a dietary supplement

is linked to FDA approval for safety and effectiveness.

hGH (human growth hormone)

released by anterior Pituitary responsible for -bone and tissue growth -maintaining blood glucose levels -increasing the uptake of glucose and amino acids into muscle cells -stimulating release of fatty acids from the fat cells -must be injected -no studies on efficacy Adverse effects -could cause acromegaly - disfiguring disease characterized by a widening of the bones, arthritis, organ enlargement and metabolic abnormalities

Ergogenic aid

something that enhances athletic performance

An athlete's first priority should be

to apply sound principles of training, including adequate nutrition, before using any nutritional supplement or ergogenic aid. Before purchasing or consuming a product, an athlete should seek guidance from a qualified professional to make sure the choice is both legal and effective.