Performance Enhancing Drugs & Ergogenic Supplements PDF

Performance Enhancing Drugs & Ergogenic supplements Dean Burkin, PhD [email protected] Objectives Be familiar with the epidemiology of ergogenic supplement use by athletes Understand why athletes use ergogenic supplements Be familiar with an approach to counseling and caring for athletes using erg...

Performance Enhancing Drugs & Ergogenic supplements Dean Burkin, PhD [email protected] Objectives Be familiar with the epidemiology of ergogenic supplement use by athletes Understand why athletes use ergogenic supplements Be familiar with an approach to counseling and caring for athletes using ergogenic supplements Be aware of specific ergogenic supplements used by athletes to improve performance Understand the risks and benefits of ergogenic supplement use Sports: The Good The Bad The Ugly Survey of U.S. Olympic Athletes Would you take a banned supplement if it was guaranteed to not be detected, and you were guaranteed to win a Gold medal? Survey of U.S. Olympic Athletes Would you take a banned supplement if it was guaranteed to not be detected and you were guaranteed to win a Gold medal, but it would kill you in 5 years? Pharmacology Ergogenic - Drugs or supplements that improve performance Recreational - Used for enjoyment or leisure purposes Therapeutic - Used for the treatment of medical conditions Prohibited Drugs & Supplements A drug of supplement is prohibited if it meets two of the following three conditions: 1. Evidence the drug or supplement can improve performance 2. Evidence that use of the drug or supplement can cause actual of potential health risks 3. Use of the drug or supplement violates the spirit of the sport according to the World Anti-Doping Agency Epidemiology of Nutritional and Ergogenic Supplement Use in High School Students 3,248 students grade 8-12 MVI (60%), weight-gain (17%), weight-loss (35%) Anabolic steroid use 1.6%, boys > girls Sources of nutrition education: professional athletes > teachers > parents > physicians “Willing to take supplement if guarantees … goals” 11-35% “Willing to take even if shorten my life” 3-6% Hoffman et al., 2008, MSSE:40 p15-24 How Physicians View Ergogenic Supplements Better safe than sorry. Just because everyone else is doing it doesn‘t mean you have to do it. Just because some is good doesn’t mean more is better. Improvement is too small to measure. The small chance of benefit is not worth the risk. Too expensive. This is a medical issue, and athletes should seek advice from physicians. How Athletes View Ergogenic Supplements Better safe than sorry. Everyone else is doing it, so I need to do it too. If some is good, more is better. Measurement error exceeds margin of winning. Even a small chance of benefit is worth any risk. Cost is not a barrier. This is a sports issue, and physicians don’t know what they are talking about. How to Talk with Athletes About Ergogenic Supplements Adopt clear, consistent non-judgmental attitude. Understand the athlete’s goals. Gain athlete’s trust. Take full history of all medications and supplements. Focus on health and side effects, not benefits, performance or ethics. Seek information, often from the Internet. Commitment to relationship even if advice rejected. Nutritional Supplement Role Models in Professional Sports—Bill Romanowski Coenzyme-Q10 Vit C Vit E Creatine EFA HMB Protein powder shake Chondroitin Glutamine Chromium Copper Zinc Magnesium (Oh, and anabolic steroids!) Common and Mostly Safe (and Sometimes Effective) Ergogenic Supplements Creatine Caffeine Creatine-I Over 95% in skeletal muscle Normal daily requirement 2 g Enhances regeneration of ATP Increased capacity for high-intensity, short-duration power and endurance training No impact on endurance exercise or VO2 max. Use in NCAA highly variable 20-30 g/d loading (5-6# beef), 2-4 g/day maintenance Expensive Creatine-II No value by itself Enhances recovery and increases training intensity Variable response (baseline levels, training) Inconsistent use Potential side effects: GI and muscle cramping, water retention, weight gain, potential muscle tears On team of 100 football players, 1 might benefit Caffeine Most widely consumed drug in world Only proven ergogenic supplement allowed by IOC Increased time to fatigue Increased lipolysis Glycogen sparing FFA mobilization Increased sub-anaerobic work CNS adenosine receptor antagonist CYP1A2 control of methylation to active metabolites Magnitude of benefit < measurement error Usual intake 100-300 mg within 1 hour of competition Study levels 200-1000 mg Minimal/no benefit in untrained, recreational athlete Dangerous and Mostly Illegal (but Often Effective) Ergogenic Supplements Anabolic steroids HMB (beta-hydroxy-beta-methylbutyrate) Human growth hormone Erythropoietin Stimulants (amphetamines) Anabolic Steroids Effective (strength, power, recovery) Dangerous (acne, testicular atrophy, liver cancer, rage and depression) Difficult to detect because of stacking regimens Inevitable (Olympic survey) Dehydroepiandrosterone (DHEA) Banned by FDA, sold as nutritional supplement. May be converted to estrogen or testosterone. Increased levels of IGF-1, GH secretion. Increased muscle mass, decreased fat mass in sedentary middle-age subjects (if they exercise!). Supplement levels (50-100 mg/d) overwhelmed by natural levels under age 30. Beta-Hydroxy-BetaMethylbutyrate (HMB) Metabolite of leucine (essential BCAA) Decreased catabolism, regulates protein metabolism Increased muscle mass No evidence of improved performance or strength Aesthetic enhancement in bodybuilding Human Growth Hormone Effective (increased muscle mass and strength, decreased body fat). Most important effect may be recovery from maximal exercise. Available synthetically. Dangerous (acromegaly, cardiomyopathy, diabetes). Impossible to detect until recently. Fragments, releasing peptides, secretagogues Erythropoietin (EPO) Effective (stimulates red blood cell formation, increased oxygen carrying capacity). Dangerous (stroke, myocardial infarction). Difficult (but not impossible) to detect. Inevitable (“better dead than second”). The Placebo Effect—”OxyRBX” 19 club-level trained runners (mean age 28 years) Told that OxyRBX had an effect similar to erythropoietin 4 subjects dropped out due to concerns about thrombosis Unblinded, athletes told when they were taking “OxyRBX” 7-day crossover trial with “washout period” in between Daily injections of 0.9% saline for “treatment” phase No injections for “control” phase Competitive 3K races at start and end of each phase 1.2% improvement in race time of “treatment” over “control” phase Difference between 1st and 4th place in 2012 Olympics < 1% MSSE 2015;47:1672-81 Amphetamines Effective (physical power, mental edge, loss of body fat). Side effects (headaches, sleep loss, anxiety). Dangerous (myocardial infarction, hyperthermia). Easy to detect. Illegal in most sports and federations. Designer stimulants (higenamine, methylhexanamine, octodrine) Dimethylamylamine— A Case Report Sympathomimetic, related to amphetamine Used to “boost” weight training and workouts 26 year-old male military veteran Taking Code Red for boosting training ALT 334 IU/L, AST 1040 IU/L, CPK 34,270 IU/L Rhabdomyolysis, supplement stopped, labs resolved 2 deaths, hemorrhagic stroke, heart failure What About Meldonium? Manufactured and distributed in Eastern Europe. Inhibits fatty acid oxidation, binds to carnitine acetyltransferase, promotes cellular energy metabolism. Protecting ischemic cells vs. promoting performance. No evidence of performance enhancement. Banned by WADA 1/1/16 Hundreds of positive tests to-date, mostly Russian athletes, most recently Russian curler. Russian Anti-Doping Agency suspended 2015. Maria Sharapova Trimetazidine (TMZ) Medication for heart-related conditions like angina pectoris Cryoprotective anti-ischemic agent by modulating cardiac metabolism Improves myocardial glucose utilization through inhibit of fatty acid metabolism Banned by the WADA in 2014 Kamila Valieva tested positive before the Beijing 2022 Winter Olympics Claims it was accidentally ingested when confused with her grand-fathers heart medication Russian coaches implicated in child abuse by providing PED Is Oxygen Ergogenic? Hyperbaric oxygen for faster recovery Hypobaric oxygen for training Live High, Train Low (LHTL) 6-9,000 feet 2-4 weeks ? Hypobaric tents Why not Live High and Train High? Special Issues for Ergogenic Supplement Use in Women Anabolic-androgenic steroids (0.1 – 4.8%) DHEA Tamoxifen (53% of bodybuilders) hGH (0.1 – 0.2%) Ephedra (26%, higher than men, weight loss) Creatine (0.4%) Inadvertent Doping Ma Huang (ephedra) Anabolic steroids (15%) Clenbuterol Selective androgen receptor modulators (Enobosarm, Ligandrol) Recent studies of amphetamine contamination Hepatoxicity à liver failure and transplant What’s New and Hot in Ergogenic Supplements Sodium citrate/bicarbonate—buffers acidosis Sodium phosphate—shifts oxygen dissociation curve to right Nitric oxide—muscle pump, sildenafil (Viagra) Glutamine—cellular repair, enhanced immunity Bovine colostrum—muscular endurance, similar to HMB Beetroot extract—reduced energy consumption, increased time to exhaustion Vinegar supplementation—slows glycogen depletion CHO mouthwash—improved running performance What’s New and Not Hot in Ergogenic Supplements Alpha-ketoglutarate Arginine Boron Linoleic acids D-Aspartic acid Fenugreek extract Glutamine GH-releasing peptides Isoflavones BCAA Phosphatidic acid Citruline EAA Glycerol Nitrates Quercetin Boron Carnitine Genetic Engineering to Improve Performance GW1516 (peroxisome-proliferator-activated receptor agonist) Conversion of type II (fast-twitch) to type I (slow twitch) myofibers AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) AMP-activated protein kinase, increases adenosine availability Increased blood flow Banned since 2011 The Role of the Microbiome in Exercise and Performance 100 trillion bacteria 10x number of cells in body 90% from two species— Bacteroidetes and Firmicutes Higher proportion of Akkermansia Muciniphila in athletes Variation in composition due to genetic (12%) and dietary (57%) influences The Role of the Microbiome in Exercise and Performance Diet and exercise influence the microbiome Likely wide range of potentially beneficial microbiota Probiotics to ameliorate GI permeability and endotoxemia in triathletes Possible influences on oxygen extraction, VO2Max, inflammatory markers, glycemic response, lactate production Microbiome transfer studies Scientific vs. Ethical Issues What we can do vs. what we should do. Conclusions Sports and exercise participation almost always beneficial. Desire to win leads to dangerous behaviors. Pressure to perform begins at an early age. Strong desire to explore ergogenic nutritional supplements. Nutritional supplements that are safe mostly don’t work. Nutritional supplements that work are mostly dangerous and/or illegal. Additional Resources Global Drug Reference Online https://www.GlobalDRO.com US Anti-Doping Agency https://www.usada.org/resources/healthpro World Anti-Doping Agency https://adel.wada-ama.org/