ERGOGENIC AIDS Andy Mc Gown MD Definition Ergo

ERGOGENIC AIDS Andy Mc. Gown, MD

Definition: • • • Ergo = work Gennan = to produce Any substance or method used to enhance performance through increased energy utilization: » production » control » efficiency

History • 3000 Years ago the Greeks ate “substances” to improve athletic performance including Strychnine. Used recently in 1904 and 1992 Olympics • 776 BC (1 st Olympiad) » Hallucinogenic mushrooms and sesame seeds • 1889 1 st Self-administered Steroids » Brown-Sequard “Testicular extracts” • 1935 Testosterone Synthesized

Goldman’s Poll • Two questions posed to 198 aspiring olympians during the 1990’s » Take banned substance if guaranteed to win a medal and not be caught » Take banned substances and not be caught and win every competition for the next 5 years but die an early death from side effects

Classification • Drugs: » » » Hormones Stimulants Narcotics Diuretics B-Blockers • “Supplements”: » » » Prohormones? Amino Acids Metals Antioxidants Herbs

Prevalence: • Estimated Use » Adolescents • 11% male (most start < 16 yo) • 2. 5% female » Adult ~ 15% • Usually recreational athletes • Swimming, Cycling, Weight lifting, Track and Field • Billion Dollar Industry

“There is no room for second place. There is only one place in my game, and that’s first place. ” -Vince Lombardi

Reasons: • • • Have to use them to be competitive Need the edge Not genetically gifted Dissatisfaction with size/ weight Peer/ Team Pressure

Human Growth Hormone • Naturally secreted by the pituitary • Normal function of GH is growth and development of every body system, including bone and muscle • Can be stimulated by propanolol, vasopressin, clonidine, and levodopa • Synthetic growth hormone

Side Effects: • • • Acromegaly (may be irreversible) Peripheral Neuropathy Coronary Artery Disease Cardiomyopathy Diabetes, Hypothyroidism, arthritis No available urine test available, but banned by NCAA and IOC

Erythropoietin • Hormone released by the kidneys in response to low Hct • Stimulates RBC production from bone marrow • Has recently been manufactured by recombinant DNA technique • Can increase Hct in renal patients by up to 35%, lasting up to 7 months • Used most by cyclists

Doping • Attributed to the Dutch word “dop” which was a narcotic mixture of opium used to stimulate racing horses

Blood Doping • Autologous Reinfusion » » » 2 units blood removed 4 -8 wks prior to competition Frozen w/ glycerol Reinfusion 1 -7 days prior to event • 1 U PRBC>>500 ml / min increase in O 2 carrying capacity • Can produce 25% improvement in endurance » The poorer the athletes conditioning the greater the benefit

Side Effects • Blood Transfusions » Heterologous • transfusion rxn (3 -10%), Hepatitis (10%), HIV (? %) » Autologous • bacterial infections • r-EPO » Polycythemia • increased viscosity >>CHF, HTN, CVA

Detection • Blood Doping and r-EPO » Banned by IOC • No Direct Test » Hct >50 » Serum Fe and Bili • Detecting post-transfusion hemolysis » Legal issues

Anabolic Steroids • • The ultimate ergogenic aid aka “Juice” Creates the Superhuman Athlete Testosterone derivatives (cholesterol) Produced in the adrenal/ testes

Anabolic/Androgenic Steroids • • • Anabolism - Constructive Catabolism - Destructive Anabolic effects : inc. skeletal mm mass anticatabolism Androgenic effects: secondary sexual characteristics - pubic hair, genital size • No Pure Anabolic Steroids

History of Steroids • • • First Available - 50’s (Dianabol) Drug Banned - 60’s Testing Initiated- ‘ 76 Athletes Banned - ‘ 83 Pan Am Games Schedule III Controlled Substance - ‘ 90 Anabolic Steroid Control Act • US Dietary Supplement Act - ‘ 94 no FDA approval if no “drug intent”

Administration: • Athletes may take up to 40 -100 x therapeutic dose (200 -2000 mg/ wk) • IM adm bypasses the liver/ PO does not • “Stacking”: using various aids in combination • “Cycling” : gradual inc. then taper over 6 -10 weeks, 1 -3 cycles /year, “bridging” between • Illicit - Nandrolone, Stanozolol (Winstrol), Methelone, Tibolone, Oxandrolone • Medical - Testosterone, Enanthate, Undelanoate, Dehydrotestosterone (patch)

Desired Effects: • • Increase in strength Increase in weight Increase in aggressiveness Increased capability of sustaining repetitive, high intensity workouts • Enhanced performance

Side Effects: • CV: MI - hypertension, inc. LDL, dec. HDL, cardiac hypertrophy, thrombosis • Endocrine: virilization, testis atrophy, azospermia, priapism, prostatic hypertrophy/ CA, gynecomastia, erectile dysfct, libido • Liver : peliosis hepatitis, hyperplasia, adenoma, no carcinoma, elevated LFTs • MS: epiphyseal closure, inc. bone density, dec. tendon strength

Side Effects (cont’d): • Skin: acne, hirsuitism, striae, androgenic alopecia, inc. sebaceous glands • Metabolic: hypernatremia, kalemia, phosphatemia, calcemia, “prediabetic” • Psychiatric : aggressiveness, extreme mood swings - depression/ mania, dependence, other drug use, “Reverse Anorexia” • Long Term - dec. life span

Specific Side Effects • Women: Virilzation: » Clitoril enlargement, Deepening of voice, Male pattern baldness, dec. breast size, libido • Children: premature closure of growth plate in long bones & short stature

“Prohormones” • • • Androstenedione DHEA Androstenediol Norandrostenedione Norandrostendiol

Androstenedione • 1/2 of the “ Mark Mc. Guire Special” • A natural steroid hormone found in all animals and some plants • Metabolite of DHEA • Precursor of testosterone • Synthesized in Adrenals/ Gonads • Metabolized in the liver to testosterone

Effects: • Benefits: Same as Testosterone » » Increased energy Enhanced recovery and growth from exercise heightened sexual arousal and function greater sense of well-being • Plasma levels of testosterone increased from 140% to 330% of normal levels after 50 mg and 100 mg doses • SE’s : Same as Testosterone • Banned by IOC, NCAA, NFL

DHEA (Dehydroepiandrosterone) • What it is: A hormone produced by adrenal gland • Claims: Anabolic effect • What is does: Increases testosterone levels • Banned by the NCAA, NFL

Stimulants • • Caffeine Amphetamines Cocaine Ephedrine

Amphetamines • WWII » Soldiers used them to counteract fatigue • 1959 Study shows Performance Enhancing Potential • Used in Sports where Speed, Power and Endurance are Required

Side Effects: • Predominantly CNS » » » Insomnia, agitation and restlessness Confusion, paranoia, hallucinations Dyskinesias • especially in facial muscles • Cardiac » HTN, arrhythmias • GI » Diarrhea • Rebound Fatigue and Depression

Caffeine • A Methylxanthine: same class as theophylline and theobromine • Exerts its’ effects by: » Translocation of Calcium for more muscular availability » Increase in c. AMP by inhibition of phosphodiesterase » Blockage of adenosine receptors, blocking the sedative properties of adenosine

Caffeine (cont’d) • • • Is banned by IOC and NCAA in large doses Legal limit = 15 micrograms / ml Equal to 6 -8 cups of coffee at one sitting, with testing within 2 -3 hours • Beneficial most in endurance events, such as cycling • Doses up to 5 mg / kg were required to see benefits. Doses of 17 mg/kg produce the maximum legal limit.

Side Effects: • Similar to s/e of other stimulants: » insomnia, irritability, nervousness » Tachcardia, arrthymias, and possibly death!

Ephedrine • What it is: Is a drug found in herbal products containing Ma haung, anti-asthmatic medications, and many cold and cough products. • Claims: Increases body fat loss • What really does: Acts as a CNS stimulant, delays fatigue by sparing body glycogen reserves. Increase in B/p respiratory, heart rate, insomnia, and nervousness • Max dose : 24 milligams per day!!!!!!

Amino Acids • • • Creatine L-Carnitine Choline Inosine HMB (B-OH-BMethylbutyrate)

Amino Acids • • Essential amino acids: found in a balanced diet Recommended protein intake: 0. 8 g /kg/day Athletes may benefit from up to 1. 4 -2. 4 g/kg/day Most beneficial for athletes on a poor diet, or vegetarians • In endurance athletes, up to 10% of energy expenditure is from protein breakdown

Creatine • The Other 1/2 of the Mark Mc. Guire “Cocktail” • Sales topped $200 million in 1998 » 13% of HS athletes » 50% of NFL players » Vast majority of Olympic sprinters and cyclists

Creatine • Methylguanidine-acetic acid - made from glycine, arginine & methionine • Estimated Daily requirement: 2 gms • Available in meats and fish (1/2 EDR) • Sold as Creatine Monohydrate • Stored in Skeletal MM

Mechanism of Action : • Methylguanidine-acetic acid - made from glycine, arginine & methionine • Estimated Daily requirement: 2 gms • Available in meats and fish (1/2 EDR) • Sold as Creatine Monohydrate • Stored in Skeletal MM

Benefits: • Improved performance in repeated bouts of high intensity strength work and sprints • Single sprint activity results are equivocal • Does not enhance endurance exercise • More work with less lactic acid production • No studies on competetion benefits • 1998 ACSM meeting: 19/19 studies showed significant ergogenic benefit

Dosing: • • • Phase: 20 -30 gm/d, x 5 -7 days Maintenance phase: 2 -5 gm/day Loading increases PCr stores by 10 -40% Normal resting levels of creatine: 100 -150 m. M/kg Most striking benefits occur in subjects with lower resting Cr level • After saturation of tissues, excessive supplementation is renally excreted

Side Effects: • • • Muscle Cramping Diarrhea Dizziness Dehydration Biggest danger: getting “impure” creatine Significant WEIGHT GAIN common 2 nd to water retention

The Perfect Supplement? • “The secret is to find something that is effective in improving performance, but not against the rules, and with no side effects” • “…no clear evidence of harmful side effects of creatine use has emerged…”--The Physician and Sportsmedicine, June 1998 • Long term effects of Creatine not yet studied: Concerns focus on effects to kidney, pancreas, and liver.

Counseling your patients • Creatine may or may not improve performance • Weight gain will occur • Side effects (especially long-term) not well known • Take a thorough medical history • Monitor renal and liver fct. • Make sure they’re taking reccomended dose

L-Carnitine • Synthesized in Liver/ Kidney from Lysine & Methionine • found in meats & dairy products • Assists in Fat transportation into muscle mitochondria for oxidation, sparing Glycogen & may prevent lactic acid accumulation • Improved endurance performance not shown in studies

HMB • Metabolite of KIC (ketoisocaproate) which is a metabolite of leucine • Leucine & KIC found to have anticatabolic effects • decreased mm proteolysis, inc. lean mm mass, inc. strength • no known side effects

Choline • Precursor for the neurotransmittor Acetyl Choline & the lipoprotein Lecithin (Phosphattidylcholine) • choline depletion in marathoners • no studies supporting

Inosine • Increases myocardial contractility • no performance enhancement in runners/ cyclists

Metals/ Minerals • • Chromium Magnesium Boron Vanadium

Chromium • • Insulin Cofactor inc. AA uptake into mm cells increase mm mass, dec. body fat found in meats, grains, raisins, apples, & mushrooms • SE’s: anemia, chromosomal damage, cognitive impairment & interstitial nephritis in excessive doses

Magnesium • Involved in ptn synthesis & mm contraction • + effects on oxygen consumption & lactate production • no change in performance

Boron • Originally thought to inc. testosterone levels • not born out in studies

Vanadium • What it is: Non-essential trace mineral • Claims: Anabolic effect, enhances insulin action • What it does: No studies to show anabolic effect. Doses>10 gms/day causes abd. Pain, cramps, green tongue, diarrhea, wt. loss

Antioxidants • Vitamins E & C • potential damage from free oxygen radicals produced by lipid peroxidation in exercise • exercise performance is not improved

Herbs • • Ginseng Yohimbe Tribulus Terresteris Ma haung

Ginseng • What it is: A root from an Asian plant (panax ginseng). • Claims: Enhanced performance. Improved recovery rate. • What it really does: Acts as an adaptogen- may boost immune system and protect cells. May cause insomnia, and should not be used if B/p is elevated. • Dose: 100 -200 mg per day used occ. 2 -3 weeks on 1 -2 weeks off

Yohimbe • What it is: Supplement derived from tree bark. • Claims: Anabolic effect, Increased virility • What it does: Stimulant effect, no anabolic effect. Can cause nervousness, HA, nausea, Vomiting, increased B/P

Tribulus Terresteris • • What is it: A plant hormone Claims: Anabolic effect What it does: Increases testosterone levels Banned by NFL

Thank You Very Much