Transcript ASMI
ERGOGENIC AIDS Andy McGown, 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
• Drugs: » Hormones » Stimulants » Narcotics » Diuretics » B-Blockers
Classification
• “Supplements”: » Prohormones?
» Amino Acids » Metals » Antioxidants » Herbs
Prevalence:
• Estimated Use » Adolescents • 11% male (most start < 16yo) • 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 O2 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 40-100x 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 McGuire 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 50mg and 100mg 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
• Caffeine • Amphetamines • Cocaine • Ephedrine
Stimulants
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 cAMP 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-B Methylbutyrate)
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 McGuire “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: 2gms • 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: 2gms • 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 mM/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 2nd 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
• Chromium • Magnesium • Boron • Vanadium
Metals/ Minerals
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>10gms/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
• Ginseng • Yohimbe • Tribulus Terresteris • Ma haung
Herbs
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: 100-200mg 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