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Sports Supplements
Andrew Gregory, MD
Assistant Professor, Orthopedics/ Pediatrics
Team Physician, Vanderbilt University
Jan. 10, 2002
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Definition: Ergogenic Aids
Ergo = work Gennan = to produce Any substance or method used to
enhance performance through increased energy utilization:– production– control– efficiency
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Classification
Drugs:– Hormones– Stimulants– Narcotics– Diuretics– B-Blockers
Supplements:– Prohormones?– Amino Acids– Metals– Antioxidants– Herbs
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Prevalence:
Estimated 11% of HS athletes, college, and professional.
Majority of Olympic swimmers, cyclists, sprinters, & weight lifters
2/3 of the 1998 Tour de France teams Billion Dollar Industry
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Reasons:
Have to use them to be competitiveHave to use them to be competitive Need the edgeNeed the edge Not genetically giftedNot genetically gifted Dissatisfaction with size/ weightDissatisfaction with size/ weight Peer/ Team PressurePeer/ Team Pressure
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Hormones
HGH EPO BHCG Steroids
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Human Growth Hormone
Normally secreted by the pituitaryNormally secreted by the pituitary Normal function of GH is growth and Normal function of GH is growth and
development of every body system, including development of every body system, including bone and musclebone and muscle
Can be stimulated by propanolol, Can be stimulated by propanolol, vasopressin, clonidine, and levodopavasopressin, clonidine, and levodopa
Synthetic growth hormoneSynthetic growth hormone
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Side Effects:
Acromegaly (may be irreversible)Acromegaly (may be irreversible) Peripheral NeuropathyPeripheral Neuropathy Coronary Artery DiseaseCoronary Artery Disease CardiomyopathyCardiomyopathy Diabetes, Hypothyroidism, arthritisDiabetes, Hypothyroidism, arthritis No available urine test available, but banned No available urine test available, but banned
by NCAA and IOCby NCAA and IOC
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Erythropoietin
Hormone released by the kidneys in Hormone released by the kidneys in response to low Hctresponse to low Hct
Stimulates RBC production from bone Stimulates RBC production from bone marrowmarrow
Has recently been manufactured by Has recently been manufactured by recombinant DNA techniquerecombinant DNA technique
Can increase Hct in renal patients by up to Can increase Hct in renal patients by up to 35%, lasting up to 7 months35%, lasting up to 7 months
Used most by cyclistsUsed most by cyclists
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Blood Doping
Induced Erythrocythemia: An increase in Hb Induced Erythrocythemia: An increase in Hb following reinfusion of an athlete’s bloodfollowing reinfusion of an athlete’s blood
Goal: to increase the oxygen-carrying Goal: to increase the oxygen-carrying capacity of Hbcapacity of Hb
Has been used as far back as 1947Has been used as far back as 1947 1984: seven US Olympic cyclists guilty1984: seven US Olympic cyclists guilty Banned by IOC in 1985Banned by IOC in 1985
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Pathophysiology
Muscles depend on ATP for energy Aerobic metabolism = breakdown of
glycogen in presence of O2 >>>ATP Aerobic metabolism-higher yield of ATP More O2 carrying capacity>>more ATP
production, more energy to muscle 1 U PRBC>>500 ml / min increase in O2
carrying capacity
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Methods:
Autologous reinfusion method: 2 units blood removed 4-8 weeks prior to competition & frozen c glycerol
Hb / Hct returns to pre-transfusion levels Reinfusion 1-7 days prior to event Can produce up to 25% improvement in
endurance, with poorer conditioned athletes showing greatest benefits
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Side Effects:
Heterologous blood: transfusion rxn (3-10%), Hepatitis (10%), HIV (?%)
Autologous blood: bacterial infections Polycythemia: increased viscosity
>>CHF, HTN, CVA Most young healthy athletes show no
side effects
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Detection:
Blood doping and Erythropoietin: banned by IOC
No known urine test to detect Testing: Measured Hct >50 Measurement of serum Fe and Bilirubin
to detect hemolysis after frozen PRBC transfusion
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Anabolic Steroids
The ultimate ergogenic aid aka “Juice” Creates the Superhuman Athlete Testosterone derivatives (cholesterol) Produced in the adrenal/ testes
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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
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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”
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Administration:
Athletes may take up to 40-100x therapeutic dose Athletes may take up to 40-100x therapeutic dose (200-2000 mg/ wk)(200-2000 mg/ wk)
IM adm bypasses the liver/ PO does notIM adm bypasses the liver/ PO does not ““Stacking”: using various aids in combinationStacking”: using various aids in combination ““Cycling” : gradual inc. then taper over 6-10 weeks, Cycling” : gradual inc. then taper over 6-10 weeks,
1-3 cycles /year, “bridging” between1-3 cycles /year, “bridging” between Illicit - Nandrolone, Stanozolol (Winstrol), Illicit - Nandrolone, Stanozolol (Winstrol),
Methelone, Tibolone, OxandroloneMethelone, Tibolone, Oxandrolone Medical - Testosterone, Enanthate, Undelanoate, Medical - Testosterone, Enanthate, Undelanoate,
Dehydrotestosterone (patch)Dehydrotestosterone (patch)
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Desired Effects:
Increase in strength Increase in weight Increase in aggressiveness Increased capability of sustaining
repetitive, high intensity workouts Enhanced performance
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Side Effects:
CV: MI - hypertension, inc. LDL, dec. HDL, CV: MI - hypertension, inc. LDL, dec. HDL, cardiac hypertrophy, thrombosiscardiac hypertrophy, thrombosis
Endocrine: virilization, testis atrophy, Endocrine: virilization, testis atrophy, azospermia, priapism, prostatic hypertrophy/ azospermia, priapism, prostatic hypertrophy/ CA, gynecomastia, erectile dysfct, libidoCA, gynecomastia, erectile dysfct, libido
Liver : peliosis hepatitis, hyperplasia, Liver : peliosis hepatitis, hyperplasia, adenoma, no carcinoma, elevated LFTsadenoma, no carcinoma, elevated LFTs
MS: epiphyseal closure, inc. bone density, MS: epiphyseal closure, inc. bone density, dec. tendon strengthdec. tendon strength
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Side Effects (cont’d):
Skin: acne, hirsuitism, striae, androgenic Skin: acne, hirsuitism, striae, androgenic alopecia, inc. sebaceous glandsalopecia, inc. sebaceous glands
Metabolic: hypernatremia, kalemia, Metabolic: hypernatremia, kalemia, phosphatemia, calcemia, “prediabetic”phosphatemia, calcemia, “prediabetic”
Psychiatric : aggressiveness, extreme mood Psychiatric : aggressiveness, extreme mood swings - depression/ mania, dependence, swings - depression/ mania, dependence, other drug use, “Reverse Anorexia”other drug use, “Reverse Anorexia”
Long Term - dec. life spanLong Term - dec. life span
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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 & thus short stature
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“Prohormones”
Androstenedione DHEA Androstenediol Norandrostenedione Norandrostendiol
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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
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Effects:
Benefits: Same as TestosteroneBenefits: Same as Testosterone– Increased energyIncreased energy
– Enhanced recovery and growth from exerciseEnhanced recovery and growth from exercise
– heightened sexual arousal and functionheightened sexual arousal and function
– greater sense of well-beinggreater sense of well-being Plasma levels of testosterone increased from Plasma levels of testosterone increased from
140% to 330% of normal levels after 50mg and 140% to 330% of normal levels after 50mg and 100mg doses100mg doses
SE’s : Same as Testosterone Banned by IOC, NCAA, NFL
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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
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Stimulants
Caffeine Amphetamines Cocaine Ephedrine
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Amphetamines
Have been used as far back as WWII when soldiers used them to delay fatigue
First study in 1959 showed significant improvement in performance
Available data suggest Amphetamines can improve performance in sports where speed, power and endurance are required
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Side Effects:
Related to drugs’ effect on CNS: insomnia, Related to drugs’ effect on CNS: insomnia, instability, agitation and restlessnessinstability, agitation and restlessness
Confusion, paranoia, hallucinationsConfusion, paranoia, hallucinations Dyskinesias, especially in facial musclesDyskinesias, especially in facial muscles Cardiac complications: HTN, arrhythmiasCardiac complications: HTN, arrhythmias GI disturbancesGI disturbances Severe rebound of fatigue and depression Severe rebound of fatigue and depression
after discontinuanceafter discontinuance
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Caffeine
A Methylxanthine: same class as A Methylxanthine: same class as theophylline and theobrominetheophylline and theobromine
Exerts its’ effects by:Exerts its’ effects by:– Translocation of Calcium for more Translocation of Calcium for more
muscular availabilitymuscular availability– Increase in cAMP by inhibition of Increase in cAMP by inhibition of
phosphodiesterasephosphodiesterase– Blockage of adenosine receptors, blocking Blockage of adenosine receptors, blocking
the sedative properties of adenosinethe sedative properties of adenosine
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Caffeine (cont’d)
Is banned by IOC and NCAA in large dosesIs banned by IOC and NCAA in large doses Legal limit = 15 micrograms / mlLegal limit = 15 micrograms / ml Equal to 6-8 cups of coffee at one sitting, with Equal to 6-8 cups of coffee at one sitting, with
testing within 2-3 hourstesting within 2-3 hours Beneficial most in endurance events, such Beneficial most in endurance events, such
as cyclingas cycling Doses up to 5 mg / kg were required to see Doses up to 5 mg / kg were required to see
benefits. Doses of 17 mg/kg produce the benefits. Doses of 17 mg/kg produce the maximum legal limit.maximum legal limit.
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Side Effects:
Similar to s/e of other stimulants:– insomnia, irritability, nervousness– Tachcardia, arrthymias, and possibly
death!
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Ephedrine
What it is: Is a drug found in herbal products What it is: Is a drug found in herbal products containing Ma haung, anti-asthmatic medications, containing Ma haung, anti-asthmatic medications, and many cold and cough products.and many cold and cough products.
Claims: Increases body fat lossClaims: Increases body fat loss What really does: Acts as a CNS stimulant, delays What really does: Acts as a CNS stimulant, delays
fatigue by sparing body glycogen reserves. fatigue by sparing body glycogen reserves. Increase in B/p respiratory, heart rate, insomnia, Increase in B/p respiratory, heart rate, insomnia, and nervousnessand nervousness
Max dose : 24 milligams per day!!!!!!Max dose : 24 milligams per day!!!!!!
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Amino Acids
Creatine L-Carnitine Choline Inosine HMB (B-OH-B-
Methylbutyrate)
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Amino Acids
Essential amino acids: found in a balanced Essential amino acids: found in a balanced dietdiet
Recommended protein intake: 0.8 g /kg/dayRecommended protein intake: 0.8 g /kg/day Athletes may benefit from up to 1.4 -2.4 Athletes may benefit from up to 1.4 -2.4
g/kg/dayg/kg/day Most beneficial for athletes on a poor diet, or Most beneficial for athletes on a poor diet, or
vegetariansvegetarians In endurance athletes, up to 10% of energy In endurance athletes, up to 10% of energy
expenditure is from protein breakdownexpenditure is from protein breakdown
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Creatine
The Other 1/2 of the “Mark Mcguire Special” - The Other 1/2 of the “Mark Mcguire Special” - The Creatine Craze - Sales expected to reach The Creatine Craze - Sales expected to reach $200 million in 1998$200 million in 1998
Use has spread: Use has spread: – 13% of HS athletes13% of HS athletes– 80% of University of Nebraska football team80% of University of Nebraska football team– 50% of NFL players50% of NFL players– Vast majority of Olympic sprinters, cyclists, Vast majority of Olympic sprinters, cyclists,
and sprintersand sprinters
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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 2000 NCAA banned distribution in training
rooms
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Pathophysiology:
Energy Substrate for muscle contraction Creatine binds Phosphorus as substrate for
formation of ATP (main source of energy of contraction)
PCr also buffers Lactic Acid After PCr is depleted must resort to glycolysis
for ATP production Net result: sustained muscular contraction,
delayed fatigue
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Benefits:
Improved performance in repeated bouts of Improved performance in repeated bouts of high intensity strength work and sprintshigh intensity strength work and sprints
Single sprint activity results are equivocalSingle sprint activity results are equivocal Does not enhance endurance exerciseDoes not enhance endurance exercise More work with less lactic acid productionMore work with less lactic acid production No studies on competetion benefitsNo studies on competetion benefits 1998 ACSM meeting: 19/19 studies showed
significant ergogenic benefit
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Dosing:
Loading Phase: 20-30 gm/d, x 5 -7 daysLoading Phase: 20-30 gm/d, x 5 -7 days Maintenance phase: 2-5 gm/dayMaintenance phase: 2-5 gm/day Loading increases PCr stores by 10-40%Loading increases PCr stores by 10-40% Normal resting levels of creatine: 100-150 Normal resting levels of creatine: 100-150
mM/kgmM/kg Most striking benefits occur in subjects with Most striking benefits occur in subjects with
lower resting Cr levellower resting Cr level After saturation of tissues, excessive After saturation of tissues, excessive
supplementation is renally excretedsupplementation is renally excreted
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Side Effects:
Muscle CrampingMuscle Cramping DiarrheaDiarrhea DizzinessDizziness DehydrationDehydration Biggest danger: getting “impure” creatineBiggest danger: getting “impure” creatine Significant WEIGHT GAIN common 2nd to Significant WEIGHT GAIN common 2nd to
water retentionwater retention
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The Perfect Supplement?
“The secret is to find something that is The secret is to find something that is effective in improving performance, but not effective in improving performance, but not against the rules, and with no side effects” against the rules, and with no side effects”
“…“…no clear evidence of harmful side effects no clear evidence of harmful side effects of creatine use has emerged…”--The of creatine use has emerged…”--The Physician and Sportsmedicine, June 1998Physician and Sportsmedicine, June 1998
Long term effects of Creatine not yet studied: Long term effects of Creatine not yet studied: Concerns focus on effects to kidney, Concerns focus on effects to kidney, pancreas, and liver.pancreas, and liver.
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Counseling your patients
Creatine may or may not improve performance
Weight gain will occur Side effects (especially long-term) not well
known Need to have renal and liver fct. Monitored
– should not be used in patients with chronic kidney/ liver disease
Do not exceed the recommended dose
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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
L-Carnitine
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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
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Choline
Precursor for the neurotransmittor Acetyl Choline & the lipoprotein Lecithin (Phosphattidylcholine)
choline depletion in marathoners no studies supporting
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Inosine
Increases myocardial contractility no performance enhancement in
runners/ cyclists
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Metals/ Minerals
Chromium Magnesium Boron Vanadium
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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
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Magnesium
Involved in ptn synthesis & mm contraction
+ effects on oxygen consumption & lactate production
no change in performance
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Boron
Originally thought to inc. testosterone levels
not born out in studies
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Vanadium
What it is: Non-essential trace mineralWhat it is: Non-essential trace mineral
Claims: Anabolic effect, enhances insulin Claims: Anabolic effect, enhances insulin actionaction
What it does: No studies to show anabolic What it does: No studies to show anabolic effect. Doses>10gms/day causes abd. Pain, effect. Doses>10gms/day causes abd. Pain, cramps, green tongue,diarrhea, wt. losscramps, green tongue,diarrhea, wt. loss
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Antioxidants
Vitamins E & C potential damage from free oxygen
radicals produced by lipid peroxidation in exercise
exercise performance is not improved
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Herbs
Ginseng Yohimbe Tribulus Terresteris Ma haung
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Ginseng
What it is: A root from an Asian plant (panax What it is: A root from an Asian plant (panax ginseng).ginseng).
Claims: Enhanced performance. Improved Claims: Enhanced performance. Improved recovery rate.recovery rate.
What it really does: Acts as an adaptogen- may What it really does: Acts as an adaptogen- may boost immune system and protect cells. May boost immune system and protect cells. May cause insomnia, and should not be used if B/p is cause insomnia, and should not be used if B/p is elevated.elevated.
Dose: 100-200mg per day used occ.2-3 weeks on Dose: 100-200mg per day used occ.2-3 weeks on 1-2 weeks off1-2 weeks off
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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
Yohimbe
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What is it: A plant hormone Claims: Anabolic effect What it does: Increases testosterone
levels Banned by NFL
Tribulus Terresteris
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Miscellaneous:
Bicarbinate Loading Coenzyme Q Linoleic Acid
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Bicarbonate Loading
Used prior to competition to neutralize lactic Used prior to competition to neutralize lactic acid produced by anaerobic activitiesacid produced by anaerobic activities
Lactic acid>>lower pH>>fatigueLactic acid>>lower pH>>fatigue May improve runners’times if taken 30 min May improve runners’times if taken 30 min
prior to competition : best in intermediate prior to competition : best in intermediate distances 800-1500 meter eventsdistances 800-1500 meter events
300mg/kg required300mg/kg required Terrible GI s/e in 50% of users--cramps, Terrible GI s/e in 50% of users--cramps,
diarrhea, ^ BPdiarrhea, ^ BP
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Coenzyme Q10 Conjugated (coQ10,Ubloquinone) Linoleic Acid
Produced by the body in mitochondria
claims: Enhances performance, delays fatigue, prevents injury
What really does:Functions as an antioxidant
Safe levels:60-200mg/day but also$$$$$
Naturally occurring fatty acid found in beef ,lamb and dairy
claims: decreases body fat ,increases muscle gain,antioxidant
What really does: No effect on performance
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References
Blue J, Lombardo J, Nutritional Aspects of Excercise: Blue J, Lombardo J, Nutritional Aspects of Excercise: Steroids & Steroid-like compounds, Clinics in Sports Steroids & Steroid-like compounds, Clinics in Sports Medicine, Vol 18, Num 3, July 1999, pp 667-689Medicine, Vol 18, Num 3, July 1999, pp 667-689
Stricker P, Other Ergogenic Agents, Sports Stricker P, Other Ergogenic Agents, Sports Pharmacology, Vol 17, Num 2, April 1998, pp283-297Pharmacology, Vol 17, Num 2, April 1998, pp283-297
Agee R, Ergogenic Aids, ASMI Lecture, Nov. 99Agee R, Ergogenic Aids, ASMI Lecture, Nov. 99
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Useful Resources
Organizations:Organizations: A) Gatorade sports science Institute 800-616-4774A) Gatorade sports science Institute 800-616-4774
B) Herb Research Foundation 303-449-2625 B) Herb Research Foundation 303-449-2625 C) USOC Drug Information Hotline 800-233-0393C) USOC Drug Information Hotline 800-233-0393
Web Sites:Web Sites: FDA:http//vm.cfsan.fda.gov/~dms/aems.html U.S. pharmacopeia:www.usp.org/did/mgraphs/botanica/index.htm Dietary Supplements Reference: http://dietary-supplements.info.nih.gov USOlympicCommittee: www.usoc.org IOC: www.olympics.org NCAA: www.ncaa.org