Sports Supplements

Andrew Gregory, MD

Assistant Professor, Orthopedics/ Pediatrics

Team Physician, Vanderbilt University

Jan. 10, 2002

Definition: Ergogenic Aids

Ergo = work Gennan = to produce Any substance or method used to

enhance performance through increased energy utilization:– production– control– efficiency

Classification

Drugs:– Hormones– Stimulants– Narcotics– Diuretics– B-Blockers

Supplements:– Prohormones?– Amino Acids– Metals– Antioxidants– Herbs

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

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

Hormones

HGH EPO BHCG Steroids

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

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

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

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

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

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

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

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

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 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)

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, 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

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

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

“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 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

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

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

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

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

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.

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 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!!!!!!

Amino Acids

Creatine L-Carnitine Choline Inosine HMB (B-OH-B-

Methylbutyrate)

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

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

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

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

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

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

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

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.

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

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

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 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

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 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

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

What is it: A plant hormone Claims: Anabolic effect What it does: Increases testosterone

levels Banned by NFL

Tribulus Terresteris

Miscellaneous:

Bicarbinate Loading Coenzyme Q Linoleic Acid

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

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

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

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