Performance Performance Enhancing DrugsEnhancing Drugs

Kristin ZenkerKristin ZenkerRevised by Corey Behrens: 3/07Revised by Corey Behrens: 3/07

CBE 555CBE 555

OverviewOverview

HistoryHistory TypesTypes Methods and FunctionMethods and Function RegulationRegulation AvailabilityAvailability Questions?Questions?

HistoryHistory Stories date back thousands of years to Stories date back thousands of years to

Ancient Olympic gamesAncient Olympic games Ground horse hooves and sheep testiclesGround horse hooves and sheep testicles

In Chinese traditional medicine to bolster In Chinese traditional medicine to bolster male body.male body. deer antlerdeer antler tiger bonetiger bone bear gall bladderbear gall bladder ginseng and other rootsginseng and other roots

Athletes in Late 19Athletes in Late 19thth/Early 20/Early 20thth century century Caffeine and strychnineCaffeine and strychnine

Dutch cyclist death in 1960 Olympic gameDutch cyclist death in 1960 Olympic game International Olympic Committee came out International Olympic Committee came out

with first list of prohibited drugs.with first list of prohibited drugs.

TypesTypes Steroids (Anabolic-Androgenic and THG)Steroids (Anabolic-Androgenic and THG) Blood Boosting EnhancersBlood Boosting Enhancers

ErythropoietinErythropoietin (EPO) (EPO) TransfusionsTransfusions

AutologousAutologous Homologous Homologous

Health SupplementsHealth Supplements AndrostenedioneAndrostenedione CreatineCreatine

Human Growth Hormone (hGH)Human Growth Hormone (hGH) StimulantsStimulants

AmphetaminesAmphetamines EphedraEphedra

SteroidsSteroids Lipid produced naturally Lipid produced naturally

by the human bodyby the human body TestosteroneTestosterone EstrogenEstrogen ProgesteroneProgesterone CholesterolCholesterol

Synthetic steroids Synthetic steroids ““Anabolic”Anabolic”

Greek : “to build up”Greek : “to build up” ““Anabolic-Androgenic”Anabolic-Androgenic”

Greek: “masculine, Greek: “masculine, masculinity”masculinity”

Steroids - HistorySteroids - History First produced in late 1930’sFirst produced in late 1930’s

hypogandism (testosterone deficiency)hypogandism (testosterone deficiency) Commonly prescribed for medical reasonsCommonly prescribed for medical reasons

Prevent loss of bone densityPrevent loss of bone density osteoporosis osteoporosis

Counter-acting body-wasting effects of HIV/AIDSCounter-acting body-wasting effects of HIV/AIDS 30% HIV infected men, 50% men with AIDS are hypoganadal30% HIV infected men, 50% men with AIDS are hypoganadal

Late 1950’s, weightlifters discovered the athletic Late 1950’s, weightlifters discovered the athletic benefitsbenefits

1991 – Congress adds anabolic steroids to U.S. 1991 – Congress adds anabolic steroids to U.S. Schedule III of the Controlled Substances Act (CSA) Schedule III of the Controlled Substances Act (CSA)

Used at least once in lifetime:Used at least once in lifetime: 2.5 percent of 8th graders2.5 percent of 8th graders 3.0 percent of 10th graders3.0 percent of 10th graders 3.5 percent of 12th graders3.5 percent of 12th graders

Steroids – How do they Steroids – How do they work?work?

Taken by injection or in pill formTaken by injection or in pill form Stimulates certain proteins involved in the Stimulates certain proteins involved in the

building of muscle tissuebuilding of muscle tissue Results in fat free muscle massResults in fat free muscle mass

Blocks action of bodily chemicals that Blocks action of bodily chemicals that signal muscle fatiguesignal muscle fatigue

““Cycling” and “Stacking”Cycling” and “Stacking” Cycling: period of 6-14 weeks of steroid use, Cycling: period of 6-14 weeks of steroid use,

then reduction then reduction Stacking: multiple drugs concurrentlyStacking: multiple drugs concurrently

Steroids – Side EffectsSteroids – Side Effects

Liver tumors and cancerLiver tumors and cancer JaundiceJaundice Fluid retentionFluid retention High Blood PressureHigh Blood Pressure Increase in LDL, decrease in HDLIncrease in LDL, decrease in HDL Elevated risk of heart attack and Elevated risk of heart attack and

strokestroke Kidney tumorsKidney tumors Severe acneSevere acne

Steroids –Side Effects, Steroids –Side Effects, cont’dcont’d

Differing side-effects by genderDiffering side-effects by gender Men Men

increased breast sizeincreased breast size shrinkage of testiclesshrinkage of testicles BaldnessBaldness reduced sperm countreduced sperm count possible impotencepossible impotence

WomenWomen development of masculine featuresdevelopment of masculine features facial hairfacial hair deepening of the voicedeepening of the voice reproductive abnormalitiesreproductive abnormalities

Emotional – increase in aggressive Emotional – increase in aggressive behavior, “roid rage”behavior, “roid rage”

Depression/Withdrawal symptoms from Depression/Withdrawal symptoms from addictionaddiction

Tetrahydrogestrinone Tetrahydrogestrinone (THG)(THG)

Oct 16, 2003 – US Anti-Doping Agency Oct 16, 2003 – US Anti-Doping Agency discloses existence, not FDA approveddiscloses existence, not FDA approved

Performance Factors:Performance Factors: In-competition strengthIn-competition strength Recovery from rigorous training/fatigueRecovery from rigorous training/fatigue

Steroid AlternativeSteroid Alternative gestrinonegestrinone trenbolonetrenbolone

““Designer” steroidDesigner” steroid Manipulated by chemistsManipulated by chemists Previously undetectablePreviously undetectable Bay Area Lab Co-operative (BALCO Scandal)Bay Area Lab Co-operative (BALCO Scandal)

2003 - Four US Track and Field Athletes2003 - Four US Track and Field Athletes

Erythropoietin (EPO)Erythropoietin (EPO) Glycoprotein Hormone (protein w/ sugar attached)Glycoprotein Hormone (protein w/ sugar attached)

Signal compound for production of red blood cellsSignal compound for production of red blood cells MW: 30,000 amuMW: 30,000 amu 165 Amino acid chain165 Amino acid chain 4 Oligosaccharide side chains4 Oligosaccharide side chains In blood plasma (Conc: 5 pmol/L)In blood plasma (Conc: 5 pmol/L)

Produced in kidneys, some in liverProduced in kidneys, some in liver Prod. Stimulated by low OProd. Stimulated by low O22 levels in blood (hypoxia) levels in blood (hypoxia)

FunctionFunction Binds to receptor on red blood cell precursor in bone marrowBinds to receptor on red blood cell precursor in bone marrow Transform precursor to mature cellTransform precursor to mature cell

Source:Source: Initially isolated from human urine 1977Initially isolated from human urine 1977 r-HuEPO (synthetic) from animal recombinant DNA techn.r-HuEPO (synthetic) from animal recombinant DNA techn.

EPO EPO Medical ApplicationsMedical Applications

AnemiaAnemia Chronic renal failureChronic renal failure Cancer chemotherapyCancer chemotherapy Blood transfusionBlood transfusion Surgery with excessive blood lossSurgery with excessive blood loss

PolycythemiaPolycythemia Excess of red blood cellsExcess of red blood cells

MethodsMethods intravenousintravenous

Side-effectsSide-effects FeverFever Blood clotsBlood clots Headache, Nausea, Vomiting, DeliriumHeadache, Nausea, Vomiting, Delirium Cardiovascular complicationsCardiovascular complications

EPO AbuseEPO Abuse Abuse among endurance sportsAbuse among endurance sports

CyclingCycling TriathlonsTriathlons MarathonsMarathons

Available starting in late 1980’sAvailable starting in late 1980’s No detection methodsNo detection methods

DosingDosing 3 injections per week for six weeks. 3 injections per week for six weeks. Vials contain varying concentrations Vials contain varying concentrations

doses are likely to vary considerablydoses are likely to vary considerably Competitive AdvantagesCompetitive Advantages

Increase oxygen carrying capacity of bloodIncrease oxygen carrying capacity of blood offset the decrease in red blood cells that occurs over offset the decrease in red blood cells that occurs over

several weeks of racingseveral weeks of racing

EPO Abuse cont’dEPO Abuse cont’d ComplicationsComplications

Extreme overuse leads to thickening of bloodExtreme overuse leads to thickening of blood Paired with increased blood viscosity from exercise related Paired with increased blood viscosity from exercise related

dehydrationdehydration Strains the heart, especially during sleep (i.e. low heart Strains the heart, especially during sleep (i.e. low heart

rate)rate) Excessive increase in heamatocrit detrimental to OExcessive increase in heamatocrit detrimental to O22

capacitycapacity Low flow rate, not deliverableLow flow rate, not deliverable Symptons akin to chronic altitude sicknessSymptons akin to chronic altitude sickness

DetectionDetection Animal (synthetic) vs. endogenous residueAnimal (synthetic) vs. endogenous residue Difficult because short half-life (5-6 hours)Difficult because short half-life (5-6 hours) Detection in blood and/or urineDetection in blood and/or urine Reliability heavily disputedReliability heavily disputed

Health SupplementsHealth Supplements

OTC health supplementsOTC health supplements CommonCommon Readily availableReadily available

Not regulated by the FDANot regulated by the FDA ExamplesExamples

AndrostenedioneAndrostenedione Creatine Creatine SOBE Adrenaline Rush: Sugar FreeSOBE Adrenaline Rush: Sugar Free

Androstenedione (Andro)Androstenedione (Andro)

Initially categorized as a testosterone Initially categorized as a testosterone precursorprecursor chemical from which body synthesizes chemical from which body synthesizes

testosteronetestosterone NFL banned in 1997NFL banned in 1997 Mark McGwire admitted to using in Mark McGwire admitted to using in

1998 when he set the HR record for 1998 when he set the HR record for most in one-seasonmost in one-season

FDA reclassified as a steroid in 2004FDA reclassified as a steroid in 2004

Androstenedione – Side Androstenedione – Side EffectsEffects

Gender differencesGender differences MenMen

decrease in testosterone prod.decrease in testosterone prod. increase in estrogen productionincrease in estrogen production AcnesAcnes decreased sperm countdecreased sperm count

WomenWomen AcneAcne masculinitymasculinity

CreatineCreatine Occurs naturally in the body in skeletal muscleOccurs naturally in the body in skeletal muscle Helps to supply energy to muscle cellsHelps to supply energy to muscle cells Made in the liver from 3 amino acidsMade in the liver from 3 amino acids

GlycineGlycine ArginineArginine MethionineMethionine

When taken as a nutritional supplement, increases the body’s supply of adenosine When taken as a nutritional supplement, increases the body’s supply of adenosine triphosphate (ATP)triphosphate (ATP)

ATP and CreatineATP and Creatine

Creatine – HistoryCreatine – History Usage documented back to the early 20Usage documented back to the early 20thth

centurycentury Publicity after 1992 OlympicsPublicity after 1992 Olympics

Linford Christie (gold metal 100 m dash), Sally Linford Christie (gold metal 100 m dash), Sally Gunnel (gold metal 400 m hurdles), Britain’s Gunnel (gold metal 400 m hurdles), Britain’s rowing teamrowing team

At time, low potency dosage supplements At time, low potency dosage supplements available in UKavailable in UK

1993 – Company Experimental 1993 – Company Experimental Applied Sciences (EAS) introduced Applied Sciences (EAS) introduced compound to sports nutrition compound to sports nutrition market under Phosphagen labelmarket under Phosphagen label

Creatine – What does it Creatine – What does it do?do?

Can be taken in as a powder mixed into Can be taken in as a powder mixed into a drink or as a pilla drink or as a pill

Creatine changed into molecule called Creatine changed into molecule called “phosphocreatine” – reservoir for “phosphocreatine” – reservoir for energyenergy

During intense exercise, broken down During intense exercise, broken down into creatine and phosphateinto creatine and phosphate Energy released is used to regenerate ATPEnergy released is used to regenerate ATP

Bigger storage of phosphocreatine in Bigger storage of phosphocreatine in muscles reduces fatiguemuscles reduces fatigue

CreatineCreatineSome studies suggest that… Some studies suggest that… creatine provides a boost for short creatine provides a boost for short

bursts of maximal effortbursts of maximal effort Helps with anaerobic exercise, no significant Helps with anaerobic exercise, no significant

effect for aerobic exerciseeffect for aerobic exercise Ingesting creatine can increase the level Ingesting creatine can increase the level

of phosphocreatine in the muscle by of phosphocreatine in the muscle by 20%20%

Increases in both total and fat free body Increases in both total and fat free body massmass

Buffer the lactic acid produced during Buffer the lactic acid produced during anaerobic work outsanaerobic work outs

Human Growth Hormone Human Growth Hormone (hGH)(hGH)

Naturally produced in the body – Naturally produced in the body – synthesized in the pituitary glandsynthesized in the pituitary gland

Synthetic version of hGH originally Synthetic version of hGH originally marketed in the 1980’s to treat kids with marketed in the 1980’s to treat kids with stunted growthstunted growth

Recent years promoted as anti-aging from Recent years promoted as anti-aging from drug companiesdrug companies

Currently banned by the governing Currently banned by the governing bodies of major sports, including the bodies of major sports, including the OlympicsOlympics

hGH – How does it work?hGH – How does it work? Influences a variety of metabolic process Influences a variety of metabolic process

involving carbohydrates, proteins, and involving carbohydrates, proteins, and fatty tissuesfatty tissues

Stimulates the body’s synthesis of the Stimulates the body’s synthesis of the proteins that form bone and muscle proteins that form bone and muscle tissuetissue

Stimulates collagen – necessary for Stimulates collagen – necessary for strengthening cartilage, bones, tendons, strengthening cartilage, bones, tendons, and ligamentsand ligaments

Increases testosterone levelsIncreases testosterone levels Stimulates the liver to produce growth Stimulates the liver to produce growth

factorsfactors

hGH – Side EffectshGH – Side Effects

Abnormal growth of facial hair and Abnormal growth of facial hair and skeletal features, liver problems, skeletal features, liver problems, irregularities in the processing of irregularities in the processing of insulin, and heart diseaseinsulin, and heart disease

If taken before or during puberty – If taken before or during puberty – leads to gigantismleads to gigantism

Taken excessively as an adult – leads Taken excessively as an adult – leads to diabetesto diabetes

Stimulants – In GeneralStimulants – In General Athletes use to provide a boost in energy Athletes use to provide a boost in energy

and alertnessand alertness Caffeine and Cocaine are 2 well known Caffeine and Cocaine are 2 well known

stimulantsstimulants Affect the nervous system – causes Affect the nervous system – causes

temporary increase in the heart rate and temporary increase in the heart rate and blood pressureblood pressure

Negative effects – heart attack, stroke, Negative effects – heart attack, stroke, hypertension, agitation, physical hypertension, agitation, physical addiction, sudden cardiac deathaddiction, sudden cardiac death

World Anti-Doping Agency (WADA) has a World Anti-Doping Agency (WADA) has a list of banned substances – includes more list of banned substances – includes more than 40 stimulantsthan 40 stimulants

Stimulants Commonly Used Stimulants Commonly Used by Athletesby Athletes

Amphetamines “speed” “crank”Amphetamines “speed” “crank” Used by cyclists and baseball players since Used by cyclists and baseball players since

1919thth century century Stimulant used to diminish the appetite, Stimulant used to diminish the appetite,

control weight, and treat disorders including control weight, and treat disorders including narcolepsy and ADDnarcolepsy and ADD

Releases stores of norepinephrine and Releases stores of norepinephrine and dopamine from nerve endingsdopamine from nerve endings

Prevents the transporters of norepinephrine Prevents the transporters of norepinephrine and dopamine from recycling themand dopamine from recycling them

Increases the concentration of the respective Increases the concentration of the respective neurotransmitters – promotes nerve impulse neurotransmitters – promotes nerve impulse transmission transmission

Stimulants, con’tStimulants, con’t

Side Effects of AmphetaminesSide Effects of Amphetamines Physiological Physiological

Short term – decreased appetite, Short term – decreased appetite, increased stamina and energy, nausea, increased stamina and energy, nausea, irregular heart beat, jitterinessirregular heart beat, jitteriness

Long term – tremors, restlessness, Long term – tremors, restlessness, anxiety, weakened immune systemanxiety, weakened immune system

PsychologicalPsychological Short term – alertness, euphoria, Short term – alertness, euphoria,

increased concentration, rapid talkingincreased concentration, rapid talking Long term – Insomnia, schizophrenia, Long term – Insomnia, schizophrenia,

aggressiveness, addiction, paranoiaaggressiveness, addiction, paranoia

Stimulants, con’tStimulants, con’t

Methylphendate “ritalin” and ModafinilMethylphendate “ritalin” and Modafinil Very similar to amphetaminesVery similar to amphetamines

EphedraEphedra Derived from a plant that contains the chemical Derived from a plant that contains the chemical

ephedrine – stimulant similar to amphetaminesephedrine – stimulant similar to amphetamines Increases the metabolic burning of fatty tissuesIncreases the metabolic burning of fatty tissues

Popular weight loss drug in late 1990’s early 2000’sPopular weight loss drug in late 1990’s early 2000’s Stimulant effects the nervous system to enhance Stimulant effects the nervous system to enhance

performance and help with activities of longer performance and help with activities of longer durationduration

Stimulants, con’tStimulants, con’t

Ephedra, con’tEphedra, con’t Late 2003, FDA announced ban of Late 2003, FDA announced ban of

ephedra from the marketplace because ephedra from the marketplace because of health concernsof health concerns Generated thousands of complaints and Generated thousands of complaints and

linked to more than 150 deaths in the USlinked to more than 150 deaths in the US Pulled off the marketPulled off the market

Side EffectsSide Effects Strokes, seizures, heart attacks, death, Strokes, seizures, heart attacks, death,

raise in blood sugar, irregular heart rhythmraise in blood sugar, irregular heart rhythm

RegulationRegulation Sports rules and regulations vary by Sports rules and regulations vary by

level and leaguelevel and league 3 most popular professional leagues – 3 most popular professional leagues –

NFL, NBA, MLB all have different drug NFL, NBA, MLB all have different drug policiespolicies

Most prominent effort to make uniform Most prominent effort to make uniform drug policies – 1999 IOC created WADAdrug policies – 1999 IOC created WADA Coordinated and administered extensive Coordinated and administered extensive

drug testing of athletes in the different drug testing of athletes in the different Olympic sportsOlympic sports

WADA published a list of hundreds of WADA published a list of hundreds of banned drugsbanned drugs Violators face heavy penaltiesViolators face heavy penalties

Availability of PEDAvailability of PED

SteroidsSteroids 1990’s most US producers stopped making 1990’s most US producers stopped making

and marketing anabolic steroids within the and marketing anabolic steroids within the USUS

Eastern Europe still producing steroids in Eastern Europe still producing steroids in quantityquantity

European anabolic steroids are the source of European anabolic steroids are the source of most medical grade steroids sold in the USmost medical grade steroids sold in the US

Creatine, Ephedra, hGHCreatine, Ephedra, hGH Found websites that it is possible to purchaseFound websites that it is possible to purchase

AvailabilityAvailability

ReferencesReferences http://www.emc.maricopa.edu/faculty/farabee/biobk/BioBohttp://www.emc.maricopa.edu/faculty/farabee/biobk/BioBo

okATP.htmlokATP.html http://www.nida.nih.gov/Infofacts/Steroids.htmlhttp://www.nida.nih.gov/Infofacts/Steroids.html http://www.drugabuse.gov/ResearchReports/Steroids/anabhttp://www.drugabuse.gov/ResearchReports/Steroids/anab

olicsteroids2.html#anchorolicsteroids2.html#anchor http://en.wikipedia.org/wiki/Steroidhttp://en.wikipedia.org/wiki/Steroid http://www.mayoclinic.com/health/performance-enhancing-http://www.mayoclinic.com/health/performance-enhancing-

drugs/SM00045drugs/SM00045 http://encarta.msn.com/encyclopedia_701765667/http://encarta.msn.com/encyclopedia_701765667/

Performance-Enhancing_Drugs.htmlPerformance-Enhancing_Drugs.html http://en.wikipedia.org/wiki/Creatinehttp://en.wikipedia.org/wiki/Creatine http://en.wikipedia.org/wiki/Amphetaminehttp://en.wikipedia.org/wiki/Amphetamine http://en.wikipedia.org/wiki/Anabolic_steroidhttp://en.wikipedia.org/wiki/Anabolic_steroid http://www.4-men.org/steroids/thg.htmlhttp://www.4-men.org/steroids/thg.html Kennedy, Michael. “Newer drugs to enhance sporting Kennedy, Michael. “Newer drugs to enhance sporting

performance.” performance.” Medical Journal of AustraliaMedical Journal of Australia. 173 (6): 314-. 173 (6): 314-317 SEP 18 2000 317 SEP 18 2000

http://www.medterms.com/script/main/art.asp?http://www.medterms.com/script/main/art.asp?articlekey=7032articlekey=7032

http://www.usdoj.gov/dea/pubs/abuse/10-steroids.htmhttp://www.usdoj.gov/dea/pubs/abuse/10-steroids.htm

Performance Enhancing Performance Enhancing DrugsDrugs

Questions????Questions????