PCOL2605 & Nursing

DRUGS IN SPORT

brent.mcparland@sydney.edu.au
Charles Perkins Centre Level 2 2W81

Research interests:
Airway mechanics & tick-borne diseases
 Objectives

› What’s the issue with using drugs

- Cheating (what), hazardous (why), ethical (how), effectiveness.

› What’s the regulatory framework

- E.g. WADA
› What’s the evidence for effectiveness
› Does it cause harm?
› Drug pharmacology
› Recent Controversy
› Chris Froome salbutamol case

2
 What I expect you to know

› Drugs relevant to certain sports and athletes providing

examples.
- What drugs have/are used to enhance performance
- Answer questions based on what drug might be useful to enhance
performance and the method by which it helps, e.g does the drug make
you more relaxed, more alert, more powerful, faster, lighter etc.
› WADA
- Understand, but not memorise categories, e.g understand the logic
behind the classification scheme such as
- why some drugs classes are in competition only
- why some are in and out of competition
- why a TUA some are not prohibited or on the monitoring list
3
 Readings

› Rang and Dale’s Pharmacology 8th edn Chapter 58 Lifestyle drugs and drugs
in sport

› WADA : https://www.wada-ama.org/

› National Measurement Institute:

http://www.measurement.gov.au/Pages/default.aspx

› Icarus a Netflix documentary about Russia’s state-sponsored doping program

Documentary Netflix Series called (Dis)Honesty: The Truth About Lies (2015)

4
 Lifestyle Drugs

Performance enhancing drugs in sport come under the umbrella of “Lifestyle

Drugs”

Lifestyle drugs are those chosen for:

pleasure e.g. cannabinoids, phenethylamines

improving performance e.g. modafinil, androgenic steroids

improving appearance e.g. botulinum toxin, minoxidil

5
 Goldman dilemma

› Questionnaire by Gabe Mirkin (1970s):

"If I could give you a pill that would make you an Olympic
champion and also kill you in a year, would you take it?"
- What % answered YES.

› Bob Goldman Dilemma 1982 (physician and World Class

weight lifter):
"If I had a magic drug that was so fantastic that if you took it
once you would win every competition you would enter from
the Olympic Decathlon to the Mr Universe, for the next five
years but it had one minor drawback, it would kill you five
years after you took it, would you still take the drug?"
http://ecx.images-
- What % answered YES amazon.com/images/I/51UeS-
zFujL._SY344_BO1,204,203,200_.jpg
- Newer studies find 1-5% (Discuss)

6
Have Athletes Changed?

7
 Ethical Debate

› Pro drugs: just let everyone take them

- Very difficult to test for drugs either currently in use or whether used in the past
- It is often said that in order to be competitive you need to take some kind of
performance enhancing drug

› Against drugs: “play true”, role models

- Many of the drugs used have untoward adverse effects
- Even if the drug is a prescription drugs that does not mean that it does not have
any adverse effects
- Long term effects of many performance drugs is unknown
- Win at all cost attitude: more drugs → ↑ chances of adverse effects (promotes
death of our genetically physical warriors)
- What message is being sent to children who see winners as role models

8
 Drugs in the Olympics

› Ancient Olympic Games Mushrooms!

› East Germans (GDR): to validate superiority of the communist
regime they had a program from 1973-1989 that included
systematic doping e.g. oral –Turinabol® (4-
chlorodehydromethyltestosterone) "blue bean”- an anabolic steroid
containing testosterone. Likely to have been occurring from
the 1950s onward.
› 1960’s Controls introduced at the 1968 Mexico Olympic
Games largely as a result of drug testing procedures
developed in Munich
› The Munich Drug Testing Laboratory still leads the world in
developing new procedures for drug testing in athletes.
 The difference between winning and coming last

Sydney Olympic Games, Men's 100m Final

Saturday 23 September 2000

1. Maurice Greene United States 09.87

2. Ato Boldon Trinidad and Tobago 09.99 Patrick Johnson
3. Obadele Thompson Barbados 10.04 9.93s 100m
Aboriginal/Irish
descent
7. Kim Collins St Kitts and Nevis 10.17

Difference between first and last: 0.3 seconds, i.e. 3%

 The Dirtiest Race in History: Seoul 1988
Who won this race????

Ben Johnson: 9.70 WR disqualified (stanozolol)

"Look at those Canadians, they don't even know how to cheat".

Quote from another Canadian athlete on what she felt

other people were thinking

12
 Disqualified: Ben Johnson Hero to Zero

‘Ben Johnson has been caught taking drugs and is expected to be

stripped of his 100m gold medal, according to International Olympic
Committee sources.’”
BJ: "A gold medal - that's something no one can take away from you."

• Drug: Olympic Doping Control Centre found stanozolol in

urine.
• Metabolism: not metabolised with first pass, but extensive
hepatic biotransformation occurs; metabolites detectable
in urine ~10 days after a single 5–10 mg oral dose.
• Detection: gas chromatography-mass spectrometry or
liquid chromatography-mass spectrometry.
• Nobbling/sabotage? Steroid different to the one his
coach claimed he had been taking right up until weeks
before Seoul. He admitted to using steroids for 8 yrs.
• Ben Johnson came back from his suspension to run a
10.16s in 1992. He failed a second drug test in 1993, the
result of which was overturned on appeal.

• Carl Lewis - tested positive to minor amounts of several

stimulants two months before the 1988 Olympics, but was
allowed to compete.

• Linford Christie – Tested positive for pseudoephedrine

after the Seoul 200m race, but IOC medical commission
allowed him to keep his medal. He later tested positive to
nandrolone in 1999 and was suspended for 2 years.
Athens 2004 Men’s 100m Gold Medal - Justin Gatlin
 8 Year Ban: Gatlin’s whistle-blower

Tetrahydrogestrinone (THG) is a designer steroid.

 Gatlin’s times

8 year decreased to a 4 year ban

10.4

10.3

10.2 1st ban (amphetamine)

100 m (s)

10.1

10

9.9
2nd ban
9.8
annulled
9.7
1995 2000 2005 2010 2015 2020

Year

17
Usain Bolt in Beijing 2008: WR 9.69s
Bolt’s new WR Berlin 9.58s
 Choose your friends wisely: Marion Jones Sydney
2000
http://www.sporting-heroes.net/content/thumbnails/00087/08565-
zoom.jpg

http://www.renewedfitness.org/ma
rion-jones-gets-back-on-the-right-
track-monday-motivation/

Confession 2007:"...with a great amount of shame...I stand before you and tell you that I
have betrayed your trust...and you have the right to be angry with me... I have let my
country down and I have let myself down (Drug used: THG “The Clear”)
Married to the shot-putter C.J. Hunter (failed drug test 4 times to nandrolone)
 Athletic Records: Women

› Marita Koch?
- Government evidence, but still
proclaims innocence
› Florence Griffith Joyner? (click)
- Speculative, left after out-of-comp
testing: HGH?

MP pictured (circled; green cap)
tumbling over the top of her horse
(May, 2012)
MP pictured (yellow circle) tumbling
over the top of her horse (May, 2016)
Even MP: Dangerous Career
2015 Melbourne Cup
June 2017, MP stood down: tested positive
to phentermine (appetite suppressant)
banned under Australian Rule of Racing.
MP pleaded guilty to taking the weight
suppressant and banned for four weeks
21
 Organisations
Court of Arbitration
World anti-doping agency International Olympic for Sport
(formed 1999) committee CAS
WADA IOC
1963-2004 drug testing was run by the IOC
Australian Crime Commission (ACC)

Australian sports anti-doping authority

http://www.asada.gov.au/
ASADA Australian sports drug testing laboratory
ASDTL WADA accredited
http://www.measurement.gov.au/Services/Pages/Drugsinsport.aspx

Different Sporting Bodies (e.g Athletics Aus etc)

 The World Anti-Doping Agency (WADA)

http://www.wada-ama.org

2012 President: John Fahey (Australian; AC)

2014: David Howman
2016: Sir Craig Reedie (pic)

Athletes are responsible for any

Prohibited Substance or its Metabolites or
Markers found to be present in their Samples
 WADA: Rationale
Doping is fundamentally contrary to the spirit of sport
• Ethics, fair play and honesty
• Health
• Excellence in performance
• Character and education
• Fun and joy
• Teamwork
• Dedication and commitment
• Respect for rules and laws
• Respect for self and other Participants
• Courage
• Community and solidarity
 Doping

• Following drug fiasco in cycling led to establishment of

WADA (1999); code introduced in 2004
• Doping: occurrence of one or more of the anti-doping rule
violations set forth in Code as set out by the World Anti-
Doping Agency (WADA)
(CNN) -- Only 10% of drugs cheats are being
caught at the Olympics. Former WADA anti-doping
chief Dick Pound told CNN.
"If you get caught you fail two
tests, a drugs test and an IQ test."
How prevalent is cheating? Anonymous survey at 2
athletics meetings in 2011: ~50% use performance Dick Pound
enhancing drugs Ulrich, R., et al., Sports Med, 2018. 48(1): p. 211-219.
https://en.wikipedia.org/wiki/Doping_at_the_1998_Tour_de_France
 WADA

How substances become prohibited

For a substance or method to be prohibited, it must meet two of the following
three conditions:
1. The substance or method has the potential to enhance or does enhance
performance in sport.
2. The substance or method has the potential to risk the athlete’s health.
3. WADA has determined that the substance or method violates the spirit of sport.

• Prohibited at all times (In- and Out- Of- Competition)

• Prohibited In Competition
• Prohibited in particular sports
• Monitoring Program/List
- to monitor drugs to ensure they are not being abused
• Therapeutic Use Exemption (TUE)
• Biological Passport
 Prohibited at all times (In- and Out- Of- Competition
Substances prohibited at all times
S0. Non-approved substances (new 2012)
S1. Anabolic Agents
S2. Peptide hormones, growth factors and related
substances and mimetics
S3. Beta-2 agonists
S4. Hormone and metabolic modulators
S5. Diuretics and other masking agents
Methods prohibited at all times
M1. Manipulation of blood and blood components
M2. Chemical and physical manipulation
M3. Gene doping
 Prohibited In Competition

Substances and Methods prohibited In-Competition

All substance categories S0-S5 and methods M1-M3 and:
S6. Stimulants
S7. Narcotics
S8. Cannabinoids
S9. Glucocorticoids
 Substances prohibited in Particular Sports

P1. Beta-blockers (sports where it may be of benefit in

terms of fine motor control: archery*, automobile,
billiards, darts, golf, shooting*, skiing/snowboarding
and underwater sports

* also Out-of-Competition

Alcohol (< 0.1 g/L = BAC 0.1%) removed from 2018
 Asthma Medication

S3. BETA-2 AGONISTS (in and out- competition)

› Inhaled salbutamol: maximum 1600 micrograms over 24 hours in divided
doses not to exceed 800 micrograms over 12 hours starting from any dose
› Inhaled formoterol: maximum delivered dose of 54 micrograms over 24 hours;
› Inhaled salmeterol: maximum 200 micrograms over 24 hours
› The presence in urine of salbutamol in excess of 1000 ng/mL or formoterol
in excess of 40 ng/mL is presumed not to be an intended therapeutic use of
the substance and will be considered as an Adverse Analytical Finding
unless the Athlete proves, through a controlled pharmacokinetic study, that
the abnormal result was the consequence of the use of the therapeutic
inhaled dose up to the maximum indicated above.

Salbutamol: 100 µg/metered dose, ie 8 puffs per 12 hrs max

Formoterol and Salmeterol: varies depending on brand; long acting so
based on max used over 24 hrs
 Asthma Medication

S9. GLUCOCORTICOSTEROIDS (in competition)

› All glucocorticosteroids are prohibited when
administered by oral, intravenous, intramuscular or
rectal routes. (inhaled OK)
 THE MONITORING PROGRAM

Monitoring Program started 2009 (Below 2019)

1. Stimulants: In-Competition only:
• Bupropion, caffeine, nicotine, phenylephrine,
phenylpropanolamine, pipradrol and synephrine.
2. Narcotics: In-Competition only:
– Codeine, hydrocodone and tramadol.
3. Glucocorticoids: In-competition (by routes of administration other
than oral, intravenous, intramuscular or rectal) and Out-of- Competition
(all routes of administration)
4. 2-ethylsulfanyl-1Hbenzimidazole (bemitil): In- and Out-
of-Competition.
5. Beta-2-agonists: In- and Out-of-Competition: any
combination of beta-2-agonists.
 Therapeutic Use Exemption & Biological Passport

› Therapeutic Use Exemption (TUE)

– ensure that athletes can be treated for a legitimate medical condition e.g. 
asthma and hypothyroidism
– If not an International‐Level Athlete then apply to National Anti‐Doping 
Organization.
› Biological Passport (dec 2009)
› The fundamental principle of the Athlete Biological Passport (ABP)
is to monitor selected biological variables over time that indirectly
reveal the effects of doping rather than attempting to detect the
doping substance or method itself.
› Modules: 1) Haematological/blood (e.g. EPO, haematocrit) and 2)
Steroidal (e.g. testosterone)
› Some sports employ biological passports: e.g cycling, track and
field, swimming, triathlon and modern pentathlon
 Major Changes to Drug Testing

› Out of competition testing (~1989) e.g. Florence Griffith Joiner retired??

› Surveillance (Tour de France 1998; Chinese swimmers 1998 - coach
found with 2 weeks supply of hGH for 4 swimmers; Lance Armstrong case)
› Blood sampling included with urine samples (introduced at Athens 2004)
› Samples since 2015 now stored for 10 years (allows for retrospective
disqualifications)
› DNA profiling of stored substances
› Markers incorporated e.g. EPO
› Cooperation with manufacturers e.g. CERA (Roche)
 Reasons for use summary

› Anabolic Agents: increase muscle development for weight lifting,

throwing and other power sports.
› Hormones: Growth hormone – hGH; Human chorionic
gonadotropin (HCG) - raises testosterone levels; erythropoeitin –
EPO to increase % rbc and ↑ O2 carrying capacity
› Beta 2 agonists: anabolic effect to ↑ muscle mass e.g clenbuterol
› Diuretics: rapid weight loss - boxing, weight lifting and dilute urine
to avoid drug detection (masking)
› Stimulants: increase alertness, wakefulness and ability to
concentrate
› Narcotic Analgesics: enable athletes to go beyond their normal
pain threshold
› Beta Blockers: calming action -archery, shooting
 Summer Olympics: disqualifications for taking
banned substances
› 1968 Mexico 1
› 1972 Munich 7
› 1976 Montreal 11
› 1980 Moscow (? No official count)
› 1984 Los Angeles 12
› 1988 Seoul 10
› 1992 Barcelona 5
› 1996 Atlanta 7
› 2000 Sydney 15 (+7 EPO if included)
› 2004 Athens 37
› 2008 Beijing 6 (now 81; also 10 positive pre-games)
› 2012 London 9 (now 116 and also 8 positive pre-games)
› 2016 Rio de Janeiro 8 (8 also positive pre-games)
https://en.wikipedia.org/wiki/Doping_at_the_Olympic_Games
 Pharmacological Champions

Floyd Landis: Testosterone Justin Gatlin: Testosterone - Marion Jones: Confessed in

Suspended until 2009 8 year ban, loss of world record 2007 to steroid use, Sydney
Olympics
 Floyd Landis: Caught

Rivalry: Lemond vs Hinault Rivalry: Armstrong vs Ullrich

 Floyd Landis: Positive T/E ratio
› urine sample: hormone testosterone to the hormone
epitestosterone (T/E ratio) 11:1 > 4:1 (permissible)

C17

• Adulthood usually ~1:1 (95th % 3.71:1)
• Since exog testosterone does not affect epiT then if T>>>>E 
likely taking exog T (C12:C13 ratio can also be used)
 What really happened?

• Is he just not telling the truth?

• Sabotage?
• Did someone alter his sample?
• If interested read this book

41
Oprah - Lance
Tour de France
 TUEs and β2-agonists

› β2-agonists potentially have anabolic-like effects and

improve recovery e.g. 8mg oral salbutamol tablets 2 wks;
a dose shown to increase sprint power in elite athletes.
› TUE (therapeutic use exemptions) abuse or not is the
question

https://www.cyclingweekly.com/news/latest-news/everything-you-
need-to-know-about-chris-froomes-salbutamol-case-362848
 Sequence of Events: Adverse Analytical Finding

› Sample collected 7th Sept 2017 Tour of Spain

› Cycling Anti-Doping Foundation (CADF)
- Sample A and B analysed
› 20th Sept: Urine salbutamol >2000 ng/ml (1000 ng/ml is
the set threshold by WADA) AAF
Froome: “My asthma got worse at the Vuelta so I
followed the team doctor’s advice to increase my
salbutamol dosage. As always, I took the greatest care to
ensure that I did not use more than the permissible dose".
› 13th Dec Team Sky make announcement of AAF
 Sequence of Events: Adverse Analytical Finding
› Event time-line
› 28 December 2017; ad-hoc procedural agreement between Union
Cycliste Internationale’s (UCI) and Chris Froome
› 31st January 2018 Chris Froome requested specific information
from WADA
› 5th March 2018 WADA responded with the specific information on the
rationale for the urine threshold limit
› UCI tribunal did not permit WADA to be included on any meetings
and WADA provided further evidence to support the threshold
› 4th June 2018 WADA received Chris Froome’s explanations wrt to
result (prior to his statement WADA wanted to run a controlled
pharmacokinetic study (CPKS))
› 28th June WADA made its decision
› 2nd July UCI closed case: No controlled pharmacokinetic study
 Salbutamol Excretion: Inhaled
Doses of inhaled salbutamol in µg are shown. In this study 8 puffs of
salbutamol did not lead to urine values above threshold nor any
improvement in performance
Nonsulphated salbutamol (cSAL)

measurements 1hr
post inhalations
Urine threshold (n=30)

800 µg
400 µg

200 µg
Wide subject
variability
placebo

Sporer BC et al (2008). Medicine and science in sports and exercise 40: 149-157 47
Controlled Pharmacokinetic Study:

Free salbutamol
Glucoronized Sal
Non-sulphated Sal

Schweizer, C., M. Saugy, and M. Kamber,

Doping test reveals high concentrations of
salbutamol in a Swiss track and field athlete.
Clin J Sport Med, 2004. 14(5): p. 312-5.
48
Simulated Results: Used in Court Case to Support
Froomes Innocence

Heuberger, J., S.C. van Dijkman, and A.F.

Cohen, Futility of current urine salbutamol
doping control. Br J Clin Pharmacol, 2018.
84(8): p. 1830-1838

+99.9% CI

• Biological Variation
• Timing
• Dehydration

mean

- 99.9% CI

49
Great debate: "Performance enhancing drugs
should be allowed in sport".
 Other Slides You May Find Interesting.

› Following slides are for interest only and are not

examinable

51
 Organised Crime and Drugs in Sports

› Collectively sport generates A$8.82 billion (2006)

Australian Bureau of Statistics
› Betting market grows at 11%
- principles of fairness
- operate in the spirit of the rules,
- never taking an unfair advantage, and making
- informed and honourable decisions at all time
 Dr Stephen Dank

Thirty-four current and former Essendon players have been cleared of taking a
banned substance during the club’s supplements program (April 1, 2015)
 2 Recent Pharmacological Champions

Maria Sharipova
Sun Yang

Evian joined Nike and Head in choosing to

maintain their partnership with the Russian, Sun Yang Chinese superstar
citing the International Tennis Federation’s swimmer (200 m freestyle
assertion that she had not doped 2016 Olympics); 3 month
intentionally (meldonium). What is this doping ban in 2014
drug? (trimetazidine)
54
 S4 Hormone and Metabolic Modulators

1. Aromatase inhibitors including, but not limited to:

2. Selective estrogen receptor modulators (SERMs) including, but
not limited to:
3. Other anti-estrogenic substances including, but not limited to:
4. Agents modifying myostatin function(s) including, but not limited,
to:
5. Metabolic modulators
- Activators of the AMP-activated protein kinase (AMPK), e.g. AICAR; and
Peroxisome Proliferator Activated Receptor δ (PPARδ) agonists e.g. GW
1516
- Insulins and insulin-mimetics
- meldonium (e.g. Maria Sharipova)
- trimetazidine (e.g. Sun Yang, Chinese swimmer)

55
 Meldonium
› Drug for Ischaemic heart disease (lack of oxygen to the heart)
- Speculative improvements in the following:
- increase in endurance performance
- improved rehabilitation after exercise
- stimulates central nervous system
- Added to the WADA list of banned substances 1 January 2016
- S4 Hormone and metabolic modulators
- 2015 WADA list of monitored drugs
- It “must” be good: 2015 European Games 662 tested: 3.5% declared use (50% won
medals) but ~9% of urine samples returned positive. Br J Sports Med doi:10.1136/bjsports-2015-
095906

- Maria said she had been using the drug for 10 years for an ongoing medical
condition. Was she confused between the trade name (Mildronate) and the
pharmacological generic name (meldonium)?
- 2 year Ban
- Not usually used for prolonged periods: safety???? Limited reports

56
 S4 Hormone and Metabolic Modulators

› Drug not approved by: U.S. Food and Drug Administration

(FDA) or its U.K. equivalent, the European Medicines Agency
› Not approved TGA (Therapeutic Goods Association) but
individuals can legally import most therapeutic goods for
personal use under the Personal Importation Scheme
https://www.tga.gov.au/personal-importation-scheme

57
 Meldonium mechanism of action

Meldonium competitively inhibits the enzyme γ-butyrobetaine hydroxylase (BBD), which

converts γ-butyrobetaine into carnitine, but also reduces carnitine adsorption by inhibiting the
sodium-coupled carnitine transporter Organic Cation/Carnitine Transporter 2 (OCTN2).

The final effect is a decreased transportation and metabolism of long-chain fatty acids leading to
decreased risk of mitochondrial injury from fatty acid oxidation.

Lippi, G., and Mattiuzzi, C. Misuse of the metabolic modulator meldonium in sports. J Sport Health Science 1-3, 2016) 58
 Trimetazidine (cardio protective)

Mechanism of action of trimetazidine (TMZ). The metabolic modulator TMZ inhibits one the
four enzymes of the β-oxidation cycle, the 3-Ketotacyl-CoA thiolase (b), this partially inhibiting
β-oxidation (a). (c) As consequence, to obtain acetyl-CoA needed to feed the TCA cycle and to
allow ATP production by respiratory chain, the cells necessarily use more glucose

DOI: 10.1002/jcsm.12097 Journal of Cachexia, Sarcopenia and Muscle (2016)

59
 They’re just medicines!

http://www.sportsintegrityinitiative.com/something-to-die-for-rebutting-the-mirkin-survey-
the-goldman-dilemma/

60
 Summary: Drugs in Sport

› World Anti-Doping Agency (WADA) annual list of Prohibited Substances.

The pharmacology behind the different classes of performance enhancing
drugs and masking substances. How effective are they? Side effects?
Methods of detection. Issues – blood sampling, out of competition testing,
monitoring, surveillance, long term storage of samples, DNA profiling,
markers in recombinant proteins, e.g. EPO. Some famous cases.

61
 End of Lecture

› Questions?
› brent.mcparland@sydney.edu.au

› Other slides may be of interest but not part of this lecture

62
 3 Years Tour de France

Tour de France 2008

Three riders caught for using EPO, including the so-called third
generation EPOs, such as Mircera® (CERA, Continuous EPO
receptor activator)

Tour de France 2009

No positives during Tour – but new agents suspected of being used

Tour de France 2010

Alberto Contador (Astana), winner, clenbuterol?
 GHRP - Australia

Note: Why are so many Australians interested in growth hormone releasing peptide?

2007 2009 2011 2013

 Essendon: vitamins and a.a
These are some of the substances that were purported to be used by the
Essendon AFL team

› Lactaway: pycnogenol
› Peptides: “amino acids”
› Melanotan 2 (not approved, darkens skin)
› Analyses sent for: IGF 1 (inter alia )
› GHRP-2 and -6, CJC-1295, thymosin Beta-4 and IGF1-LR3 and
mechano growth factor AOD-9604, tribulus and colostrum

Dr Stephen Dank
 Outcome of Essendon Investigation

› The tribunal was comfortably satisfied that the substance thymosin

beta-4 was at the relevant time a prohibited substance under the
[anti-doping] code," he said.
› "The tribunal was not comfortably satisfied that any player violated
clause 11.2 of the AFL Anti-Doping Code.“
› ASADA chief executive Ben McDevitt said “What happened at
Essendon in 2012 was, in my opinion, absolutely and utterly
disgraceful,".
Milk or Androstenedione
 Anabolic steroids OK in US baseball?

› Androstenedione (anabolic steroid)

- banned by the IOC and the US National Football
League
- available OTC in drug stores in the US and until
recently was legal in US major league baseball.
› In 1998, Mark McGwire - 196 cm tall and 114 kg - breaks
Babe Ruth’s 1927 record of home-runs in a single
season.
› Finally admits in 2010 he used androstenedione
› 2008 Beijing dropped baseball and softball

Babe Ruth
 Nandrolone from exercise or the food chain?

› The large number of positive tests for nandrolone metabolites

(including 19-norandrosterone) led to concerns that these
may be the result of 19-norsteroids as a result of high level
exercise or via the food chain.
› WADA issued a technical document on this issue on 24 May
2004.
› They concluded that exercise does not increase physiological
levels of 19-norandrosterone significantly and certainly not
sufficient to approach the threshold of 2ng/mL in the urine.
 Dietary Nandrolone

› Regarding dietary nandrolone WADA stated: ‘Although highly improbable,

the intake of a substantial amount of non-castrated pig offal, in which the
presence of norsteroids such as 19-nortestosterone has been
demonstrated, could result in the excretion of 19-norandrosterone in an
amount above the threshold during a few hours after injection.’
 At Seoul, athletes were found using:

› Stimulants - caffeine*, pemoline, pseudoephedrine

› Beta-blockers - propanolol
› Diuretics - frusemide
› Anabolic Steroids - stanozolol
› The sensitivity and accuracy of drug testing
procedures has reached an extremely high level of
sophistication.
*exceeding maximum concentration of 12 mg/L in the
urine.
Balco founder: Victor Conte

Victor Conte with

Barry Bonds (baseballer)

Dr. Don Catlin, Director,

UCLA Olympic Analytical
Laboratory, Los Angeles
Victor Conte, the brains behind Balco, the Californian laboratory that was
exposed as one of the most comprehensive doping operations in sports
history, is out of prison, back in business and working with professional
athletes again.

Overall, how prevalent is doping in athletics? “I believe that of the 10,000

athletes that competed in Sydney [in the 2000 Olympics], at least half of
them had used some sort of performance-enhancing substances,” Conte
said. “They have linked 15 people to me. My question is, where did the
other 4,985 people get their stuff?”
 Drugs and MOAs

› Cannabinoids such as tetrahydrocannabinol (THC) come from cannabis and target

cannabinoid receptors such as CB1 and CB2 receptors.
- Most of the classical effects of THC are through CB1 activation (Gi/o coupled usually, Gs rarely)
in the CNS; endogenous ligands for the receptor include: anandamide and 2-arichidonoylglycerol
(2-AG).
› Phenethylamines is group of molecules that include the amphetamine-like substances
such as MDMA (Ecstasy).
- MDMA is an amphetamine derivative that unlike most which mainly increase DA and NA, MDMA
also increases the release of 5HT and inhibits reuptake with the 5HT transporter (SERT). It’s
effects therefore lie somewhere between lysergic acid (LSD) and amphetamine (see below).
- Amphetamine: competitive inhibitor of both DA and NA transporters but not SERT. Along with
uptake of amphetamine through the transporters they passively diffuse through the neurone pm
to act on the vesicular monoamine pump (VMAT-2) consequently causing displacement of either
DA or NA into the cytosol which then is reverse transported into the synapse. Both these mechs
increase dopamine and NA within the synapse.
› Modafinil: MOA ? possibly a weak inhibitor of the dopamine transporter, but also known
to increase histamine in the hypothalamus
› Botulinum toxin,
› Minoxidil
75
 Some Useful Links

› NMI (National Measurement Institute) website is useful with associated links –

especially the “student opportunities” link
http://www.measurement.gov.au/Pages/Student-Opportunities.aspx
›
› ASDTL is now part of Measurement Australia and the National Measurement Institute
› http://www.measurement.gov.au/Services/Pages/Drugsinsport.aspx
›
› Measurement Australia have moved from Pymble to Delhi Rd in North Ryde (near
CSIRO) http://www.measurement.gov.au/Pages/contact.aspx
›
› Some of their research projects are listed here
http://www.measurement.gov.au/ScienceTechnology/Pages/ADSL.aspx#
›
› Antidoping Rule Violation Panel – (andrew.mclachlan@sydney.edu.au)

76
 Athlete Biological Passport (ABP)

› Athlete Biological Passport Operating Guidelines & Compilation of

Required Element (65 page document); v4 2013
› Five sports employ biological passports: cycling, track and field,
swimming, triathlon and modern pentathlon

› Early 2000 (marker for blood doping)

- 1st published 2009
› Haematological and Steroidal Modules
- rEPO or blood transfusions
- Isotope Ratio Mass Spectrometry (exog steroids): C12:C13 ratio
 Prescribing Habits of Physicians as Described by
Goldman

Where do you draw the line between drug categories?

Physicians prescribe drugs

Restorative only
Drugs
Restorative
(therapeutic)
Restorative + Ergogenic
Ergogenic

http://ecx.images-
Nothing amazon.com/images/I/51UeS-
zFujL._SY344_BO1,204,203,200_.jpg

78
 Within a sporting context, a drug may be taken for
a variety of reasons

› Legitimate therapeutic purposes

› Performance continuation
› Recreational use
› Performance enhancement
› Clear distinctions cannot always be made between the
various uses
 London 2012

› WADA announced (John Fahey) from 71,649

test 107 athletes failed prior to games ie out of
competition (covered a period of 6 mths before
16th July)
› During the "In-competition" period (16 July to
12 August 2012) Olympic competitors tested at
any time without notice or in advance.
- 24 tested positive provisionally banned by their
sporting body
- 9 tested positive and sanctioned by IOC
- 4 medals returned
 London 2012

https://wada-main-prod.s3.amazonaws.com/resources/files/PlayTrue-2012-02-London-Games-web-EN.pdf 81