Drugs in Sport by Mottram, David R. -- Read -- Imperial Library of Trantor

Index

Contents Contributors Section I The basis for and regulation of drug use in sport

Chapter 1 An introduction to drugs and their use in sport

1.1 Definition of a drug 1.2 Classification and description of drug names 1.3 Development of new drugs 1.4 Dosage forms for drug delivery to the body 1.5 The absorption, distribution, metabolism and elimination of drugs

Absorption Distribution Metabolism Elimination

1.6 Effect of exercise on pharmacokinetics 1.7 Drugs and their targets 1.8 Agonists and antagonists 1.9 Side effects of drugs 1.10 Complex drug reactions 1.11 Drugs and the law

The definition of a medicinal product

Classes of medicinal products

1.12 Why drugs are used in sport

Legitimate therapeutic use of drugs Performance continuation Recreational/social use

Amphetamines Cocaine Caffeine Narcotics Alcohol Cannabinoids

Performance enhancement

1.13 References

Chapter 2 A historical perspective of doping and anti-doping in sport

2.1 Introduction 2.2 The ancient Olympic and Roman games 2.3 Nineteenth century 2.4 Early twentieth century 2.5 Nineteen forties and nineteen fifties 2.6 Nineteen sixties 2.7 Nineteen seventies 2.8 Nineteen eighties 2.9 Nineteen nineties 2.10 Two thousand and beyond 2.11 The race between doping and anti-doping 2.12 References

Chapter 3 Medicines for Olympic and Commonwealth Games

3.1 Introduction 3.2 The Games polyclinic 3.3 Medical services at sporting venues 3.4 The Games formulary

Drugs for the Winter Games versus Summer Games Drugs for dental use Drugs for disasters Tropical and international medicine Traditional medicines Quality testing of drugs

3.5 Patterns of drug use 3.6 Prescribing procedures

Prescribing by team doctors Importation of drugs for team use

3.7 Drug information services 3.8 Summary 3.9 References

Section 2 Substances and methods prohibited in sport

Chapter 4 Anabolic agents

4.1 Introduction 4.2 The testosterone family

Biosynthesis The biochemistry and physiology of testosterone Mode of action of testosterone

Metabolism

The physiological role of testosterone

Androgenic effects Anabolic effects

4.3 Structural analogues of testosterone: the anabolic steroids

Clinical uses of androgens/anabolic steroids

Replacement therapy in men Replacement therapy in women Gynaecological disorders Protein anabolism Anaemia Osteoporosis Growth stimulation

Side effects of androgens

In females In children In males General side effects

4.4 Anabolic steroids and sport

Sources, supply and control Patterns of administration and use

Cycling Pyramiding Stacking

The prevalence of anabolic steroid abuse Efficacy of anabolic steroids

Effects on muscle Effects on behaviour Effects on muscle repair

4.5 Precursors, nandrolone and steroid metabolites

5-α-dihydrotestosterone (DHT) Nandrolone

4.6 Anabolic steroid side effects with particular reference to athletes

Cardiovascular

Blood volume Salt and water retention Hypertension Ventricular function Effects on blood lipids and lipoproteins Blood-clotting

Carcinomas Sex-related side effects

Fertility Effects on libido Gynaecomastia Specific actions in female athletes

Tendon damage Glucose regulation Behavioural effects and addiction Long-term risks of anabolic steroid abuse Indirect consequences of anabolic steroid abuse

4.7 Detection of testosterone and anabolic steroids

Tests for anabolic steroids Detection of testosterone misuse Steroid profiling Cooperation with law enforcement agencies

4.8 Other anabolic agents

Clenbuterol and other Beta-2 agonists (β2-agonists) Selective androgen receptor modulators (SARMs) Tibolone

4.9 References

Chapter 5 Peptide hormones and related substances

5.1 Introduction 5.2 Erythropoiesis-stimulating agents 5.3 Human growth hormone (hGH)

Introduction Release of human growth hormone Human growth hormone action

Effects on muscle Effects on bone Effects on metabolism Effects on adipose tissue Effects of exercise on hGH

Administration and supply of hGH Growth hormone disorders

5.4 The abuse of hGH in sport

Side effects associated with hGH abuse in sport Who abuses growth hormone and why? Detection of hGH abuse

The indirect “markers” approach to hGH doping detection The direct “isoform” approach to hGH doping detection

5.5 Human chorionic gonadotropin (hCG)

Therapeutic use hCG abuse in sport Side effects of hCG in sport Prevalence of hCG abuse

5.6 Luteinizing hormone (LH) and its use in sport 5.7 Insulin and its use in sport 5.8 Corticotropins

Administration of ACTH Abuse of ACTH Detection of ACTH

5.9 References

Chapter 6 Beta-2 agonists

6.1 Introduction 6.2 Asthma and its treatment

Definition Epidemiology Pathophysiology Trigger factors

6.3 Exercise and asthma

Prevalence of asthma in athletes Pathogenesis of exercise-induced asthma (EIA)

6.4 Management of asthma

Stepping down

6.5 Management of exercise-induced asthma (EIA)

Non-drug treatment Drug treatment with β2-agonists

6.6 Pharmacology of b2-agonists

Bronchodilation Anabolic effects of β2-agonists

6.7 β2-agonists and the WADA prohibited list

Therapeutic Use Exemption regulations with respect to β2-agonists

6.8 The use of β2-agonists in sport

Prevalence of β2-agonists in sport Cases involving β2-agonists

Barcelona Olympics, 1992 The “Festina Affair”, 1998 Jessica Hardy, 2008

Do β2-agonists enhance performance?

6.9 References

Chapter 7 Hormone antagonists and modulators

7.1 Introduction 7.2 Hormone antagonists and modulators and the WADA prohibited list 7.3 Clinical use of hormone antagonists and modulators

Aromatase inhibitors Selective oestrogen receptor modulators (SERMs) Other anti-oestrogenic substances Agents modifying myostatin function(s)

7.4 The use of hormone antagonists and modulators in sport 7.5 References

Chapter 8 Diuretics and other masking agents

8.1 History of diuretics and other masking agents in sport

Case studies involving masking agents

Pedro Delgardo, 1988 8th Swimming World Championships, Australia, 1998 World Nordic Skiing Championships, Finland, 2001 Zach Lund, 2006

8.2 Action and use of diuretics in sport

Clinical uses of diuretics Diuretics as masking agents Diuretics in sports requiring weight limitation or categorisation Diuretic use with other prohibited substances Other uses of diuretics associated with sport

8.3 Action and uses of other masking agents in sport

Probenecid Plasma expanders Epitestosterone Alpha reductase inhibitors

8.4 Current WADA classification of diuretics and masking agents 8.5 References

Chapter 9 Enhanced oxygen transfer

9.1 Introduction 9.2 Physiology

Erythropoiesis Oxygen transport Regulation of erythropoiesis

Erythropoietin in health

9.3 Erythropoietin

Mode of action of erythropoietin Recombinant erythropoietin Detection of EPO Abuse of EPO

9.4 Blood doping

Blood transfusion Methods of blood doping Testing for blood doping Abuse

9.5 Blood substitutes

Haemoglobin-based oxygen carriers (HBOCs) Perfluorocarbons (PFCs)

9.6 Haemoglobin modifiers

Plasma volume expanders

9.7 Actovegin 9.8 Biological passports 9.9 Conclusion 9.10 References

Chapter 10 Prohibited methods

10.1 Current (2010) WADA regulations with respect to chemical and physical manipulation 10.2 Prevalence of chemical and physical manipulation in sport

WADA statistics relating to chemical and physical manipulation Case studies of attempted chemical and physical manipulation

Katrina Krabbe, 1992 Michelle de Bruin (née Smith), 1998 Galabin Boevski, 2003 Rebeca Gusmão, 2007 Olga Yegorova, 2008

10.3 Techniques for identifying chemical and physical manipulation 10.4 References

Chapter 11 Gene doping

11.1 Introduction 11.2 Methods of genetic modification 11.3 Genes that might enhance athletic performance 11.4 Methods of detection 11.5 The practicalities and risks of gene doping 11.6 Summary 11.7 Acknowledgements 11.8 References

Chapter 12 Stimulants

12.1 History of stimulant use in sport

Case studies related to stimulants

Tommy Simpson Kelli White Andreea Raducan Alain Baxter Martina Hingis Richard Gasquet

12.2 Types of stimulants and their modes of action

Ephedrine, methylephedrine and cathine Amphetamines

The mode of action of amphetamine Pharmocokinetics The effect of amphetamines on human mood and performance Adverse effects of amphetamines

Cocaine

Pharmacology Pharmacokinetics Adverse effects

12.3 Stimulants and sport

Ephedrine and other sympathomimetics in sport Adverse effects of sympathomimetics in athletes Amphetamines in sport Adverse side effects of amphetamines in athletes Effects of cocaine in athletes and on exercise Adverse effects of cocaine in athletes

12.4 Stimulants and the WADA prohibited list 12.5 References

Chapter 13 Narcotic analgesic drugs

13.1 Introduction 13.2 Pain and nociception 13.3 Mechanism of action of narcotic analgesics 13.4 Side effects of narcotic analgesics 13.5 The use of narcotic analgesics in sport

Indirect enhancement of performance Cycling Long-distance running Runner’s high Equestrian sport World Anti-Doping Agency statistics Therapeutic Use Exemption

13.6 References

Chapter 14 Cannabinoids

14.1 What are cannabinoids?

The source of cannabinoids Mode of action of cannabinoids Effects and side effects of cannabinoids Cannabis use in society

14.2 History of cannabis in sport

Addition to the prohibited list Case studies relating to cannabinoids

Ross Ribagliati, 1998 Tomas Enge, 2002 Michael Phelps

14.3 Cannabinoids in sport

The use of cannabinoids within sport Are cannabinoids performance enhancing? Adverse effects of cannabinoids in sport The consequences of cannabinoid use for other competitors

14.4 Cannabinoids and the WADA prohibited list

WADA regulations with respect to cannabinoids Prevalence of adverse findings for cannabinoids Passive ingestion of cannabinoids Should cannabinoids be on the WADA prohibited list?

14.5 References

Chapter 15 Glucocorticosteroids

15.1 Introduction 15.2 The functions and side effects of glucocorticosteroids

Mechanisms of action of glucocorticoids

15.3 Local steroid injections 15.4 Other uses of glucocorticoids 15.5 WADA regulations for the use of glucocorticosteroids 15.6 References

Chapter 16 Alcohol

16.1 Introduction 16.2 Anxiety and performance 16.3 Metabolism of alcohol 16.4 Action of alcohol on the nervous system 16.5 Alcohol and health 16.6 Alcohol and physiological responses to exercise 16.7 Alcohol in aiming sports 16.8 Alcohol and sports accidents 16.9 Overview 16.10 References

Chapter 17 Beta blockers

17.1 What are beta blockers?

Mode of action of beta blockers Effects of beta blockers Side effects of beta blockers

17.2 History of beta blockers in sport 17.3 Beta blockers and the WADA prohibited list

WADA regulations with respect to beta blockers Prevalence of adverse findings for beta blockers

17.4 The use of beta blockers in sport

Adverse effects of beta blockers in sport Potential benefit of beta blockers in sport

17.5 References

Section 3 Substances and methods permitted in sport

Chapter 18 Supplements for high intensity exercise

18.1 Introduction 18.2 Energy metabolism and fatigue 18.3 Creatine

Muscle creatine loading Creatine and performance Creatine and single bouts of high intensity exercise Creatine and repeated bouts of high intensity exercise Creatine and strength

18.4 Sodium bicarbonate 18.5 Beta-alanine 18.6 Conclusion 18.7 References

Chapter 19 Supplement use in sport

19.1 Introduction 19.2 Extent of supplement use 19.3 Why supplements are used 19.4 Types of supplements

Classification Vitamins Proteins and amino acids Carbohydrates Ginseng Creatine L-Carnitine Caffeine Glucosamine

19.5 Availability of supplements 19.6 Problems associated with supplement use

WADA regulations Misleading advertising, inaccurate labelling and supplement contamination Accuracy and quality of advice on supplement use Case studies involving supplements

Professional footballers in 2001 Greg Rusedski, 2003

19.7 Advice for athletes 19.8 References

Chapter 20 Caffeine

20.1 Introduction 20.2 Pharmacology 20.3 Mechanisms of action 20.4 Performance-enhancing properties

Endurance exercise Anaerobic exercise Resistance exercise Intermittent exercise Cognitive function

20.5 Caffeine combinations 20.6 Therapeutic actions 20.7 Adverse side effects 20.8 Caffeine use and WADA regulations 20.9 Summary 20.10 References

Chapter 21 Over-the-counter stimulants and herbal preparations

21.1 Introduction 21.2 Upper respiratory tract (URT) conditions and exercise 21.3 Treatment of URT conditions

The common cold and influenza Sinusitis Allergic rhinitis

21.4 Weight loss 21.5 Relief from fatigue and drowsiness 21.6 Sympathomimetic amines

Potential side effects of sympathomimetic amines Reputed ergogenic effects Sympathomimetic amine use and WADA regulations

21.7 Methylxanthines 21.8 OTC herbal stimulants

Guarana Ephedra sinica/Ma Huang Citrus aurantium

21.9 Summary 21.10 References

Chapter 22 Non-steroidal anti-inflammatory drugs

22.1 Introduction 22.2 The inflammatory response

Changes in microcirculation during the inflammatory response Leucocytes in inflammation Acute and chronic inflammation

22.3 The treatment of sporting injuries

The use of non-steroidal anti-inflammatory drugs to treat inflammatory conditions

Aspirin Naproxen Ibuprofen Indomethacin Piroxicam Diclofenac Phenylbutazone

Equestrian sport Duration of NSAID treatment The use of NSAIDs to enhance performance in endurance sports Topical NSAIDs in sports injury

22.4 References

Chapter 23 Melatonin and related substances

23.1 Background 23.2 Melatonin and biological rhythms 23.3 Other properties of melatonin 23.4 Exercise and the melatonin rhythm 23.5 Melatonin and thermoregulation 23.6 Melatonin and jet-lag 23.7 Alternatives to melatonin: the benzodiazepines 23.8 Overview 23.9 References

Chapter 24 Hypoxic chambers and other artificial environments

24.1 Introduction 24.2 Exercise at altitude 24.3 Adaptations to altitude

Physiological adaptations Altitude simulation

Does it work? How does it work?

24.4 WADA attitude to artificially induced hypoxic conditions 24.5 Conclusion 24.6 References

Section 4 The extent of doping in sport

Chapter 25 Prevalence of drug misuse in sport

25.1 Introduction 25.2 Statistics on doping control in sport

Statistics from WADA-accredited laboratories Statistics derived from national surveys

25.3 Surveys into drug misuse in sport 25.4 A perspective on the prevalence of drug misuse in sport through medical practitioners 25.5 General discussion 25.6 References

Appendix Synopsis of drugs used in sport

Section 1. WADA-prohibited drugs and methods

Anabolic androgenic steroids