Drugs in Sport Fifth Edition Edited by David R. Mottram Routledge Taylor & Francis Group LONDON AND NEW YORK
Contents Contributors xv SECTION I The basis for and regulation of drug use in sport I 1 An introduction to drugs and their use in sport 3 1.1 Definition ofa drug 3 1.2 Classification and description ofdrug names 3 1.3 Development of new drugs 4 1.4 Dosage forms for drug delivery to the body 5 1.5 The absorption, distribution, metabolism and elimination of drugs 6 1.6 Effect of exercise on pharmacokinetics 9 1.7 Drugs and their targets 9 1.8 Agonists and antagonists 10 1.9 Side effects of drugs 11 1.10 Complex drug reactions 13 1.11 Drugs and the law 14 1.12 Why drugs are used in sport 16 1.13 References 19 2 A historical perspective of doping and anti-doping in sport 21 2.1 Introduction 21 2.2 The ancient Olympic and Roman games 21 2.3 Nineteenth Century 23 2.4 Early twentieth Century 23
viii Contents 2.5 Nineteen forties and nineteen fifties 24 2.6 Nineteen sixties 24 2.7 Nineteen seventies 24 2.8 Nineteen eighties 27 2.9 Nineteen nineties 27 2.10 Two thousand and beyond 28 2.11 The race between doping and anti-doping 31 2.12 References 33 3 Medicines for Olympic and Commonwealth Games 35 MARK STUART 3.1 Introduction 35 3.2 The Games polyclinic 36 3.3 Medical Services at sporting venues 37 3.4 The Games formulary 38 3.5 Patterns of drug use 41 3.6 Prescribing procedures 42 3.7 Drug information Services 44 3.8 Summary 44 3.9 References 45 SECTION 2 Substances and methods prohibited in sport 47 4 Anabolic agents ^ ALAN J. GEORGE AND 4.1 Introduction 49 4.2 The testosterone family 49 4.3 Structural analogues of testosterone: the anabolic steroids 55 4.4 Anabolic steroids and sport 58 4.5 Precursors, nandrolone and steroid metabolites 63 4.6 Anabolic steroid side effects with particular reference to athletes 65 4.7 Detection of testosterone and anabolic steroids 73 4.8 Other anabolic agents 75 4.9 References 76
Contents ix 5 Peptide hormones and related substances 82 ALANJ. GEORGE AND 5.1 Introduction 82 5.2 Erythropoiesis-stimulating agents 82 5.3 Human growth hormone (hgh) 82 5.4 The abuse ofhgh in sport 86 5.5 Human chorionic gonadotropin (hcg) 90 5.6 Luteinizing hormone (LH) and its use in sport 92 5.7 Insulin and its use in sport 93 5.8 Corticotropins 94 5.9 References 94 6 Beta-2 agonists 98 DAVID J. ARMSTRONG AND 6.1 Introduction 98 6.2 Asthma and its treatment 98 6.3 Exercise and asthma 100 6.4 Management of asthma 102 6.5 Management of exercise-induced asthma (EIA) 103 6.6 Pharmacology ofß 2 -agonists 105 6.7 ß 2 -agonists and the WADA prohibited list 107 6.8 The use ofß 2 -agonists in sport 110 6.9 References 112 7 Hormone antagonists and modulators 115 7.1 Introduction 115 7.2 Hormone antagonists and modulators and the WADA prohibited list 115 7.3 Clinical use of hormone antagonists and modulators 116 7.4 The use of hormone antagonists and modulators in sport 118 7.5 References 119 8 Diuretics and other masking agents 121 8.1 History of diuretics and other masking agents in sport 121 8.2 Action and use of diuretics in sport 124 8.3 Action and uses of other masking agents in sport 126
x Contents 8.4 Current WADA classification of diuretics and masking agents 128 8.5 References 130 9 Enhanced oxygen transfer 132 DAVID J. ARMSTRONG 9.1 Introduction 132 9.2 Physiology 133 9.3 Erythropoietin 137 9.4 Blooddoping 143 9.5 Blood substitutes 146 9.6 Haemoglobin modifiers 148 9.7 Actovegin 149 9.8 Biological passports 150 9.9 Conclusion 151 9.10 References 151 10 Prohibited methods: chemical and physical manipulation 155 10.1 Current (2010) WADA regulations with respect to chemical and physical manipulation 155 10.2 Prevalence of chemical and physical manipulation in sport 156 10.3 Techniques for identifying chemical and physical manipulation 158 10.4 References 159 11 Gene doping 160 DOMINIC J. WELLS 11.1 Introduction 160 11.2 Methods of genetic modification 161 11.3 Genes that might enhance athletic Performance 163 11.4 Methods ofdetection 166 11.5 The practicalities and risks ofgene doping 167 11.6 Summary 168 11.7 Acknowledgements 168 11.8 References 168
Contents xi 12 Stimulants 173 12.1 History of stimulant use in sport 173 12.2 Types of stimulants and their modes of action 175 12.3 Stimulants and sport 183 12.4 Stimulants and the WADA prohibited list 188 12.5 References 190 13 Narcotic analgesic drugs 193 PETER N. ELLIOTT 13.1 Introduction 193 13.2 Pain and nociception 194 13.3 Mechanism of action of narcotic analgesics 195 13.4 Side effects of narcotic analgesics 195 13.5 The use of narcotic analgesics in sport 196 13.6 References 198 14 Cannabinoids 199 14.1 What are cannabinoids? 199 14.2 History of cannabis in sport 201 14.3 Cannabinoids in sport 202 14.4 Cannabinoids and the WADA prohibited list 203 14.5 References 205 15 Glucocorticosteroids 207 PETER N. ELLIOTT 15.1 Introduction 207 15.2 The functions and side effects of glucocorticosteroids 207 15.3 Local steroid injections 210 15.4 Other uses of glucocorticoids 211 15.5 WADA regulations for the use of glucocorticosteroids 212 15.6 References 212 16 Alcohol 214 THOMAS REILLY 16.1 Introduction 214 16.2 Anxiety and Performance 215
xii Contents 16.3 Metabolism of alcohol 218 16.4 Action of alcohol on the nervous System 220 16.5 Alcohol and health 222 16.6 Alcohol andphysiological responses to exercise 224 16.7 Alcohol in aiming sports 226 16.8 Alcohol and sports accidents 230 16.9 Overview 231 16.10 References 232 17 Betabiockers 235 17.1 What are beta blockers? 235 17.2 History of beta blockers in sport 239 17.3 Beta blockers and the WADA prohibited list 239 17.4 The use of beta blockers in sport 241 17.5 References 242 SECTION 3 Substances and methods permitted in sport 245 18 Supplements for high intensity exercise: creatine and other ergogenic aids 247 DON MACLAREN 18.1 Introduction 247 18.2 Energy metabolism andfatigue 247 18.3 Creatine 248 18.4 Sodium bicarbonate 254 18.5 Beta-alanine 255 18.6 Conclusion 256 18.7 References 256 19 Supplement use in sport 262 19.1 Introduction 262 19.2 Extent of Supplement use 262 19.3 Why Supplements are used 263 19.4 Types of Supplements 264
Contents xiii 19.5 Availability of Supplements 266 19.6 Problems associated with Supplement use 267 19.7 Advice for athletes 270 19.8 References 271 20 Caffeine NEIL CHESTER 274 20.1 20.2 20.3 20.4 20.5 20.6 20.7 20.8 20.9 20.10 Introduction 274 Pharmacology 275 Mechanisms of action 276 Performance-enhancing properties 278 Caffeine combinations 282 Therapeutic actions 284 Adverse side effects 284 Caffeine use and WADA regulations 285 Summary 288 References 288 21 Over-the-counter stimulants and herbal preparations 294 NEIL CHESTER 21.1 Introduction 294 21.2 Upper respiratory tract (URT) conditions and exercise 295 21.3 Treatment of URT conditions 295 21.4 Weightloss 298 21.5 Relief from fatigue and drowsiness 298 21.6 Sympathomimetic amines 299 21.7 Methylxanthines 307 21.8 OTC herbal stimulants 309 21.9 Summary 311 21.10 References 311 22 Non-steroidal anti-inflammatory drugs 317 PETER N. ELLIOTT 22.1 Introduction 317 22.2 The inflammatory response 317 22.3 The treatment of sporting injuries 323 22.4 References 332
xiv Contents 23 Melatonin and related substances THOMAS REILLY AND JIM WATERHOUSE 333 23.1 Background 333 23.2 Melatonin and biological rhythms 335 23.3 Other properties of melatonin 336 23.4 Exercise and the melatonin rhythm 337 23.5 Melatonin and thermoregulation 338 23.6 Melatonin andjet-lag 340 23.7 Alternatives to melatonin: the benzodiazepines 344 23.8 Overview 349 23.9 References 350 24 Hypoxie chambers and other artificial environments 354 DAVID J. ARMSTRONG 24.1 Introduction 354 24.2 Exercise at altitude 354 24.3 Adaptations to altitude 355 24.4 WADA attitude to artificially induced hypoxic conditions 363 24.5 Conclusion 366 24.6 References 366 SECTION 4 The extent of doping in sport 371 25 Prevalence of drug misuse in sport 3^3 25.1 Introduction 373 25.2 Statistics on doping control in sport 373 25.3 Surveys into drug misuse in sport 380 25.4 A perspective on the prevalence ofdrug misuse in sport through medical practitioners 381 25.5 General discussion 383 25.6 References 384 Appendix: Synopsis of drugs used in sport Index 400 386