Drug Use and Abuse in Sports

Drug Use and Abuse in Sports

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Drug Use and Abuse in Sports Lily Lum, BScPharm, CSPI, BScPharm, CSPI Date of Revision: January 2013

Introduction

Olympic athletes of ancient Greece are believed to have used herbs and mushrooms to improve athletic performance.1,2 Now, in the age of the modern Olympic games, athletes continue to take substances that are not officially permitted (prohibited substances) to boost their performance and give them an advantage to win. Ergogenic (performance-enhancing) drug use or doping is defined as “the administration of or use by a competing athlete of any substance foreign to the body or of any physiological substance taken in abnormal quantity or taken by an abnormal route of entry into the body with the sole intention of increasing in an artificial manner his/her performance in competition.”1 Sports organizations have developed anti-doping policies and drug testing programs in order to protect the health of the athletes and to keep competition fair and drug free.3 Although drugs carry potential adverse effects, most athletes who use them view the risk to benefit ratio as favourable.4 Ergogenic aids come from many sources and the list often appears endless as access to such products is easy, especially with use of the Internet. Ergogenic aids may be prescription or nonprescription drugs, recreational drugs such as alcohol and marijuana, nutritional supplements and herbal or natural products.

Nonprescription Drugs

A number of agents found in nonprescription products are used as ergogenic aids (Table 1). Table 1: Common Ergogenic Aids Found in Nonprescription Products

1,2,3,4,5,6

Evidence for Performance Enhancement

Drug/Drug Class

Reason for Use

Adverse Effects

Caffeine

Increased alertness; reduced perception of fatigue; increased endurance

Nervousness, insomnia, tremors, diuresis

Inconclusive or conflicting evidence; found in stimulants, combination analgesic products.

Codeine

Treatment of pain allows athlete to participate while injured but has potential to further aggravate injury

Dizziness, lightheadedness, drowsiness, nausea or vomiting, constipation

Inconclusive or conflicting evidence; found in combination analgesic products and cold preparations.

Creatine

Muscle-performance enhancer

Dizziness, diarrhea; liver and kidney toxicity at high doses

Evidence to support.7,8,9

Cyproheptadine

Promotes appetite and weight gain

Drowsiness

No evidence or theoretical, based on pharmacologic actions.

Sympathomimetics (e.g., phenylephrine,

Increased subjective energy (“energizing”

Restlessness, nervousness,

No evidence or theoretical, based on

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Drug/Drug Class

Reason for Use

Adverse Effects

Evidence for Performance Enhancement

pseudoephedrine)

effect), decreased appetite and increased metabolism

tachycardia, arrhythmias, hypertension

pharmacologic actions; found in many cold preparations.

Prescription Drugs

Many prescription drugs are also used as ergogenic aids (Table 2). Anabolic steroids are the best known. They are synthetic derivatives of the male sex hormone testosterone.1 Individuals use anabolic steroids primarily to increase muscle mass and strength. Athletes who take anabolic steroids employ unusual dosing regimens in an attempt to increase the effects of the drugs, prevent detection or decrease the occurrence of drug-related adverse effects. Stacking is a technique where several different anabolic agents (oral and injectable) are used concomitantly in order to produce a synergistic effect. Cycling is a dosing technique with on and off periods of drug use. Pyramiding is another dosing technique where low doses are initiated, increased to a plateau sometimes 10–100 times the recommended therapeutic dose and then tapered down to the original level.1,4,10 Much of what is known about the side effects of anabolic steroids involves patients receiving therapeutic doses for treatment of disease. The adverse effects of the high doses used in some doping regimens are not fully understood. 1,2,3,4,5,6,10,11

Table 2: Common Ergogenic Aids Found in Prescription Products

Evidence for Performance Enhancement

Drug/Drug Class

Reason for Abuse

Adverse Effects

Anabolic steroids

Increase muscle mass and strength

Liver toxicity; acne; gynecomastia in males; masculinization in females; premature closure of the growth centres of long bones (adolescents); psychiatric effects such as psychosis, aggression, euphoria, depression

Evidence to support.8

Beta1-adrenergic antagonists

Reduce anxiety, hand tremor and heart rate

Dizziness or lightheadedness; unusual tiredness or weakness; sexual dysfunction

No evidence or theoretical, based on pharmacologic actions.

Beta2-agonists

Anabolic effects

Dizziness, lightheadedness, nervousness, tremor, nausea, increased heart rate

Inconclusive or conflicting evidence (no evidence with inhaled formulations).

Diuretics

Promote excretion of prohibited substances; decrease weight before official weigh-ins in sports with weight classes (e.g., boxing, martial arts)

Dizziness or lightheadedness; photosensitivity (with thiazides)

No evidence or theoretical, based on pharmacologic actions.

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Drug/Drug Class

Reason for Abuse

Adverse Effects

Evidence for Performance Enhancement

Peptide hormones and analogues: Epoetin alfa (erythropoietin), darbepoetin

Increase red blood cell production, increasing aerobic capacity

Chest pain; shortness of breath; increased blood pressure

Conflicting evidence.6,12,13,14

Peptide hormones and analogues: Human growth hormone

Anabolic effects

If growth hormone is given to children or adults with normal growth, who do not need growth hormone, serious unwanted effects may occur including: development of diabetes; abnormal growth of bones and internal organs such as the heart, kidneys and liver; atherosclerosis and hypertension

Inconclusive or conflicting evidence.

Probenecid

Promote urinary excretion of a prohibited substance

Headache; joint pain, redness, or swelling; loss of appetite; nausea

No evidence or theoretical, based on pharmacologic actions.

Sildenafil, tadalafil

Increase oxygen supply by causing vasodilation in the lungs

Prolonged erection

Inconclusive or conflicting evidence.11,15

Tamoxifen

Reverse gynecomastia caused by steroids

Hot flushes, weight gain in females; sexual dysfunction in males

No evidence or theoretical, based on pharmacologic actions.

Recreational Drugs

Alcohol and marijuana may be abused by athletes with the misconception that these recreational drugs can reduce anxiety. However, alcohol and marijuana can actually impair athletic performance.1,3 In sports requiring precision, such as riflery events, alcohol in low doses may reduce essential tremor and is prohibited in competition. In-competition use of Δ9-tetrahydrocannabinol (THC) and all cannabimimetics is also prohibited.

Nutritional Supplements, Herbals or Natural Products

There are countless products (e.g., chromium picolinate, creatine) described as nutritional supplements, herbals or natural products with claims of possessing anabolic properties or other ergogenic effects.6,16 Because of the known toxicity associated with anabolic steroids, natural products are perceived as less or not harmful, and they are also more accessible to the public. Herbal or natural products are often promoted in a misleading fashion and usually have no scientific evidence to support their claims of anabolic or performance-enhancing effects.16 The Canadian Centre for Ethics in Sport (CCES) believes the use of most supplements poses an unacceptable risk for athletes and their athletic careers.17 Supplements may intentionally contain prohibited substances or may be inadvertently contaminated with prohibited substances.

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CCES states that athletes have a personal responsibility to consider all the risks associated with supplements they plan to take.18 If athletes choose to use supplements, they should take the following precautions to reduce their risk of ingesting a prohibited substance: Get a written guarantee through a direct enquiry to the manufacturer that the product is free of any substances on the WADA Prohibited List. Ask if the manufacturer is prepared to stand behind its product.

Ask the manufacturer if any products containing prohibited substances are manufactured at the same plant as the supplement. The NSF Certified for Sport program (see Resource Tips) can help athletes identify products that have been tested to confirm their content and purity. Creatine is widely used as an ergogenic aid. It is a naturally occurring compound produced by the liver, kidneys and pancreas from the amino acids glycine, arginine and methionine. Most individuals also consume 1–2 g exogenous creatine daily, primarily from meat and fish.7 Creatine is promoted as improving muscle strength and outcomes in short-duration, anaerobic events. Studies on its effectiveness are conflicting. It may improve performance in power sports (e.g., weight lifting, sprinting) but has not demonstrated any benefit in endurance sports (e.g., cycling, cross-country running).7,8 Creatine is taken as a loading dose of 5 g 4 times a day for the first 4–6 days followed by the standard dose of 2 g daily for the next 3 months.8 Because of the theoretical concerns of dehydration and heat illness during sporting events, athletes taking creatine are recommended to drink 6–8 glasses of water per day.8 Side effects are usually minimal and include nausea, vomiting, diarrhea, muscle cramps and weight gain (the latter is thought to be due to water retention). The greatest safety concern with long-term use of creatine is effects on renal function.7,8,19 There have been several case reports in the literature describing compromised renal function with the use of creatine.8 Androstenedione is a precursor of testosterone and estrone. There is some evidence that it may elevate testosterone levels and increase strength and muscle mass during resistance training.7 Information on the side effects of long-term use is not available but these are expected to be similar to those of anabolic steroids.7 Though it is illegal in Canada, some athletes may obtain supplies from sources in the United States or the Internet.

Prohibited Substances/Therapeutic Use Exemptions

Athletes are not permitted to use prohibited substances because they are believed to enhance performance. If a prohibited substance or method is used by the athlete for a specified, legitimate medical condition, they must apply for a Therapeutic Use Exemption. Some substances are not prohibited but the athlete must submit a Declaration of Use when taking them for medical reasons. Table 3 lists categories of drugs that may be considered prohibited substances in amateur sports. The list of prohibited substances may vary among different sport organizations and is subject to change. The World Anti-Doping Agency (WADA) annually publishes the WADA Prohibited List which is the international standard that designates what substance and method is prohibited in and out of competition. It also indicates whether a substance is prohibited only in a particular sport. Other substances are included in the Monitoring Program; these are not prohibited but WADA monitors their use in order to possibly detect patterns of misuse by athletes. These lists can be accessed through the CCES website (see Resource Tips). Table 3: Substances Prohibited in Amateur Sports

17

Prohibited

Examples

Comments

Anabolic androgenic steroids and other

androstenedione

Prohibited at all times

dehydroepiandrosterone

Clenbuterol (a beta2-agonist) is included as an

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Prohibited

Examples

Comments

anabolic agents

fluoxymesterone

anabolic agent.

nandrolone stanozolol

testosterone Beta2-agonists

formoterol

salbutamol salmeterol

terbutaline

Beta1-adrenergic antagonists

acebutolol atenolol

metoprolol

propranolol Caffeine Diuretics and masking agents

When given orally or by injection, beta2-agonists may have anabolic effects.

Therapeutic doses of formoterol, salbutamol and salmeterol by inhalation are not prohibited. Terbutaline by inhalation requires a Therapeutic Use Exemption.

Prohibited during competition in certain sports, e.g., billiards, darts, golf. Archery and shooting prohibit beta-blocker use both during and outside competition. Not on the Prohibited List but included in the Monitoring Program since 2004.

acetazolamide desmopressin furosemide

Prohibited because they are used to promote urinary excretion of a prohibited substance.

hydrochlorothiazide probenecid

spironolactone triamterene Glucocorticoids

fluticasone

hydrocortisone

methylprednisolone prednisone Hormone and metabolic modulators

anastrozole clomiphene

exemestane fulvestrant

Prohibited when administered by oral, IV, IM or rectal routes. Glucocorticosteroids administered by IV injection, IM injection, oral or rectal routes require a Therapeutic Use Exemption. Prohibited at all times. Insulin is permitted only to treat athletes with certified insulin-dependent diabetes. A Therapeutic Use Exemption form must be completed.

insulin

letrozole

raloxifene tamoxifen

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Prohibited

Examples

Comments

Opioids

fentanyl

Some opioids and derivatives such as codeine, dextromethorphan, diphenoxylate and propoxyphene are permitted. Hydrocodone and tramadol are included in the Monitoring Program (2012).

hydromorphone meperidine morphine

oxycodone Peptide hormones, growth factors and related substances

chorionic gonadotropin (HCG)

luteinizing hormone (LH) in males erythropoietin

growth hormone and other growth factors Stimulants

ephedrine

fenfluramine

methylhexaneamine (dimethylamylamine, DMAA)

Oral decongestants containing phenylephrine are included in the Monitoring Program. Use of decongestant nasal sprays is permitted.

methylphenidate modafinil

phentermine

pseudoephedrinea Pseudoephedrine (>150 µg/mL urinary level) is prohibited in competition; lesser amounts are permitted but are included in the World Anti-Doping Agency (WADA) 2012 Monitoring Program. Although the urinary threshold should not be attained with therapeutic use of pseudoephedrine, WADA suggests discontinuing the drug 24 hours before competition.20

a

Resource Tips

Canadian Centre for Ethics in Sport (CCES). Available from: www.cces.ca. By phone: 613-521-3340 or 1-800-672-7775. By email: [email protected] or [email protected]. NSF International Certified for Sport Program. Available from: www.nsfsport.com. World Anti-Doping Agency (WADA). Available from: wada-ama.org. By phone: 514-904-9232. By email: [email protected].

Suggested Readings

Ahrendt DM. Ergogenic aids: counseling the athlete. Am Fam Physician 2001;63:913-22. Calfee R, Fadale P. Popular ergogenic drugs and supplements in young athletes. Pediatrics 2006;117:e577-89. Canadian Centre for Ethics in Sport (CCES). 2012 Substance classification booklet. Ottawa: CCES; 2012. Available from: www.cces.ca/files/pdfs/CCES-PUB-SubstanceClassification-E.pdf. Catlin DH, Murray TH. Performance-enhancing drugs, fair competition, and Olympic sport. JAMA 1996;276:231-7.

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National Institutes of Health (NIH). National Institute on Drug Abuse (NIDA). Research Report Series: Anabolic steroid abuse. August 2006. Available from: www.drugabuse.gov/publications/research-reports/anabolic-steroid-abuse.

References 1. Wagner JC. Enhancement of athletic performance with drugs. An overview. Sports Med 1991;12:250-65. 2. Merchant WF. Medications and athletes: increasing your sports medicine knowledge. Am Drug 1992;206:6-13. 3. Catlin DH, Murray TH. Performance-enhancing drugs, fair competition, and Olympic sport. JAMA 1996;276:231-7. 4. Goldwire MA, Price KO. Sports pharmacy: counseling athletes about banned drugs. Am Pharmacy 1995;NS35:24-30. 5. Woolley BH. The latest fads to increase muscle mass and energy. A look at what some athletes are using. Postgrad Med 1991;89:195-8, 201-5. 6. Ahrendt DM. Ergogenic aids: counseling the athlete. Am Fam Physician 2001;63:913-22. 7. Barnes CL, Kushner JM. Use of creatine and androstenedione to enhance athletic performance. US Pharm 2001;26:47-9. 8. Calfee R, Fadale P. Popular ergogenic drugs and supplements in young athletes. Pediatrics 2006;117:e577-89. 9. Jenkinson DM, Harbert AJ. Supplements and sports. Am Fam Physician 2008;78:1039-46. 10. National Institutes of Health (NIH). National Institute on Drug Abuse (NIDA). Research Report Series: Anabolic steroid abuse: Why do people abuse anabolic steroids? How are anabolic steroids abused? August 2006. Available from: www.drugabuse.gov/publications/research-reports/anabolic-steroid-abuse. Accessed October 20, 2012. 11. Hsu AR, Barnholt KE, Grundmann NK et al. Sildenafil improves cardiac output and exercise performance during acute hypoxia, but not normoxia. J Appl Physiol 2006;100:2031-40. 12. Birkeland KI, Stray-Gundersen J, Hemmersbach P et al. Effect of rhEPO administration on serum levels of sTfR and cycling performance. Med Sci Sports Exerc 2000;32:1238-43. 13. Pommering TL. Erythropoietin and other blood-boosting methods. Pediatr Clin North Am 2007;54:691-9. 14. Heuberger JA, Cohen Tervaert JM, Schepers FM et al. Erythropoietin doping in cycling: lack of evidence for efficacy and a negative risk-benefit. Br J Clin Pharmacol 2012 Dec 6. [Epub ahead of print]. 15. Guidetti L, Emerenziani GP, Gallotta MC et al. Effect of tadalafil on anaerobic performance indices in healthy athletes. Br J Sports Med 2008;42:130-3. 16. Barron RL, Vanscoy GJ. Natural products and the athlete: facts and folklore. Ann Pharmacother 1993;27:607-15. 17. Canadian Centre for Ethics in Sport (CCES). 2012 Substance classification booklet. Ottawa: CCES; 2012. Available from: www.cces.ca/files/pdfs/CCES-PUB-SubstanceClassification-E.pdf. Accessed October 5, 2012. 18. Canadian Centre for Ethics in Sport (CCES). Athlete zone: Supplements. Available from: www.cces.ca/en /supplements. Accessed February 16, 2012. 19. Lattavo A, Kopperud A, Rogers PD. Creatine and other supplements. Pediatr Clin North Am 2007;54:735-60. 20. World Anti-Doping Agency (WADA). Additional information in regards to the reintroduction of pseudoephedrine to the 2010 Prohibited List. Available from: www.wada-ama.org/Documents/World_Anti-Doping_Program /WADP-Prohibited-list/WADA_Additional_Info_Pseudoephedrine_2010_EN.pdf. Accessed October 12, 2012.

Drugs and Sport — What You Need to Know

Some people think that taking drugs or other substances (such as steroids) will build their muscles, make them look better and improve their sports ability. How many products tell us they can make us faster, slimmer or less tired? Be cautious and avoid such products. They may be harmful.

What products are safe?

It is now well known that steroids cause serious side effects. Steroids can cause liver problems and mood changes. Men and boys may find that they develop breasts. Women and girls may begin to show male

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characteristics such as a deeper voice and more body hair.

Ask your pharmacist for information on the side effects of drugs or other substances. Avoid any product that has not been studied for side effects.

What products are prohibited in sports?

To find out what substances are prohibited in your sport, check with the World Anti-Doping Agency (WADA) and your national or local organization.

Carefully check the list of ingredients for any medication you are taking. Refer to the annual WADA Prohibited List for information on what substances are prohibited. This list is subject to change each year and is available on the WADA website www.wada-ama.org. If you have any questions about your medications, consult your pharmacist.

What drugs are legal?

The majority of drugs require a prescription from your doctor. While it is possible to get some drugs illegally, it is never wise to do that.

What if you have to take drugs for an illness?

Athletes can take some drugs for an illness or medical condition as long as they declare the drug in advance and apply for a Therapeutic Use Exemption. Contact the Canadian Centre for Ethics in Sport (CCES) for more information before taking any medications or supplements.

CPhA assumes no responsibility for or liability in connection with the use of this information. For clinical use only and not intended for for use by patients. Once printed there is no quarantee the information is up-to-date. [Printed on: 03-03-2016 05:48 AM] RxTx, Compendium of Therapeutics for Minor Ailments © Canadian Pharmacists Association, 2016. All rights reserved

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