DRUGS BANNED IN SPORT

The use of performance-enhancing substances or techniques to augment an athlete’s ability to succeed in competitive sports is a pertinent and timely topic for athletes, coaches, and any involved health care provider. The use of these agents or methods, whether legal or illegal, can occur at all levels of sports – from high school or college student athletes, to international Olympic competitors, to professional athlete celebrities. At the professional and Olympic level, each athlete is responsible for the drugs they consume and knowing if any of these substances are on the World Anti-Doping Code Prohibited List, which is published yearly by the World Anti-Doping Agency (WADA).

2017 WADA Prohibited List

World Anti-Doping Code Prohibited List

The World Anti-Doping Code Prohibited List is an International Standard. The List groups substances and methods by those that are banned at all times (in and out of competition), those that are banned in-competition only, and those that are banned by a particular sport. If an athlete has a legitimate medical reason to use one of the banned agents, a Therapeutic Use Exemption (TUE) may be granted only after extensive review. This List was originally published in 1963 under the direction of the International Olympic Committee. As of 2004, the World Anti-Doping Agency is in charge of updating and publishing the List each year.

Athletic drug testing is done to detect banned substances or performance enhancing agents in competitive-level athletes. In the U.S, drug testing may occur in Olympic-level sports, National Collegiate Athletic Association sports (NCAA), and professional sports. The U.S. Anti-Doping Agency (USADA) is the national anti-doping organization for the Olympic movement in the United States. With the USADA, as noted in the WADA code, testing may occur in competition or out of competition and can occur at any time and at any location. Testing can result in disqualifications, sanctions, and stripping of medals and world titles, as seen with professional cyclist Lance Armstrong.

Drugs such as

  • Erythropoietin (EPO or epoetin alfa)
  • Anabolic steroids
  • Stimulants
  • Human Growth Hormone
  • Diuretics

have been shown to impart significant performance enhancing effects. However, these substances can also be associated with dangerous and possibly life-threatening side effects. Athletes should avoid these performance-enhancing substances not only because they may compromise the privledge to compete, but also because they can be harmful or even fatal with long-term use.

Substances prohibited at all times

  • S0. Non-approved Substances
  • S1. Anabolic Agents
  • S2. Peptide Hormones, Growth Factors and Related Substances
  • S3. Beta-2 Agonists
  • S4. Hormone and Metabolic Modulators
  • S5. Diuretics and Other Masking Agents

Substances prohibited in-competition

  • S6. Stimulants
  • S7. Narcotics
  • S8. Cannabinoids
  • S9. Glucocorticosteroids

Substances prohibited in particular sports

  • P1. Alcohol
  • P2. Beta-Blockers

Blood doping

Blood doping is the injection of red blood cells, related blood products that contain red blood cells, or artificial oxygen containers. This is done by extracting and storing one’s own blood prior to an athletic competition, well in advance of the competition so that the body can replenish its natural levels of red blood cells, and subsequently injecting the stored blood immediately before competition. The resulting unnatural level of red blood cells improves oxygen transport and athletic endurance; thus, it is prohibited in most events.

Banned androgenic agents

Banned androgenic agents are either anabolic steroids, which increase testosterone and epitestosterone, thereby improving muscle strength and endurance, or beta-2 agonists (see adrenergic beta-agonist). Andro, DHEA, stanozolol, testosterone, and nandrolone, or derivates (see below) are banned anabolic steroids. Beta-2 agonists can act as bronchodilators and increase heart rates, in addition to their mild androgenic effects. Other banned androgenic agents include bambuterol, clenbuterol, salbutamol, tibolone, zeranol, zilpaterol, and selective androgen receptor modulators. While a few of the banned drugs are endogenous, that is they are normally produced in the human body, most of the banned drug are exogenous drugs chemically produced.

Exogenous anabolic androgenic steroids

This is the complete list of exogenous (non-natural) androgenic agents banned as of January 1, 2012:

  • 1-Androstenediol
  • 1-Androstenedione
  • Bolandiol
  • Bolasterone
  • Boldenone
  • Boldione
  • Calusterone
  • Clostebol
  • Danazol
  • Dehydrochlormethyltestosterone
  • Desoxymethyltestosterone
  • Drostanolone
  • Ethylestrenol
  • Fluoxymesterone
  • Formebolone
  • Furazabol
  • Gestrinone
  • 4-Hydroxytestosterone
  • Mestanolone
  • Mesterolone
  • Metenolone
  • Methandienone
  • Methandriol
  • Methasterone
  • Methyldienolone
  • Methyl-1-testosterone
  • Methylnortestosterone
  • Methyltestosterone
  • Metribolone
  • Mibolerone
  • Nandrolone
  • 19-Norandrostenedione
  • Norboletone
  • Norclostebol
  • Norethandrolone
  • Oxabolone
  • Oxandrolone
  • Oxymesterone
  • Oxymetholone
  • Prostanozol
  • Quinbolone
  • Stanozolol
  • Stenbolone
  • 1-Testosterone
  • Tetrahydrogestrinone
  • Trenbolone

Drugs with similar structures and biological activity are also banned because new designer drugs of this sort are always being developed in order to beat the drug tests.

Endogenous anabolic androgenic steroids

The following substances, ordinarily produced naturally in the body, are prohibited when administered from outside the body.

  • Androstenediol
  • Androstenedione
  • Dihydrotestosterone
  • Prasterone (dehydroepiandrosterone DHEA)
  • Testosterone

METABOLITES AND ISOMERS

Metabolites and isomers of endogenous anabolic androgenic steroids, including:

    • 5α-Androstane-3α,17α-diol
    • 5α-Androstane-3α,17β-diol
    • 5α-Androstane-3β,17α-diol
    • 5α-Androstane-3β,17β-diol
    • Androst-4-ene-3α,17α-diol
    • Androst-4-ene-3α,17β-diol
    • Androst-4-ene-3β,17α-diol
    • Androst-4-ene-3β,17α-diol
    • Androst-5-ene-3α,17α-diol
    • Androst-5-ene-3α,17β-diol
    • Androst-5-ene-3β,17α-diol
  • 4-Androstenediol
  • 5-Androstenedione
  • Epi-dihydrotestosterone
  • Epitestosterone
  • 3α-Hydroxy-5α-androstan-17-one
  • 3β-Hydroxy-5α-androstan-17-one
  • 7α-Hydroxy-DHEA
  • 7β-Hydroxy-DHEA
  • 7-Keto-DHEA
  • 19-Norandrosterone
  • 19-Noretiocholanolone

Other anabolic agents

  • Clenbuterol
  • Selective androgen receptor modulators (SARMs)
  • Tibolone
  • Zeranol
  • Zilpaterol

Hormones and related substances

Certain peptide hormones increase bulk, strength, and oxygen-carrying red blood cells.

Erythropoiesis-stimulating agent

Erythropoiesis-stimulating agents such as erythropoietin (EPO), darbepoetin (dEPO), hypoxia-inducible factor (HIF) stabilizers, methoxy polyethylene glycol-epoetin beta (CERA) and peginesatide (Hematide); growth hormone (hGH), insulin-like growth factors (IGF-1, etc.), fibroblast growth factors (FGFs), hepatocyte growth factors (HGF), mechano growth factors (MGFs), platelet-derived growth factor (PDGF), vascular endothelial growth factor (VEGF), chorionic gonadotropin (banned in men only), somatotrophin (growth hormone), insulins and corticotrophins, corticosteroid mimics, and their releasing factor, are banned.

Also banned are any other growth factor affecting muscle, tendon or ligament protein synthesis/degradation, vascularization, energy utilization, regenerative capacity or fiber type switching; and other substances with similar chemical structure or similar biological effects.

Beta-2 agonists

All beta-2 agonists and their D– and L-isomers, are banned. However, formoterol, salbutamol, salmeterol, and terbutaline may be used with a “therapeutic use exemption”, only in the inhaled form.

Hormone antagonists and modulators

Hormone levels of a particular hormone, like testosterone, can be changed not only by administering it, but also by altering related hormones. For example, the estrogens estrone and estradiol are biosynthetically produced by the enzyme aromatase, respectively, from androstenedione and testosterone, which are both produced from 17α-hydroxyprogesterone. Thus, when the body senses low levels of estrogen, the precursor compounds 17α-hydroxyprogesterone, androstenedione, and testosterone are up-regulated. Likewise, interfering with a hormone’s receptor leads to similar effects. Because of these natural hormone-hormone interdependent biosynthetic pathways and hormone-receptor interactions, all aromatase inhibitors, including anastrozole, letrozole, aminoglutethimide, exemestane, formestane, and testolactone are banned. Selective estrogen receptor modulators, including raloxifene, tamoxifen and toremifene are banned. Clomiphene, cyclofenil, fulvestrant, and all other anti-estrogenic substances are banned. Myostatin inhibitors are banned. Metabolic modulators including peroxisome proliferator-activated receptor delta (PPARδ) agonists (e.g., GW 1516), PPARδ-AMP-activated protein kinase (AMPK) axis agonists (e.g. AICAR) are also banned.

Stimulants

Stimulants directly affect the central nervous system, increasing blood flow and heart rate. Stimulants that are banned include amphetamines, beta-2 agonists, ephedrine, pseudoephedrine, fencamfamine, cocaine, methamphetamines, mesocarb, and other substances with similar chemical structures and biological effects, including the following:

  • Adrafinil
  • Adrenaline (local use allowed)
  • Amfepramone
  • Amiphenazole
  • Amphetamine
  • Amphetaminil
  • Armodafinil (active enantiomer of Modafinil)
  • Benfluorex
  • Benzphetamine
  • Benzylpiperazine
  • Bromantane (Ladasten)
  • Cathine (5 ug/ml urine limit)
  • Clobenzorex
  • Cocaine
  • Cropropamide
  • Crotetamide
  • Cyclazodone
  • Dimethylamphetamine
  • Ephedrine
  • Etamivan
  • Etilamphetamine
  • Etilefrine
  • Famprofazone
  • Fenbutrazate
  • Fencamfamin
  • Fencamine
  • Fenetylline
  • Fenfluramine
  • Fenproporex
  • Furfenorex
  • Heptaminol
  • Isometheptene
  • Levmethamfetamine
  • Meclofenoxate
  • Mefenorex
  • Mephentermine
  • Mesocarb
  • Methamphetamine (D-)
  • 4-Methylamphetamine
  • Methylenedioxyamphetamine
  • Methylenedioxymethamphetamine
  • Methylephedrine
  • Methylphenidate
  • Modafinil
  • Nikethamide
  • Norfenefrine
  • Norfenfluramine
  • Octopamine
  • Ortetamine
  • Oxilofrine
  • Parahydroxyamphetamine
  • Pemoline
  • Pentetrazol
  • Phendimetrazine
  • Phenmetrazine
  • Phentermine
  • 4-Phenylpiracetam (carphedon)
  • Prenylamine
  • Prolintane
  • Propylhexedrine
  • Selegiline
  • Sibutramine
  • Strychnine
  • Tuaminoheptane

Diuretics and masking agents

Diuretics, which increase the production of urine, and masking agents, chemical compounds which interfere with drug tests, are banned for two reasons. First, by decreasing water retention and thus decreasing an athlete’s weight, an important consideration in many speed sports, they increase the speed of an athlete. Secondly, increased urine production depletes the concentration of both the banned drugs and their metabolites, making their detection more difficult. Masking agents, on the other hand, work by making drug tests ineffective, leading to false-negative results. Desmopressin, plasma expanders (such as glycerol; intravenous administration of albumin, dextran, hydroxyethyl starch and mannitol), probenecid, and other substances with similar biological effects are also banned. Local application of felypressin in dental anesthesia is not prohibited.

Diuretics

The following diuretics, and chemicals with similar structure or biological activity are banned:

  • Acetazolamide
  • Amiloride
  • Bendroflumethiazide
  • Bumetanide
  • Canrenone
  • Chlorthalidone
  • Chlorothiazide
  • Etacrynic acid
  • Furosemide
  • Hydrochlorothiazide
  • Indapamide
  • Metolazone
  • Spironolactone
  • Triamterene

Narcotics and cannabinoids

Narcotic analgesics decrease the sensation of serious injuries, allowing athletes to continue training for competition after serious injuries. While some painkillers are allowed, including codeine, the following are banned:

  • Buprenorphine
  • Dextromoramide
  • Diamorphine (heroin)
  • Fentanyl and its derivatives
  • Methadone
  • Morphine
  • Oxycodone
  • Oxymorphone
  • Pentazocine
  • Pethidine

The cannabis products marijuana and hashish are also banned in competition due to their cannabinoid content

Glucocorticoids

Glucocorticoids are a class of corticosteroids that affect the metabolism of carbohydrates, fat, and proteins, and regulate glycogen and blood pressure levels.They possess pronounced anti-inflammatory activity and cause alteration of connective tissue in response to injuries. The anti-inflammatory and connective tissue effects of glucocorticoids might mask injuries, leading to more serious injuries to athletes. Because of this and metabolic regulation effects, the administration of any glucorticoid orally, rectally, intraveniously, or intramuscularly is prohibited and requires a therapeutic use exemption. Topical uses of glucocorticoids does not require an exemption.

Beta blockers

Beta blockers are prohibited during competition in a number of sports; out of competition, they are prohibited only in archery and shooting. The prohibited beta blockers include:

  • Acebutolol
  • Alprenolol
  • Atenolol
  • Betaxolol
  • Bisoprolol
  • Bunolol
  • Carteolol
  • Carvedilol
  • Celiprolol
  • Esmolol
  • Labetalol
  • Levobunolol
  • Metipranolol
  • Metoprolol
  • Nadolol
  • Oxprenolol
  • Pindolol
  • Propranolol
  • Sotalol
  • Timolol

Therapeutic Use Exemptions

Therapeutic Use Exemptions (TUEs) is a term used by WADA and the United States Anti-Doping Agency to denote banned substances that are “required to take to treat an illness or condition”. These exemptions are regulated by the International Standard for Therapeutic Use Exemptions (ISTUE). The detection of such substances in samples is labelled by WADA as an “Adverse Analytical Finding” (AAF), which is distinct from “Anti-Doping Rules Violations” (ADRV)