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Sports Pharmacology in Athletes - Drug Action & Testing in Athletics

Pharmacology in Athletics

Pharmacology is very important in athletics. Pharmaceuticals produce physiological responses in the body. These physiological responses can affect performance. Exercise also causes physiological responses. Therefore, exercise can influence the actions of pharmaceuticals. In most cases, when athletes take prescription or over the counter medications, exercise does not have detrimental affects on the drugs actions, but the medications can have detrimental affects on performance and wellness. For instance, athletes often take over the counter cold medications.

These medications contain chemical compounds that accelerate the heart rate, cause nervousness, and other physiological reactions. During exercise this can reduce an athletes ability to perform and can put them at risk for harm. Athletes compete with these medications in their systems all the time and have few reported problems, but in certain situations it can be harmful.

Races in the Olympics are won by thousandths of a second. Any edge an athlete can gain will in fact increase his/her chance of winning the gold medal and millions of dollars in endorsements. Performance enhancing substances have become increasingly popular. Triathletes have been known to abuse albuterol a drug used to treat asthma. They claim it helps them breath better when they compete.

Sprinters, football players, and baseball players have all been recently accused of abusing anabolic steroids. They claim it makes them bigger, stronger, and more powerful. Therefore, by abusing these drugs and altering physiological processes in their body, these drug abusing athletes gain an advantage. Thus, rules have been made banning certain substances from competition. This puts everyone on a level playing field.

Doctors now have to be careful when prescribing drugs because most are banned by the International Olympic Committee, NCAA, and many other professional athletic organizations. Athletes who test positive for these drugs can be disqualified from an athletic event, suspended for up to a season, or banned for life from competition. The best and safest alternative for athletes is to compete in what is considered to be all natural competition (no performance enhancing drugs) and not to abuse drugs.

Drug Action

In order to understand drugs, one must know how drug compounds act while in the body. Drugs are taken to produce an effect on certain physiological functions in the body. Many factors will determine the magnitude of the effect of the drug, such as method of administration of the drug, frequency, duration, and dosage.

Drugs can be administered in many different ways, orally, IV, etc. In fact, athletes can contract drugs from eating animals treated with certain drugs. These usually show up as false positives during a drug test. The way in which a drug enters the body will greatly influence its effect on the body. Pharmaceuticals can be administered in many different combinations such as once a day, twice a day, and as needed. This represents the frequency in which the drug is administered. Drugs are also administered over a duration of time such as two weeks.

Finally, drugs can be administered in certain dosages such as 200 mg. These factors will determine the effects of the drug within the body. It must also be mentioned that drugs can react with other drugs or compounds with in the body. This can have no effect, it can be dangerous, or it may be fatal. Drugs should only be prescribed by a physician and over the counter drugs are best taken when they are approved by a physician. Consult with your pharmacist or doctor before you take over the counter medications.

To produce a physiological effect, drugs must reach a certain concentration at its site of action. The site of action is the area or tissue in which it is acting on in order to produce a physiological change. Also the chemical compounds of the pharmaceutical must be absorbed and transported properly. The concentration of a drug at its site of action is influenced by various processes which may be divided into three phases of drug activity: pharmaceutical, pharmacokinetics, and pharmacodynamics.3 These processes are too complicated to explain on this website and therefore will not be explained at this time.


Drug Testing in Athletics

Drug testing has been around since the late 1950s. In the past athletes who abuse drugs, have gained an advantage over non-drug using athletes. The unfortunate thing is some athletes have abused drugs and lost their life from it. Others have been ridiculed by the media and shamed by the world. The fact is, some drugs are needed throughout an athlete’s career.

Drugs are used to treat illnesses, psychological states, and they are used in sports therapy to enhance the recovery of an injury. Since athletes have abused these drugs in the past to enhance performance, it has lead to the onset of drug testing in sports. Almost all athletic organizations do some form of drug testing. This helps to put all athletes on a level playing field and keeps athletes from causing harm to themselves from the side effects of the performance enhancing substances.

There are two ways to test for drugs in the human body. The first way is to use a blood sample. It is also the most accurate. The second way is to take a urine sample. The testing of urine involves analysis of drug metabolites (final excretion products). These metabolites must be detected in the urine for an athlete to be guilty of drug abuse. Most of the time urine analysis is used to test for substances because it is easy and non-invasive.

Most athletic organizations feel that blood samples cause unnecessary trauma to the athlete, risk for transmission of diseases from needle use, and a violation of legal and religious rights. Although because athletes are now using more natural compounds to gain the edge such as human growth hormone (HGH), human chorionic gonadotropin (HCG), testosterone, and erythropoietin; officials must now consider the use of blood samples to detect variations of these compounds. The following tables are a list of banned substances by their classes as listed by the International Olympic Committee in 2001. 1

List of Banned Substances by the IOC 20011

NOTE: The following list does NOTcontain the most recent banned substances. Please contact the IOC, NCAA, or other governing organization to review the must current list of banned substances.

Stimulants Amineptine, Amiphenazole, Amphetamines, Bromantan, Bupropion, Caffeine, Cocaine, Ephedrines, Fencamfamine, Mesocarb, Methylphenidate (Ritalin), Pentetrazol, Pipradrol
Salbutamol, Terbutaline, Strychnine
Narcotics Buprenorphine, Dextromoramide, Diamorphine (Heroin), Methadone, Morphine, Pentazocine, Pethidine (Meperidine Demerol)

Anabolic Steroids/
Beta 2-Agonist/
Anabolic Agents

Androstenediol, Androstenedione, Bolasterone, Boldenone (Dehydrotestosterone; Vet.), Clenbuterol, Clostebol, Danazol, Dehydrochlormethyltestosterone (Oral-Turinabol; Chlorodianabol), Dehydroepiandrosterone (DHEA), Dihydrotestosterone (DHT), Drostanolone
Ethylestrenol, Formebolone, Fluoxymesterone (Halotestin), Furazabol, Mesterolone (Proviron), Metandienone (Dianabol), Methandriol, Methyltestosterone (Metandren), Mibolerone, Nandrolone (Nortestosterone), 19-Norandrostenediol, 19- Norandrostenedione, Norethandrolone (Nilevar), Oxandrolone (Anavar), Oxymesterone (Oranabol), Oxymetholone (Anadrol), Stanozolol (Winstrol), Stenbolone, Testosterone, Trenbolone
Diuretics Acetazolamide, Bendroflumethiezide (Naturetin), Bumetanide, Chlorthalidone, Canrenone, Ethacrynic Acid (Edecrin), Furosemide (Lasix), Hydrochlorothiezide (Esidrix), Spironolactone, Triamterene
Peptide Hormones, Mimetics, and Analogues Corticotrophins (ACTH), EPO (Erythropoietin), HCG (Human Chorionic Gonadotropin, prohibited in males only), HGH (Human Growth Hormone; Somatotrophin), Insulin (permitted only with certified insulin dependent diabetes), Insulin-Like Growth Factor (IGF-I), Pituitary and Synthetic Gonadotrophins (Luteinizing Hormone, prohibited in males only), Clomiphene (prohibited in males only), Cyclofenil (prohibited in males only), Tamoxifen (prohibited in males only)
Beta Blockers Acebutolol, Alprenolol (Sinalol), Atenolol (Tenormin), Betaxolol, Esmolol, Labetalol, Metoprolol (Lopressor), Nadolol (Corgard), Oxprenolol (Inderal),
Masking Agents Bromantan, Epitestosterone, Probenecid


Alcohol is primarily ethanol and comes in the form of beer, wine, and liquor. Approximately 90% of the population drink alcohol in some manner. The dangers of alcohol abuse by athletes comes in two effects. One is its diuretic effect and two is its nervous system impairment. Athletes usually don’t drink prior to competition.

However, they usually consume large amounts of alcohol after a game to celebrate a win or drown their sorrows in a loss. This is dangerous because athletes are dehydrated after competition. Consuming alcohol can increase the state of dehydration and electrolyte loss. When an athlete consumes alcohol before competition he/she suffers nervous system impairment. This can make an athlete prone to injury and will not allow the athlete to thermoregulate properly. It will also cause a total decrease in performance.

Alcohol affects exercise in many ways. It affects the cardiovascular system by altering sympathetic nervous system activity. This can cause an increase in blood pressure, a vasodilatation of peripheral vessels, and can complicate an already complex heart rate during exercise. Alcohol affects energy substrates such as carbohydrate metabolism.

It lowers resting muscle glycogen, decreases gluconeogenisis (formation of glucose in the liver), has been known to decrease blood glucose levels, and decreases aerobic capacity. Alcohol also has a direct affect on performance do to its nature as a central nervous system depressant, which decreases an athlete’s ability to exert maximum effort, and alcohol decreases hand eye coordination. Finally alcohol has been known to decrease the respiratory rate.2 The effects of alcohol on athletes clearly points out that it decreases athletic performance and makes athletes prone to injury.

Tobacco (Nicotine)

Tobacco is abused by many athletes. It administers the drug known as nicotine, and comes in the form of cigarettes, cigars, chew, and skoal. In some sports tobacco abuse is a fad. For instance, baseball and softball players are widely known for their use of smokeless tobacco (chew and skoal). The amount of nicotine within the body depends on the delivery mechanism, dosage, and uptake of the drug (e.g. 2 cigarettes per hour).

The mechanism in which tobacco is delivered also affects the amount of toxic substances delivered to the body. Cigarette smoking can deliver approximately 4,000 compounds to the lungs and 60 of those compounds are known carcinogens.3 Nicotine is an addictive and athletes who are addicted should consider stopping the abuse of this drug. Most doctors can treat and counsel athletes on nicotine addiction.

Once in the body nicotine can cause nervousness and anxiety among athletes. It may also increase heart rate which further complicates the body’s ability to maintain homeostasis during exercise. Nicotine can increase blood pressure by vasoconstriction of peripheral vessels.

If athletes smoke tobacco around other non-smoking athletes then the non-smoking athletes could suffer from irritated nasal and sinus passages due to second hand smoke. This may lead to upper respiratory tract infections. Therefore, tobacco use amongst athletes should be avoided at all cost to prevent the above mentioned affects on performance and to prevent harm to other non-smoking athletes.

Cannabis Drugs: Marijuana/Hashish

Cannibis drugs are derived from hemp plants (cannabis sativa). Marijauna contains hundreds of different chemicals termed cannabinoids. Of all the chemicals, two have been noted for their affects on the body. They are THC (delta-9-tetrahydrocannabinol) and CBD (cannabidiol). It is believed that the major psychoactive affect is caused by THC. Marijauna can be smoked or swallowed whole. It is usually smoked as a “joint” and generally it is mixed and baked in brownies to be swallowed whole.

Cannibis drugs seem to act as central nervous system depressants. They are considered to be sedative-hypnotic-anesthetics or psychedelic drugs. These drugs alter perception, thought, and feelings. THC peaks in the blood stream within a few minutes and last for up to four hours. It is metabolized by the liver and the majority of it is excreted in the bile and feces. However, trace amounts of unmetabolized THC are found in the urine.3

Few athletes abuse these drugs because they are banned by all athletic organizations and athletic performance is altered by the psychedelic effects and side effects. Side effects include tachycardia (increased heart rate), delayed bradycardia (decrease in heart rate), delayed hypotension, red eyes, dry mouth and throat, delayed gastrointestinal disturbances, fear, panic, paranoia, disorientation, memory loss, confusion, and possible vasovagal syncope.3 Any athlete who abuses these drugs should be reported to the coach, athletic trainer, or team physician, so that the problem can be dealt with carefully.


Caffeine is found in many beverages, medications, and supplements. It is usually orally ingested and peak effects occur 15-45 minutes after ingestion. Caffeine has been reported to be excreted in non-exercising adults after 3.0-7.5 hours after ingestion. It is considered to be a flow limited drug, therefore its elimination rate during exercise can be delayed.

This is because of alterations in blood flow during exercise. Sustained exercise decreases the systemic clearance and elimination rate of caffeine. Caffeine causes a release of catecholamines (e.g. epinephrine), which gives one the nervous energy feeling often associated with caffeine use.2

Athletes ingest caffeine whether it is to enhance performance, a social drink, or to help ward off lathargia. However, increasing use by athletes to enhance performance has lead to the banning of this substance by certain organizations. Therefore, simply having a cup of coffee can cause one to be disqualified if test results are positive. Athletes use caffeine because it stimulates the central nervous system, enhances neuromuscular transmission, enhances fat utilization for energy and spares muscle glycogen, and improves skeletal muscle contractility.2

The down fall is it increases heart rate, systolic blood pressure, may cause gastrointestinal discomfort, and resting urine output (may lead to dehydration pre/post exercise). There is an ongoing debate about whether or not caffeine delays fatigue. Athletes must be careful when ingesting caffeine prior to performance as it may be contraindicated or it could cause disqualification.

Anabolic-Androgenic Steroids

Testosterone is the chief natural male hormone produced primarily by the testes and is responsible for the masculinizing and tissue building effects observed during male adolescence and adulthood. Anabolic-andronergic steroids are derivatives of testosterone.

Testosterone is not effective when taken by itself because it is rapidly metabolized in the liver. Pharmaceutical companies have altered the structure of testosterone so that it can be used by certain tissues. Synthetic testosterone can be delivered by transdermal patches, injections, nasal sprays, gels, creams, and orally. Dosages are usually given in cycles every day for 6-12 weeks.

Not only is steroid use illegal in athletics, it precedes many harmful side affects on the liver, serum lipids, reproductive system, coronary arteries, cerebrovasculature, prostate, skin (achne), behavior disorders, and immune function. It has lead to cardiovascular risk factors.1 Abuse of steroids by any athlete is strictly prohibited. Any athlete known or suspected should be reported and counseled on weaning themselves off of steroids.



Athletes abuse amphetamines because they experience a decreased sense of fatigue. However, athletes do sustain increases in blood pressure, increases in heart rate, redistribution of blood flow to skeletal muscles, and mobilization of energy substrates. One of the uses of amphetamines is to promote weight loss. This can be dangerous because it can cause body fat percent to drop to dangerous levels in some athletes. Amphetamines suppress hunger and can increase the risk of athletes reducing glycogen stores.2 This may reduce the performance capabilities of athletes. Amphetamine abuse by athletes is not recommended and any athlete using these drugs should be counseled.


By: Craig Angle - ME.d, ME.d, ATC, CSCS

Author of the book: How to Raise a Successful Athlete

Former CEO:  The Athlete Project  


1.       Bahrke, M. S., & Yesalis, E. C. (2002). Performance Enhancing Substances in Sport and Exercise. Human Kinetics: Champaign, IL

2.       Reents, Stan. (2000). Sport and Exercise Pharmacology. Human Kinetics: Champaign, IL

3.       Salerno, Evelyn. (1999). Pharmacology for Health Professionals. Mosby: St. Louis

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