DRUGS OF ABUSE IN SPORTS

Presented by-Dr. Rajesh A Kamtane,3rd year PG,Dept. of Pharmacology,MIMS,Hyderabad

Doping can be defined as use by a competing athlete of any substance foreign to the body or any physiological substance taken in an abnormal quantity or taken by an abnormal route of entry into the body with the sole purpose of increasing his/ her performance in an artificial and unfair manner.

Hence, International Olympic Committee (IOC) has banned the use of performance enhancing drugs in sports since 1964.

Since 2004, World Anti- Doping Agency (WADA), has taken over the IOC and has redefined doping as violations of one or more of the anti- doping rules mentioned in WADA code.

Sr. No.

The anti- doping rule violations mentioned in WADA code

1. Presence of prohibited substance or its metabolites in an athletes bodily specimen.

2. Use of a prohibited substance or a prohibited method.

3. Possession of a prohibited substance or a prohibited method.

4. Dealing in any prohibited substance or a prohibited method.

5. Administration or attempted administration of any prohibited substance or a prohibited method to any athlete.

Sr. No.

The anti- doping rule violations mentioned in WADA code

6. Refusing or evading sample collection.

7. Violation of athlete availability for out- of- competition testing including failure to provide whereabouts information.

8. Tampering or attempting to tamper, with any part of doping control.

Prohibited substances1.Anabolic agents2.Hormones and related agents3.Beta 2 adrenergic agonists4.Agents with anti- estrogenic

activity5.Diuretics and other masking

agents6.Stimulants7.Narcotics8.Cannabinoids9.Glucocorticoids 10.Alcohol

Prohibited methods

1.Enhancement of oxygen transfer by blood doping or administrating artificial oxygen carriers.

2.Gene doping

3.Pharmacological, physical or chemical manipulation

ANABOLIC ANDROGENIC STEROIDS

1. Drugs like stanozolol, nandrolone, oxymetholone, methandienone are 19- nortestosterone derivatives which possess a higher anabolic activity compared to their inherent androgenic activity.

2. The ration of androgenic : anabolic activity of testosterone is 1 : 1, but anabolic steroids have ratio between 1: 3 to 1 : 10.

3. Anabolic steroids increase protein synthesis, enhance muscle mass, improve appetite resulting in weight gain and sense of well being.

4. Anabolic steroids are most commonly abused by

athletes to increase muscle mass, strength and their

performance.

5. An anabolic steroid abuser usually takes up to 26 to

30 times the therapeutic dose to improve

performance.

Other anabolic agents-

Zeranol--- non- steroidal estrogen analogueZilpaterol, Clinbuterol---sympathomimetic drugs

Adverse effects of Anabolic Androgenic

Steroids1. High blood pressure

2. High blood cholesterol levels

3. Fluid retention

4. Risk of heart disease

5. Severe acne

6. Thinning of hair & baldness

7. Liver disorders

8. Psychological disturbances

a.Mood swings

b.Aggression

c.Delusions

d.Impaired judgement

e.Depression

f. Nervousness and extreme irritability

9. Sexual and reproductive disorders

In males-a.Atrophy of the testiclesb.Loss of libidoc.Decreased sperm productiond.Breast and prostate enlargemente.Decreased hormone levelsf. Sterility

In females-g.Menstrual irregularitiesh.Infertilityi. Masculinizing effects such as facial hair,

decreased breast size, deepening of voice, enlargement of clitoris

OTHER HORMONES AND RELATED SUBSTANCES-

These include erythropoietin, growth hormone, insulin like growth factor, human chorionic gonadotrophin, leutinizing hormone, insulin, corticotrophin.

Erythropoietin-

1. Mainly of renal origin, stimulates growth of RBCs.

2. It is an essential growth factor for erythrocytic progenitors in bone marrow.

3. Abused by athletes to improve aerobic performance by increasing the oxygen availability to the tissues.

4. Adverse effects--- hypertension, increase in hematocrit value—leading to thrombosis

Growth hormone-

1. Athletes abuse GH to increase height and to enhance muscle mass.

2. Adverse effects– acromegaly, gigantism, metabolic and endocrine disorders.

Insulin like growth factor-

1. IGF are peptides involved in regulation of cell proliferation, differentiation and apoptosis.

2. Particularly, IGF-1 is a critical modulator of skeletal muscle growth when administered locally rather than systemically.

3. The infusion of IGF-1 into the target tissues such as selected skeletal muscle results in significant increase in total protein and DNA content, an effect that is highly desirable for athletic performance.

Human Chorionic Gonadotrophin (hCG)-

1.When injected into males, hCG stimulates leydig cells of testes to produce testosterone and epitestosterone.

2.A 50 % increase in plasma testosterone concentration has been measured 2 hours after i.m. injection of 6000 IU of hCG.

Leutinizing hormone (LH)-

3. It stimulates testosterone production by testes.

4. Its abuse is limited by its scarcity and high cost and also because its half life is 50 % less than hCG.

Insulin-

1.Insulin and its synthetic analogues are prohibited for use by athletes who are not suffering from insulin dependent DM.

2.Insulin inhibits protein breakdown (anti- catabolic effect).

3.A therapeutic use exemption is required prior to participation in a game for which written notification is to be sent to WADA.

Corticotrophin (ACTH)-

1.ACTH increases the levels of endogenous corticosteroids in the blood.

2.Its synthetic derivative, ‘Synacthen’ is administered as depot formulation.

3.ACTH abuse is limited to short term boosting of corticosteroids in an attempt to reduce lethargy and produce positive effects on mood during training and competition.

Beta 2 adrenergic agonists-

1.Commonly used to treat asthma, however if taken systemically, they may have anabolic effects.

2.Hence, all beta 2 agonists are prohibited, except the inhaled ones.

3.Therapeutic use exemption is required for use of inhaled beta 2 agonists (formeterol, salmeterol, salbutamol, terbutaline) to treat asthma.

Agents with anti- estrogenic activity-

1.The aromatase pathway transforms testosterone and androstenedione to estrogen.

2.Aromatase inhibitors block aromatase enzyme which converts androgen to estrogen, thus increasing the androgen levels.

3.Arimidex, Femara, Aromasin are commonly used aromatase inhibiotors in pill form.

Masking agents

These are the products that have potential to impair excretion of prohibited substances, to conceal their presence in urine or other samples, or to change the hematological parameters.

1.DiureticsAthletes use diuretics for—

a.Acute reduction of weight which may offer advantage in sports such as boxing, judo or weight lifting where competition is in weight categories.

b.To overcome fluid retention induced by AAS.

c.To modify excretion rate of urine and to alter urinary concentration of prohibited drugs.

Adverse effects---electrolyte imbalance, muscle cramps, dehydration.

2. EpitestosteroneUsed to mask detection of testosterone in urine sample.

3. ProbenecidUsed to mask presence of drugs or their metabolites because of its ability to alter the excretion rate of acidic metabolites.

4. Alpha reductase inhibitorse.g. finasteride, dutasteride help to mask steroid abuse.

5. Plasma expandersUsed to mask erythropoietin misuse.

Stimulants

1. Examples– amphetamines, methamphetamines, phenmetrazine, methylphenidate, cocaine, ephedrine.

2. They produce alertness, wakefulness, hallucinations and increase the ability to concentrate.

3. They may improve capacity to exercise strenuously or produce decreased sensitivity to pain by reducing fatigue.

4. Due to its anorectic effect, weight categorized sports people like boxers and wrestlers use these drugs to lose weight prior to competition.

5. Cocaine when snorted, affects brain within a few minutes, peak comes within 15-20 minutes.

6. Injected cocaine takes about 15 seconds to reach brain. The individual feels energetic and hyper alert.

7. Adverse effects– headache, anxiety, confusion, restlessness, HTN, tachyarrhythmias, withdrawal symptoms on discontinuation after regular use, malnutrition and psychiatric disturbances when used for long term.

Narcotic analgesics

1. Under the influence of narcotics, pain signals to the brain are suppressed. Hence, athletes may abuse these drugs to perform better in spite of musculoskeletal injuries.

2. e.g. it is possible for weight lifters to rupture muscles by attempting lifting weights that exceed their normal lifting capacity, if they take enough narcotics before their attempts.

Glucocorticoids

1.Can be abused in sports for pain suppression and euphoria.

2.Hence, banned by WADA to use them systemically.

3.When medically necessary, local and intra- articular injections are allowed under medical supervision.

Restricted drugs in particular sports-

1.Beta blockers–

These drugs are abused by the athletes to stop hands

and body from shaking while performing in sports like

shooting and archery that require accuracy and steady

hands.

2. Alcohol–

being CNS depressant, it slows down the reflexes, can

be dangerous in many circumstances.

Prohibited methods

1.Enhancement of oxygen transfer by-

a.Blood dopingb.Administering artificial oxygen carriers or

plasma expanders. (perfulorocarbons, haemoglobin based oxygen

carriers, liposome encapsulated haemoglobins)

2. Gene doping.

3. Pharmacological, physical or chemical manipulation-

e.g. catheterization, urine substitution or swapping, tampering with and inhibition of renal excretion by using masking agents.

Blood doping

1.It is used by athletes engaged in aerobic athletic activities such as long distance running and cross country skiing or cycling.

2.It is done to increase their total aerobic power by increasing transport of oxygen to contracting muscles.

Gene doping

3. Is defined as non-therapeutic use of genes or genetic elements that have capacity to enhance athletic performance.

4. Repoxygen gene, which was designed for treatment of anaemia, could be abused by athletes to boost their stamina.