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Drugs of abuse in sports
1. DRUGS OF ABUSE IN
SPORTS
Presented byDr. Rajesh A Kamtane,
3rd year PG,
Dept. of
Pharmacology,
MIMS,Hyderabad
2. 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.
3. 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.
4. 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.
5. Sr.
No.
The anti- doping rule violations mentioned
in WADA code
6. Refusing or evading sample collection.
7. Violation of athlete availability for out- ofcompetition testing including failure to provide
whereabouts information.
8. Tampering or attempting to tamper, with any
part of doping control.
6. Prohibited substances
1.Anabolic agents
2.Hormones and related agents
3.Beta 2 adrenergic agonists
4.Agents with anti- estrogenic activity
5.Diuretics and other masking agents
6.Stimulants
7.Narcotics
8.Cannabinoids
9.Glucocorticoids
10.Alcohol
7. Prohibited methods
1. Enhancement of oxygen transfer by
blood doping or administrating artificial
oxygen carriers.
2. Gene doping
3. Pharmacological, physical or chemical
manipulation
8. 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.
9. 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 agentsZeranol--- non- steroidal estrogen analogue
Zilpaterol, Clinbuterol---sympathomimetic drugs
10. Adverse effects of Anabolic
Androgenic Steroids
1.
2.
3.
4.
5.
6.
7.
High blood pressure
High blood cholesterol levels
Fluid retention
Risk of heart disease
Severe acne
Thinning of hair & baldness
Liver disorders
11. 8. Psychological disturbances
a. Mood swings
b. Aggression
c. Delusions
d. Impaired judgement
e. Depression
f. Nervousness and extreme irritability
12. 9. Sexual and reproductive disorders
In malesa. Atrophy of the testicles
b. Loss of libido
c. Decreased sperm production
d. Breast and prostate enlargement
e. Decreased hormone levels
f. Sterility
In femalesa. Menstrual irregularities
b. Infertility
c. Masculinizing effects such as facial hair, decreased breast size,
deepening of voice, enlargement of clitoris
13. OTHER HORMONES AND RELATED
SUBSTANCESThese include erythropoietin, growth hormone, insulin
like growth factor, human chorionic gonadotrophin,
leutinizing hormone, insulin, corticotrophin.
14. Erythropoietin1. 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
15. Growth hormone1. Athletes abuse GH to increase height and to enhance
muscle mass.
2. Adverse effects– acromegaly, gigantism, metabolic
and endocrine disorders.
16. Insulin like growth factor1. 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.
17. 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)1. It stimulates testosterone production by testes.
2. Its abuse is limited by its scarcity and high cost and
also because its half life is 50 % less than hCG.
18. Insulin1. 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.
19. 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.
20. Beta 2 adrenergic agonists1. 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.
21. Agents with anti- estrogenic activity1. 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.
22. 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.
23. 1.Diuretics
Athletes 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.
24. 2. Epitestosterone
Used to mask detection of testosterone in urine sample.
3. Probenecid
Used to mask presence of drugs or their metabolites because of
its ability to alter the excretion rate of acidic metabolites.
4. Alpha reductase inhibitors
e.g. finasteride, dutasteride help to mask steroid abuse.
5. Plasma expanders
Used to mask erythropoietin misuse.
25. 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.
26. 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.
27. 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.
28. 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.
29. 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.
30. Prohibited methods
1. Enhancement of oxygen transfer bya. Blood doping
b. Administering artificial oxygen carriers or plasma expanders.
(perfulorocarbons, haemoglobin based oxygen
carriers, liposome encapsulated haemoglobins)
2. Gene doping.
3. Pharmacological, physical or chemical
manipulatione.g. catheterization, urine substitution or
swapping, tampering with and inhibition of renal
excretion by using masking agents.
31. 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
1. Is defined as non-therapeutic use of genes or genetic
elements that have capacity to enhance athletic performance.
2. Repoxygen gene, which was designed for treatment of
anaemia, could be abused by athletes to boost their stamina.