SLW E-book Flashcards
There are many drug classes that are prohibited by WADA in and out of competition. These classes include:
● Anabolic Agents e.g. Nandrolone, Oxabolone
● Peptide Hormones, Growth Factors e.g. Erythropoietins (EPO), hGH 176-191
● Beta-2 Agonists e.g. Fenoterol, Procaterol
● Hormone and Metabolic Modulators e.g. Letrozole, Tamoxifen (SERM)
● Diuretics and Masking Agents e.g. Furosemide, Desmopressin
● Stimulants e.g. Benfluorex, Modafinil
● Narcotics e.g. Oxycodone, Diamorphine
● Cannabinoids e.g. Cannabis, Δ9-tetrahydrocannabinol
● Glucocorticoids e.g. Hydrocortisone, Betamethasone
Peptide Hormones:
Erythropoietin (EPO)
● EPO is a glycoprotein hormone found in the kidneys which regulates the production of red blood cells in bone marrow.
● After EPO binds to its cell surface receptor, it activates signal transduction pathways that interfere with apoptosis and stimulates erythroid cell proliferation.
● Podocytes are sensitive to low blood oxygen content (hypoxia) and will release EPO when oxygen is low. EPO stimulation allows the bone marrow to produce more red blood cells. This increases the oxygen-carrying capacity of the blood.
● Medically, artificial EPO is given to patients with chronic kidney disease that were chronically anaemic (i.e. people whose bone marrow is suppressed, in order to help
them have more energy and increase day to day function.
● Artificial EPO is also indicated in patients with symptomatic anaemia in chemotherapy
Perceived benefits of EPO use to athletes:
● In sport, EPO has been used to improve performance in various disciplines, such as:
athletics and cycling.
● Here, EPO is used as a performance enhancing drug (PED) through injection (intravenously or subcutaneously) stimulating red blood cell (RBC) production.
● The proliferation of RBCs means that more oxygen can be delivered to the muscles.
● This delays the onset of fatigue, meaning an athlete can run harder and for longer duration. Hence, its widespread use in sports that demand an athlete to perform for long periods. For example in athletics, particularly amongst long distance runners, or in cycling.
EPO is believed to increase
EPO is believed to increase red blood cell production, reduce fatigue and improve endurance by increasing the rate of red cell production. It is also believed to increase the metabolism and the healing process of muscles because the extra red cells can carry more oxygen and nutrients.
Anabolic Androgenic Steroids:
Nandrolone decanoate
● Nandrolone decanoate is an example of an anabolic steroid, produced naturally in the body in small amounts.
● It is primarily used to treat osteoporosis in postmenopausal women however, this is no longer recommended.
● Typically, it is administered intramuscularly, but it can also be taken orally as a tablet.
● Nandrolone decanoate shares the actions of endogenous androgens such as testosterone. It promotes protein anabolism (process of protein formation from amino acids) and stimulates appetite, which results in a reversal of catabolic process and negative nitrogen balance. This improves the rate of development for muscle tissue
● Clinically, increases in lean body mass in patients with cachexia (weakness and wasting of the body due to severe chronic illness) are noted with Nandrolone decanoate use.
Perceived benefits of Nandrolone decanoate:
● It is common to see nandrolone use amongst athletes, especially in weightlifting and bodybuilding, because they believe that it can increase body weight and lean body mass to a better extent than training alone and helps speedy recovery in between training sessions. Therefore, users can train more frequently and improve muscle development.
● It is the promotion of protein anabolism that aids the development of muscle tissue.
● Surveys have revealed that the use of anabolic steroids among adolescents is not only linked to performance purposes but also to improve body image.
Stimulant:
Methylhexanamine
● Methylhexanamine also known as 1, 3-dimethylamylamine (1, 3-DMAA) or dimethylamylamine (DMAA) is a neurological stimulant, that has structural similarities
to amphetamine, methamphetamine, and MDMA.
● Its structural similarity with the amphetamine class can lead to a false positive result for amphetamines, therefore, it should not be used by athletes competing in competitions that test for amphetamines.
● Structurally, DMAA is a straight chain, 7 carbon, and aliphatic amine.
● It was first introduced as a nasal decongestant for allergic rhinitis in the 1940s, but was removed from the market in the 1970s as an approved drug due to safety concerns. It was only added to the WADA list in 2009 and more recently DMAA is used as a neurological stimulant and “party pill”.
● Due to its structural similarities, its mechanism of action may be as an adrenaline mimetic; inducing the same effects as adrenaline and the preceding compounds in vivo. Its stimulatory action is also comparable to the action of caffeine as it causes a quick energy increase, but does so by different mechanisms in the brain.
● Methylhexanamine also known as 1, 3-dimethylamylamine (1, 3-DMAA) or dimethylamylamine (DMAA) is a neurological stimulant, that has structural similarities to amphetamine, methamphetamine, and MDMA.
● In higher doses DMAA is associated with increased blood pressure, and can lead to cardiovascular complications, for example, myocardial infarction, shortness of breath and tightening of the chest.
● Due to the biological activity of DMAA, it may work synergistically with caffeine increasing the risks of experiencing side effects.
Perceived benefits of Methylhexanamine:
● Supplements containing DMAA are marketed to for athletes, as it is noted that DMAA is associated with weight loss, muscle building and overall performance enhancement which appeals to athletes as they believe it will aid their performance and recovery.
● DMAA also shares structural similarity to Propylhexedrine, a stimulant drug and nasal decongestant used in the US, which may have fat-burning effects in vivo.
● DMAA is also used to stimulate an increase in mental energy and focus
Potential side effects of AAS abuse
Physiological side effects include:
- Acne
- Male pattern baldness
- Liver Damage*
- Premature closure of the growth centres of long bones (in adolescents) which may result in stunted growth*
- Stunted growth and disruption of puberty in children
Psychological side effects include:
- Increased aggressiveness and sexual appetite, sometimes resulting in abnormal sexual
and criminal behaviour, often referred to as “Roid Rage”.
- Withdrawal from anabolic steroid use can be associated with depression, and in some cases, suicide.
Gender Specific side effects of AAS include:
Male Breast tissue development* Shrinking of the testicles Impotence Reduction in sperm production
Female Deepening of the voice* Cessation of breast development Growth of hair on the face, stomach and upper back Enlarged clitoris* Abnormal menstrual cycles
Peptide Hormones and Growth Factors
human growth hormone (hGH), erythropoietin (EPO), insulin, human chorionic gonadotropin (HCG), and adrenocorticotropin (ACTH)
Physiological effects of PH and GF include:
● Hypertension (EPO/hGH) ● Blood cancers/leukaemia (EPO/hGH) ● Anaemia (EPO) ● Strokes (EPO) ● Myocardial infarction ● Pulmonary embolism (EPO) ● Feminization (HCG) ● Thyroid problems (hGH)
Human Growth Hormone (hGH) - Physiological effects include:
- Severe headaches, Loss of vision
- Acromegaly (Protruding or enlarged jaw, brow, skull, hands and feet)
- High blood pressure and heart failure
- Diabetes (type 2) and tumours
- Osteoporosis
Beta-2 agonists
The primary medical use of these compounds is to treat conditions such as asthma and other respiratory ailments. Some studies have shown beta-2 agonists have performance-enhancing effects when consistently high levels are present in the blood. The prominent physiological effects include the following:
- Palpitations
- Headaches
- Sweating
- Nausea
- Muscle cramps
- Nervousness
Diuretics
The primary medical use of these compounds is to treat conditions such as hypertension, kidney disease and congestive heart failure. Taken without medical supervision or taken incorrectly, can result in hypokalaemia and possibly even death. The resulting physiological effects of diuretics include: ● Dehydration ● Muscle cramps ● Dizziness or fainting ● Drop in blood pressure ● Loss of coordination and balance
