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PRINCIPAL DOPING SUBSTANCES AND THEIR SIDE EFFECTS
By Info
Jun 18, 2006
Introduction
Any sport may be defined as a game of intelligence and a challenge of ideas combined with the expression of perfection of the human body and its movement. There are no sports which involve a course on pharmacology. Unfortunately, the misuse and abuse of pharmacologically active substances have become so widespread in present day sports that the safety, the health and the longevity of far too many athletes are now compromised. In a sense, the initial pursuit of the sporting activity has been perverted.
Even the youngest athletes, both professionals and amateurs, have not been spared. Their trainers, physicians and other assistants have already given them countless pills, tablets, ointments, injections, vitamins and other potions. The goals are numerous: to stimulate, to calm, to numb the pain caused by a wound, to enhance performance, to reduce inflammation, sometimes to suppress anxiety.
As a result, many athletes have come to believe that successful development in the world of sports is impossible without pharmacologically active substances. There are not many drugs that such athletes wouldn't take in order to improve performance, to feel calm or to feel better. Some people say that is simply impossible to resist…
It is thus essential that all athletes, beginners and professionals alike, fully understand that the use of a forbidden substance may have severe consequences. Indeed, athletes often have no knowledge about the immediate and delayed toxic effects of many medical drugs.
On the one hand, it has become very easy to obtain both approved substances and illicit drugs. On the other hand, the seemingly medical information that is available is often of pseudo-scientific nature. As a result, it has become difficult to differentiate acceptable practices from hazardous techniques.
In writing this document, our wish was to provide the reader with simple and straightforward information, based on our current objective understanding of the relationship between the principal doping substances and the occasionally toxic side effects commonly observed in cases of abuse and utilization outside the commonly accepted medical context.
According to G.-I. Wadler et B. Hainline (authors of L’athlète et le dopage, drogues et médicaments (The Athlete and Doping, Drugs and Medication), Collection Sport et enseignement, Editions Vigot, Paris, 1993), athlete doping and drug addiction have their roots in pharmacological research aimed at improving athletic performance with ergogens.
Conversely, doping testing in athletes is an attempt to prevent any artificial ergogen advantage conferred by an illicit drug, as well as the associated immediate or delayed impact on the athlete’s health.
An athlete consumes ergogens to gain an advantage in the face of physical and emotional challenges in a sports competition. However, as seen in the table below, the advantages conferred by a particular substance must be seriously evaluated in terms of the performance health damage ratio.
Because of practical, legal and ethical considerations, it is difficult to evaluate the effects that a substance may have on an athlete’s performance. Indeed, one cannot carry out pharmacological experiments on healthy individuals without a therapeutic justification.
Moreover, volunteers cannot be subjected to the same conditions experienced by athletes engaged in doping. This limitation is explained by the fact that the levels of drugs that are used in doping are 10-, 50- and sometimes even 100-fold higher than the accepted therapeutic values. The cheaters do not seek the therapeutic activity of a substance but secondary effects that appear only at levels that are never reached during normal treatment.
Finally, it is usually difficult to extrapolate the standard pharmacological parameters because of many variables, such as the degree of purity of the drug, mode of intake, the dose response effect and the relation between time of intake and time of effort.
There are three main categories of drugs that are used by athletes today :
1. Ergogen substances or techniques that are aimed at improving performance. Typical examples include testosterone, anabolic steroids, stimulants such as amphetamines, and peptide hormones such as growth hormone and erythropoietin.
2. Medical drugs. This category includes substances prescribed for treating specific medical conditions and that are used in manners that are contrary to conventional clinical practice.
3. Uncontrolled substances sold on the open market for recreational purposes or pleasure.
This category includes illegal drugs or drugs that are taken at very high doses relative to standard prescription levels. The result is a modification in the mood and in the perception of the athlete.
List of substances and associated side effects:
The list presented below includes the main substances or classes of substances that cause well documented side effects on the human organism. The knowledge about certain PFCs is still very fragmentary and we have omitted them form our compilation. Moreover, besides the substances listed here, there are many other pharmacologically active compounds or medical drugs that also have specific side effects (see J.-P. de Mondenard : Dictionnaire des substances et procédés dopants en pratique sportive (Dictionary of doping substances and behaviors) ; Editions Masson, Paris, 1990).
It is important to realize that the substances presented here are normally used to treat specific diseases or serious health conditions: they have strong biological activity and are not to be consumed without forethought as if they were some nutritional supplement, such as vitamins or amino acid concentrates. As a rule, any plan to use a pharmacologically active substance must always be validated by a physician, who in turn must confirm the rightfulness of the approach, regardless of dosage and the health condition of the athlete.
ACTH or Corticotrophin
ACTH is used in an attempt to increase the corticosteroid levels in the blood, and to produce the associated euphoric effects on the organism. The use of these products may cause an allergic reaction, in particular in individuals that have a predisposition towards asthma, urticaria, eczema, etc. Drug injections can cause severe reactions, such as anaphylactic shock.
Undesirable side effect of ACTH include many different reactions such as:
- Water retention, edema
- Hyperglycemia
- Blood hypertension
- Modification in the psyche
- Osteoporosis
- Decrease in resistance to infections
Amphetamines
Amphetamines were first synthesized in 1887. In addition to their principal effects, amphetamines have different activities on different levels, mediated by more or less specific receptors in the organism. The desired effects include a sense of well-being, a decrease in
the perception of fatigue, an increase in self-confidence, in motor function and a decrease in appetite.
In contrast to anabolic drugs which are used during the athlete's training, amphetamines are usually consumed just prior to competition. Indeed, there are no positive long term effects. In fact, most of the main pharmacological effects of amphetamines resemble those of cocaine. One athlete may want to increase his concentration and awareness, another one will consume massive doses to become more aggressive and develop endurance, and a runner, for instance, may feel ready to deploy more instant energy and speed.
An individual may be inclined to increase the doses of amphetamines to obtain the same stimulating effects experienced in the very beginning. This results in rapid addiction. The initial use, the extended use and high-dosage use of amphetamines may all provoke severe
side effects, as shown in the table below:
|
Acute or early onset side effects |
Chronic use side effects |
|
Average |
Severe |
|
|
Impatience |
Confusion |
Addiction |
|
Vertigo |
Fights |
Weight loss |
|
Tremors |
Delirium |
Psychosis |
|
Irritability |
Paranoia |
Paranoid delirium |
|
Insomnia |
Hallucinations |
Dyskinesia |
|
Euphoria |
Convulsions |
Behavioral disorders compulsive/ stereotypical / repetitive |
|
Uncontrolled movements |
Cerebral hemorrhage |
Vascularity |
|
Cephalgia |
Angina pectoris/ infarction of
the myocardium |
Neuropathies |
|
Palpitations |
Blood hypertension |
|
|
Anorexia |
Circulatory collapse |
|
|
Nausea |
|
|
|
Vomiting |
|
|
|
|
|
|
A brutal withdrawal after repeated use of amphetamines may result in chronic fatigue,
lethargy, somnolence and depression.
An amphetamine user may display the following external signs:
|
Changes in one's judgement capacity |
| Repeated occurrence of wounds |
|
Increase in recuperation time |
|
Side effects that penalize a sports activity (see above) |
|
Repeated variations in the mood (stimulation of anxiety) |
|
The face of amphetamine: external signs of the amphetamine user
- Facial expression of anxiety
- Pinched nose
- Dilated pupils
- Teeth grinding (bruxism)
- Dry mouth
- A nauseous state
- Paleness of mucous membranes and on the finger tips (nails)
- Cold extremities
- Goose bumps
- Sudation
- Palpitations
- Accelerated or lowered heartbeat
- Hyper or hypotension
- Erection
- Loss of vision in the absence of visible eye alterations (amaurosis)
- Nervousness
- Tics: frequent touching of one's face
- Disorientation relative to people and places
- Mistrust of one's entourage and the impression of being constantly watched
- Incoherent speech
- Violent acts
- Psychosis (severe personality problem which alters the perception and understanding of reality) |
|
Addiction |
| The habit is essentially psychological |
|
There is a tendency to use dangerous associations of medical drugs |
|
Anabolic substances (steroids)
This class of doping substances includes all steroids that possess anabolic properties,
meaning that they cause an extensive increase in the muscular mass. This effect is never isolated: a more or less pronounces androgen activity is also present. This chapter also deals with testosterone.
These ergogen substances are generally used without interruption and during several weeks preceeding a competition. The preferred method is "piling up" oral ingestion and injections.
The amount of the substances used exceeds dramatically the standard doses recommended in a therapeutic procedure.
There has been a report of an athlete diagnosed with AIDS and whose sole risk factor was sharing needles to inject anabolic steroids. It is not uncommon to discover that anabolic steroids bought on the black market have not been adequately sterilized and are deliberately mislabeled. The possible complications arising from the use of such unknown and impure preparations are unimaginable.
The side effects associated with the use of anabolic steroids have been scientifically observed and documented
|
Anomalies in the function of the liver |
| Benign and malignant liver tumors (liver cancer) |
| Hypercholesterolemia (excessive blood cholesterol levels) |
|
Prostate Adenocarcinoma (prostate cancer) |
| Hypertension spells |
| Infarction of the myocardium |
| Diabetes |
| Sleep apnoea syndrome |
|
Hypogonadotropic hypogonadism and testicular atrophy (decrease in the size of testicles) |
| Azoospermia (disappearance of sperm in the semen), reversible sterility |
|
Feminization : gynecomastia (breast development in men) and high-pitched, castrato-like voice |
| Behavioral modifications (aggressiveness, groundless violence) – psychiatric troubles |
| (addiction to anabolic products) |
| Humoral immunity problems |
|
Acne |
|
Muscular rupture |
| Hair loss |
|
Premature suture of the epithelial cartilage in the prepubescent child which results in an arrest of growth in the young athletes |
|
Irreversible virilization or masculinization in women
- Husky voice (which can also become screeching)
- Hirsutism : appearance of body hair in regions that are normally hairless (face, regions
between and around nipples, back, shoulders, the back of thighs, infra-umbilical and
intergluteal regions): the average life span of body hair is two years and excessive body
hair may sometimes appear as late as one year after the end of hormone absorption
- development of male pattern baldness
Virilization of the female fetus |
In addition to the above-mentioned symptoms, there are subjective reactions to the intake of anabolic substances:
| Modifications in sex drive (increases and decreases) |
| Fainting and vertigo |
| Headaches |
| Lethargy or excessive aggressiveness |
| Psychiatric effects: steroid-induced rage or spells of extreme violence |
| Tics |
|
Dependence |
Non steroid anti-inflammatory drugs Severe undesirable side effects of NSAID drugs are rare. The common side effects include irritations and bleeding of the gastric mucous membranes.
The other undesirable effects are :
|
Skin eruptions |
|
Ear ringing |
|
Edemas |
|
Bronchial spasms |
Sever diarrhea is a classic side effect of mefenamic acid (Ponstan).
Asthma and sports, see Ephedrine, beta-2 stimulants and corticosteroids
Barbiturates such as benzodiazepines and alcohol are usually not considered as ergogen drugs.
However, there is scientific evidence that barbiturates and benzodiazepines may have beneficial effects in some specific situations. Indeed, both substances are effective in reducing tremors, which is important in some easily identified sports activities. This soothing action has been extensively studied in cases of epileptic spells.
The side effects of theses substances are significant:
|
Sedation |
| Reduced acuteness of vision |
| Lowered vigilance (very important when driving a motorized vehicle) |
| Problems with walking and keeping balance |
| Decrease in memorization capacity |
| Euphoria |
| Withdrawal insomnia |
| Dependence |
| Tolerance |
| Clinical withdrawal syndrome |
|
Respiratory distress |
|
Coma |
Beta-blockers
The undesirable effects of beta-blockers stem from their inhibitory properties. Asthma
sufferers in particular should avoid products belonging to this category since they can cause
bronchial spasms. Certain beta-blockers, such as propranolol, may cause insomnia,
nightmares and even a depression syndrome.
Some male users also experience sexual difficulties, such as impotence and weakened
erection.
The use of beta-blockers should be strictly prohibited in case of asthma, cardiac
insufficiency, digestive tract hemorrhages, occult bleeding, significant bradycardia (above 50
heartbeats per minute) and insulin-dependent diabetes.
The following undesirable effects are observed when these drugs are used :
| Hypoglycemia |
| Troubles with digestion |
| Asthenia |
| Cramps |
| Cephalgia, vertigo, diplopia |
| Raynaud’s disease : circulation problems in the extremities upon exposure to cold ; the fingers turn pale |
| Insomnia, nightmares |
| Mood alterations (depressive tendencies) and changes in the libido |
|
Hypothernia |
| Cardiac insufficiency |
| Cardiac rhythm problems |
| Anaphylactic shock after a hymenoptera sting (bee, wasp, etc.) |
| Numerous drug interactions |
|
Caffeine
Caffeine resembles cocaine and amphetamines in that it essentially stimulates the central
nervous system in a dose-dependent fashion. Caffeine is known to have many deleterious
effects on the health consulting the table below, one should distinguish the chronic effects of
caffeine from acute effects following absorption of this stimulant (which may constitute doping behavior).
| Acute intoxication, severe |
Acute intoxication, less severe |
Chronic intoxication |
| Peptic ulcer |
Nervousness, excitation |
Increase in cholesterolemia |
| Delirium |
Irritability |
Increased risk of ischemic cardiopathy |
| Convulsions |
Insomnia |
Teratogenic activity |
| Coma |
Tachycardia |
Carcinogenic activity |
| Arrhythmia |
Blood hypertension |
Risk of breast fibrocystic |
| lesions |
Palpitations |
Problems with digestion , in particular when coffee is mixed with milk |
|
Death (the lethal dose is
approximately 6 liters
depending on the brewing strength of coffee or caffeine content of the liquid) |
Headaches |
|
|
Tremors |
|
|
Exaggerated fear or anxiety |
|
|
Increased levels ofcholesterol and higher risk of heart attack |
|
|
|
|
Cannabis (Marijuana, Hashish, Kif, …)
Cannabis has been cultivated for centuries but cannabis-derived products have been available world-wide only starting second world war. The interest in this plant stems from its psychotropic properties. Most countries consider cannabis as an illegal drug. Over the recent past, the quality of the drug has improved dramatically : the levels of active substances inplants bred nowadays are 10- to 30-fold higher than 15 years ago. Hence, it is difficult to still consider cannabis as a harmless product. Indeed, certain preparations found on the present
day market are extremely potent. Consequently, there is a corresponding increase in the principal undesirable side effects which are listed below:
| Psychiatric effects |
Cardiovascular effects |
| Panic attacks |
Tachycardia |
| Delirium |
Orthostatic hypotension |
| Psychosis |
Increase in carboxyhemoglobin |
| Loss of motivation syndrome |
|
|
Broncho-pulmonary effects |
| Immunological effects |
|
|
Rhinitis |
| Decrease in cellular immunity Pharyngitis |
Pharyngitis |
| Decrease in monocyte maturity Bronchitis |
Bronchitis |
|
Bronchial spasms |
|
Endocrinological effects |
Squamous bronchial metaplasia |
|
Pulmonary fibrosis |
|
Decrease in sperm production |
Pneumomediastinum |
|
Inhibition of ovulation in women |
|
|
Gynecomastia in men |
|
|
|
|
Negative effects affecting performance |
|
|
|
|
Increase in recuperation time after exerciseand in the duration of muscle aches . |
Bloodshot and light-sensitive eyes |
|
A faster onset of fatigue during exercise |
Mood hyper-instability: rapid switch from euphoria to depression |
|
Acceleration of cardiac rhythm |
Hallucinations |
|
Enhanced feeling of thirst |
Deterioration in vigilance and coordination :dangerous when driving a vehicle |
| Loss of motivation |
|
|
|
Cocaine
Cocaine abuse in the adult represents a significant risk. Competition merely increases the
cardiovascular side effects through cardiac hyper-stimulation accompanied by arrhythmia
and heart attacks.
The principal side effects caused by cocaine are listed in the table below :
|
Cardiovascular
complications |
Cerebrovascular
complications |
Neuropsychiatric
complications |
|
|
|
|
Ventricular arrhythmia |
Cerebral infarction |
Convulsions |
|
Sudden death |
Brain Hemorrhage |
Exacerbation of the Gilles de
la Tourette syndrome |
|
Angina pectoris |
Meningeal hemorrhage |
Cephalgia |
|
Infarction of the myocardium |
Transitory cerebral ischemia |
Visual scotoma |
|
Aortic dissection |
|
Blindness |
|
Myocarditis |
|
Optical neuritis |
|
Tachycardia |
gyneco-obstetrical complications |
|
|
|
Habit formation |
|
Premature detachment of placenta
|
Insomnia |
|
Ear-Nose-Throat
complications |
Spontaneous abortion |
Mental confusion |
|
Congenital malformations |
Aggressiveness |
|
Osteolytic sinusitis |
Transplacental or milkmediated Mother-infant transfer and secondary withdrawal syndrome
|
Paranoid delirium |
|
Necrosis et perforation of the nose septum |
|
Visual and tactile hallucinations |
|
Loss of sense of smell |
|
Repetitive behaviors |
|
Miscellaneouscomplications |
Stereotyped movements of the mouth and tongue |
|
Complications related to drug addiction |
Liver toxicity |
Anorexia |
|
Gastrointestinal ischemia |
Specific delirium |
|
HIV infection P |
neumomediastinum |
Thymic troubles linked to
hallucinogens |
|
Bacterial infections |
Hyperthermia |
Sex problems |
|
Viral hepatitis |
|
|
Codeine, opiates and other morphine derivatives
The use of pain killers is frequent in sports, especially among athletes engaged in violent activities (such as boxing for instance). Often, the fear of losing a place or not fulfilling a contractual obligation leads to an obsession to keep the fight in spite of any type of wound or
handicap. The most common effect of this class of substances is sedation, providing habitual doses are used. One must be aware of physical and psychological addiction induced by many opiates which are justly classified as narcotics:
| Nausea |
| Vomiting |
| Vertigo |
| Memory loss |
| Mood problems |
| Pruritus |
| Constipation |
| Delirium |
| Convulsion crises |
| Addiction |
|
Withdrawal syndrome |
Corticosteroids
As seen in the table, the undesirables side effects associated with these substances are so severe that they should never be administered in the absence of a medical imperative:
| Hydro-electrolytic imbalance leading to edemas and increase in body weight |
|
Increase in glycemia (blood sugar levels) and appearance of glycosuria (presence of glucose in the urine) |
| Increase in blood pressure |
|
Decrease in antibodies and natural defense mechanisms leading to higher susceptibility towards infections |
| Gastric pyrosis (heartburn and regurgitation) and gastrointestinal ulceration |
| Diffuse osteoporosis with an increased risk of fractures and delayed bone repair |
| Alterations in the walls of blood vessels with possible formation of blood clots leading to embolism |
| Decrease in muscle nutrition, risk of severer muscular atrophy |
| Eye disorders : keratitis, glaucoma, cataract |
| Dangerous effects on the fetus |
| Disorders of the nervous system: convulsions, muscular cramps |
| Psychiatric disorders: mood alterations, insomnia, sometimes even genuine maniacdepressive psychoses |
|
Decrease or even arrest in the growth in young athletes |
Diuretics
All diuretics have the same side effects: dehydration, hypovolemia, muscular cramps, and orthostatic hypotension. Biochemical shifts in potassium levels (kaliemia) may be life threatening if strong modification are induced by diuretics.
Ephedrine (and phenylpropanolamines)
They are present in many innocuous pharmaceutical preparations used to treat benign conditions such as a cold. One must be very cautious in examining this class of substances since there are over 50 derivatives which have similar effects. The table shows the acute side effects caused by ephedrine analogs (effects are ordered by severity)
| Moderate effects |
Severe effects |
| Nervousness |
Agitation |
| Irritability |
Confusion |
| Insomnia |
Paranoia |
| Anorexia |
Mania |
| Vertigo |
Hallucinations |
| Cephalgia |
Ictus / Transitory ischemic attack |
| Tachycardia |
Cerebral vascularisation |
| Palpitations |
Cerebral hemorrhage |
| Slight increase in blood tension |
Severe hypertension |
|
Myocardial ischemia |
| Intolerance reactions |
Ventricular arrhythmia |
|
Rhabdomyolysis |
| Should never be combined with an anti- depressant |
May cause convulsive crises in epileptics |
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