Laurent RIVIER, Ph.D., chemist and toxicologist, Scientific Director of the Swiss
Institute of Doping Analysis, Martial SAUGY, Ph.D., biochimiste, Technical Director
of the Swiss Institute of Doping Analysis, and Professor Patrice MANGIN Md Ph.D.,
forensic scientist, Director of the Swiss University Institute of Forensic Medicine,
Lausanne, Switzerland.
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.
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
2
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 :
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 sepcific 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:
3
Amphetamines
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:
A brutal withdrawal after repeated use of amphetamines may result in chronic fatigue,
lethargy, somnolence and depression.
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.
5
The side effects associated with the use of anabolic steroids have been scientifically
observed and documented:
In addition to the above-mentioned symptoms, there are subjective reactions to the intake of
anabolic substances:
Severe undesirable side effects of NSAID drugs are rare. The common side effects include
irritations and bleeding of the gastric mucous membranes.
Skin eruptions
Ear ringing
6
Edemas
Bronchial spasms
Sever diarrhea is a classic side effect of mefenamic acid (Ponstan).
Barbiturates et Benzodiazepines
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.
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.
Hypoglycemia
Troubles with digestion
7
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).
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 in
plants 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 :
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 :
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
10
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:
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.
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)
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- May cause convulsive crises in epileptics
11
depressant
Erythropoietin
This peptide hormone is used in medical practice in cases of severe anemia and during
treatment of chronic renal insufficiency, such as in dialysis patients. In each case, there is a
specific evaluation of the benefits vs. the dangers of this type of treatment. The first clinical
trials involving erythropoietin started in 1985 and it is hence premature to draw a clear picture
of the side effects. Nevertheless a few undesirable consequences have already been
identified:
In women In men
Pregnancy
In terms of doping, the desired effect is the increase in cardiac capacity during the first
months of pregnancy. Later there is an increase in blood volume, in the number of red blood
cells and in hemoglobin. Apparently the resulting enhancement in oxygen delivery to the
muscles translates into a 10% increase in the deployment of effort.
The risks stem from the vulnerability of the fetus starting with the third month of pregnancy.
A abortion planned after the key competition represents a significant danger for the woman if
it is carried out in a non-medical environment by unexperienced hands. There may also be a
great psychological impact.
Uncertainties remain about the safety of exogenous hGH as a therapeutic treatment. We still
do not know what influence it may have on normal individuals, even though there is a good
12
The table below summarizes the side effects linked to the presence of high hGH levels in the
adult (the same side effects are noticed in children; in addition, there is an occurrence of
gigantism due to the increase in the linear growth of bone tissue).
There have also been reports of the development of anti-growth hormone anti-bodies after
administration of exogenous growth hormone. This causes an interference with endogenous
hormone activity and necessitates an immunological surveillance. In order to avoid
hyperglycemia, it is also necessary to monitor blood glucose levels. An injection of this
hormone affects very fundamental processes of regulation. It may upset the balance of
thyroid and corticotropic hormones, which will have a major impact on the individual's health.
One should point out that a bovine growth hormone may be found on the market and that a
horse growth hormone may soon become available as well. These substances have no
activity on the human organism but they may cause an irreversible sensitization which can
lead to severe consequences (anaphylactic shock) if the exposure is repeated. Yet another
type of hormone may be found on the black market: the extractive growth hormone. It is
actually extracted from the pituitary gland of corpses. In this particular scenario, the industrial
method used to purify the hormone does not guarantee the removal of other biological
molecules such as prions. Based on the well-known scenario of contamination that led to the
mad cow disease, which is transmitted by a prion, one cannot exclude a similar
contamination by a prion present in an extractive hGH preparation from an individual that
died from the Creutzfeldt-Jakob's disease. This type of encephalitis, believed to be caused
by an infectious agent resembling a slow virus, has an incubation period in humans that is
close to 15 years !
Insulin causes hypoglycemia. If the organism does not produce insulin in sufficient amounts,
as is the case in certain types of diabetes, additional insulin is injected to reach normal
physiological balance. In this scenario, physical sports activities are entirely acceptable.
Unfortunately, this state of balance is so difficult to maintain that many physicians
recommend that diabetics abstain from any serious physical activity, especially sports that
demand a high energy input. The international sports regulating bodies prohibit the non-
therapeutic use of insulin for one main reason: insulin induces growth hormone release. In
itself, insulin causes a number of side effects some of which are listed below:
Nicotine
In the present context, we will only deal with the toxic effects of passive smoking. Indeed,
athletes do not consume tobacco in large amounts (passive smoking, in a closed space
shared with smokers, is a marginal toxicological occurrence in terms of doping behavior). On
the other hand, chewing tobacco or snuff are popular practices in certain countries which
often cause serious diseases.
Periodontal decay
Teeth abrasion
Hyperkeratosis of the mouth mucous membranes
Gingivitis
Leukoplasia
Anomalies of the sense of taste : dysgeusia
Problems with olfaction : dysosmia
Spinocellular epithelioma of the oral cavity
Dependence and withdrawal syndrome
Halitosis: bad breath
PFCs (Perfluorocarbons)
These substances are all composed of fluorine, carbon and hydrogen atoms, but have
important structural differences. Unlike erythropoietin, all PFCs are synthetic and hence
never occurr naturally in the organism. Although they are in principle inert molecules, PFCs
can dissolve large quantities of gas, including oxygen. Various PFC preparations (emulsions
containing egg yolk lecithin or phospholipid) are currently undergoing clinical tests. The goal
is to provide temporary oxygen supply to the brain and other tissues in patients that have lost
important amounts of blood and whose vital functions are in danger. Little is known about the
long-term effects of these substances on the human organism. The toxicity of repeated
treatment is also unclear in situations other than extensively invasive surgical operations. In
terms of tolerance by the organism, the physical and chemical state of the preparation is as
important as its biological purity. Indeed, intra-venous injection is the only means to make
PFCs participate in gas exchange. The clinical preparations currently tested have been found
to have the following side effects:
Probenecid
This substance is used to mask the use of doping substances, anabolic drugs in particular,
by delaying their elimination. The medical application of Probenecid is to treat gout
rheumatism. It may cause the following undesirable effects:
Cephalgia
Anorexia
Nausea
Stomach aches
Vertigo
Frequent micturition
Anemia
Possible anaphylactic-like reactions with fever
Dermatitis and other skin irritations
Because of possible HIV infection, blood transfusions performed outside a hospital context
are simply too dangerous to be even considered as an option. This is common knowledge. It
is important to emphasize the risk of a shock if the donor and the recipient are incompatible.
While homologous transfusions are safer, they also represent a significant hazard. Only
medical surroundings can ensure the absolutely sterile conditions required by transfusion.
Vitamins
An excessive uptake of vitamin leads to well known side effects which vary with each
vitamin. The following effects are worth mentioning:
Diarrhea
Nausea
15
Urticaria
Muscular weakness
Fatigue
Cephalgia
Anorexia
Blood hypertension
Cardiac Arrhythmia
Cirrhosis
Teratogen activity
Conclusions
The conclusion is clear: one should never use medication or pharmacologically active
substances without appropriate advice from a physician. If the medical drugs available today
are very potent and effective in treating disease, they also strongly affect healthy individuals
which may be tempted to use them, even though there is absolutely no therapeutic need.
One must never forget that the side effects of a drug are always present but that the
beneficial effects are felt only in case of a disease that has to be treated. The magnitude of
the side effects is of course dependent on the amount of the drug that is consumed.
Unfortunately, this amount is often excessive. The athlete that relies on doping is under
pressure to obtain quick results. Naturally, there is a strong temptation to increase the doses
to really push one's luck. We wish to emphasize yet another point: it is necessary to check
the purity of all substances of uncertain origin. Some products on the black market are
grossly mislabeled and preparations for injection are often contaminated with bacteria or
even viruses. In such cases, there is a significant risk to develop a serious condition and put
a definitive end to one's athletic career. Clearly, the game of doping is not worth playing.
(The majority of the definitions below are taken from the Dictionnaire français de Médecine et
de Biologie en 4 volumes (French Dictionary of Medicine and Biology in 4 Volumes) A.
Manuila, L. Manuila, M, Nicole et H. Lambert. Paris : Masson, 1971)
Cecity Blindness.
liver diseases.
Micturition Urination.
Paranoia (paranoid delirium) From the times of Hippocrates and through the
Middle Ages, paranoia was a synonym of mental
disease. Until the 1920's and under the
influence of the German school, paranoia
referred to mental disorders affecting the
intelligence, as opposed to emotions. Today, it
designates a hallucinatory or interpretative
systematic delirium.