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Brain doping

Brain doping with nootropics (“smart drugs”) refers to the use of pharmaceuticals by healthy people with the aim of improving concentration, alertness, attention, memory, learning or mood, among other things. Brain doping has been detected, for instance, among students and people working in demanding professions. Brain doping drugs are used in the treatment of various diseases, such as Alzheimer’s disease, attention deficit hyperactivity disorder (ADHD), and schizophrenia. Some of the substances that are used for brain doping purposes include amphetamine, modafinil, piracetam, ephedrine, and pseudoephedrine.

Amphetamine

Amphetamine has a long history of medical and recreational use. It has a stimulating effect on the central nervous system similar to that of cocaine. Among other things, amphetamine is a stimulating substance, which enhances the mood, increases a sense of vigour, reduces the appetite, and (in moderate doses) improves concentration. [8, 20] Amphetamine is used as a doping substance for its stimulating effect, but also to increase fat burning and workout output.

Adverse effects

Amphetamine excites the body functions, which is linked to the risk of life-threatening complications. Amphetamine can induce agitation, restlessness, the loss of appetite, convulsions, arrhythmias, hyperthermia, intracranial bleeding or Disseminated Intravascular Coagulation (DIC) syndrome. Ingesting high doses may trigger psychosis. Recurring amphetamine use may lead to severe addiction. Tolerance to the effects of the substance increases with use [8, 20, 21]. Amphetamine is also commonly abused. After cannabis, it is one of the most popular among drugs in Finland.

Ephedrine and pseudoephedrine

 

Ephedrine

Ephedrine is an alkaloid obtained from the plants of the genus Ephedrai. However, most ephedrine is synthetically made. Ephedrine is related to amphetamine and its effect is similar. Ephedrine excites the central nervous system mainly by increasing noradrenaline activity in the adrenergic receptors and bringing a stimulating effect. [21]

In Finland, it is mainly used in the treatment of temporary nasal congestion. The purpose of use for doping purposes is to give power and explosiveness to the training, improve effort tolerance, and reduce fatigue. Ephedrine is also used for its metabolism-boosting and fat-burning effect. [4, 22]

Learn more about ephedrine: https://dopinglinkki.fi/en/info-bank/doping-substances/ephedrine.

Pseudoephedrine

Pseudoephedrine is an isomer of ephedrine. Compared with ephedrine, pseudoephedrine does not induce tachycardia or increased blood pressure to the same extent. It does not stimulate the central nervous system as strongly either. In order to achieve the performance capacity-enhancing effect of pseudoephedrine, the doses should be so high that the adverse effects would likely exceed the potentially added performance capacity. There is no certainty about the performance capacity-enhancing effect of pseudoephedrine, but according to the research it is more effective than a placebo. Among other things, pseudoephedrine increases blood flow to the muscles and reduces fatigue. [8]

Adverse effects

The adverse effects of ephedrine include tremors, palpitations, and an increase in blood pressure. Ephedrine can induce the states of confusion or paranoia, as well as severe arrhythmias, in sensitive individuals or if taken in excessive doses. High quantities of this drug in connection with strain may lead to heatstroke, dangerous arrhythmias or death. [9, 21] The adverse effects of pseudoephedrine are similar to those of ephedrine.

Modafinil

Modafinil is a stimulant, but its mechanism of action is different from that of amphetamine or ephedrine. It is used as a pharmaceutical for the treatment of narcolepsy and drowsiness, as well as in the treatment of memory or attention deficit hyperactivity disorders, Alzheimer’s disease, and depression. In healthy people, modafinil helps to maintain wakefulness and to prevent cognitive problems caused by sleep deprivation. [2, 5, 7]

Modafinil use is associated with a stimulating and pleasure-enhancing effect, but the evidence for its euphoric effect when taken orally is weak. Users can pursue faster effects by snorting powdered tablets. For intravenous use, modafinil is too insoluble. Modafinil reduces appetite and the most common kinds of harm include dizziness, disturbed sleep, abdominal pain, nausea, and indigestion. [2, 5]

Mechanism of action

Modafinil affects several different parts of the brain. Presumably, the most important vitality-enhancing effect of modafinil targets the hypothalamus at the base of the diencephalon, where it activates the neural pathways, which use orexins (i.e. hypocretins) as their neurotransmitters, and which are important in the regulation of the states of sleeping and waking. It also activates the sympathetic alpha-1-receptors of the central nervous system, increases the activity of exciting glutamine and histamine neurotransmitters, and strengthens the effects of serotonin in the cerebral cortex. Additionally, it reduces the activity of the nerve cells, which use the inhibitory gamma-aminobutyric acid as their neurotransmitter. Modafinil is absorbed well through the intestines, it metabolizes in the liver, and its half-life is 10–14 hours. Peak concentrations in the plasma occur two to four hours after ingestion. The exact mechanisms that promote staying awake are not precisely known. [2, 5, 7]

Adverse effects

Modafinil can induce pleasure and addiction, but clearly less than amphetamine. It is tolerated well in therapeutic doses, but it may present some side effects, including insomnia, headaches, nervousness, anxiety, aggressiveness, an increase in blood pressure, and cardiac symptoms. [2, 5, 13]

Methylphenidate

Methylphenidate is a stimulant and a common attention deficit hyperactivity disorder (ADHD) medication. It is also used in the treatment of narcolepsy and brain injuries. [24, 25] Methylphenidate may also enhance cognitive performance capacity and this is why it is used for brain doping. Absorption by oral ingestion is slow and the euphoriant effect is low. Methylphenidate is also used for substance abuse purposes and as its pharmaceutical use has become increasingly common, this type of abuse has increased accordingly.

 

Adverse effects

Methylphenidate has a number of commonly recognized adverse effects. Some of these include upper respiratory tract infections, the loss of appetite, reduced appetite, slightly reduced weight development, and retardation of height growth. Additionally, there may be occurrences of agitation, anxiety, depression, irritation, tics, upper abdominal pain, diarrhea, nausea, stomach problems, vomiting, dry mouth, and indigestion. [24, 25]

Piracetam

Piracetam is a stimulant, which is used for treating conditions, such as Alzheimer’s and Parkinson’s disease and tic disorders. [23]. Piracetam may have a memory-enhancing effect on healthy people as well.

Mechanism of action

In pharmacotherapeutic terms, piracetam is a member of the psychostimulant and nootropic group. By structure, it is a derivative of gamma-Aminobutyric acid (GABA). Its precise mechanism of action is unknown. Piracetam possibly has some neuroprotective properties, which are mediated by effects targeting the cell membrane. Piracetam has been found to bind to the polar ends of the phospholipids of the cell membrane, whereupon it is assumed to promote adenosine triphosphate (ATP) production, neurotransmission, and second messenger activity. Piracetam is eliminated quickly through the kidneys and its half-life is four to six hours in healthy young adults. [22]

Adverse effects

The adverse effects of piracetam may include hyperkinesis, drowsiness, ataxia, balance disorders, headache, insomnia, abdominal pain, diarrhea, vomiting, itching, and eczema. No life-threatening adverse effects of this substance have been detected. [23]

Caffeine

Caffeine is a legally used chemical compound occurring in plants, which affects the human central nervous system. Its chemical name is 1,3,7-trimethylxanthine.  Nowadays, caffeine is added to many foods. Caffeine is present in coffee as a natural ingredient, but also in tea and cocoa. Synthetic caffeine is added, for example, to energy drinks, cola drinks, and energy bars. [14] The effect of caffeine shows quickly: about half an hour after ingestion. Caffeine is absorbed through the digestive track into the blood and it halves in about three to six hours. Caffeine excites the central nervous system, which appears as a stimulating effect. Caffeine affects the brain through the adenosine receptor and one to two cups of coffee is enough to bring about the stimulating effect on adults. Potentially, caffeine has some positive effects during endurance sports performance, based on the accelerated fat metabolism and the quickened glycogen use. [16] Caffeine may also have positive effects on fitness training and the reduction of muscle pain afterwards. [15] According to a recent study, however, the effects of caffeine in the improvement of sports performance depend on individual reactivity. Due to this, case-by-case studies are recommended in the future. [17]

Adverse effects

Caffeine is a chemical and its mechanism of action is medicinal. When used in large quantities, it is linked to adverse effect, such as caffeine intoxication. Its symptoms include restlessness, nausea, tremors, and palpitations. In the event of severe intoxication, convulsions may also occur. Symptoms of intoxication may develop when the daily caffeine intake exceeds 400 mg. Most commonly, these symptoms will begin to occur in adults at a daily dose of about 600 mg. [14]. Children and young people are harmed by caffeine more easily than adults.

Caffeine intoxication symptoms have been detected in children and adolescents with doses of 160–200 mg. [14, 18]. The use of energy drinks, sports drinks or wellness drinks is not recommended for those who are caffeine sensitive, pregnant or under the age of 15. [20]

Pregnant women should not have more than two cups of coffee per day. [19]. A developing embryo is not able to process caffeine normally. This is why the caffeine intake of expectant mothers should be less than 300 mg daily [14].

Ville Leskinen
Master of Health Sciences (MHSc)
Dopinglinkki

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