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Amphetamine

July 27, 2019

Amphetamine is a central nervous system stimulant. Being chemically related to catecholamines, it induces the release of noradrenaline. Noradrenaline, in turn, induces classic sympathetic effects, such as rising heart rate, blood pressure, and respiration [1].

Amphetamine was synthesized in 1887 and its medicinal use began in the 1930s. Due to its stimulating effect, amphetamine has already been used during World War II [2]. So Amphetamine can be seen as one of the first fitness doping substances ever used. [3]. A number of derivatives have been obtained from amphetamine. These include substances, such as methamphetamine, methylene dioxy amphetamine (MDA) and methylenedioxymethamphetamine (MDMA or ‘Ecstasy’) [4].

Amphetamine absorbs well through the digestive track and it is available in tablet form. It can also be ingested nasally or intravenously [2]. Amphetamine has a rather long half-life, averaging approximately 19 hours [5].

Medical use

Amphetamine and its derivatives are used in the treatment of attention deficit hyperactivity disorder (ADHD). They enhance concentration and reduce restlessness, among other things. The potency of the medication often appears quickly. Pharmacotherapy for ADHD can be initiated by a specialist in behavioral disorders. There have been attempts to develop weight-loss drugs from amphetamine derivatives without the adverse effects of amphetamine. These attempts have not been entirely successful, however [2].

Purpose of use as a doping substance

The potency of amphetamine for improving performance has been researched already since the 1950s. Amphetamine has been found to enhance anaerobic performance, but it has little or no effect on aerobic performance. The dosage plays an important role in terms of performance capacity. Large doses would appear to increase aggressiveness, whereas smaller doses increase alertness. The main effects of amphetamine on performance capacity are related to improved reaction time when fatigued, increased strength and endurance, increased lactic acid during maximum performance, and reduced body fat [4].

Because amphetamine reduces appetite, it can be used to boost dieting. So amphetamine and its derivatives have been used as weight-loss drugs, but due to their adverse effects, they are no longer used in the field of medicine for losing weight [2].

Amphetamine can also be used for the so-called brain doping: in other words, to enhance cognitive skills. Amphetamine use aims to keep the user alert and enhance learning results or coping at work, for example. No benefit from amphetamine has been demonstrated for healthy young people, however. On the contrary, delusional thoughts and a feeling of panic may weaken performance [2].

Adverse effects

Some of the medicinal adverse effects of amphetamine include insomnia, the loss of appetite, anxiety, psychosis symptoms, as well as increased heart rate and blood pressure. Other adverse effects associated with amphetamine use include perspiration, headache, accelerated respiration, tremors, as well as arthralgia and myalgia [2, 4].

Especially when combined with heavy exertion, amphetamine may trigger sudden death or raise the risk of such through arrhythmia or heatstroke. Amphetamine has been linked to a number of fatalities in sports [4, 5].

Fatigue and exhaustion are important feelings and safeguards that protect our bodies from dangerously high levels of stress [6]. These feelings can be bypassed by the effect of amphetamine and performance output will then be enhanced. Consequently, the muscle temperature may rise dangerously high during and after exertion [7].

All stimulants, which have a structure similar to amphetamine, can induce catecholamine-induced cardiotoxicity [8, 9]. Raised catecholamine levels can lead first to the contraction of the blood vessels, a rapid heartbeat, and high blood pressure, then to the lack of oxygen in the heart. This can result in cardiac hypertrophy, fibrosis, or necrosis [8].

In most cases, it can be assumed that the personality changes induced by the prolonged use of small doses will gradually normalize once the use is discontinued. However, using large doses for long may leave some permanent changes of behavior, such as paranoia [2].

Tolerance to the numerous effects of amphetamine develops quite quickly. An amphetamine addict may become psychotic, aggressive, and anti-social. Depression may be associated with the discontinuation of amphetamine use [2].

 

Joni Askola
Master of Health Sciences (MHSc),
Dopinglinkki

 

[1] Momaya A, Fawal M, Estes R. Performance-enhancing substances in sports: a review of the literature. Sports Med. 2015;45(4):517–531
 
[2] Korpi E, Linden AM. 2018. Amfetamiini ja sen johdannaiset. Lääketieteellinen farmakologia ja toksikologia. Duodecim 
 
[3] Salasuo M, Piispa M. 2012. Kuntodoping: Näkökulmia dopingaineiden käyttöön huippu-urheilun ulkopuolella. Nuorisotutkimusverkosto/ Nuorisotutkimusseura, Julkaisuja 120. Helsinki. s. 48 
 
[4] Avois L, Robinson N, Saudan C, Baume N, Mangin P, Saugy M. Central nervous system stimulants and sport practice. Br J Sports Med. 2006;40(1): i16–i20
 
[5] Docherty J. Pharmacology of stimulants prohibited by the World Anti-Doping Agency (WADA). Br J Pharmacol. 2008;154(3):606–622
 
[6] Noakes T. Fatigue is a brain-derived emotion that regulates the exercise behavior to ensure the protection of whole body homeostasis. Front Physiol. 2012; 3:82
 
[7] Morozova E, Yoo Y, Behrouzvaziri A, Zaretskaia M, Rusyniak D, Zaretsky D, Molkov Y. Amphetamine enhances endurance by increasing heat dissipation. Physiol Rep. 2016;4(17): e12955
 
[8] Angell P, Chester N, Sculthorpe N, Whyte G, George K, Somauroo J. Performance enhancing drug abuse and cardiovascular risk in athletes: implications for the clinician. Br J Sports Med. 2014;46(1): i78–84
 
[9] Turpeinen A, Kivelä A. 2014. Sydänlihastulehduksen aiheuttajat. Sydänsairaudet. Duodecim, Terveysportti
 


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