Early elixirs: Amphetamine

Clinical
By
Scott Casey
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From wonder drug to scourge. The synthesis of amphetamine has had a profound effect on society as well as attitudes towards drugs.

From its use treating asthma and nasal congestion, to being prescribed for depression, epilepsy, drug and alcohol addiction and more, amphetamines have touched many areas of healthcare.

First synthesised by Lazar Edeleanu in 1887, alpha-methylphenethylamine (contracted by Edeleanu to amphetamine) was the ­first amphetamine and was derived from the Ephedra plant.¹ However, Edeleanu never experimented with its effects.

This was left to American scientist Gordon Alles. Four decades later, in an unrelated effort to create an improved version of the drug Ephedrine to treat asthma, Alles began experimenting with beta-phenyl-isopropylamine.¹ He was injected with 50 mg and within minutes his sinuses were clear, his blood pressure rose and he became happy with a general ‘feeling of well being’.

Mechanisms

Amphetamines increase the activity of the monoaminergic system, releasing dopamine while inhibiting its metabolism and reuptake. They also increase the release of noradrenaline and serotonin.

At therapeutic doses, amphetamine causes effects such as euphoria, increased wakefulness, improved cognitive control and fatigue resistance.

In 1932, Mr Alles patented orally active amphetamine salts, while just a year later US pharmaceutical company Smith Kline and French (SKF) developed and marketed the Benzedrine Inhaler, a capped tube containing an oily amphetamine base.²

The two joined forces and by 1937 the American Medical Association gave advertising approval for Benzedrine Sulfate tablets, for use in treatment of mild depression, fatigue, Parkinson’s disease and narcolepsy, but with an emphasis on ‘improving mood’. In a little over a year, SKF was selling more than $300,000 of Benzedrine pills in the USA, with the coming of World War II creating millions more in sales.² During the war, fighter pilots and troops were supplied with Benzedrine to stay alert for long periods during bombing missions or in battle.²

Local use

Australia was not immune to the growing demand for amphetamines, with Benzedrine marketed to everyone from housewives to introverted people, those suffering from depression, and even pregnant women.³

From the earliest days, there were reports of abuse of amphetamines, but it was the rise in the use of amphetamines recreationally by young people in the 1960s and 1970s in Australia which led to restrictions.4

In 1967, Federal Parliament passed the Narcotic Drugs Act which started the restriction of amphetamines (for both licit and illicit use), and a host of other drugs, as global drug enforcement regimes began to expand.5

Today, amphetamine is a Schedule 8 drug; in forms such as dextroamphetamine sulfate it is indicated for treatment of attention de­ficit hyperactivity disorder and narcolepsy.

References

1. Moore, EA. The Amphetamine Debate: The Use of Adderall, Ritalin and Related Drugs for Behavior Modification, Neuroenhancement and Anti-Aging Purposes. First Edition. USA: McFarland Health Topics; 2011. p20.

2. Hicks, J. Fast Times: The Life, Death, and Rebirth of Amphetamine. Science History Institute, Spring 2012. At: https://www.sciencehistory.org/distillations/magazine/fast-times-the-life-death-and-rebirth-of-amphetamine

3. Williams, L. The Strange History of Methamphetamines. news.com.au, 2017 Aug 10. At: http://www.news.com.au/lifestyle/health/health-problems/the-strange-history-of-methamphetamines/news-story/b82f848ee30767a69ae6fff719f122da

4. State Library of New South Wales. Drugs and the Law. Chapter 12 – History of drug laws – Australia [Website]. At: http://legalanswers.sl.nsw.gov.au/drugs-and-law-hot-topics/history-drug-laws-australia

5. Macintosh, A. Drug Law Reform: Beyond Prohibition. [Internet] The Australia Institute, Discussion Paper Number 83, February 2006. At:  http://www.tai.org.au/documents/dp_fulltext/DP83.pdf