15.6: Stimulants
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- Aug 20, 2021
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What is a Stimulant?
These classes of chemicals induce alertness and stimulant the brain and nervous system. Side effects of stimulant use include wakefulness, increased speech, and motor activity, and decreased appetite. Amphetamines are a type of stimulant that incorporates a nitrogen-containing organic functional group. These compounds have been noted to block the reuptake of dopamine.
Figure 15.6.1: The skeletal structure of phenethylamine. (Copyright, http://countyourculture.com/2010/11/02/phenethylamine-and-amphetamine/)
Early Stimulant Use
For over 5000 years, the Chinese have extracted the compound Ephedrine from locally grown Ephedra plants. Native peoples of the United States were known to isolate this compound as well. Both cultures used Ephedrine to treat asthma, hay fever, and congestion. Ephedrine was noted to have a stimulant effect on its users. Chemically similar to adrenaline, ephedrine was a more stable compound and could be taken orally. By the mid-1920s, the pharmaceutical company, Eli Lily, synthesized ephedrine and introduced it into western medicine.
Figure 15.6.1: : https://commons.wikimedia.org/wiki/C...phedra_viridis. (Copyright, https://commons.wikimedia.org/wiki/User:Dcrjsr)
Ephedrine can decrease appetite, increase blood pressure and heart rate, and cause sleeping problems. Mental health can be affected by ephedrine use. Patients may experience hallucinogens, anxiety, and chemical dependence.
Figure 15.6.2: Chemical structure of Ephedrine, done using BKchem. (Copyright, https://commons.wikimedia.org/wiki/User:Bryan_Derksen)
Amphetamines
While researching the synthesis and application of ephedrine, organic chemists decided to focus on constructing more stimulant-based compounds. These compounds, called amphetamines, are defined as having a basic molecular formula including C9H13N. Amphetamines are a mixture of two compounds, levoamphetamine and dextroamphetamine, that are mirror images of one another. Dextroamphetamine, often referred to as d-amphetamine, has a more powerful stimulant effect than levoamphetamine.
Figure 15.6.3: Skeletal formulae of two amphetamine enantiomers: (R)-(−)-amphetamine (also known as L-amphetamine or levoamphetamine), and
- (S)-(+)-amphetamine (also known as D-amphetamine or dextroamphetamine). (https://commons.wikimedia.org/wiki/U...Vaccinationist, PubChem).
In 1932, the amphetamine, Benzedrine, was available to purchase over-the-counter. This inhaled amphetamine was used primarily by asthmatics and people who had lower than normal blood pressure. By the mid-1930s, other OTC formulations of amphetamines were utilized to treat narcolepsy and attention deficit hyperactivity disorder (ADHD). Noted side-effects of using amphetamines were: increased energy, appetite suppression, and decreased need for sleep. By 1959, the Food and Drug Agency (FDA) banned all over-the-counter forms of amphetamines.
Figure 15.6.3: http://www.museedeslettres.fr/public...ed5db0dc7e0eee. (Copyright,https://commons.wikimedia.org/wiki/User:Prosopee).
Methamphetamine
Around 1919, Japanese scientists synthesized a methylated (CH3) version of amphetamine. This new chemical was purified by crystallization. It could be packaged in pill or injectable form. By 1938, methamphetamine was marketed as an antidepressant in Germany. Also, the German government decided to supply Nazi soldiers with millions of tablets. L and D- amphetamines were used by Allied soldiers as well.
Figure 15.6.4: Chemical structure of Methamphetamine. (Copyright, https://commons.wikimedia.org/w/inde...edit&redlink=1)
Prescription Amphetamines
Dextroamphetamine and Amphetamine(Adderall/Adderall XR) or mixed amphetamine salts -ADHD and narcolepsy. could raise blood pressure. Pre-existing heart condition -consult with a physician. Diarrhea/Constipation/Weight loss/Insomnia/Dry Mouth/Palpitations/Changes in Libido. Effects of Adderall (9 hours) and Adderall XR (10-13 hours)
Dextroamphetamine (Dexedrine)-ADHD and narcolepsy. Pre-existing heart condition -consult with a physician. Diarrhea/Constipation/Weight loss/Insomnia/Dry Mouth/Palpitations/Changes in Libido
Lisdexamfetamine (Vyvanse/Tyvense/Elvanse)- ADHD, binge eating disorder, same types of side effects as seen as above. Effects last up to 14 hours
Non-amphetamine Stimulants
Figure 15.6.4: D-methylphenidate-plane. (Copyright, https://en.Wikipedia.org/wiki/User:Angsaar).
Methylphenidate (Concerta/Ritalin)- ADHD and narcolepsy. blurry vision, dry mouth, sleeping issues, anxiety, and dizziness. Circulation issues/raise blood pressure/heart rate. If have a heart condition, discuss it with a physician.
Note: All prescribed stimulants are Scheduled II.