Drugs and Substances: Learn It 3—Stimulants

Stimulants

stimulants

Stimulants are drugs that tend to increase overall levels of neural activity. Many of these drugs act as agonists of the dopamine neurotransmitter system. Dopamine activity is often associated with reward and craving; therefore, drugs that affect dopamine neurotransmission often have abuse liability.

 

Drugs in this category include cocaine, amphetamines (including methamphetamine), cathinones (i.e., bath salts), MDMA (ecstasy), nicotine, and caffeine.

An illustration of a presynaptic cell and a postsynaptic cell shows these cells’ interactions with cocaine and dopamine molecules. The presynaptic cell contains two cylinder-shaped channels, one on each side near where it faces the postsynaptic cell. The postsynaptic cell contains several receptors, side-by-side across the area that faces the presynaptic cell. In the space between the two cells, there are both cocaine and dopamine molecules. One of the cocaine molecules attaches to one of the presynaptic cell’s channels. This cocaine molecule is labeled “bound cocaine.” An X-shape is shown over the top of the bound cocaine and the channel to indicate that the cocaine does not enter the presynaptic cell. A dopamine molecule is shown inside of the presynaptic cell’s other channel. Arrows connect this dopamine molecule to several others inside of the presynaptic cell. More arrows connect to more dopamine molecules, tracing their paths from the channel into the presynaptic cell, and out into the space between the presynaptic cell and the postsynaptic cell. Arrows extend from two of the dopamine molecules in this in-between space to the postsynaptic cell’s receptors. Only the dopamine molecules are shown binding to the postsynaptic cell’s receptors.
Figure 1. As one of their mechanisms of action, cocaine and amphetamines block the reuptake of dopamine from the synapse into the presynaptic cell.

Cocaine

Cocaine can be taken in multiple ways. While many users snort cocaine, intravenous injection and inhalation (smoking) are also common. The freebase version of cocaine, known as crack, is a potent, smokable version of the drug. Like many other stimulants, cocaine agonizes the dopamine neurotransmitter system by blocking the reuptake of dopamine in the neuronal synapse, extending the feeling of pleasure from the release of dopamine.

Amphetamines

Amphetamines have a mechanism of action quite similar to cocaine in that they block the reuptake of dopamine in addition to stimulating its release.

In recent years, methamphetamine (meth) use has become increasingly widespread. Methamphetamine is a type of amphetamine that can be made from ingredients that are readily available (e.g., medications containing pseudoephedrine, a compound found in many over-the-counter cold and flu remedies). Despite recent changes in laws designed to make obtaining pseudoephedrine more difficult, methamphetamine continues to be an easily accessible and relatively inexpensive drug option (Shukla, Crump, & Chrisco, 2012). Stimulant users seek a euphoric high and feelings of intense elation and pleasure, especially those users who take the drug via intravenous injection or smoking.Methamphetamine in its smokable form, often called “crystal meth” due to its resemblance to rock crystal formations, is highly addictive. The smokable form reaches the brain very quickly producing an intense euphoria that dissipates almost as fast as it arrives, prompting users to continue taking the drug. Users often consume the drug every few hours across days-long binges called “runs,” in which the user often forgoes food and sleep. In the wake of the opiate epidemic, many drug cartels in Mexico are shifting from heroin production to the production of highly potent but inexpensive forms of methamphetamine. This low cost coupled with a lower risk of overdose than opiates makes crystal meth a popular choice among drug users today (NIDA, 2019). Using crystal meth poses a number of serious long-term health issues, including dental problems (often called “meth mouth”), skin abrasions caused by excessive scratching, memory loss, sleep problems, violent behavior, paranoia, and hallucinations. Methamphetamine addiction produces an intense craving that is difficult to treat.

While amphetamines are often abused, there are also instances where amphetamines are a treatment option for various medical conditions or disorders.

Amphetamines, such as Adderall, are commonly prescribed to children diagnosed with attention deficit hyperactivity disorder (ADHD). It may seem counterintuitive that stimulant medications are prescribed to treat a disorder that involves hyperactivity, but the therapeutic effect comes from increases in neurotransmitter activity within certain areas of the brain associated with impulse control.

MDMA

MDMA (3.4-methelynedioxy-methamphetamine, commonly known as “ecstasy” or “Molly”) is a mild stimulant with perception-altering effects. It is typically consumed in pill form. Users experience increased energy, feelings of pleasure, and emotional warmth. Repeated use of these stimulants can have significant adverse consequences. Users can experience physical symptoms that include nausea, elevated blood pressure, and increased heart rate. In addition, these drugs can cause feelings of anxiety, hallucinations, and paranoia (Fiorentini et al., 2011).

Normal brain functioning can be altered after repeated use as a result of an overall depletion of the monoamine neurotransmitters (dopamine, norepinephrine, and serotonin). Depletion of certain neurotransmitters can lead to mood dysphoria, cognitive problems, and other factors. This can lead to people compulsively using stimulants such as cocaine and amphetamines, in part to try to re-establish the person’s physical and psychological pre-use baseline. (Jayanthi & Ramamoorthy, 2005; Rothman, Blough, & Baumann, 2007).

Caffeine

Caffeine is another stimulant drug. While it is probably the most commonly used drug in the world, the potency of this particular drug pales in comparison to the other stimulant drugs described in this section. Generally, people use caffeine to maintain increased levels of alertness and arousal. Caffeine is found in many common medicines (such as weight loss drugs), beverages, foods, and even cosmetics (Herman & Herman, 2013).

While caffeine may have some indirect effects on dopamine neurotransmission, its primary mechanism of action involves antagonizing adenosine activity (Porkka-Heiskanen, 2011). Adenosine is a neurotransmitter that promotes sleep. Caffeine is an adenosine antagonist, so caffeine inhibits the adenosine receptors, thus decreasing sleepiness and promoting wakefulness.

While caffeine is generally considered a relatively safe drug, high blood levels of caffeine can result in insomnia, agitation, muscle twitching, nausea, irregular heartbeat, and even death (Reissig, Strain, & Griffiths, 2009; Wolt, Ganetsky, & Babu, 2012).

In 2012, Kromann and Nielson[1] reported on a case study of a 40-year-old woman who suffered significant ill effects from her use of caffeine. The woman used caffeine in the past to boost her mood and to provide energy, but over the course of several years, she increased her caffeine consumption to the point that she was consuming three liters of soda each day. Although she had been taking a prescription antidepressant, her symptoms of depression continued to worsen and she began to suffer physically, displaying significant warning signs of cardiovascular disease and diabetes. Upon admission to an outpatient clinic for treatment of mood disorders, she met all of the diagnostic criteria for substance dependence and was advised to dramatically limit her caffeine intake. Once she was able to limit her use to less than 12 ounces of soda a day, both her mental and physical health gradually improved. Despite the prevalence of caffeine use and the large number of people who confess to suffering from caffeine addiction, this was the first published description of “cola dependence” appearing in scientific literature.

Nicotine

Nicotine is highly addictive, and the use of tobacco products is associated with increased risks of heart disease, stroke, and a variety of cancers. Nicotine exerts its effects through its interaction with acetylcholine receptors. Acetylcholine functions as a neurotransmitter in motor neurons. In the central nervous system, it plays a role in arousal and reward mechanisms.

Nicotine is most commonly used in the form of tobacco products like cigarettes or chewing tobacco; therefore, there is a tremendous interest in developing effective smoking cessation techniques. To date, people have used a variety of nicotine replacement therapies in addition to various psychotherapeutic options in an attempt to discontinue their use of tobacco products. In general, smoking cessation programs may be effective in the short term, but it is unclear whether these effects persist (Cropley, Theadom, Pravettoni, & Webb, 2008; Levitt, Shaw, Wong, & Kaczorowski, 2007; Smedslund, Fisher, Boles, & Lichtenstein, 2004).

Vaping as a means to deliver nicotine is becoming increasingly popular, especially among teens and young adults. Vaping uses battery-powered devices, sometimes called e-cigarettes, that deliver liquid nicotine and flavorings as a vapor. Originally reported as a safe alternative to the known cancer-causing agents found in cigarettes, vaping is now known to be very dangerous and has led to serious lung disease and death in users.
To learn more about some of the most commonly abused prescription and street drugs, check out the Commonly Abused Drugs Chart and the Commonly Abused Prescription Drugs Chart from the National Institute on Drug Abuse.
  1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3598894/ ↵