Stress and Relaxation

Stimulants and Sedatives: The Good, the Bad, and the Ugly

Use now, pay later? Problems associated with common stimulants and sedatives

In our go-go-go world, it’s easy to feel drawn to stimulant substances to keep us going and sedatives to help us relax. Whether it’s coffee to get through the day and a glass of wine after work, or medications such as methylphenidates or amphetamines to keep us cognitively “on” and a benzodiazepine to help us wind down later, it’s likely that we all have been somewhere on the spectrum of stimulation and sedation. Not surprisingly, each of these substances comes with an array of potential side effects, particularly when we depend upon them chronically or use them in excess.

Stimulants

Whether it be in coffee, tea, chocolate, or energy drinks, caffeine is the drug of choice for many. Caffeine stimulates the central nervous system, promoting wakefulness and increased attention.[1] Acute caffeine intake has been shown to enhance working memory-related brain activation,[2] enhance post-study memory consolidation,[3] decrease fatigue, improve exercise performance,[4] and increase attention.[5] However, excessive caffeine consumption can cause restlessness, insomnia, headaches, and digestive complaints,[6] while even typical doses can increase urinary urgency and frequency, anxiety, and blood pressure, particularly in sensitive individuals who already experience these challenges.[7],[8],[9] In children, caffeine consumption can adversely affect brain and bone development and increase risk-taking behaviors.[10],[11] Higher caffeine consumption in children is also associated with anxiety and depression.[12] Chronic use of caffeine also has an abuse or dependence potential,[13],[14] as many whom have tried to give up the use of this substance likely have seen, with withdrawal symptoms like headaches,[15] impaired memory,[16] irritability, and mood changes.[17]

Energy drinks mixed with alcohol, a common selection of younger bar and dance club enthusiasts, are associated with binge drinking, alcohol dependence, increased impulsivity, and high-risk behaviors – so much that this habit alone should be considered high-risk drinking.

Energy drinks, of course, bring us caffeine plus an array of energy-stimulating nutrients such as B vitamins, taurine, guarana, ginseng – plus a hefty dose of sugar. Energy drinks mixed with alcohol, a common selection of younger bar and dance club enthusiasts, are associated with binge drinking, alcohol dependence, increased impulsivity[18] and high-risk behaviors[19] – so much that this habit alone should be considered high-risk drinking.[20] Multiple cases of a heartbeat irregularity known as atrial fibrillation after the intake of energy drinks have also been reported in young individuals,[21],[22] shedding light on the concern for heart problems, particularly in individuals with a family history.[23]

Stimulant medications like methylphenidates and amphetamines are seeing a heyday like no other as well, with the rate of prescription of these drugs quadrupling over the last decade.[24],[25] Although in childhood, boys are approximately five times more likely to be prescribed a medication such as these for attention deficit issues,[26] in adulthood, women have a higher rate of stimulant prescription than men.[27] Although prescription rates are high, actual use population wide is far greater, with 5% to 35% of college students reporting non-prescribed stimulant use.[28] There is a high potential for misuse and abuse, as medications such as these affect dopamine pathways,[29],[30] triggering the dopamine reward pathways commonly stimulated in addictions.[31] The dangers of these medications are many. Adverse effects include irregular heart rhythm, insomnia and sleep problems, decreased appetite, headache, abdominal pain, hallucinations, paranoia, delusional disorder, aggressive behavior, irritability, depression, and suicidality.[32],[33]

Sedatives

Many people have a drink or two to help them fall asleep at night. Although alcohol acts as a sedative to promote sleep, many don’t realize that alcohol actually alters sleep patterns, leading to poor sleep quality.[34] Alcohol consumption in higher amounts has been shown to lead to sleep disturbances in the second half of the night, while tolerance also develops to the initial sedative effects. Additionally, alcohol use in the evening can be a contributor to increased issues of gastroesophageal reflux (or “heartburn”) at night, as the normal night-time clearing of the esophagus is impaired by even moderate amounts of alcohol.[35] Alcohol worsens sleep apnea, reducing oxygen levels in the brain during the first hour of sleep.[36] All of these factors can contribute to increased daytime sleepiness and patterns of dependence. The chronic use and abuse of alcohol can contribute to the development of many other health complications including cancer,[37] cardiovascular disease,[38] and dementia,[39] giving us many reasons to avoid dependent or excessive use of this substance.

Although alcohol acts as a sedative to promote sleep, many don’t realize that alcohol actually alters sleep patterns, leading to poor sleep quality.

Another common sedative is first-generation antihistamines, which non-selectively act in the central and peripheral nervous systems. This over-the-counter medication has well-known sleep-promoting effects but has been shown to contribute to mild cognitive deficits in the elderly, causing disorganized speech, delirium symptoms, altered consciousness, and increased need for urinary catheter placement.[40],[41],[42] Common side effects not limited to the elderly include daytime sleepiness, constipation, not being able to urinate completely, dry mouth, blurred vision, and increased eye pressure.[43],[44],[45] Many of these things the elderly are also at greater risk for, and the effects of this medication can easily be overlooked or blamed on “old age.”

Major classes of prescription medications approved for treatment of insomnia include benzodiazepines and nonbenzodiazepine hypnotics. Meta-analysis has shown that benzodiazepines help us fall asleep only 4.2 minutes faster than placebo and significantly increase total sleep duration by 61.8 minutes.[46] Several of the nonbenzodiazepine hypnotics have a short half-life, making them only effective for helping us fall asleep, but not necessarily in keeping us asleep through the night. The extended-release formats are better at keeping us asleep through the night, but may begin to accumulate in the body, and come with the warning that users should not drive or engage in other activities that require complete mental alertness even the next day.[47] Potential side effects with both categories of drug are many, including: performing activities one is not aware of during sleep (eating, having sex, walking), memory impairments, daytime sleepiness, next day impairments, hallucinations, aggressive behavior, inability to form new memories, lightheadedness, motor incoordination, worsening of sleep apnea, and dependence.[40],[48] In the elderly, the use of these medications contribute to falls and cognitive decline,[46],[49] while a dramatic increase in suicide rate has also been seen.[50]

As per many medications and central nervous system-affecting substances, appropriate and non-appropriate use of each of these substances is common. Chronic or excessive use of these drugs may be cause for concern. Thankfully, many nutritional supplements also are available that support sleep and relaxation, as well as healthy energy levels and cognitive function through the day.

 

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The Day the Coffee Doesn’t Do It…
Less Circus, More Zen at School and Beyond

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