How Do Sleeping Pills Work - Featured

How Do Sleeping Pills Work and What Are Their Effects?

by Dr. Lina Velikova, MD

Many people resort to the use of sleeping pills to get a restful night’s sleep. In the pharmacy, you can find a wide variety of over-the-counter and prescription sleeping pills, as well as natural herbal extracts. But how do sleeping pills work? Some of them are merely soothing, and others directly cause sleep. 

Since insomnia is as old as humanity, substances such as alcohol, opium, and herbs were used as “drugs” to interfere with sleep since well before the 20th century. Most experts say that sleeping pills are a short-term solution to the problem. Prolonged use may exacerbate insomnia, especially when you stop taking the medication. But if you need it, which sleeping pill or natural aid is right for you? 

How Do Sleep Aids Work?

Sleeping pills are also called hypnotics because they activate hypnogenic zones in the cortical structures, suppress the ascending reticular activating system, and enhance the retention effect of the GABAergic system. Put simply, sleeping pills are designed to initiate, maintain, or prolong sleep. Essentially, the overall sleeping pill effect is similar to the influence of narcotic drugs except that they don’t extend to the spinal cord.  

When examining the cortex of the large hemisphere under the influence of sleeping pills (by electroencephalographic examination), wave synchronization was detected, similar to physiological (natural) sleep. This indicates that the low and high-amplitude fluctuations of alpha and gamma waves from natural sleep can be induced by most sleeping pills’ ingredients. And there’s another similarity between medicated and natural sleep: both enable brain cells to recover, reduce catabolic (degradation) processes, and increase anabolic processes.

The significant difference, however, is that anabolic processes (the processes of building molecules) occur much more significantly in natural sleep than they do in medicated sleep. These processes are essential for cell renewal and growth and for the body as a whole.

Prescription sleeping aids restore phosphorus and oxygen metabolism in the central nervous system. Some of them have been shown to prevent the reduction of adenosine triphosphate (ATP) in the brain, which is responsible for storing energy and transporting it in cells. Retention of higher CNS functions during sleep plays a protective role against brain cell damage. This explains the healing role of sleeping pills when it comes to damage to both nerve cells and internal organs.

Sleeping aid prescriptions include medicines in the following groups: barbiturates, benzodiazepines, piperidinediones, and quinazolinone derivatives, as well as various combinations between them. These drugs also produce anxiolytic, sedative, and anti-seizure effects—which is why they’re considered sedatives or sleep and anxiolytic agents. Keep in mind, the way each drug interacts with the body will also be determined by its specific dosage. 

Sleeping Pills That Actually Work

There are two types of sleeping pills, categorized by how long they act on the system. These are short-acting hypnotics (which serve to initiate sleep) and long-acting hypnotics (used to provide a sufficient duration of sleep). 

Barbiturates, for example, disrupt the ratio of the two phases of sleep in favor of the NREM phase. For this reason, they often lead to headaches, fatigue, and drowsiness the next day. Benzodiazepines retain the ratio of the two phases of sleep and are used more often to initiate sleep. Another group of sleeping pills that knock you out instantly include quinazoline derivatives, which help you achieve a sleep duration of 6–8 hours. 

These sleeping pills might also be a combination of different agents to help initiate sleep. These could be as combinations of barbiturates; barbiturates in combination with other drugs; or sleeping pills and sedatives in combination (but not barbiturates). 

The idea that a pill can solve sleep problems instantly is very appealing. Unfortunately, sleeping pills do not cure the underlying cause of insomnia. In fact, they can even exacerbate the problem in the long run. Keep in mind, sleep medicines, including sleeping pills that are over the counter, are recommended for short use, often at the beginning of behavioral therapy to help a patient with severe insomnia. 

In general, sleeping pills and other similar medications are most effective when used in the short term, for example, when traveling to different time zones, for recovery from medical procedures, as a supportive treatment for a concussion, and so on.

What Are the Best Natural Sleeping Aids?

How Do Sleeping Pills Work - Valerian

Here are some of the most commonly used remedies for sleep disorders and how they help you sleep:

Melatonin

When it gets dark outside, the brain begins to produce a hormone called melatonin. This hormone regulates the sleep-wake cycle by telling the brain when it’s time to sleep. The brain produces less melatonin when it’s light out and more when it gets dark. The older you are, the less melatonin your brain produces.

Melatonin for sleep can be especially helpful for people who change time zones to avoid jet lag symptoms. Sleep aids like this could also be beneficial for older people or those who work night shifts. In recent years, many manufacturers have marketed foods and beverages containing melatonin, offering its benefits to consumers. However, doctors are skeptical about their effectiveness.

Roots of Valerian

Valerian is a sedative, used since ancient times. It’s an essential component in herbal sleep medicines. It’s been proven that valerian facilitates sleep and improves sleep quality.

Prescription Sleeping Pills

Usually, for more severe sleep disorders, doctors prescribe medicines such as zopiclone, zolpidem, alprazolam, or diazepam. Unfortunately, these drugs have severe side effects and lead to addiction. 

Sleeping pills and tranquilizers (sedatives) are intended to help with anxiety and insomnia.  They belong to the group of substances that suppress the functions of the central nervous system. For this reason, some of them are used to control epileptic seizures. In almost all cases, their use should be for a short period.

Antihistamines

Traditionally, these are used as anti-allergy products. The first generation of antihistamines have a strong sedative effect and can successfully be used as sleep medications. Some of the antihistamines that have a sedative effect are diphenhydramine, doxylamine, cyclizine, and chloropyramine. However, new-generation antihistamines like cetirizine or loratadine have no sedative effect. 

Side Effects and Other Concerns

Sleeping pills come in the form of multicolored tablets and capsules; other aids for sleep come in the form of a solution for injection or suppositories. Regardless of how they’re administered, these products all lead to short-term and long-term effects. 

These effects include depressing the central nervous system, which means that the medication inhibits brain functions. The person taking sleeping medication will become calm and relaxed, but they may also feel sleepy, dizzy, and emotionally indifferent. They can no longer concentrate fully and their reflexes slow down. 

People taking these medications may overestimate his or her own abilities, which leads to some risks, such as having trouble driving. In fact, operating machinery and performing other dangerous activities under the influence of sleeping pills and tranquilizers are extremely dangerous and should not be allowed. This can be the case even if they take over the counter sleeping pills.

The use of sleeping pills and tranquilizers can quickly cause a strong dependence—both physically and psychologically. This also means it doesn’t take long before users need to increase the amount they take to produce the same effect. 

What’s more, the long-term effects of these medications include addiction, fatigue, memory impairment, laziness, and sometimes muscle weakness. It’s also essential to emphasize that the combination of sleeping pills and alcohol can cause a fatal central nervous system depression.

Despite the differences between the specific substances, they all act similarly, and today they are often referred to under the general term “benzodiazepines.” In the past, barbiturates were the class of sedatives commonly prescribed for anxiety and insomnia, but after the 1990s, their medical use as an insomnia medication has declined dramatically. The main reason for this is that barbiturates have a very high potential for abuse. 

Nowadays, it is already well-known that benzodiazepines are a frequently abused medication and can easily be highly addictive. However, despite these serious drawbacks, their medical use is not diminished.  

What Are the Disadvantages of Taking Sleeping Pills?

How Do Sleeping Pills Work - Disadvantages

Many people have problems with anxiety, stress, fatigue, or depression, all of which can cause a sleep disorder. Benzodiazepines reduce the brain’s sensitivity to external stimuli by slowing down brain functions. As a result, the environment seems more relaxed, although it hasn’t changed. Some benzodiazepines have a calming effect, while others cause sleep. Often for sleep problems, fast-acting sleeping pills are prescribed, whereas long-term medications are recommended for anxiety and stress during the day. 

In fact, sleeping aids do not solve problems, but rather mask them. The only thing that helps is to trace the causes of the issues and to work to solve them. The use of benzodiazepines for a more extended time makes finding problems under the surface much more difficult. For this reason, treatment with benzodiazepines should be for as short a duration as possible, almost never exceeding two weeks. However, treatment may need to be longer for people with epilepsy. 

Most importantly, keep in mind that the prolonged use of most the strongest sleeping pills leads to addiction. One of the solutions to this problem is regular contact between the doctor and the patient taking benzodiazepines because this ensures the medication is monitored. The new use of benzodiazepines is to control withdrawal symptoms in people who are addicted to alcohol and opioids.

One of the biggest risks of using sleeping pills is overdose. A benzodiazepine or barbiturate overdose occurs mostly in combination with other central nervous system depressants (opiates/opioids, other barbiturates, alcohol, etc.). The symptoms of an overdose include the following:

  • Drowsiness
  • Ataxia (impaired coordination)
  • Dysarthria (impaired speech)
  • Nystagmus (rapid, involuntary eye movements)
  • Areflexia (delayed or missing reflexes)
  • Apnea (respiratory arrest)
  • Loss of muscle tone
  • Hypotension (low blood pressure)
  • Benzodiazepine-induced cardio-respiratory depression (suppression of cardiac activity and breathing)
  • Barbiturate-induced respiratory depression (respiratory depression or arrest)
  • Convulsions due to barbiturates
  • Coma
  • Death

What Are Most Sleeping Pills’ Side Effects?

The effects of sleeping pills depend on the substance itself, the amount of the active ingredient present, the time of administration, and the duration of use. 

This type of medication can help a person feel more at ease—improving feelings of nervousness and anxiety. However, the user may subsequently develop feelings of indifference or begin having problems concentrating. Other annoying side effects may occur, such as headache, extreme fatigue, a feeling of emptiness, drowsiness, or melancholy. And some sleeping pills can decrease one’s libido. 

Below, we’ve listed the four most common side effects of prescribed sleeping pills:

Constant Daytime Sleepiness

Most of the people who take a sleeping pill for the first time report having severe drowsiness the next day. It’s often accompanied by difficulty concentrating, confusion, and delayed reactions. The body manages to adapt to such conditions, and over time the brain successfully dulls this feeling of drowsiness. Even so, this doesn’t mean that the side effect has been overcome. 

Hallucinations and Nightmares

Blocking certain brain centers under the influence of some common sleeping pills can help certain types of sleep problems, such as difficulty falling asleep (i.e., classic the insomnia definition). However, it can trigger others. Long-term use of sleeping pills leads to an increase in complaints of short daily hallucinations or a restless sleep accompanied by nightmares.

Exacerbation of Sleep Apnea

For people whose sleep problems are triggered by sleep apnea, taking sleeping pills can make both problems worse. Sleep apnea is provoked by blocking the airways during sleep, and the sedative effect of some notably strong sleeping pills can further weaken muscle tone and worsen the symptoms of sleep apnea.

Increased Risk of Dementia

Many studies in recent years have linked excessive use of sleeping pills to an increased risk of permanent brain degeneration and the development of various forms of dementia, including Alzheimer’s disease. This type of medication is considered to be a risk factor when used for more than three months. 

Some of the long-term effects of sleeping pills may also include physical signs such as dry mouth, nausea, headache, vision problems, anterograde amnesia, gastrointestinal disorders, skin issues, and irregular menstruation in women.

All of these side effects can be considered a source of broad public concern. After all, more than 4% of people over the age of 20 use these medications worldwide. 

Some of the more specific sleep aid side effects may be the following:

  • A short-term feeling of euphoria
  • Difficulties in speech and breathing, fatigue, disorientation, and lack of coordination because these medications slow the normal functioning of the brain
  • Impaired short-term memory, judgment, and coordination
  • Irritability, paranoia, or suicidal ideation and thoughts
  • Some people have a paradoxical reaction and may become agitated or aggressive

Are Sleeping Pills Bad for You?

How Do Sleeping Pills Work - Are they bad

It’s common for a person to rapidly develop a tolerance to sleeping pills and tranquilizers. The drugs lose their sleeping effects after only two weeks at the same dosage, and after four months, they no longer affect anxiety. Because of this, people who use them regularly need to increase their dose in an attempt to achieve the same initial impact.

The most pronounced symptom of psychological dependence is an overwhelming desire for use. This can continue for months after discontinuation of the more dangerous sleeping pills, especially if the patient hasn’t undergone any addiction treatment.

As with other drugs and alcohol, the user most often doesn’t realize that he or she is avoiding deeper problems. The primary reason a patient uses sleeping pills and tranquilizers is because they want to escape from their difficulties—and this makes the risk of addiction particularly high. 

Benzodiazepines and barbiturates should not be taken as sleeping aids during pregnancy or while breastfeeding, even though these periods can be marked with insomnia. It’s known that a large number of their active ingredients are passed to the fetus or into the breastmilk, which can damage the baby’s health.

Sleeping pills can damage multiple systems and organs in the body. More specifically, they produce lesions, which can occur with different frequency and severity in different people, making these side effects difficult to predict.

Going off a Sleeping Aid

A person who wants to stop after long-term use of benzodiazepines will face a difficult task. The initial problem might return in full force (rebound syndrome). Withdrawal symptoms such as headache, sweating, severe anxiety, tremor, nausea, sleep problems, and more will also occur. And finally, some people become very vulnerable, aggressive, or depressed when they stop using the pills. 

When it isn’t a simple over the counter sleep aid, discontinuing the use of many sleeping pills without medical attention can be very dangerous. The withdrawal period usually lasts for several weeks, but some people continue to suffer from several symptoms over a long period. Treatment depends on how large the dose of the drug was, the duration of use, and the patient’s psychological and physiological state.

Using a Natural Sleep Aid as a Safe Alternative to Sleeping Pills

The good news is that there are some natural sleep remedies you can get without a prescription or dangerous side effects. These natural alternatives to the potentially harmful and addictive sleeping pills can be your best choice for a good night’s sleep. What’s more, they’re also safe sleeping aids for kids.   

Melatonin

Since we mentioned this remedy previously, we’ll add only to be careful when taking it as a dietary supplement. Too much of it can do you more harm than good. Instead of using artificial sources of melatonin, you can obtain it naturally from foods like nuts and cherries. However, in the case of melatonin, the side effects are not so pronounced. Therefore, in capsules, it’s considered to be one of the better, safe sleeping pills.

Cherries

This beautiful fruit not only tastes great, it’s an excellent natural source of melatonin. Besides, cherries are rich in antioxidants and fiber, so they’re great for eating before bed, no matter how long you sleep each night.

L-tryptophan

L-tryptophan is an amino acid commonly associated with turkey meat. It’s key to the production of serotonin. Serotonin is a chemical substance that regulates mood, a sense of well-being, and health. Serotonin is an effective, natural sleeping aid—more serotonin means faster and more comfortable sleep. Since the body doesn’t naturally produce L-tryptophan, you should get it from food. Some great sources include poultry, fish, eggs, and beef.

Valerian

Valerian is an herb grown in Europe and Asia. It may not have a pleasant smell, but people have been using it to help get better sleep since the second century. That says a lot about its properties. But don’t just trust the history books. The NCBI’s systematic review and meta-analysis verified valerian’s effectiveness as an over the counter sleeping aid. Research shows that valerian root extract taken twice a day helps menopausal women have a more restful sleep.

5-HTP

5-hydroxytryptophan is a chemical that the body can produce after acquiring L-tryptophan. 5-HTP is converted to serotonin, which can help you fall asleep faster. But drinking 5-HTP as a dietary supplement has also been shown to combat depression and the effects of fibromyalgia.

FAQs

Can sleeping pills kill you?

Yes, they can. The disadvantage of barbiturates is that they can lead to addiction after a very short period. This makes them very dangerous, carrying the risk of an overdose that can be deadly. And abruptly stopping leads to withdrawal symptoms.

In the early 20th century, scientists synthesized a barbiturate called “barbital” in the laboratory and announced it as a new substance affecting sleep. In 1956, the action of benzodiazepines was discovered. At the time, scientists thought that benzodiazepines were less dangerous than barbiturates, but later it turned out that their use also carries significant risks. These risks include the aforementioned danger of overdosing on sleeping pills, and the risk of death from doing so.

The perfect sleeping pill or the ideal sedative has not yet been discovered. However, if you are not using these medications for extended periods of time, if you follow your prescribed dose, and if you never combine alcohol with other nervous system suppressants, they will not kill you.

How long does it take for a sleeping pill to wear off?

The higher the dose, the longer it takes the body to eliminate the active ingredient, and the longer the substance acts on your system. With some benzodiazepines, complete elimination may take more than 200 hours.

A person who takes this kind of substance daily might start a new dosage while the old one hasn’t yet stopped working. As a result, the sleep medication begins to accumulate, and unpleasant side effects can occur. These include headache, fatigue, a feeling of emptiness, dizziness, and a depressed mood. Withdrawal symptoms when stopping short-acting benzodiazepines can begin 10–12 hours after the last time you took the drug, and in long-acting ones, after 1–3 days. Discontinuing use without medical advice is not recommended.

Can sleeping pills cause cancer?

A study reported that some of the sleeping pills and aids such as zolpidem, eszopiclone, temazepam, and zaleplon are associated with developing cancer, as well as early premature death. The study showed this risk in the 6%–10% of Americans who use the mentioned prescribed medications compared to those who take no sleep aids.

Can you take a sleep aid every night?

It is not recommended to take these medications every night. Sleeping pills are not the solution to the underlying problem—insomnia, chronic pain, stress, financial concerns, anxiety, etc. They can only mask the issue. Worse, their prolonged use (over two weeks) leads to addiction, and the need for higher and higher doses of their chosen sleep aid, which is hazardous.

Conclusion

Many people may not need sleep medication if they practice good sleep hygiene. This involves falling asleep at the same time, avoiding snacks after dinner, quitting afternoon coffee, avoiding screens before bedtime, etc.

However, sleeping pills are an effective means of improving sleep, targeting millions of people with chronic insomnia. However, the side effects of sleeping pills may far outweigh their high effectiveness against insomnia. And with chronic sleep problems being recognized as a socially significant problem in many countries, it becomes increasingly important to clarify the cost we pay to improve our sleep with sleeping pills.

Sleeping pills are not miracle medications. But knowing how they work can reduce the risk of developing an addiction. In this way, perhaps instead of asking, “How do sleeping pills work?” perhaps we should question how well they really help us. Don’t start taking them until you’ve tried out the best all-natural remedies. No matter what, sleeping pills should be taken only after a doctor’s decision and only for the short-term management of severe sleep disorders.

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