How does a sleeping pill work

How Sleeping Pills Work: OTC and Prescription Drugs

From dependency risks to a.m. drowsiness, not all sleep aids work alike. Which is right for you?

Time-crunched by work, play, and family, Americans are getting less sleep than ever. TV commercials promise a good night's rest that's as close as the medicine cabinet, and millions take over-the-counter and prescription aids to help them sleep.

Taken properly, sleeping pills give enormous benefit to people suffering from an inability to get restful sleep. At the same time, the rise in the use of sleep medication has been accompanied by reports of abuse and unpleasant side effects.

How do these medicines work on the brain and in the body? What are the side effects to look for -- and what about the risk of dependence? We talked to the experts to get insights into sleeping pills: everything from A to (your) Z's. If you're taking a sleep aid, or think you should, here's what you need to know.

How Sleep Aids Work

All sleep medications work on the brain to promote drowsiness. Some drugs are specially designed as sleep aids; others are medicines with sedation as a side effect.

The guide that follows includes most commonly used sleeping pills. Remember, talk to your doctor before you use a sleep aid.

Sleeping Pills for Mild Insomnia

Diphenhydramine is an over-the-counter medicine commonly taken for allergy symptoms. One of its side effects is drowsiness, and for this reason diphenhydramine is often used as a sleep aid. Many of the most popular over-the-counter sleep aids contain diphenhydramine:

  • Excedrin PM
  • Nytol
  • Tylenol PM

Diphenhydramine helps those with mild, infrequent insomnia. For someone with persistent insomnia, however, "it's not a very good drug," according to Milton Erman, MD, clinical professor of psychiatry at the University of California, San Diego. "Very little data show that it helps people get good sleep."

Diphenhydramine can also cause unwanted sleepiness in the morning, according to Susan Esther, MD, member of the board of directors of the National Sleep Foundation.

Other side effects of diphenhydramine include:

  • Difficulty urinating
  • Confusion or delirium

These occur most in people over 65, who should avoid taking diphenhydramine. Younger people shouldn't take diphenhydramine for more than two weeks, because tolerance can develop.

Common Prescription Sleep Aids

Selective Gamma-aminobutyric acid (GABA) medications are among the newest sleep medicines and include:

  • Ambien (zolpidem tartrate)
  • Ambien CR (zolpidem tartrate extended release)
  • Lunesta (eszopiclone)
  • Sonata (zaleplon)

These sleeping pills work on the GABA receptors in the brain, which help control our level of alertness or relaxation.

The selective GABA medications target only a certain type of GABA receptor, one believed to be more dedicated to promoting sleep.

"They're more rapid in onset, more selective in their action, and less prone to side effects," says Arthur Spielman, PhD, professor of psychology at the City College of the City University of New York. In most people, selective GABA medicines are metabolized completely before morning.

Because selective GABA medicines don't work on all the GABA receptors throughout the brain, "they are thought to be relatively safer" than benzodiazepines, the older drugs on which they're based, "with less addictive potential," says Esther.

However, selective GABA medicines do have potential side effects, which are usually mild and include:

  • Memory disturbances
  • Behavior changes prior to sleep
  • Hallucinations

Ambien and other medicines in this class have also been blamed for episodes of "confusional arousal" -- what most of us would call sleepwalking. In a few well-publicized cases, people drove cars or wandered away from home after taking the drugs. These cases represent only a tiny percentage of the number of people who have taken these medicines, however.

The Latest Prescription Sleep Medicine

Sleep-wake cycle modifiers:Ramelteon (Rozerem) is the newest prescription sleep medicine, and the only drug in its class. Ramelteon acts directly on the body's sleep-wake cycle, or circadian rhythm.

The sleep-wake cycle is partially controlled by a part of the brain called the hypothalamus. Ramelteon binds specifically to melatonin receptors in this "circadian clock" area of the brain, promoting sleep. "This might be good for a 'night owl' trying to get to sleep for a new job," says Esther.

Because its activity is limited to one part of the brain, ramelteon has few side effects compared to other medicines that act more generally. Its risk of physical dependence is thought to be essentially zero. However, all sleep medicines can cause psychological dependence.

Ramelteon also does not seem to have any potential for abuse, so it is not controlled like benzodiazepines and selective GABA medicines such as Ambien, Lunesta, or Sonata. So far, it has not been shown to cause hallucinations or sleepwalking.

Studies show that ramelteon works well in older adults with chronic insomnia. Because it acts on a part of the brain that controls hormones, ramelteon may affect hormone levels if taken for extended periods. This can reduce sex drive in men or make it harder for women to get pregnant.

Older Sleep Aids

Benzodiazepines are older medicines that effectively help people get to sleep, and were previously the most commonly used sleep medicines. Drugs in the benzodiazepine class include:

  • Ativan (lorazepam)
  • Halcion (triazolam)
  • Restoril (temazepam)
  • Valium (diazepam)
  • Xanax (alprazolam)

Benzodiazepines activate GABA receptors in the brain, causing sedation and relaxation and promoting sleep. Because they act on various types of GABA receptors throughout the brain, though, benzodiazepines have other effects:

  • Reduced anxiety
  • Muscle relaxation
  • Poor memory of some events while taking the drug
  • Euphoria

Benzodiazepines are only available by prescription. While they are sometimes the right medicine, benzodiazepines should be used with caution:

  • People who take benzodiazepines regularly may develop tolerance, or even a physical dependence on the drug (addiction).
  • Benzodiazepines have a relatively high potential for abuse.
  • They are not appropriate for long-term use.

"You wouldn't want to use them more than a few days," or longer in rare cases, according to Esther.

These days, physicians prescribe benzodiazepines infrequently, because newer medicines generally work as well without as much potential for abuse or dependence.

Tricyclic Antidepressants as Sleep Aids

Physicians usually prescribe tricyclic antidepressants, called TCAs, for depression or chronic pain. TCAs include:

  • Adapin (doxepin)
  • Aventyl (nortriptyline)
  • Elavil (amitriptyline)
  • Pamelor (nortriptyline)
  • Sinequan (doxepin)
  • Trazodone (desyrel)

For people with depression or chronic pain who also suffer from insomnia, TCAs may play a role in treatment. But because they act throughout the brain, tricyclic antidepressants can have pronounced side effects:

  • Blurry vision
  • Dry mouth
  • Difficulty urinating
  • Dizziness

The lower doses used for treatment of insomnia tend to reduce these effects. These medicines can be useful for "someone who has failed better agents or is anxious about the other medicines," says Erman.

Good Sleep Habits: Part of the Sleep Solution

Experts agree that while sleeping pills can be an important and necessary part of a successful sleep program, they can't be the only answer.

"Medicines can be helpful, but they shouldn't be a quick fix," says Esther. "They need to be part of a balanced plan of habits and common sense."

According to the National Sleep Foundation and others, good sleep habits should include:

  • No caffeine later in the day
  • Avoid nicotine or alcohol two to three hours before bedtime.
  • Use your bedroom only for sleeping and sex.
  • Maintain a regular sleep-wake schedule on all days, including weekends.
  • Exercise regularly but complete it several hours before bedtime.
  • Finish eating at least 2-3 hours before bedtime
  • Create a restful sleep environment by reducing noise, light, and temperature extremes with ear plugs, window blinds, an electric blanket, or air conditioner.

Sleeping Pills: The Risk of Dependence

All sleep medicines have the potential to cause dependence, according to sleep experts. Dependence means not being able to stop taking the drug without problems. Nearly always, this is a psychological dependence.

According to Erman, "If you're used to taking the drug to sleep, going without it will make you anxious, and in fact, unable to sleep"-- even though you're not physically dependent on the medicine.

If you feel you're dependent on a sleep medicine, see your doctor. They will address the problem with you. Your doctor may refer you to a sleep specialist.

Taking benzodiazepines regularly can lead to a physical tolerance and dependence, or addiction. If you've been taking these medicines for a prolonged period, do not stop abruptly. See your doctor and work out a schedule to stop taking them safely.

Types, Side Effects & Treatment

What are sleeping pills?

As the name suggests, sleeping pills help you catch some sleep. People who have sleep disorders like insomnia may take these medications to help them fall asleep. Sleeping medicines can also help you stay asleep if you’re prone to waking up in the middle of the night.

What are other names for sleeping pills?

Sleeping pills go by many names:

  • Hypnotics.
  • Sedatives.
  • Sleep aids.
  • Sleep medicine.
  • Tranquilizers.

How do sleeping pills work?

There are various types of sleeping pills. Each works differently. Some sleep aids cause drowsiness, while others silence the area of the brain that keeps you alert.

How effective are sleeping pills?

Studies show that sleeping pills aren’t that helpful in promoting a good night’s rest. Most people who take sleep aids fall asleep about eight to 20 minutes faster than those without medicine. On average, you might get an additional 35 minutes of shuteye.

Generally, sleep aids should be for short-term use. They may be most helpful if a stressful life event, such as a divorce or death in the family, is keeping you awake.

Who might need sleeping pills?

An estimated one in seven Americans have long-term insomnia. Sleep difficulties become more common as you age. Approximately one in three older people take some type of sleep medicine.

What are the types of over-the-counter (OTC) sleeping pills?

Any adult can buy OTC sleep medications at a store. OTC sleep aids often contain an antihistamine. This drug treats allergies, but it can also make you drowsy.

Some people take melatonin or valerian supplements to help them sleep. Melatonin is a hormone your body naturally produces that promotes sleep. Valerian is an herb that supposedly aids relaxation and sleep.

Although these sleep aids are easily accessible, you should check with your healthcare provider before taking them. Drugs in over-the-counter sleep aids (including supplements) can interfere with other medications or make health conditions worse.

What are the types of prescription sleeping pills?

Prescription sleeping pills are stronger than over-the-counter ones. You need a prescription from your healthcare provider to get these pills.

Types of prescription sleeping pills include:

  • Antidepressants.
  • Benzodiazepines.
  • Z-drugs (Ambien® and Lunesta®).

What are the potential side effects of sleeping pills?

Approximately eight out of 10 people experience a hangover effect the day after taking sleep medicine. They feel drowsy, have muddled thinking and experience dizziness or balance problems. These daytime effects can negatively impact your ability to drive, work, go to school and complete daily tasks.

Over-the-counter and prescription sleeping pills (and supplements) can cause these side effects:

  • Constipation or diarrhea.
  • Dry mouth.
  • Headaches.
  • Muscle weakness.
  • Digestive problems, including gas, heartburn and nausea.

What are the potential risks or complications of sleeping pills?

When you take sleeping medicines night after night, your body may start to depend on them. When you stop the medicine, your insomnia may come back worse than before. This effect is called rebound insomnia.

If you’ve used sleep aids for a long time, talk to your healthcare provider about how to stop safely. It may take months to stop taking the pills.

You also shouldn’t mix sleep aids with other sedatives or alcohol. There’s a possibility of overdosing.

What are the potential risks or complications of prescription sleeping pills?

Some prescription sleep medicines may bring on parasomnia. This disruptive sleep disorder can cause dangerous behaviors while you’re still mostly asleep. People who take Z-drugs, in particular, may sleepwalk or eat, take medications, talk or even drive, all while unaware that they’re doing these things. You may appear to be awake, but your brain is not fully alert. Most people don’t remember doing these things after they wake up.

Benzodiazepines can be addictive and lead to substance abuse. To lower this risk, healthcare providers only prescribe these sleeping pills for short-term use. You’re more likely to get a prescription for Z-drugs instead.

Are sleeping pills safe during pregnancy?

Any medication you take while pregnant or breastfeeding passes to the baby. Check with your healthcare provider before taking any over-the-counter sleeping pills or supplements. For extreme insomnia, a provider may prescribe a short-term sleep aid.

Are sleeping pills safe for children?

Some parents give over-the-counter antihistamine medications to children to help them sleep. These medicines aren’t approved for sleep purposes. There’s a risk of overdosing a child.

Don’t give a child supplements like melatonin. There’s no research on their safety in children.

Currently, there are no prescription sleep medicines available for children. Changing a child’s sleep behaviors is often the best way to improve sleep.

How can I sleep better without sleeping pills?

Cognitive behavioral therapy (CBT) is an effective tool for improving sleep and curing insomnia. Behavioral changes often improve sleep without the need for medications.

You may want to:

  • Avoid large meals and alcohol before bed.
  • Cut back on caffeine, including coffee, sodas and chocolate, throughout the day and especially before bedtime.
  • Quit smoking.
  • Relax with soothing music, a good book or meditation.
  • Shut off electronic devices at least 30 minutes before bedtime.
  • Stay physically active during the day. Try to get outside, if possible.
  • Stick to a sleep schedule (same bedtime and wake-up time) even on weekends.
  • Turn your bedroom into a dark, quiet and cool sanctuary.

When should I contact my healthcare provider?

You should contact your healthcare provider if you are taking sleeping pills and experience:

  • Chronic fatigue.
  • Confusion or memory issues.
  • Parasomnia behaviors.
  • Problems focusing or completing tasks like driving.
  • Severe upset stomach.

A note from Cleveland Clinic

Staring at the clock or tossing and turning is no way to spend your nights. Still, you should talk to your healthcare provider before trying an over-the-counter sleep aid. A prescription sleeping pill may be a better choice. Often, nondrug treatments and behavioral changes are all you need for improved slumber. Your healthcare provider can figure out what’s causing your insomnia and suggest the best plan to help you rest easier.

Sleeping Pill Addiction: Why Sleep Pills Are Unsafe

In today's world, almost everyone has occasional sleep problems. To eliminate them, doctors prescribe medication, but if the recommendations of medical experts are not followed correctly, addiction to sleeping pills can appear. But why does it occur and how to avoid it?

Sleeping pills: characteristics and uses

Sleeping pills are psychoactive drugs that help fight insomnia and improve the quality of sleep. They depress the central nervous system, as a result of which a person feels relaxed and it becomes easier for him to fall asleep. Most sleeping pills are available by prescription, but there are also over-the-counter drugs.

The market for insomnia medicines offers a wide range of both strong sleeping pills and herbal remedies with a sedative effect.

Typically, sleeping pills are prescribed for a short period of time, no more than 14 days. These drugs are fast-acting and are used only symptomatically, that is, they are used as needed. Long-term use of the medications in question can lead to addiction and cause a number of side effects.

When does dependence on sleeping pills occur?

When using sleeping pills for more than 2 weeks, physical and psychological addiction to them occurs. The first is that the dose of the drug prescribed by the doctor ceases to help a person fall asleep and he begins to increase it on his own. The second implies that a person assures himself that without a pill he will not be able to go to sleep and begins to believe in it.

How do you know if you are addicted to sleeping pills?

To do this, you can familiarize yourself with the list of the following symptoms, and the appearance of at least one of them in the patient will indicate addiction.

The main signs of dependence on sleeping pills:

  • desire to take pills before each bedtime;
  • frequent trips to the doctor for sleeping pills prescriptions or continuous purchase of over-the-counter drugs;
  • long-term daily use of sleep tablets;
  • objection and irritation in response to the recommendation of relatives to stop drinking pills for insomnia;
  • memory impairment, fatigue, apathy;
  • occurrence of withdrawal syndrome when trying to stop taking sleeping pills;
  • change in habits, behavior and possible decrease in working capacity.

However, addiction and addiction must be distinguished. Habituation means that the human body gets used to a certain dosage of the drug and stops responding to it, as a result of which a person cannot fall asleep even when taking sleeping pills. Therefore, the patient begins to arbitrarily increase the dosage of the medication, and this is categorically not recommended.

Addiction to sleeping pills is quite difficult to get rid of. So, if a person took sleeping pills for a long time, and then abruptly refused them, he will experience a withdrawal syndrome and exacerbation of insomnia.

The severity of the hypnotic withdrawal syndrome in different people can vary depending on a number of factors, such as the severity and duration of addiction. Some sleep medication withdrawal symptoms can be life-threatening if not treated promptly.

Sleeping pill withdrawal syndrome may include:

  • sleep problems, insomnia;
  • body spasms;
  • convulsions;
  • anxiety;
  • increased anxiety;
  • irritability;
  • craving for sleeping pills;
  • shivering (tremor) and circulatory problems;
  • confusion;
  • hallucinations;
  • increased sweating;
  • increased heart rate;
  • nausea, vomiting.

This is not a complete list of symptoms. In each individual case, the number of withdrawal symptoms present may differ.

A person who cannot fall asleep on his own without taking sleeping pills and takes sleep pills for more than 2 weeks, and then decides to stop them completely, as a result experiences worsening insomnia. That is why doctors treat this addiction by gradually reducing the dose of drugs.

Most patients begin to show signs of withdrawal hours or days after stopping the drug. Their disappearance is observed after about 1-2 weeks. However, it is known that psychological symptoms can persist even for a month. These include insomnia, anxiety, irritability, agitation, mood swings, and poor concentration.

Please note! As a result of taking pills for insomnia, changes in the breathing process may occur, namely changes in the frequency and duration of inhalations and exhalations. This feature of the drugs is dangerous for people with asthma and chronic lung diseases. Therefore, before taking these medications, be sure to consult your doctor.

How exactly do sleeping pills affect a person?

The mechanism of action of hypnotics

Hypnotics enhance and concentrate the processes of inhibition in the cerebral cortex, and also weaken the processes of excitation in the central nervous system (CNS). Such drugs inhibit the transmission of nerve impulses along the polysynaptic reflex arc (the path from the receptor to the spinal cord). In addition, they also increase the action of the inhibitory neurotransmitter GABA (gamma-aminobutyric acid) and increase the content of GABA and serotonin (a neurotransmitter) in the midbrain and hypothalamus.

In other words, sleeping pills act as central nervous system depressants, and the strength of their action depends on the dosage level. A small amount of the drug usually has a moderately hypnotic effect, with a slightly larger dosage, a pleasant "numbness" is caused. "Numbness" refers to the sleep-like state for which some people take sleeping pills. However, taking large doses of sleeping pills is not recommended, as this can lead to negative consequences.

Overdose of insomnia medications can lead to blackouts, feelings of depression, depressed mood, slow reactions, and a host of other side effects. An overdose of sleeping pills is not safe for life, so these drugs should be taken only according to the recommendations of the attending physician.

Please note! After taking any sleeping pills, it is forbidden to drive a car, start working with mechanisms, and even engage in simple tasks that require concentration, such as cooking.

Only with the correct, and, most importantly, short-term intake of sleep tablets, they will have the desired effect, namely, help to fall asleep faster and improve the quality of sleep.

Before choosing a sleeping pill, you should understand what sleeping pills are and how they differ from each other.

Types of sleeping pills: pharmaceutical classification

Currently, 3 groups of sleeping pills are distinguished in pharmacy: benzodiazepine derivatives, barbituric acid derivatives (barbiturates) and cyclopyrrolone derivatives, as well as other chemical groups.

Benzodiazepine derivatives

These drugs enhance the action of the GABA neurotransmitter (gamma-aminobutyric acid), which slows down brain activity, thereby helping people fall asleep faster and rest longer. Due to the sedative, muscle relaxant (muscle relaxation) and hypnotic effects, benzodiazepines are widely used to improve sleep and treat nervous disorders.

Gidazepam IC is a prominent representative of benzodiazepine derivatives. This is a prescription drug that works when taken short-term for up to 2 weeks.

Long-term use of benzodiazepines can lead to a number of side effects, among which there is a reduction in the duration of deep sleep and gradual addiction to the drug, due to which people can independently increase the dose, which is unsafe for health.

Barbituric acid derivatives

They have a depressant effect on the central nervous system of a person and thus help him fall asleep faster. Currently, barbiturates hypnotics are not used as widely as they used to be. The reason for this is addiction to barbiturates and a large list of side effects.

Signs of barbiturate abuse:

  • erratic behavior, mood swings;
  • restlessness, anxiety;
  • difficulty concentrating;
  • falsification of prescriptions for the purchase of the drug;
  • the occurrence of a depressive state;
  • brief memory loss;
  • redness, inflammation of the skin, rash;
  • aggressive behavior.

The most popular drug from the barboval group is Barboval, and the most dangerous and not recommended for use is Phenobarbital.

Derivatives of cyclopyrrolone and other chemical groups

This includes all other hypnotics not classified as benzodiazepine derivatives and preparations from the barbiturate group. Their main active ingredients may be:

  • zopiclone;
  • methaqualone;
  • zolpidem;
  • doxylamine;
  • bromisated;
  • vita-melatonin.

These drugs act similarly to benzodiazepine derivatives by increasing the level of the neurotransmitter GABA (gamma-aminobutyric acid). This, in turn, reduces brain activity, causing drowsiness.

Instead of acting on a few receptors in the brain like benzodiazepines, the drugs in question only act on a few of them and therefore cause fewer side effects. However, there have been cases when taking these drugs led to memory loss and fatigue the next day.

Name of hypnotics in this group:

  • Sondox;
  • Donormil;
  • Vita-melatonin.

Drinking derivatives of cyclopyrrolone and other chemical groups in case of sleep problems should be no more than 14 days and strictly according to the doctor's prescription.

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How to get rid of addiction to sleeping pills?

Overcoming addiction to drugs can be a very difficult task, both physically and mentally. It takes a lot of patience and determination to get through difficult phases without medication.

If you feel addicted or addicted to sleeping pills, you should contact your healthcare professional immediately. It is the doctor who will be able to find a way out of this situation and help the patient overcome addiction. In addition, psychological or therapeutic support can help in getting rid of addiction.

Not everyone notices addiction symptoms when taking medication. That is why it is very important to realize that you are addicted to a drug or may already have an addiction.

There is still no precise definition of the amount of time required to overcome addiction to sleeping pills. On average, it takes 2 to 4 weeks to overcome addiction to sleeping pills.

Take care of yourself and use any medicine strictly as prescribed by your doctor.

In addition to sleeping pills, there are many other drugs that help you fall asleep faster, and one of them is glycine. Learn about the most obscure properties of the popular drug in our new article on the benefits of glycine and the scientific evidence for its effectiveness.

Do you know that some of our dreams can be dangerous to health, and their frequent occurrence can even lead to nervous breakdowns? What are these dreams? Read the article about why we sleep and what dreams are considered the most unsafe.

Is there a link between sleep and weight loss? Scientists, answering this question, came to unexpected conclusions. And our new material is devoted specifically to the topic of the influence of the amount of nightly rest on the fight against excess weight.

apteka24. ua is the first online pharmacy you can trust.

This editorial has been verified for accuracy by family doctor Medical Plaza Medical Center - Borisova Tatyana Ivanovna.


Addiction to Sleeping Pills / Addiction Center

Using medication: What can help when trying to stop taking sleeping pills and sedatives? / NCBI

What Is Sleeping Pill Withdrawal? /Addiction Center

Understanding the Side Effects of Sleeping Pills / WebMed

Withdrawal Status / WHO


treatment methods can only be carried out by your doctor! Self-medication may not be safe for your health. is not responsible for possible negative consequences resulting from the use of information posted on the site by users of

How do sleeping pills work and what is insomnia

Science has 82 types of sleep disorders, including such exotic as stopping breathing during sleep - "apnea". The study of such disorders is carried out by a special science of sleep - somnology. After examining and taking anamnesis, somnologists can prescribe special sleeping pills, the principle of which we will tell you about.

Anastasia Bliznetsova

Perhaps everyone in this life has suffered from insomnia. On the eve of a holiday, before a difficult exam or interview, and sometimes just "because of the full moon." Everyone struggles with the inability to fall asleep in different ways - someone drinks sleeping pills, someone drinks a glass of cognac at night, someone herbal tea, and some try to ensure a calm and quick falling asleep by following simple rules - ventilate the room before going to bed and drink a glass warm milk. All this is effective in its own way, but it does not help everyone. And although knowledge of the mechanisms of sleep in itself does not save from insomnia, nevertheless, this topic is close to everyone.

Do not self-medicate! In our articles, we collect the latest scientific data and the opinions of authoritative health experts. But remember: only a doctor can diagnose and prescribe treatment.

What is sleep

Sleep is a specific state of the nervous system, which manifests itself in the interruption of human ties with the outside world. As Leonardo da Vinci said about sleep, “sleep is a desired state, which, once achieved, disappears for consciousness.”

Little is known about sleep. The mechanisms of the brain that cause or regulate sleep and awakening are relatively well studied, but, for example, to the question “why sleep at all?” There is no definite answer yet, although there are many hypotheses. For example, some believe that unnecessary neural connections are destroyed during sleep, saving the brain from storing meaningless information. But so far it is only obvious that sleep is a biological human need: everyone has heard about the terrible torture of insomnia, and there is no doubt that sleep is necessary.

Falling asleep

In the nervous system, activity is regulated by two types of neurons - excitatory and inhibitory. They, respectively, release either excitatory or inhibitory neurotransmitters. The former excite the activity of the postsynaptic neuron, the latter suppress it. Sleep pills have their hypnotic effect on the body due to the influence of inhibitory mediators on the brain structure, which is responsible for "tuning" the nervous system to active work (it is called the reticular activating system).

The main mediator that induces sleep is serotonin. Under its influence, neurons of a certain part of the brain are excited, which in turn activate neurons that release inhibitory neurotransmitters. Norepinephrine, on the contrary, is responsible for awakening. The subtleties of the interaction of brain structures with serotonin and norepinephrine have not been studied, but it is known for sure that they take some part in the regulation of sleep and wakefulness.

Further, it is obvious that if the inhibitory mediators are not enough to extinguish the activity of the desired part of the brain, falling asleep does not occur. As an illustration, everyone can remember that we usually cannot fall asleep when our nervous system is in an excited state - this is manifested in the fact that we cannot get rid of obsessive thoughts, constantly tossing and turning - we are either hot, or cold, or uncomfortable, we are annoyed by any rustle, etc.


According to various sources, from 25 to 50 percent of the world's population suffers from insomnia, and 95 percent have experienced it at least once in their lives. Interestingly, insomnia indirectly affects even mortality - people with sleep disorders are 2.5 times more likely to get into car accidents. Insomnia is defined as a decrease in the amount and quality of sleep (and sometimes a change in the timing of sleep).

Everything is clear with quantity, but about quality (this is when you slept for twelve hours, but still “did not get enough sleep”) must be said separately. Research shows that normal sleep always has several phases - namely five. During each phase, the nature and amplitude of the waves of electrical activity of the brain on the encephalogram changes - according to these signs they are divided. In fact, the phase of sleep determines its depth: the first phase is the most superficial sleep, the fifth is the deepest. The fifth phase is also called REM sleep, or REM sleep, and the first four phases are therefore called non-REM sleep. To avoid confusion, I would like to emphasize that it is REM sleep that is the deepest and, although breathing and heartbeat are speeded up, the skeletal muscles of the sleeper are completely relaxed. Almost all people awakened during this phase say they have had dreams.

So, it is known that the amount of REM and non-REM sleep must be balanced in a certain way. If any phases in a dream are missing, or they are very short, a person does not receive the necessary rest in a dream. For example, in one experiment, rats that were woken up whenever they entered REM sleep very soon went into nervous exhaustion and then death.

Although everyone's need for sleep is different, everyone feels the amount and quality of sleep subjectively, assessing whether he "gets enough sleep" or not. Some (Napoleon Bonaparte is said to be one of these) feel cheerful after four hours of sleep, and some (including the author) even after eight hours with difficulty force themselves to wake up. And, of course, there are "owls" and "larks".

"For ease of reference" insomnia is classified according to the period in which difficulties with sleep appear - that is, there are presomnic disorders (problems with falling asleep), intrasomnic (frequent awakenings) and postsomnic (early waking up, daytime sleepiness, decreased performance in the morning).

Sleeping pills

The mechanism of action of sleeping pills is very complex and, like sleep itself, has not been studied enough, but what is known is quite enough for a general acquaintance with their action. Today, a well-known inhibitory neurotransmitter is gamma-aminobutyric acid (GABA). For the first time, gamma-aminobutyric acid was discovered in the brain by E. Roberts and S. Frenkel in 1950 year. But its main property - the ability to reduce the activity of the nervous system - was discovered in 1963 by the English scientist K. Krnevich. Thus, to create a sleeping pill means either to increase the effect of GABA on neurons, or to increase its amount in the nervous system.


The very first sleeping pills were discovered experimentally long before the existence of GABA was known. These were barbiturates (for example, veronal).

The mechanism of their action of these hypnotic drugs was already clarified during studies of the mechanisms of inhibition in the nervous system - it was found that the postsynaptic receptors of neurons responsible for inhibition are sensitive not only to GABA, but to varying degrees and to some other substances - in particular, to derivatives of barbiturates. Barbiturates, by attaching to such receptors, lengthen the time of GABA exposure, and also enhance this effect.

However, due to the fact that receptors sensitive to barbiturates are responsible not only for sleeping pills, but also for anticonvulsant and relaxing effects, these sleeping pills have a very pronounced side effect on the body (some drugs are even used in the treatment of epilepsy ). In addition, with prolonged use of them as sleeping pills, the most important phase of REM sleep is shortened, that is, sleep is different from normal (in fact, sleep after such sleeping pills is only a physical state similar to sleep). Another trouble is the development of drug dependence with constant use for 1-3 months (and addiction develops in general in two weeks). Today, barbiturates are practically not used as sleeping pills.


After the discovery of GABA, an attempt was made to use the acid itself in its pure form as a sleeping pill (gamma-aminobutyric acid is a white powder soluble in water). However, it turned out that GABA practically does not get from the blood to the brain and, accordingly, the drug is ineffective, and has no effect on the human body.


In further studies, it was found that some postsynaptic disorders are sensitive to benzodiazepine derivatives, and in the 60s of the XX century, the second generation of sleeping pills appeared. Benzodiazepines also indirectly (by attaching to "their" receptors) enhance the action of GABA. Since the receptors sensitive to these drugs are mainly responsible for the hypnotic effect, they have less side effects on the body than barbiturates. But some of the problems still remained: addiction, withdrawal syndrome, the need to constantly increase the dosage. In addition, although the REM phase is not shortened, the phase ratio does not correspond to physiological sleep, and heavy waking and daytime sleepiness limit the use of these hypnotics (in particular, you should not drive a car during the treatment period).

Latest generation

Further progress in the treatment of insomnia was marked by the discovery of several different types of receptors. It turned out that by selectively influencing some of them, it is possible to very accurately influence the braking mechanisms. This is how selective drugs appeared - the latest generation of sleeping pills. These are derivatives of imidazoperidine (ivadal) and cyclopyrrolone (imovan). The number of side effects they have is minimal, and the distribution of sleep phases is natural. True, the ideal has not yet been achieved - with prolonged use, there is still a danger of developing addiction. It is important to know that the effect of all sleeping pills is enhanced by alcohol (and vice versa, the effect of alcohol is potentiated by sleeping pills).


Histamine is one of the most important mediators of wakefulness, so blocking histamine receptors (that is, receptors for neurons that are excited by histamine) also produces a hypnotic effect.

Drugs that block histamine receptors are called antihistamines. Their main task is to treat allergies, however, some pills can act as sleeping pills - this is considered a harmful additional property. However, some of these drugs (for example, diphenhydramine, pipolfen, donormil) have such a strong effect that they are considered full-fledged sleeping pills.

Fortunately, modern antihistamines are almost completely devoid of hypnotic effects, since they do not pass through the blood-brain barrier (the defense mechanism of the brain) and do not affect the nervous system. Therefore, they can be taken constantly, without fear that during the flowering period of some next plant to which your body is hypersensitive, you will have to choose between sneezing and sleeping at work.


Melatonin is a neurohormone that is synthesized in our body from serotonin in the pineal gland, retina and intestines. The enzymes responsible for converting serotonin to melatonin are inhibited by light, so melatonin production is light dependent.

In humans, about 70% of the daily melatonin production occurs at night. Melatonin is somehow involved in the regulation of human circadian (daily) rhythms, that is, the rhythms of sleep and wakefulness. In particular, under the influence of melatonin, the amount of GABA in the nervous system increases.

Melatonin is considered a mild sleeping pill and is recommended for minor sleep disturbances, including for faster adaptation when flying to other time zones. It also accelerates the adaptation of the body in a stressful situation and exhibits immunostimulating and antioxidant properties.

The ideal sleeping pill

In the light of the above, it becomes clear that very often the problem with insomnia is the usual overexcitation, so the recommendations to “read at night” and “drink valerian” (which, by the way, also acts as a sleeping pill) can be effective . However, the scale of the production of sleeping pills indicates that it still has little effect on anyone.

The goal of any pharmacological research into sleeping pills is, of course, to find the perfect sleeping pill. In dreams, it is seen as follows: it acts quickly, does not lose effectiveness with prolonged use, is safe in case of overdose, does not have any effects other than sleeping pills, and also does not affect awakening, does not disturb sleep phases and does not change their normal ratio, does not cause disorders of the nervous system. system and problems upon termination of use.

So far, such a medicine has not yet been created, and it is unlikely that it will appear in the near future, although even now the first sleeping pills seem to be downright poison compared to modern ones.

Poisoning by sleeping pills

Sleeping pills are sold by prescription in our pharmacies.

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