Sleeping Pills

Sleeping pills – this is a short name for a fairly large and very heterogeneous group of drugs that contribute to the onset and maintenance of sleep of sufficient duration and depth. The full name of this group of drugs is hypnotics.

Currently, there is a wide range of drugs with a hypnotic effect, but in most cases this is their additional or secondary, but not the main effect. To the group of hypnotics the same drugs include only such drugs, for which this action is the main one.

Soporific drugs are referred to the drugs acting on the central nervous system, because their effect is realized due to activation or suppression of the production of biologically active substances (neurotransmitters), as well as changes in the work of certain receptors of neurons.

The concept of the phases of sleep and its possible violations

To understand what the action of hypnotic drugs is directed at, it is necessary to know the structure of sleep and the types of its possible disturbances.

Violations can be triggered by various causes, such as:

• Violation of the rhythm of sleep-wakefulness, for example, during night duty;
• Psychological overstrain, especially in the evening hours;
• Mental illness (eg, depression, anxiety disorder, schizophrenia, etc.);
• Taking medications that activate the central nervous system (caffeine, theophylline, etc.);
• Somatic diseases (hypertension, pain, cough, etc.);
• Various syndromes that disturb sleep (eg, apnea, restless legs syndrome).

In addition, sleep disorders can be caused by unknown causes, and in this case they are called idiopathic. Long-term courses of using hypnotic drugs are shown precisely with idiopathic sleep disorders. If the dream is broken due to any of the above reasons, then it is necessary first of all to treat the underlying disease, and to apply hypnotic drugs sporadically, only if necessary.

Sleep disorders are classified into the following species, depending on which particular component of the carotid structure is affected:

• Presomantic disorders – only the process of falling asleep is disturbed;
• Intrasomal disorders – the depth of sleep is disturbed, the person sleeps superficially and often wakes up;
• Postmodern disorders – a person wakes up early and can not fall asleep any more, and during the whole day he is troubled by drowsiness.

Sleeping drugs can eliminate all types of sleep disorders, promoting normal sleep and providing sufficient depth and duration of the sleepy period. However, not all drugs can influence all the variants of sleep disorders. A fairly large proportion of sleeping pills normalizes only one or two kinds of sleep disorders. Therefore, before choosing and using a hypnotic drug, one should identify the type of sleep disorders and choose a medicine whose action is aimed at arresting this particular disorder.

Classification of hypnotics

At present, clinical practice uses anatomo-therapy-chemical (ATX) drug classification, which simultaneously takes into account both the structure of the active substance, and the anatomical structures to which the drug acts and the spectrum of its therapeutic activity. Thanks to the consideration of three parameters at once, it is the classification of ATC that is most complete and convenient for practical use, since it allows the physician to orientate in different properties of the drug.

So, at present, according to the ATC classification, all sleeping pills are divided into the following varieties:

1. Barbiturates:

• Amobarbital;
• Aprobarbital;
• Butobarbital;
• Vinbarbital;
• Vinylbital;
• Heckobarbital;
• Heptabarbital;
• Methohexital;
• Proxybarbal;
• Reposal;
• Secobarbital;
• Talbutal;
• Thiopental sodium;
• Phenobarbital;
• Cyclobarbital;
• Ethylbobital.

2. Barbiturates in combination with other drugs:

• Bellataminal (phenobarbital + ergotamine + alkaloids of belladonna);
• Reladorm (diazepam + cyclobarbital).

3. Benzodiazepine derivatives:

• Brotisolam;
• Doxefiazepam;
• Kvazepam;
• Loprazolam;
• Lormetazepam;
• Midazolam;
• Nitrazepam;
• Oxazepam;
• Temazepam;
• Triazolam;
• Flunitrazepam;
• Flurazepam;
• Cinolazepam;
• Estazolam.

4. Drugs that have similar effects with benzazepepines and are GABA-receptor agonists (Z-preparations):

• Zopiclone;
• Zolpidem;
• Zaleplon.

5. Aldehydes and their derivatives:

• Chloral hydrate;
• Chloralodol;
• Acetylglycinamide chloral hydrate;
• Dichloro-phenazone;
• Paraldehyde.

6. Piperidinedinedione derivatives:

• Glutetimide;
• Metiprilone;
• Pyrithildione;
• Thalidomide.

7. Melatonin receptor agonists:

• Ramelteon;
• Taximelteon;
• Melatonin.

8. Blockers of histamine receptors:

• Diphenhydramine;
• Doxylamine.

9. The orexin receptor agonist:

• Suvoreksant.

10. Other sleeping pills:

• Bromizoval;
• Valnoktamide;
• Hexapropimate;
• Clomethiazole;
• Methaqualone;
• Methylpeptinol;
• Niaprazine;
• Propiomazine;
• Triclofos;
• Ethochlorvinol.

In this classification, for convenience of search, only international names (INN) of preparations are given, which are usually indicated in the instructions for use as active substances. The same active substance can be contained in several synonyms, which have exactly the same effect.

Most barbiturates and benzodiazepines listed in the classification are currently used only in rare cases in a specific hospital practice, that is, in hospitals. For outpatient use, only a few hypnotic barbiturates and benzodiazepines are actually used. Most often barbiturates use phenobarbital, and from benzodiazepines – flunitrazepam, nitrazepam and some others. In addition, the above classification lists all the hypnotic drugs used in different countries, so their list is much broader than that available in Russia, Ukraine, Belarus, Moldova, etc.

In addition to the ATC classification, all sleeping pills are divided into two large groups – with narcotic and non-narcotic type of action. Drugs with a narcotic type of action include all barbiturates and aldehydes. All other sleeping pills have a non-narcotic type of action. The subcategory of sleeping pills in a category with a narcotic and non-narcotic type of action is very important, since the first are the fastest to get addictive.

Also, practicing physicians widely use the classification of hypnotics according to the duration of their action, according to which they allocate short, medium and long-acting drugs. Sleeping pills of different duration of action are given in the table.

Classification of hypnotics according to the duration of the action is of great practical importance, since it allows selecting a drug for each particular person, providing the necessary effects. For example, if a person is only disturbed by the process of falling asleep, then short-acting hypnotics are recommended, as they will ensure a quick immersion in sleep, and will not cause morning fatigue and breakdown. In a superficial sleep with frequent awakenings, it is recommended to use sleeping pills of medium duration, since they will provide a good, high quality, deep sleep, which in the morning will give the person a feeling that he has perfectly rested. If a person wakes up early in the morning and can not fall asleep any more, it is necessary to use long-acting sleeping pills that will ensure a sufficient duration of sleep, eliminating an early awakening.

Sleeping effect of drugs (hypnotic effect)

In general, the mechanism of action of all hypnotic drugs reduces to a decrease in the intensity of excitation processes in the central nervous system and increased inhibition. The ratio of inhibition of excitation and enhancement of inhibition in different drugs is different, which causes differences in the duration and nature of their action.

So, hypnotic drugs of short action preferentially suppress excitation processes, as a result of which inhibition naturally begins to prevail, and the person falls asleep. This mechanism of action is optimal for eliminating difficulties in falling asleep when it is hard for a person to fall asleep, but when this happens, he sleeps normally – deeply and without frequent awakenings. The undoubted advantage of preparations of this type of action is that they do not disturb the normal structure of sleep, without causing a change in the duration and correlation of its phases. As a result, after taking a somnolent short action in the morning, a person wakes up to sleep and rested well.

Sleeping drugs of medium duration have the ability not only to reduce the excitement, but also to increase the inhibition slightly, so that their effect lasts longer and allows to influence not only the asleep process, but also the quality of sleep. These medicines well eliminate the problem of superficial sleep and frequent nocturnal awakenings, which allows a person to sleep well and not feel broken in the morning.

Sleeping drugs long-term action simultaneously inhibit excitation and dramatically increase inhibition, which explains their long-term effect. These drugs are effective for any sleep disturbance – and with prolonged sleep, and a shallow dive into sleep, and with frequent nocturnal or early morning awakenings.

Otherwise, hypnotics of each particular group have their own mechanism of action, different from others.

Thus, barbiturates cause sleep even with severe insomnia, but change the normal structure of sleep, so that a person can see very bright dreams, nightmares, etc. Therefore, such a dream is not complete. The effect of barbiturates is realized by their interaction with GABA receptors, which become more sensitive to their mediator – GABA (gamma-aminobutyric acid). Because of the longer action of GABA on the structure of the brain, excitation is suppressed and braking is activated.

Benzodiazepines also affect GABA receptors, but are safer than barbiturates because they do not cause serious side effects, and the dependence is much more.

Benzodiazepine-like Z-drugs (Zopiclone, Zolpidem, Zaleplon) also exert their effects through the effect on GABA receptors. However, unlike benzodiazepines and barbiturates, Z-preparations selectively bind to the central receptors, causing increased inhibition, which leads to rapid falling asleep and qualitative sleep. These drugs do not change the structure of sleep, do not cause drowsiness during the day, they are not characterized by severe side effects and habituation develops very slowly, and therefore Z-drugs are currently the most widely used means for eliminating insomnia.

Gistaminoblokatory are also very effective drugs, the effect of which is due to the acceleration of the GABA receptor. It is gistaminoblokatory are the safest sleeping pills at the moment, so they are allowed to apply even for children. In addition, gistaminoblokatory are the only drugs that can be used in the syndrome of apnea. However, all of the above applies only to preparations containing doxylamine as an active ingredient. The remaining histaminoblockers used as hypnotics (eg, diphenhydramine, hydroxyzine, doxylamine, promethazine) inhibit the paradoxical phase of sleep and cause pronounced sleepiness in the morning hours and headaches. The undoubted advantage of hypnotic groups of histamine blockers is the complete absence of dependence even with prolonged use.

Aldehydes and Clomethiazole have a very rapid effect and practically do not change the normal structure of sleep. However, Clomethiazole rapidly causes drug dependence.

Soporific – the rules of choice and use of drugs

Currently, the use of sleeping pills is considered justified in the following situations:

1. The causes of insomnia are not identified.
2. The causes of insomnia can not be completely eliminated.

When choosing a hypnotic, the type and severity of sleep disorders should be considered. So, in the case of difficulties with falling asleep and a normal dream, for the rest of the time you should choose a hypnotic short or medium action. At the same time, if the severity of the disorders is not too high, then it is optimal to use any means except for benzodiazepines and barbiturates. Currently, with difficulties of falling asleep, doctors recommend using the following drugs – Zopiclone, Zolpidem, Zaleplon, Melatonin, Clomethiazole, Niaprazinum or Propimiousum.

These drugs can be used in case of difficulty falling asleep at any time. For example, if a person can not fall asleep in the evening, then before taking to bed, you can take any given medicine. Also, this medicine can be taken in the event that a person wakes up at night and can not fall asleep again.

If a person is disturbed by frequent nocturnal awakenings and superficial sleep, then he should choose a medication among means with medium or short duration of action. If sleep disorders are not severe, then you should also choose new drugs, giving up benzodiazepines and barbiturates. Doctors recommend choosing a drug from the following:

• Chloral hydrate;
• Doxylamine;
• Methaqualone;
• Melatonin.

If you need a quick effect, then the drugs with chloral hydrate are optimal, but they can not be taken for a long time, as they quickly become addictive. If you need a drug that can be used for a long time, Doxylamine is optimal. All other drugs can be used for a limited period of time, however long enough to form a new sleep reflex, and a person could give up sleeping pills.

At early morning awakenings after which it is impossible to fall asleep, it is recommended to use drugs of long or medium action. People whose constant work is associated with the need for high reaction rates and concentration of attention should not use long-acting sleeping pills, since their frequent side effect is lethargy, drowsiness and drowsiness during the day. Since most of the hypnotics of this group refer to benzodiazepines and barbiturates, you should use them with extreme caution. In order not to resort to potent and rapidly inducing benzodiazepines and barbiturates, it is recommended to select a drug from the following:

• Bromovazole;
• Doxylamine;
• Zolpidem;
• Zopiclone.

In principle, when choosing a sleeping pill should always be guided by the rule that benzodiazepines and barbiturates can be used only in case of emergency in case of severe insomnia, when other means are ineffective. However, after achieving a positive effect with the use of barbiturates and benzodiazepines, you should switch to taking other sleeping pills that do not have such a strong and strong ability to form relationships.

The general current trend is that sleeping pills of choice are Zopiclone, Zolpidem, Zaleplon and Doxylamine, which provide a quick sleep, practically do not disturb the normal structure of sleep, do not cause numerous serious side effects such as addiction, daytime drowsiness, headaches, etc.

Any sleeping pill should be taken 15 to 30 minutes before bedtime.

Sleeping Pills (List)

Let’s give a list of hypnotic drugs in alphabetical order, regardless of the group to which this or that drug belongs. In the list, we will first indicate the international name of the active substance, and then in brackets the commercial names under which the drug can be sold in pharmacies.

Soporifics of all forms of release

So, now in the pharmaceutical markets of the CIS countries there are the following sleeping pills:

• Bellataminal (phenobarbital + ergotamine + alkaloids of belladonna);
• Bromizoval (Bromizoval, Bromural);
• Brotisolam;
• Hexobarbital (Hexenal);
• Diphenhydramine (Diphenhydramine, Grandim, Dymedrol);
• Doxylamine (Valocordin-Doxylamine, Donormil, Rellip);
• Zopiclone (Zopiclone, Zopiclone 7.5 – SL, Imovan, Piklodorm, Relaxon, Somnol, Slipwell, Thorson);
• Zolpidem (Hypnogen, Zolpidem, Zolsana, Zonadin, Iwadal, Nitrest, Oniria, Sanvall, Snovitel);
• Zaleplon (Andante, Zaleplon);
• Clomethiazole (Geminearrin);
• Melatonin (Melaxen, Circadian, Melaxen Balance, Melarena, Melatonin);
• Methohexital (Brietal);
• Methaqualone;
• Midazolam (Midazolam-Hameln, Dormikum, Flormidal, Fulsed);
• Nitrazepam (Berlidorm 5, Nitrazadon, Nitram, Nitrosam, Radedorm 5, Eunotin);
• Oxazepam (Nozepam, Tazepam);
• Temazepam (Signopam);
• Thiopental sodium (Thiopental, Thiopental-CML);
• Triazolam;
• Phenobarbital (Luminal);
• Flunitrazepam (Rohypnol);
• Flurazepam (Apo-Flurazepam);
• Cyclobarbital (Reladorm);
• Estazolam (estazolam);
• Chloral hydrate.

Listed in the list of drugs are available in various forms – solutions for intravenous and intramuscular injections, tablets and drops for oral administration.

Sleeping pills in tablets

Sleeping pills in tablets are as follows:

• Andante (capsules);
• Apo-Flurazepam (capsules);
• Bellataminal;
• Berlidorm 5;
• Bromizoval;
• Heminearrin (capsules);
• Hypnogen;
• Diphenhydramine;
• Donormil;
• Iwadal;
• Zolpidem;
• Zolsana;
• Zonadin;
• Zopiclone 7.5-SL;
• Melaxen;
• Melaxen Balance;
• Melarena;
• Nitrazadone;
• Nitrazepam tablets;
• Nitram;
• Nitrust;
• Nitrosam;
• Nozepam;
• Piklodorm;
• Radedorm 5;
• Reladorm;
• Relaxon;
• The Raslip;
• Rohypnol;
• Sanvall;
• Signopam;
• Slipwell;
• Snovitel;
• Somnol;
• Tazepam;
• Thorson;
• Phenobarbital;
• Flormidal;
• Chloral hydrate;
• Circadian;
• Estazolam;
• Eunotin.

Sleeping pills in drops

Sleeping preparations, released in drops, are as follows:

• • Valokordin-Doksilamin – drops for oral administration;
  • Grandim – solution for oral administration;
  • Onria – drops for oral administration;
  • Phenobarbital – solution for oral administration.

Sleeping pills without prescriptions (list)

Since almost all the hypnotic drugs act on the central nervous system and can cause serious side effects, such as respiratory depression, decreased performance, drowsiness, and others, and to provoke addiction, most of them are prescribed by a doctor. All benzodiazepine hypnotics and barbiturates are released strictly according to special recipes. Sleeping pills from other groups in most cases are also prescription.

Currently, without a medical prescription, you can buy the following sleeping pills:

• Andante;
• Valocordin-Doxylamine;
• Donormil;
• Melaxen;
• Melaxen Balance;
• Melarena;
• The Raslip;
• Circadian.

Homeopathic remedies that promote normalization of sleep, such as Nervocheel and Uspokoy, are also dispensed without a doctor’s prescription. In addition, the domestic pharmaceutical market there are herbal sleeping pills, which are also sold without a doctor’s prescription, but in many situations are quite effective. The most effective herbal preparations with hypnotic and sedative effect are the following:

• Dormiplant tablets;
• Persen tablets;
• Novo-Passit solution;
• Corvalol solution.

If there is a need for a strong hypnotic, and you can not prescribe a prescription from a doctor, you can buy Valocordin drops, which contain phenobarbital. Then you should drink the maximum allowable single dose of drops, after which the sleep is almost guaranteed to come.

Rapid sleeping pills

Various sleeping pills cause the onset of sleep in 5 to 30 minutes. Drugs that can “lull” a person 5 to 15 minutes after use are considered to be quick sleeping pills. However, their speed is relative, since the onset of sleep within 15 to 30 minutes after taking is also a good enough indicator, since during this time a person manages to lie comfortably in bed, relax, think about something pleasant, and on this background gently and imperceptibly sink in a dream. Therefore, strictly speaking, all modern sleeping pills can be called relatively fast.

But the fastest sleeping pills that cause falling asleep literally within 5 to 15 minutes after taking are the following drugs:

• Donormil;
• Reladorm;
• The Raslip;
• Chloral hydrate.

Severe sleeping pills

The following drugs belong to strong sleeping pills:

1. Barbiturates:

• Bellataminal;
• Hexobarbital (Hexenal);
• Methohexital (Brietal);
• Phenobarbital (Luminal);
• Cyclobarbital (Reladorm).

2. Benzodiazepines:

• Midazolam (Midazolam-Hameln, Dormikum, Flormidal, Fulsed);
• Nitrazepam (Berlidorm 5, Nitrazadon, Nitram, Nitrosam, Radedorm 5, Eunotin);
• Oxazepam (Nozepam, Tazepam); Temazepam (Signopam);
• Triazolam;
• Flunitrazepam (Rohypnol);
• Flurazepam (Apo-Flurazepam).

3. Z-preparations:

• Zopiclone (Zopiclone, Zopiclone 7.5 – SL, Imovan, Piklodorm, Relaxon, Somnol, Slipwell, Thorson);
• Zolpidem (Hypnogen, Zolpidem, Zolsana, Zonadin, Iwadal, Nitrest, Oniria, Sanvall, Snovitel);
• Zaleplon (Andante, Zaleplon).

4. Heterocyclic Compounds:

• Chloral hydrate.

5. Melatonin receptor agonists:

• Melaxen;
• Melaxen Balance;
• Melarena;
• Circadian.

The above drugs are the strongest sleeping pills, but most of them are dispensed from pharmacies only on prescription.

Strong sleeping pills without recipes

The only powerful sleeping pills that can always be bought without a prescription are medications from a group of melatonin agonists, such as Melaxen, Melaxen Balance, Melarena and Circadian. These drugs are allowed for OTC, because they are safe, they are very difficult to overdose, and they are not addictive.

In addition, in some pharmacies without a prescription, you can buy a strong sleeping pills Andante, which is theoretically included in the list of prescription drugs, but it is not a means of subject accounting, like narcotic substances, benzodiazepines and barbiturates, and therefore it is sometimes released freely.

If a person needs a powerful sleeping pill for periodic application from case to case, then Valocordin drops can be used because they contain phenobarbital. When using Valocordin as a potent sleeping pill should be taken for 20 – 30 minutes before bedtime, the maximum allowable single dose of the drug. It is impossible to use Valocordin constantly, as this will cause addiction and numerous side effects, however, from time to time this option can be used.

Sleeping, not addictive

Unfortunately, all hypnotic drugs in one way or another are addictive, which is expressed in the formation of physical and psychological dependence. However, in some drugs, dependence is formed quickly, and in others – very slowly. That is, the severity of the dependence and the duration of its formation are different for different drugs. Such a slow formation of dependence can be equated to the lack of addiction.

Thus, most rapidly (approximately 3 to 4 months), the dependence on barbiturates and benzodiazepines is formed, and it is the heaviest from the drugs of the same groups. Slower (approximate within 5 – 6 months) formed a dependence on Z-drugs (Zolpidem, Zopiclone, Zaleplon), Chloralhydrates and others. However, the severity of the formed dependence on these drugs is not inferior to that of benzodiazepines and barbiturates.

There is almost no dependence on melatonin preparations (Melaxen, Circadian, Melaxen Balance, Melaren, Melatonin), doxylamine (Valocordin-Doxylamine, Donormil, Rellip) and diphenhydramine (Diphenhydramine, Grandim, Dimedrol).

Sleeping pills for children

Children almost never have sleep disorders that require treatment with serious sleeping pills. As a rule, insomnia in children is caused by overexcitation, excessive activity or any unpleasant sensations, for example, pain, runny nose, etc. Therefore, in order to help a child fall asleep, it is necessary, first, to try to eliminate the cause, and secondly, to give him safe soothing means. Such sedatives can be considered analogues of sleeping pills for children.

At the present time, the following can be considered as conventional children’s sleeping pills (sedatives):

• Nervocheel (homeopathic remedy);
• Dormickind (homeopathic remedy);
• Notta (homeopathic remedy);
• Glycine;
• Bayu-Bai;
• Central;
• Collection “Children’s soothing”;
• Collection “Mother’s Tale”;
• Collection “Evening tale.”

It is not recommended to give the child as a sleeping pill self-cooked decoctions and infusions of herbs, because they can not control the concentration of active substances.

If the problem of insomnia in a child is serious, then to eliminate it you can use Diphenhydramine or Phenobarbital. However, these drugs should be used only under the supervision of a doctor.

Good sleeping pills

Now, drugs that provide a quick sleep and a quality, deep, full sleep without awakening during the night, and also do not cause fast addiction are considered to be good sleeping pills. In addition, good sleeping pills should not cause drowsiness and absent-mindedness during the day and at the same time provide a feeling of cheerfulness, freshness and a surge of strength in the morning. Z-group preparations (Zolpidem, Zopiclone, Zaleplon), melatonin agonists (Melaxen, Circadian, Melaxen Balance, Melaren) and agents containing doxylamine (Valocordin-Doxylamine, Donormil, Rellip) fully meet these requirements.

Home sleeping pills (sleeping pills at home)

At home, you can prepare sleeping pills on the basis of medicinal herbs, which are brewed or infused. The most effective are the following herbs:

• Valerian;
• Motherwort;
• Peppermint;
• Field mint;
• Hawthorn;

You can make sleeping pills by simply brewing a tablespoon of chopped herbs with a glass of boiling water and leaving for 20 to 30 minutes. After that, the infusion should be filtered through gauze and slowly drunk in a relaxed atmosphere.