Topical sleeping pills for the treatment of insomnia

A long process of falling asleep, frequent awakenings result in a bad mood and drowsiness throughout the day. People are forced to resort to sleeping pills to get enough sleep. The pharmaceutical industry produces various drugs against insomnia. Some of them not only normalize sleep, but have many side effects that cause harm to the body - addiction, impaired attention, severe psycho-emotional disorders. Therefore, if you have symptoms of insomnia, do not rush to the pharmacy for a sleeping pill. Consult a specialist who can help you choose a medicine that will promote normal sleep in each specific situation. The fight against insomnia will be effective if you establish the causes of its occurrence and choose the right therapy.

Benzodiazepine-type hypnotics

These are hypnotics that have a strong sedative effect, suppress anxiety and fear, and have a pronounced hypnotic effect. The drugs can also relieve cramps and relax muscles. The mechanism of action is associated with stimulation of GABA receptors (GABA - gamma-aminobutyric acid), increasing the flow of chlorine ions into the neuron and thereby reducing its excitability.

Today, benzodiazepines are practically not used to treat sleep disorders. This is due to a large number of unwanted side effects. Some specialists use benzodiazepine drugs in short courses if there is a history of mental illness (panic attacks, anxiety disorder, epilepsy).

They use fast-acting products (help you fall asleep in 5 minutes) with a short elimination period:

• Triazolam;
• Temazepam.

Benzodiazepine sedative

They are indicated for the treatment of transient sleep disorders or for a short course; they are not recommended for pregnant and lactating women, children under 18 years of age, as well as for individual sensitivity. Common side effects are the desire to sleep during the day, headaches, and ataxia (unsteadiness when walking).

While taking benzodiazepine drugs, the development of addiction, dependence and withdrawal syndrome is possible! There is evidence of the possibility of changes in behavior or thinking processes, expressed in aggression, violence, and the occurrence of delusional hallucinations!

Major neuroleptics - antipsychotics (quetiapine)

Quetiapine is also used for the treatment of psychotic disorders and depressive and/or anxiety conditions in combination with insomnia that is not treatable with other drugs.

They have many serious side effects: hepatotoxicity, that is, a harmful effect on the liver, restless legs syndrome, akathisia, that is, restlessness, and weight gain; therefore, they are prescribed for the treatment of insomnia, as a rule, in cases where other drugs are ineffective. Often these antipsychotics are combined with antidepressants.

Antipsychotics are powerful medications. They are rarely used solely to treat insomnia, as there are many other medications available, but if the treating physician believes that antipsychotic medications are necessary, they may be the primary treatment for insomnia.

When taking antipsychotics, there is an increase in total sleep time and deep sleep phase.

For the treatment of nonpsychotic disorders associated with insomnia, doses of antipsychotics are generally lower than for the treatment of psychotic disorders.

Barbiturates

Derivatives of barbituric acid, which can have a strong sedative effect on the central nervous system (central nervous system) up to anesthesia. Phenobarbital is considered a striking example of this group of drugs. Like benzodiazepine drugs, barbiturates today have an extremely narrow therapeutic use, mainly:

• for the treatment of epilepsy;
• introduction to superficial anesthesia;
• in veterinary medicine for euthanasia of animals.

Very rarely, they may be prescribed for the treatment of sleep disorders.

Phenobarbital has the following effects:

• sleeping pills, sedative;
• instant muscle relaxation;
• relieves cramps;
• eliminates anxiety;
• anesthetic.

Antiepileptic and hypnotic drug from the group of barbiturates

Side effects include short-term memory loss, drowsiness, severe weakness, anxiety, and the appearance of hallucinations. Barbiturates cause drug addiction (dependence). Dispensed with a doctor's prescription.

General recommendations for prevention

To overcome insomnia and wake up refreshed and refreshed in the morning, you should follow just a few simple rules.

1. Follow a routine and lead a healthy lifestyle.
2. Be physically active and move more during the day.
3. Switch to small meals and do not overeat.
4. Avoid the consumption of strong alcoholic and tonic drinks, energy drinks.
5. Create comfortable sleeping conditions in your own bedroom.
6. Set aside half an hour in the evening for relaxation and ritual.
7. Do not resort to sleeping pills for the slightest sleep disturbance.
8. If necessary, give preference to herbal remedies.

Non-benzodiazepine drugs (z-group) for the treatment of insomnia

They differ from benzodiazepines in the structure of the molecule, but have a similar mechanism of action on the central nervous system. Representatives of this group (Zolpidem, Zopiclone, Zaleplon) have a hypnotic effect due to binding to GABA receptors. They are mainly used in elderly patients in short courses, since long-term use is addictive.

Studies by American physiologists show that there are no clear differences in the soporific effect on the patient’s body between benzodiazepines and z-drugs. There are still discussions in scientific circles about the effectiveness and safety of using this group for the treatment of insomnia.

In normal doses, these drugs do not have anticonvulsant, anxiolytic or muscle relaxant effects. They speed up the time it takes to fall asleep, reduce the number of night awakenings, and improve the overall quality of night sleep. A positive aspect is the absence of daytime sleepiness. The drugs are used daily before bedtime, 1 tablet. Z-drugs are usually well tolerated, but sometimes side effects such as weakness and drowsiness are possible. Contraindications are similar to benzodiazepines.

Modern sleeping pills Z-groups

With prolonged use, addiction may occur!

Prospects[edit | edit code]

Understanding the molecular structure of the subtypes of excitatory glutamate receptors and inhibitory GABA receptors, consisting of different subunits, will make it possible to express the genes of the corresponding subunits in cell cultures and, based on their effect on them, to select selective ligands with the desired effect and minimal side effects. But progress in the treatment of insomnia will be based both on the search for new drugs with improved pharmacokinetics and pharmacodynamics, and on the thoughtful use of non-drug methods, including behavioral psychotherapy, sleep hygiene and exercise.

Histamine receptor blockers

Donormil (doxylamine) has been known since the mid-20th century as a non-addictive remedy for insomnia. It has anticholinergic, hypnotic and sedative effects, does not change the slow phase of sleep, improves its duration and quality. In a large study involving 340 patients with sleep insomnia, Donormil was compared with the z-group, in particular, Zolpidem. The results revealed their almost identical positive effect on sleep, a small number of side effects, a small percentage of addiction (for Zolpidem), and a good response to the drug.

Donormil is available without a prescription; deep sleep at night continues 7-10 days after stopping treatment. Indications for use are temporary sleep disturbances. Contraindications: age under 15 years, hypersensitivity to doxylamine and similar drugs, glaucoma, prostate diseases.

Caution in treatment with Donormil is necessary in patients with sleep apnea syndrome, as the drug can worsen the course and frequency of respiratory arrests!

A drug that has a hypnotic and sedative effect

Research shows that Donormil is the safest for pregnant women at any stage. The drug is not recommended during breastfeeding. The course of treatment is designed for 5 days, 1-2 tablets 15 minutes before bedtime. If insomnia continues, consult a doctor. Donormil can cause dry mouth, constipation, urinary retention, blurred vision due to its M-anticholinergic effect, and also daytime drowsiness, which requires increased caution while driving.

Literature[edit | edit code]

• Amin, J., and Weiss, DS GABAa receptor needs two homologous domains of the p-subunit for activation by GABA but not by pentobarbital. Nature 1993, 366:565–569.
• Balter, M.B., and Uhlenhuth, E.H. New epidemiologic findings about insomnia and its treatment. J. Clin. Psychiatry, 1992, 53(suppl):34-39.
• Beckstead, MJ, Weiner, JL, Eger, EI II, Gong, DH, and Mihic, SJ Glycine and gamma-aminobutyric acid(A) receptor function is enhanced by inhaled drags of abuse. Mol. Pharmacol 2000, 57:1199–1205.
• Cavallaro, R., Regazzetti, M. G., Covelli, G., and Smeraldi, E. Tolerance and withdrawal with zoldipem. Lancet 1993, 342:374–375.
• DeLorey, T. M., and Olsen, R. W. y-Aminobutyric acid A receptor structure and function. J Biol. Chem 1992, 267:16747–16750.
• Dresser, GK, Spence, JD, and Bailey, DG Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition. Clin. Pharmacokinet., 2000, 38:41-57.
• Dujardin, K., Guieu, J. D., Leconte-Lambert, C., Leconte, P., Borde-ries, P., and de La Giclais, B. Comparison of the effects of zolpidem and flunitrazepam on sleep structure and daytime cognitive functions . A study of untreated insomniacs. Pharmacopsychiatry, 1998, 31:14-18.
• Fleming, JA The difficult to treat insomniac patient. J. Psychosom. Res., 1993,37(suppl 1):45-54.
• Ffrench-Mullen, JM, Barker, JL, and Rogawski, MA Calcium current block by (—)-pentobarbital, phenobarbital, and CHEB but not ^-pentobarbital in acutely isolated hippocampal CA1 neurons: comparison with effects on GABA-activated Cl- current . J Neurosci 1993,13:3211—3221.
• Frenkel, C., Duch, D.S., and Urban, B.W. Molecular actions of pentobarbital isomers on sodium channels from human brain cortex. Anesthesiology 1990,72:640-649.
• Griffiths, RR, Sannerud, CA, Ator, NA, and Brady, JV Zolpidem behavioral pharmacology in baboons: self-injection, discrimination, tolerance and withdrawal. J. Pharmacol. Exp. Ther., 1992, 260:1199–1208.
• Guglielminotti, J., Maury, E., Alzieu, M., Delhotal Landes, B., Becque-mont, L., Guidet, B., and Offenstadt, G. Prolonged sedation requiring mechanical ventilation and continuous flumazenil infusion after routine doses of clorazepam for alcohol withdrawal syndrome. Intens. Care Med 1999,25:1435-1436.

Melatonin-based products

Melaxen

Melaxen is synthesized from plant amino acids and belongs to the pharmacological group of adaptogens. Each tablet contains 3 mg of melatonin. The active drug easily passes through the BBB (blood-brain barrier) and has a hypnotic effect, therefore it is considered the best for the treatment of insomnia. Natural melatonin is a pineal gland hormone produced in the dark and normalizes circadian rhythms.

Due to the above factors, this remedy for insomnia effectively affects the process of falling asleep, increases the quality and depth of sleep, does not cause a feeling of weakness in the morning, and eliminates nightmares. Melaxen is used not only to treat insomnia, but also:

• when changing time zones;
• temporary insomnia caused by stress;
• has an immunomodulatory effect.

Adaptogen that normalizes physiological sleep

During and after treatment, no addiction or dependence syndrome was detected.

Dosage for therapy: half or a whole tablet half an hour before bedtime. Can be used for a long time, but only after consulting a doctor. Contraindications include: myeloma, lymphoma, diabetic patients, pregnancy, leukemia, kidney disease.

Roserem (ramelteon)

Melatonin receptor antagonist. Selectively binds to types 1 and 2 melatonin receptors in the suprachiasmatic nucleus. Regulates the time of falling asleep, improves the overall depth of night's rest, can be used for a long time (according to American studies of this drug). Rozerem does not affect GABA receptors, therefore it does not have an anxiolytic or anticonvulsant effect.

Side effects (clinical trials):

• increased risk of cancer;
• teratogenic effect on the fetus;
• increase in blood prolactin levels compared to placebo.

Side effects on health appear with long-term use of the drug. Available in the form of tablets of 8 mg of active substance. The doctor decides how to use Rozerem. Mainly used abroad.

"Melaxen"

The drug is an effective and harmless sleeping pill, so it is sold in pharmacies without a prescription. This is an effective chemical analogue of the natural hormone. Generics: "Metaton", "Melatonin", "Melapur".

The medication stabilizes sleep, especially with primary insomnia in patients of retirement age, so it should not be used by people over fifty-five years of age, as well as by those who suffer from insomnia with impaired sleep quality.

Tablets for sound sleep are recommended for use for insomnia associated with shift work schedules, flights to other countries, and stress. Side effects are extremely rare.

Contraindications for use:

1. Increased sensitivity to components.
2. Liver disorders.
3. Autoimmune diseases.
4. Childhood.
5. Work that requires increased attention.
6. Pregnancy.
7. Lactation.

An excessive increase in the dosage of the drug can cause drowsiness, dizziness, and impaired coordination of movements. No therapy is required; after half a day the medicine is eliminated from the body.

Herbal remedies for insomnia

Herbal medicines that can help against insomnia can be divided into complex and single-component ones. Let's take a closer look at the combined group. Pharmacy windows display a huge number of products based on herbal ingredients, biostimulants for the treatment of insomnia, and this list is also supplemented by homeopathic medicines, preparations from organ extracts, microelements, and vitamins.

It is worth immediately noting that many of them have not passed the required clinical trials and studies of safety and effectiveness. That is why the choice of a particular pharmaceutical drug must be approached with all responsibility, following the recommendations of your doctor. Otherwise, there is a high risk of aggravating the existing sleep disorder or developing chronic insomnia.

Persen

A remedy for insomnia based on lemon balm, valerian and mint. Has the following effects:

• sedative, mild hypnotic effect;
• antispasmodic effect;
• eliminates nervous tension;
• reduces sensitivity to stress;
• helps you fall asleep faster.

Herbal medicine with sedative effect

The effect develops after several days of regular use. The medicine is also suitable for children over 12 years of age. Persen is contraindicated during pregnancy and lactation, with a deficiency of sucrose and lactase, and diseases of the biliary tract. Take 2-3 tablets before bed, but no more than 12 per day. Persen can be prescribed to patients with sleep disturbances for up to two months. Further treatment is possible after consultation with a doctor.

Novo-Passit

The composition includes several herbs with a sedative, sedative and antispasmodic effect. Indications for use are similar to the previous drug. For convenience, Novo-Passit is available in the form of drops and tablets. Course of treatment for insomnia: 1 tablet (or 5 ml of solution) 3 times a day. If your sleep does not return to normal within a week, you should consult a doctor.

Dormiplant

An effective drug based on valerian and lemon balm makes it easier to fall asleep, reduces nightmares and night awakenings, does not cause drowsiness during the day, and does not depress psychomotor reactions and attention.

Sedative with extracts of valerian and lemon balm

Neurostabil

The phytocomplex has a mild sedative, hypnotic, and sedative effect, increases resistance to stress, and regulates blood pressure. Thanks to its active components, Neurostabil has a positive effect on sleep phases. It is not a medicine; it is used for increased emotional excitability and associated insomnia. The course of treatment is determined by the doctor, as a rule, take 1 tablet 3 times a day for a long time.

Sonilyuks

A relatively new drug that has appeared on the market since 2020. Indicated for various sleep disorders in adults and children over two years of age. In addition, Sonilyux treats anxiety and increased fatigue.

Compound:

• Gaba Alishan (high mountain green tea);
• castoreum;
• lofant;
• complex of 32 herbs.

Sonilyux is available in the form of drops; you need to take 1 dosed spoon three times a day.

Biogenic concentrate of plant extracts and natural components

Nervochel

Homeopathic complex remedy from the German company Heel for the treatment of anxiety, increased excitability, suspiciousness, vascular dystonia, restlessness, as well as insomnia. Indicated half an hour before meals, 1 tablet 3 times a day. The tablet should be kept under the tongue until completely dissolved. The course lasts 2-3 weeks under the supervision of a doctor. Can be prescribed to children from three years of age. Side effects are very rare.

When treating insomnia with pharmacological drugs or homemade tinctures, it should be remembered that any sleep disturbances can be eliminated simply by normalizing its regime and behavioral therapy. In some cases, they resort to combined treatment using hypnosis, psychoanalysis, auto-training, and physical therapy. Yoga, relaxation methods, aromatherapy, self-analysis, elimination of negative factors leading to insomnia, and normalization of the nervous system help a lot. In any case, before using this or that sleep aid, you need to consult a competent specialist in this field. Only after this can you safely begin therapy and be confident in its effectiveness.

Indications

Various medications, including pills to improve sleep, can give the body proper rest. They are used in the presence of the following conditions:

1. Sleep disorders.
2. Having trouble falling asleep and waking up multiple times.
3. Tension, anxious thoughts.
4. Neurotic disorder.
5. Irritability.
6. Violations of daily biorhythms.
7. Stress.
8. Psychosomatic diseases.
9. Psychopathological diseases in alcoholism.
10. Autonomic disorders.
11. Memory deterioration.
12. Depressive disorders.
13. Hormonal imbalances.
14. Age-related changes.

What are the best sleep pills?

Indications for "Restful Sleep"

The drug is prescribed for preventive purposes to prevent depression, support the body in stressful situations, in particular, during the following pathological processes:

1. Neuroses.
2. Loss of sleep.
3. Depressive disorders.
4. Chronic fatigue.

According to research, the combination of natural substances with minerals and vitamins has a positive effect on the functioning of the entire body.

The complex protects nerve cells and also supports cheerfulness, eliminates memory problems, treats Alzheimer's disease and similar ailments.

The duration of the treatment and prophylactic course and daily dosage is determined by a medical specialist.

"Doctor Sleep"

A herbal sedative produced in capsules. Extracts of medicinal plants have sleeping pills, anti-stress, and sedative properties. Does not provoke addiction.

Intended use of Doctor Sleep:

1. Sleep disorder.
2. Insomnia is a sleep disorder characterized by insufficient duration or quality of sleep, or a combination of these phenomena, over a significant period of time.
3. Stress.
4. Anxiety.
5. Irritability.
6. Depressive disorders.

"Doctor Sleep" is prohibited for children under twelve years of age and persons who have increased sensitivity to certain substances.

Sleep hormone

Melatonin regulates sleep and wakefulness, eliminates insomnia, eliminates stress, stabilizes blood pressure, prolongs life, and increases the body's defenses.

Melatonin eliminates certain types of headaches and has antioxidant and antitumor effects. It is possible to increase hormone levels naturally. To do this, you need to go to bed no later than twelve at night, sleep in a dark room and for a long time. After all, the component in the body is formed at night, from midnight to four o’clock.

If there is a deficiency of melatonin, it must be taken additionally, in the form of tablets to improve sleep (can be purchased without a prescription at the pharmacy). Taking the drug:

1. Improves sleep
2. Eliminates stress.
3. Increases immunity.
4. Regulates blood pressure and brain function.
5. Reduces cholesterol levels.
6. Relieves headaches.

No negative effects from consuming the sleep hormone have been recorded. At risk, as a rule, are pregnant women, as well as nursing mothers, and people with serious illnesses. However, it is not recommended for other people to use sleeping pills without consulting a doctor.

Causes of insomnia

Very often, insomnia is simply confused with worsening sleep. Insomnia occurs when a person cannot fall asleep under good circumstances.

If the reason for this is some other factors (noise, light, etc.), then we cannot say with confidence that you have this particular illness. There are a huge number of causes of insomnia, but, in general, there are several main and common ones:

1. Stress. This category also includes depression and emotional outbursts. Moreover, as for the latter, it can be either negative emotions or positive emotional stress. Every day we get stressed at work and do you know what this means? Chronic insomnia! If this is your situation, then I would advise you to think and change your view of what is really important.
2. Frequent use of psychoactive substances. We can include alcohol, cigarettes and products containing caffeine into this category.
3. Somatic diseases: ulcers, high blood pressure, attacks of cardiac ischemia.
4. The most basic reason is adaptation to the new pace of life. Every day this pace is increasing. We don't have enough 24 hours a day to have fun with our family, meet friends, visit our parents, get in shape at the beauty salon, go to the gym and finish all the accumulated work. Therefore, we stretch our activity to more than 15 hours a day. Have you ever wondered why 24-hour establishments providing services are so popular now? Precisely because the pace of life is accelerating exponentially, especially in large cities.

Example from life

I'll tell you an example from life. My dad is a successful man. He works in a large company, he has a high and well-paid position. But his job is endlessly stressful. He has a lot of responsibility, during working hours he is constantly on the phone, sometimes he doesn’t even have time to go to lunch.

And so it has been for fifteen years. For fifteen years he sleeps a maximum of 5-6 hours and wakes up at night. Of course, dad is used to this way of life. But is it good for your health?