Melatonin for insomnia - benefits, dosages and my experience

What are the health benefits of melatonin?

Research shows that small doses of melatonin help you fall asleep faster without causing side effects like sleeping pills. Melatonin also makes jet lag easier for the body to handle.

Melatonin has a number of other benefits, such as improving well-being, strengthening the immune system and reducing the level of free radicals in the body.

Recent studies also confirm that melatonin has antioxidant effects, is an immunomodulator in the fight against cancer and relieves sleep disorders. Research is still ongoing, and some of the effects of melatonin on the body have not yet been discovered.

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When and how best to take medications

Experts advise taking these remedies only immediately before bed, about half an hour before. On long trips, it is better to take a tablet (1.5 mg) before going to bed. Often the remedy is prescribed 3-4 days before the trip in order to synchronize the biological cycles and rhythms of our body. Do not bite the tablet and wash it down with water.

When asking the question “How to take melatonin?”, remember that this should only be done in accordance with the usual rhythm of sleep and wakefulness. So, if you sleep at night, then you should not take the drug during the day, because it is this hormone that is responsible for the clarity of our body’s biorhythms. In addition, it has been proven that in daylight the hormone is destroyed, and this once again confirms the need to take it only in the evening.

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How much does melatonin cost?

Melatonin is sold in sports nutrition stores and pharmacies.

The higher the dosage of the active substance, the higher the cost of the product.

For example, if a capsule contains 1 mg of melatonin, 90 capsules at a pharmacy will cost you about 400 rubles. Sports nutrition manufacturers use a higher dosage - 3, 5 or even 10 mg. The average cost of 180 capsules with a dosage of 3 mg of melatonin in sports nutrition stores is about 600 rubles.

Problems when using the drug Melatonin

There is no exact data on the effect of artificial hormone on the body. However, several problems were identified:

1. Decreased body temperature. The hormone provokes a slight decrease in body temperature. This does not affect healthy people, but patients who have difficulty with thermoregulation should take this into account
2. Interaction with sleeping pills. If melatonin-based drugs are taken with classic sleeping pills, the side effects increase many times over. At the same time, muscle reactions also worsen.
3. Blood thinning. Melatonin helps reduce blood clotting. Therefore, before using such drugs, especially in high doses during treatment with Warfarin, it is necessary to consult a specialist.

Thus, Melatonin is a medicine that can interact with other medications. If you use it, it is recommended to inform your doctor.

Taking melatonin as a sports nutrition

Scientists have found that melatonin protects cells, strengthens the immune system and slows tumor growth. According to laboratory tests on mice, melatonin slows down the aging process. However, you should not flirt with such a powerful hormone.

Although high dosages of melatonin cause no apparent harm immediately, long-term side effects are unknown. Even 1 mg, the smallest dosage found in sports nutrition products, is 3 times the normal level of melatonin in the body.

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Side effects, risks and harm

The hormone is considered safe, the harm of melatonin can be expressed in individual intolerance to the drug, nausea, vomiting, loss of coordination, fatigue, thirst. You may feel unwell and tired in the morning.

Taking certain pharmaceutical drugs can cause:

• irritation,
• increased excitability,
• increased heart rate,
• headache,
• migraine,
• blurred vision,
• attention disorder
• night sweats,
• dizziness.

It is recommended to avoid driving as melatonin can affect coordination and attention. Should not be used by children as there are no studies on the effects of some drugs on children. Can slow down growth and sexual development in children.

Who should not take melatonin?

It is not recommended for pregnant or breastfeeding women to take melatonin, as it is unknown how the hormone will affect the baby; people with allergies or autoimmune diseases (by stimulating the immune system, melatonin can aggravate existing problems); people with cancer of the immune system - lymphoma or leukemia (for the same reason); healthy children who already produce melatonin in abundance. It is also not recommended for women planning to conceive, as high dosage melatonin may act as a contraceptive.

In any case, before starting treatment, you should consult a therapist.

Indications and contraindications

Indications

Disturbance of sleep rhythm is the main indication for the use of the drug, insomnia, irritability and stress affecting the quality of sleep.

Contraindications:

• Diabetes.
• Autoimmune diseases.
• Individual sensitivity to the drug.
• Leukemia.
• Lymphoma.
• Myeloma.
• Epilepsy.

Attention! Taking melatonin is prohibited for children under 12 years of age; for adolescents, the drug is prescribed only by a doctor.

Is melatonin safe?

Melatonin –

one of the least toxic substances known.

In the studies, people took 6 grams of melatonin, which is 600 to 3,000 times the normal dosage. No traces of toxicity were found. The only significant side effect of high dosages of melatonin is drowsiness and slower reaction times. In the longest study to date, a high dose of melatonin (75 mg per day) was given to 1,400 women in the Netherlands for 4 years and had no effect on their health.

What is melatonin and what is it for?

Melatonin is a hormone produced by the pineal gland. Its quantity affects the quality and quantity of sleep and related processes. The benefits and harms of the presence or absence of a substance are associated with the ability to control the “activity-rest” cycle.

The hormone acts most at night, when falling asleep. It is believed that it strengthens the immune system and helps avoid premature aging. The main beneficial property is improving the quality of sleep and protecting against stress.

There is a theory that it is beneficial as a preventative against cancer. This ability is poorly studied, so you should avoid considering it a cure for oncology.

In addition to correcting the circadian rhythm, melatonin is beneficial for men, eliminating potency problems. The harm of the substance to males is identical to the harm to women.

Side effects

The drug is well tolerated by patients because its chemical structure is similar to the natural hormone melatonin, which is produced by the pineal gland. The use of drugs can provoke:

• development of daytime sleepiness;
• dizziness;
• night sweats;
• headache;
• discomfort in the abdominal area;
• confusion;
• irritability;
• asthenia;
• agitation;
• short-term feeling of anxiety;
• decreased visual acuity;

In case of persistent adverse reactions, it is recommended to discontinue use of the drug and consult a doctor.

Description of the active substance MelatoninMelatonin.

Formula: C13H16N2O2, chemical name: N-acetamide. Pharmacological group: hormones and their antagonists/synthetic analogue of pineal gland hormone (epiphysis). Pharmacological action: hypnotic, adaptogenic, antioxidant.

Pharmacological properties

Melatonin slows down the release of gonadotropins and, to a lesser extent, other hormones of the adenohypophysis - thyrotropin, corticotropin, somatotropin. Melatonin normalizes circadian rhythms, increases the content of GABA in the central nervous system and serotonin in the hypothalamus and midbrain, changes the activity of pyridoxal kinase, which is involved in the production of GABA, serotonin and dopamine. Melatonin regulates daily changes in body temperature and locomotor activity, the sleep-wake cycle, and has a positive effect on the emotional and personal sphere, intellectual and mnestic functions of the brain. Melatonin helps normalize night sleep, improve its quality and organize biological rhythm. Melatonin reduces the frequency of attacks of dizziness, headaches, and improves mood. Accelerates falling asleep, reduces the number of night awakenings, improves well-being after waking up in the morning, does not cause a feeling of weakness, lethargy and fatigue. Melatonin makes dreams more emotionally rich and vivid. Adapts the body to rapid changes in time zones, reduces stress reactions, and regulates neuroendocrine functions. Melatonin has antioxidant and immunostimulating properties, prevents the development of neoplasms and atherosclerosis. Melatonin has the most pronounced effect during prolonged and severe sleep disturbances. The pineal gland hormone melatonin ensures synchronization of insulin secretion and glucose homeostasis with the alternation of light and dark times of the day. A disruption of the alliance between melatonin-mediated circadian rhythms and insulin secretion is observed in diabetes mellitus (DM) types 1 and 2 (T1DM and T2DM). Insulin deficiency in T1DM is accompanied by an increase in melatonin production in the pineal gland. T2DM, on the contrary, is characterized by decreased melatonin secretion. In genome-wide studies, variants of the melatonin receptor gene MT2 (rs1387153 and rs10830963) are associated with fasting glycemic levels, β-cell function and T2DM. Melatonin increases β-cell proliferation and neogenesis, improves insulin sensitivity, and reduces oxidative stress in the retina and kidneys in experimental models of diabetes. Further research is needed to assess the therapeutic value of this hormone in patients with diabetes, but for now diabetes mellitus is listed as a contraindication. After oral administration, melatonin is completely and quickly absorbed and easily penetrates tissue barriers, including the blood-brain barrier. Melatonin has a short half-life and is eliminated from the body quickly.

Method of use of melatonin and dose

Melatonin is taken orally (regardless of food intake) once a day, 30–40 minutes before bedtime, 1–5 mg. During melatonin therapy, bright lighting should be avoided. You should not take non-steroidal anti-inflammatory drugs, beta-blockers, or drugs that depress the central nervous system together with melatonin. Melatonin is not recommended for use by drivers during work and people whose professions involve high concentration of attention. Women wishing to become pregnant should be informed that melatonin has a weak contraceptive effect.

Hypersensitivity, autoimmune and allergic diseases, chronic renal failure, lymphogranulomatosis, lymphoma, leukemia, myeloma, diabetes mellitus, epilepsy, pregnancy, breastfeeding.

Interaction of melatonin with other substances

Melatonin mutually enhances the effects of beta-blockers and drugs that have a depressant effect on the central nervous system. Melatonin is incompatible with glucocorticoids, MAO inhibitors, and cyclosporine.

Overdose

An overdose of melatonin increases the side effects. Gastric lavage and symptomatic treatment are necessary.

Product reviews Melatonin 3 mg (Ultimate Nutrition) 60 caps

Interaction of melatonin with other substances

Melatonin works together with some vitamins

Vitamin C, vitamin D3 and vitamin E are important antioxidants. Melatonin also has antioxidant activity. It can interact with each of these vitamins separately, which helps enhance the effect of the vitamins and melatonin. (, , )

The combination of vitamin D3 and melatonin may stop the growth of human breast cancer ().

Additionally, in damaged DNA, melatonin and vitamin C work together to produce powerful antioxidant effects. ()

Meanwhile, vitamin E and melatonin work together to stop oxidative damage in rats' livers. ()

Melatonin enhances the effects of alpha lipoic acid

In animal experiments, it was shown that alpha-lipoic acid (thioctic acid, thioctacid) acts as an endogenous antioxidant by binding free radicals . This means that it stops oxidative damage and has antioxidant properties. However, these antioxidant effects are quite weak. ()

When using alpha lipoic acid in combination with melatonin, its ability to block DNA damage increases 3 times compared to use without melatonin. ()

THREATS TO DNA INTEGRITY (left) AND THE POSITIVE EFFECT OF MELATONIN IN PROTECTING DNA FROM THESE THREATS (https://www.mdpi.com/1420-3049/23/3/530/htm)

Melatonin stimulates the effect of glutathione

Glutathione is a powerful antioxidant that not only protects the cell from oxidative stress, but also determines the redox characteristics of the intracellular environment. However, glutathione does this less effectively without the presence of melatonin. ()

Melatonin and glutathione in combination demonstrate a greater antioxidant effect than when used individually. Their combined antioxidant activity showed greater effect in rat liver. ()

Melatonin also stimulates glutathione activity in the brain of rats. They work together to eliminate peroxides and free radicals that cause oxidative damage. ()

Synergistic effects of melatonin and selenium

The microelement selenium exhibits the ability to act on free radicals. This means that selenium can stop free radicals from damaging cells and DNA. Selenium protects nerve cells and restores the activity of antioxidant enzymes. ()

Cerebral ischemia is a painful condition that occurs when there is not enough blood flow to the brain. This can lead to the death of brain tissue or even the development of a stroke. Oxidative damage from free radicals can lead to cerebral ischemia. ()

Melatonin and selenium jointly improve the condition of cerebral ischemia (experiments on male rats). This combination reduced damage to brain tissue and prevented inflammation. ()

Melatonin works together with galantamine

Galantamine is a cholinesterase inhibitor, a drug used for Alzheimer's disease, and is a drug with antioxidant properties. It also helps protect nerve cells in the brain. ().

Human nerve cells treated with a combination of galantamine and melatonin showed good protection against oxidative damage . Very small concentrations of each of these substances had no effect on their own. However, the combination of both demonstrated strong antioxidant effects. ()

Melatonin reduces EGCG toxicity

EGCG (epigallocatechin gallate), a type of catechin, is the responsible compound in green and black tea . EGCG prevents oxidative damage and protects cellular DNA. ()

However, large doses of EGCG extract in supplements or green tea can damage liver cells. Melatonin reduces the toxicity of EGCG in case of overdose. ()

In one study, scientists gave mice toxic and lethal doses of EGCG. Melatonin extended the survival time of mice given these huge toxic doses of EGCG. ()

Melatonin promotes the antioxidant effects of resveratrol

Resveratrol is known as an antioxidant and anti-inflammatory substance. However, under some conditions, resveratrol may also exhibit properties that promote oxidative stress. Resveratrol promotes oxidative damage to cellular DNA in the presence of transition metal ions (oxides of copper, silver, gold). ()

Resveratrol, in the presence of other antioxidants, loses its oxidizing property and acts as an antioxidant . Melatonin is able to reverse DNA damage caused by the oxidative effects of resveratrol with great efficiency. However, melatonin and resveratrol, when combined, do not combine to enhance the beneficial effects of each of these substances. ()

Introduction

Melatonin is the main hormone of the pineal gland, which transmits information about the external light regime to the internal environment of our body. The level of melatonin production indicates daytime or nighttime. The highest amount of melatonin (30 times more) is produced at night and the lowest during the day. The maximum concentration of melatonin is observed between midnight and 05.00 am with a peak of production at 03.00 am, but the onset of increased melatonin production occurs after 21.00 pm.

MELATONIN INFORMES THE WHOLE BODY ABOUT THE LEVEL OF EXTERNAL LIGHT (MORNING, AFTERNOON, EVENING, NIGHT)

In the human body, the hormone melatonin is produced from the amino acid tryptophan, which is involved in the synthesis of the neurotransmitter serotonin, and this substance, in turn, is converted into melatonin. In addition to the main amount of melatonin synthesized in the brain, some small part of melatonin is produced by cells of the gastrointestinal tract.

Melatonin is very important for maintaining our body's circadian rhythm Increasing lighting reduces its production, and decreasing light brightness increases melatonin levels. People with healthy circadian rhythms and normal pineal gland function produce approximately 70% of their daily amount of melatonin at night.

PEAKS IN MELATONIN AND CORTISOL PRODUCTION DURING THE DAY

Melatonin levels naturally decrease with age , so after age 60 it becomes increasingly difficult to fall asleep and have sound, long-lasting sleep. Some studies have shown that healthy levels of melatonin can prevent and even treat certain types of cancer (breast cancer, prostate cancer and colon cancer), the risk of which increases greatly with age. This is why it is very important to maintain healthy pineal gland function and melatonin production as the body ages.

DECREASE IN MELATONIN PRODUCTION WITH AGE. AFTER 60 YEARS, MELATONIN PRACTICALLY DOES NOT DECREASE, BEING AT VERY LOW VALUES

Release form and effect of the drug

The manufacturer of Vita-melatonin is the Ukrainian pharmaceutical company Kiev Vitamin Plant. The drug is available in the form of round, flat-cylindrical white tablets with a dividing strip in the center. The pills are placed in blister packs of 10 pieces. Each box made of thick paper contains 30 tablets (3 blisters) and instructions for use.

The active substance of the drug is melatonin, a hormone produced by the pineal gland (epophysis) and involved in the regulation of human circadian rhythms. Its mass fraction in one pill is 0.003 g. In addition to melatonin, the drug contains calcium in the form of stearate, microcrystalline cellulose, lactose and starch obtained from potatoes as auxiliary components.

The drug has a pronounced hypnotic and sedative effect. Its use allows you to slow down the production of gonadotropins, somatotropin, thyrotropin and corticotropin in the adenohypophysis and increase the level of serotonin and gamma-aminobutyric acid in the hypothalamus. Under the influence of these processes, a person’s circadian rhythms of sleep and sexual function are restored, mental abilities and physical endurance increase, and the body’s resistance to stressful situations increases. In elderly people, the drug normalizes blood pressure and pulse, and prevents exacerbation of hypertension during psycho-emotional stress.

Melatonin has a systemic effect on the body, penetrates the placenta and the blood-brain barrier. Metabolized primarily in the liver. The maximum content of the active component in the patient’s blood occurs after 20 minutes, in saliva - after 1 hour. The bioavailability of Vita-melatonin does not exceed 50%. Its elimination from the body occurs through the genitourinary system with urine.

Treatment of depression

Treatment of depression is not always effective, regardless of the availability of a large number of antidepressants. It has been found that almost 90% of people with depression have sleep problems and various other disorders: difficulty falling asleep, frequent awakenings at night, waking up in the morning with a feeling of anxiety.

Taking melatonin normalizes sleep and, as a result, makes it easier to cope with depression.

At the same time, long-term use of melatonin or violation of the rules of administration (taking during the day) can provoke depression as a negative side effect.

What are the signs that indicate you have a melatonin deficiency?

If you have puffy eyes, you look tired, you look older than your age, your hair is graying prematurely, and your behavior is becoming increasingly irritable and anxious, then your body may have decreased production of melatonin.

An equally clear signal of this is shallow sleep, without dreams, as well as gloomy thoughts that overcome you before falling asleep. If you feel like you never get enough sleep, don't cope well with daylight saving time, and are feeling tense and anxious, it's obviously time to seek advice from your doctor to determine the right dosage of a melatonin supplement.

Be healthy!

Instructions for use of synthetically produced hormone

To prevent the sleeping pill Melatonin from causing harm, the patient must take it according to the instructions. Since not all drugs are the same, the label should be carefully studied.

Typically, Melatonin dosage is as follows:

1. Before going to bed, you need to drink from 1 to 10 mg of the active substance.
2. The optimal amount has not been officially established.

It is important for patients to know that all supplements sold over the counter are not regulated by health authorities. Therefore, preference should be given to companies that have proven themselves to be the best.

Signs of low melanin levels

The main function of melanin is protection against ultraviolet radiation and some carcinogenic factors. This substance screens, absorbs and distributes the energy of solar rays. Part of the ultraviolet energy is converted into thermal radiation, and the remainder is used by the body in various photochemical reactions.

Thanks to this, malignancy of the epidermis into malignant neoplasms does not occur. A layer of pigment surrounds the cell nucleus, protecting genetic information.

Additional functions of melanin and its precursor melatonin:

• reduction of general stress in the body;
• neutralization of aggressive fragments of molecules - free radicals;
• stimulation of metabolic processes;
• water-soluble forms of the substance are capable of performing transport functions;
• promotes adaptation to various living conditions;
• reduction of manifestations of dystrophy in the endocrine glands and liver.

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There are a number of pathological conditions in which melanin levels can decrease. In addition, external factors influence the production of protective pigment.

What causes a decrease in melanin:

1. Imbalance in the hormonal sphere, long-term use of steroids and other drugs containing hormones.
2. Deficiency of vitamins and minerals.
3. Genetic predisposition.
4. Lack of sunlight.
5. Private stressful situations.

Signs of deficiency are largely cosmetic in nature. But behind them lie various pathological processes in the body.

Symptoms of pigment deficiency:

• increased sensitivity to sunlight;
• too light skin or whitish spots on the epidermis;
• uneven tan;
• early chronoaging with the appearance of gray hair and wrinkles at a young age;
• change, fading of the iris;
• vitiligo – loss of pigment in various parts of the body;
• the birth of an albino child.

If such symptoms are present, then it is necessary to reconsider your lifestyle and undergo examination by a doctor. To increase the level of pigmentation, it is recommended to adhere to a healthy diet and take vitamin complexes.