Melatonin and COVID-19

Detection of melatonin

In 1958, the team of Aaron Lerner, a professor of dermatology from Yale University in the USA, managed to isolate a new compound from the epiphyses of cows, which, when introduced into the skin of a tadpole, lightened it.
The substance blocked the production of melanocyte-stimulating hormone, which is why it was called “melatonin”. Later they discovered that the open compound is synthesized in the body mainly at night. This was associated with daily periods of rest and wakefulness, and for two decades melatonin was considered only a sleep hormone that regulates human circadian rhythms.

What is melatonin for?

Melatonin is a hormone produced by the pineal gland, or “pineal gland,” a part of the brain so called because it is shaped like a small bump.
Modern science believes that melatonin appeared billions of years ago, living beings began to produce it as a substance that captured oxygen molecules in the air when there was an excess of it. Now melatonin performs many important functions in our body and is known to support circadian rhythms. The circadian rhythm is the body's internal clock. It tells the body when to sleep and when to wake up.

Melatonin production

80% of melatonin is produced by the pineal gland, a 100-125 mg pineal gland located in the brain. The remaining 20% of melatonin is produced by special cells:

digestive tract;
bronchi and lungs;
kidney;
pancreas;
prostate and ovaries;
retina, other organs and tissues.

Melatonin is produced even by blood cells: eosinophils and lymphocytes.
This discovery was made in 1974 by Soviet scientists Nathan Tanfelevich Raikhlin and Igor Moiseevich Kvetnoy. This “peripheral” melatonin does not affect circadian rhythms, working exclusively at the local level.

Action of melatonin

The “sleep hormone”
begins to be produced between 20 and 22 hours (earlier for early risers, later for night owls). The concentration of melatonin peaks from midnight to two o'clock in the morning, and by six to seven o'clock in the morning it drops to its minimum level.

How does melatonin work?

Absorbs free radicals - unstable molecules that damage organs and tissues, lead to decreased immunity, the development of tumors and cardiovascular diseases.
It is the strongest natural immunomodulator, restores damaged cells, prevents diseases, including cancer.
It has a pronounced chronobiotic effect: it regulates daily and seasonal biorhythms.
Promotes sleep, is responsible for calm restorative sleep, bringing natural rest.
Regulates the functioning of the endocrine system, normalizes body temperature.
Acts as an antidepressant and prevents the occurrence of certain mental disorders.
Slows down the rate of aging, increases life expectancy.

What lowers melatonin levels?

Age. After 45-50 years, the production of natural melatonin decreases.
Light. The pineal gland can only produce melatonin in the dark. If the lights are turned on at night, the production of the hormone slows down until it stops completely. The glow of the screens of a mobile phone, tablet, laptop, computer or TV reduces the synthesis of melatonin.
Smoking.
Drinking alcoholic or caffeinated drinks.
Taking nonsteroidal anti-inflammatory drugs (NSAIDs), vitamin B12, and some other medications.

What increases melatonin production?

Lack of light at bedtime
Calcium
Magnesium
Vitamin B6
A nicotinic acid.

Melatonin: properties, deficiency symptoms, contraindications

03.01.2022

Melatonin is also called hormone or night hormone because this is when the body produces the most of it. It is responsible for the proper regulation of the human circadian rhythm. What happens when the pineal gland produces too little of this substance? Who should complement it?

What is melatonin and what are its properties?

Melatonin is a hormone produced by the pineal gland, a gland located in the head. The important thing is that this happens exclusively in the dark. That is why it is otherwise called the night hormone . The more it is released into the blood , the more you want to sleep, and eventually the person falls asleep. The highest concentration of melatonin in the body occurs between midnight and three o'clock in the morning.

It is worth knowing that it is one of the elements responsible for regulating the human biological clock. What does it mean? It is responsible for regulating the rhythms of sleep and wakefulness.

Melatonin for Sleep – When Should You Supplement?

One of the main indications for the use of melatonin is circadian rhythm disorders, as well as sleep disorders. It is recommended for people suffering from so-called primary insomnia , that is, whose quality of sleep is very poor. In addition, it is also used for sleep-wake cycle disorders. This phenomenon is called "jet lag" and refers to rapid changes in time zones, such as when traveling. It may also be useful for sleep disorders associated with shift work.

Melatonin deficiency - symptoms

Melatonin deficiency has several symptoms. If you notice some of these signs, see your doctor to determine the level hormones in your body and possibly correct it. What exactly is melatonin deficiency?

sleep disorders
feeling of physical exhaustion
neuroses
poor physical condition
exacerbation of symptoms of concomitant diseases

However, that's not all. As it turned out, too low levels of melatonin can increase the likelihood of developing breast , prostate, and colon cancer .

Melatonin - overdose and contraindications

It is undeniable that melatonin, like any other drug, can be overdosed. It is not toxic to humans, and for this reason such cases are indeed rare, but they do happen. You should be aware that symptoms of melatonin overdose appear after taking about 8 tablets at a time.

But when should melatonin not be used at all?

with increased sensitivity to it
if you have liver
if you drink alcohol
for autoimmune diseases

Remember that pregnant, breastfeeding women and children are also not recommended to take melatonin.

Published in Medicines Premium Clinic

The use of synthetic melatonin analogues in medicine

Most often, melatonin preparations are used to treat various sleep disorders.
Conducted studies prove the effectiveness of melatonin for acute insomnia: the time to fall asleep decreases, the quality of night sleep and its duration improve. Taking melatonin is justified in case of chronobiological disorders, when a person often changes time zones or works on a shift schedule alternating night and day shifts.

“Sleep hormone” drugs cannot be used as a usual sleeping pill. They help only with failures caused by a decrease in melatonin production. In other cases there will be no effect.

Melatonin is not prescribed for:

chronic insomnia;
maintaining the daily secretion of your own melatonin;
normal biological rhythms.

Where is melatonin?

Melatonin is produced in the body. Melatonin is also found in some foods and can be synthesized artificially from animal pineal hormone. Nowadays you can find many melatonin preparations in pharmacies in the form of medicines or nutritional supplements, so let’s figure out together who needs to take melatonin and how safe it is.

There are several indications for taking melatonin:

Delayed sleep phase syndrome (DSPS or night owl syndrome) is a rare pathology when a person’s biorhythms are disrupted, such people cannot sleep and get up late. Research shows that taking melatonin by mouth shortens the time it takes to fall asleep and speeds up sleep onset in people with this condition. However, a year after stopping therapy, the problem may return.
Insomnia. According to studies, short-term use of melatonin reduces the time to fall asleep for insomnia by about 7-12 minutes. Melatonin has been shown to improve sleep and sleep problems in comorbid conditions such as depression, schizophrenia, epilepsy, autism, and various cognitive impairments. Melatonin may reduce evening confusion and restlessness in people with Alzheimer's disease, Parkinson's disease, dementia, and traumatic brain injury, but does not improve cognitive performance.
Insomnia caused by beta blockers. Sleep disturbance caused by certain blood pressure medications can be regulated with melatonin. Melatonin has been shown to slightly shorten the time it takes to fall asleep, but its effect on sleep quality and overall sleep time is unclear. Melatonin may also be beneficial for older adults who have a physiological melatonin deficiency.
Disorder of daily biorhythms due to long-distance flight. Most studies show that melatonin can improve certain symptoms of jet lag, such as daytime sleepiness and fatigue. It also helps you quickly adapt to a new time zone.
Migraine. According to many domestic and foreign studies, melatonin helps prevent migraines in adults and children, and the attacks that occur pass away faster.
Shift work. It has not been fully proven whether melatonin can improve the quality and duration of daytime sleep in people who work at night.
Circadian rhythm disturbances in blind people. Melatonin helps regulate biorhythms in blind people.
Sleep disorders in children. Small studies have shown that melatonin may help treat sleep problems in children with various forms of developmental delays. However, developing a daily routine and healthy bedtime habits is usually recommended as a starting point.

Is it safe to take melatonin?

Although melatonin is not as effective as some sleeping pills, it has fewer side effects than other medications. In rare cases, it causes headaches, dizziness, mild anxiety, and decreased concentration.

Since melatonin has a certain sedative effect, for the first 5-6 hours after taking it you should refrain from driving and working with technically dangerous mechanisms.

Although melatonin is a fairly safe substance, the decision to take it should be discussed with your doctor. The doctor will determine the indications and contraindications, help you choose the dosage if he thinks that you need to take melatonin and determine the duration of the course of treatment. As a rule, after stopping taking melatonin, sleep disturbances return, since taking the hormone does not help to regulate its production by the body, but is only a temporary measure. Therefore, in addition to prescribing melatonin, the doctor will give recommendations on how to eliminate the causes of disturbed sleep, how to restore the disrupted mechanisms of falling asleep and maintaining normal sleep.

Dietary supplement or medicine?

There is still no consensus among doctors whether to consider melatonin a medicine or a biologically active supplement (dietary supplement).
IN THE USA

The Food and Drug Administration (FDA) has not approved it for medical use, so melatonin is sold over-the-counter as a dietary supplement.
In the European Union and Australia,
melatonin is considered a medicine, sold by prescription and used to treat insomnia in children, adolescents and people over 55 years of age.

In Russia

Dosage forms of the drug and dietary supplements have been registered and can be purchased in pharmacies and sports nutrition stores without a prescription.

Melatonin is used as an adjuvant therapy for:

peptic ulcer of the stomach and duodenum;
hypertension;
Alzheimer's disease and other memory disorders;
depression and other diseases.

Research into the pharmacological activity and effectiveness of melatonin is ongoing. To date, more than 26 thousand scientific papers have been published, each of which opens up new pages in the use of this amazing substance.

The COVID-19 pandemic, caused by the SARS-CoV-2 virus, has forced scientists to actively study the effect of melatonin on the course of this disease. As a result, the usual “sleep regulator” began to be used in a complex of means of auxiliary therapy for COVID-19. In the fall of 2020, it was even used to treat US President Donald Trump. US
Melatonin Reviews The electronic scientific library medRxiv published a report in October 2022 on a research work in which 800 cases of severe COVID-19 were studied. It turned out that patients who initially had high levels of their own melatonin, and those who received the hormone in the form of a drug, were significantly more likely to survive in intensive care. Melatonin increased the chances of recovery, both from coronavirus and any other infection that affects the lungs.

Canada and Argentina.

The work was published in the journal Diseases in November 2022. A joint study from the University of Toronto and the Pontifical Catholic University found that the disease may be more severe in older people due to decreased levels of melatonin. Melatonin in adequate doses prevents the development of an aggressive form of COVID-19, and also supports the effect of the anti-coronavirus vaccine.

Brazil.

Data published by Melatonin Research in early 2022. Scientists from the University of Sao Paulo have proven that melatonin, which is produced by the cells of the alveoli of the lungs, becomes a barrier to coronavirus. This may be why people with high levels of melatonin do not become infected with Covid or experience the disease easily. Regina Pekelman, the author of the study, is confident that using nasal drops or a spray with melatonin is an effective means of combating COVID-19.

To enter the human body, SARS-CoV-2 viruses must bind to angiotensin-converting enzyme 2 (ACE2) receptors located on the surface of lung cells. Only by combining with ACE2 do coronaviruses enter the cell and begin to multiply, leading to disease.

Melatonin reduces the number of free ACE2 receptors, as a result, the number of connections between the virus and the enzyme is reduced, which leads to damage to a minimum number of cells, which means the coronavirus infection will occur in a mild form.

Additionally, melatonin reduces the inflammatory response at the site of virus entry and controls the immune response, preventing the development of a “cytokine storm.” And since it is the violent cytokine reaction that leads to a fatal result, its suppression increases the patient’s chances of surviving and avoiding serious complications.

In our country

sufficient scientific experience has not yet been accumulated to confirm the fact that melatonin prevents severe COVID-19, and the mechanism of action of melatonin on the human body has not yet been sufficiently studied. However, empirical evidence provides encouraging results and supports the positive effect of melatonin on the outcome of COVID-19.

Melatonin preparations are available in Russia without a prescription, but you should not take them without an in-person consultation with a doctor, either to correct sleep disorders or to prevent or treat COVID-19.

Melatonin Evalar tab 3 mg 100 pcs

Pharmacological group:

Adaptogenic agent ATC code: N05CH01.
Pharmacodynamics:
Melatonin is a synthetic analogue of the pineal gland hormone; synthesized from amino acids of plant origin. It has an adaptogenic, sedative and hypnotic effect. Normalizes circadian rhythms. Increases the concentration of gamma-aminobutyric acid (GABA) and serotonin in the midbrain and hypothalamus, changes the activity of pyridoxal kinase, which is involved in the synthesis of GABA, dopamine and serotonin. Regulates the sleep-wake cycle, daily changes in locomotor activity and body temperature, has a positive effect on the intellectual and mnestic functions of the brain, on the emotional and personal sphere. Promotes the organization of biological rhythm and normalization of night sleep, has a hypnotic effect. Improves sleep quality, speeds up falling asleep, reduces the number of night awakenings, improves well-being after waking up in the morning, and does not cause a feeling of lethargy, weakness and fatigue when waking up. Makes dreams more vivid and emotionally rich.

Adapts the body to rapid changes in time zones, reduces stress reactions, and regulates neuroendocrine functions. Adapts the body of weather-sensitive people to changes in weather conditions. Shows immunostimulating and antioxidant properties.

Does not cause addiction or dependence.

Pharmacokinetics:

Absorption Melatonin after oral administration is rapidly absorbed from the gastrointestinal tract. In elderly people, the rate of absorption may be reduced by 50%. The kinetics of melatonin in the range of 2-8 mg is linear. When administered orally at a dose of 3 mg, Cmax in blood plasma and saliva is achieved after 20 minutes and 60 minutes, respectively. The time to reach the maximum Tmax concentration in the blood serum is 60 minutes (normal range 20-90 minutes). After taking 3-6 mg of melatonin, the maximum concentration of Cmax in the blood serum is usually 10 times higher than the endogenous melatonin in the blood serum at night. Concomitant meals delay the absorption of melatonin.

Bioavailability The oral bioavailability of melatonin ranges from 9 to 33% (approximately 15%).

Distribution In in vitro studies, the binding of melatonin to plasma proteins is 60%. Melatonin binds primarily to albumin, alpha1 acid glycoprotein, and high-density lipoproteins. The distribution volume Vd is about 35 liters. It is quickly distributed into saliva and passes through the blood-brain barrier and is detected in the placenta. The concentration in cerebrospinal fluid is 2.5 times lower than in plasma.

Biotransformation Melatonin is metabolized primarily in the liver. After oral administration, melatonin undergoes significant transformation during its initial passage through the liver, where it is hydroxylated and conjugated with sulfate and glucuronide to form 6-sulfatoxymelatonin; the level of first-pass metabolism can reach 85%. Experimental studies suggest that isoenzymes CYP1A1, CYP1A2 and, possibly, CYP2C19 of the cytochrome P450 system are involved in the metabolism of melatonin. The main metabolite of melatonin, 6-sulfatoxymelatonin, is inactive.

Excretion Melatonin is excreted from the body by the kidneys. The average half-life (T1/2) of melatonin is 45 minutes. Excretion is carried out in the urine, about 90% in the form of sulfate and glucuronic conjugates of 6-hydroxymelatonin, and about 2-10% are excreted unchanged.

Pharmacokinetic parameters are affected by age, caffeine intake, smoking, and oral contraceptives. In critically ill patients, accelerated absorption and impaired elimination are observed.

Elderly Patients Melatonin metabolism is known to slow down with age. At different doses of melatonin, higher values of the area under the concentration-time curve (AUC) and Cmax were obtained in the elderly, which reflects a reduced metabolism of melatonin in this group of patients.

Patients with impaired renal function No accumulation of melatonin was observed during long-term treatment. These data are consistent with the short half-life of melatonin in humans.

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