Melatonin Review, Uses, Doses and Effects

Role of Melatonin in Human Body

A certain part of the human brain, the pineal gland, emits the special organic bioactive compound called melatonin. Its definition is as follows — a hormone, which is secreted by the epiphysis cerebri in inverse ratio to the amount of the ambient light, and used by mammals to regulate sleep. In layman’s terms, when the melatonin level increases, our body starts getting ready to go to bed. Normally, we produce this signaling biogenic substance when it gets dark. The pineal gland reacts to a command from the eye, and then this tiny organ (not bigger than a pea) initiates a number of processes:

• body temperature decreases a little;
• the heart beats slower and arterial tension goes down;
• breathing becomes even, deep, and infrequent;
• the brain gradually shuts down and we fall asleep.

It is not that melatonin does all this work, no, it is only a signal to all organs that it is getting dark, and they have to switch to night mode.

Actually, the sleep hormone serves to adjust the activity of your organism to the day-night cycles, and in the old days everything was simple. When the sun sank below the horizon, the eyes of our forefathers sent the message to the suprachiasmatic nuclei, which is a part of hypothalamus directly wired to retina via the optic nerves. It understood that night was coming, and it activated the pineal gland to secret the hormone melatonin. In the morning, with the first rays of the sun, the production of melatonin stopped, and people woke up. This way, the human inner clock entrained with the sunsets and sunrises.

Modern technologies have changed the lives of humans markedly, as nowadays we are surrounded by artificial sources of light. Electric bulbs, the neon lights of the cities, and the screens of our gadgets and monitors of our computers — everything interferes with the natural day and night schedule. We are exposed to light 24/7, and our brains do not know when to start producing melatonin anymore. It is very bad for healthy circadian rhythms, and can completely disable the internal clock. People mix up days and nights, losing their sleep, which leads to chronic fatigue and bad mood.

The word “melatonin” was first implemented by the American physician and professor Aaron Lerner. He derived it from the bovine pineal body, but back then he did not know anything about its role in a human’s life. Only in 1975 did the journal “Science” published an article where the authors established a correlation between the urinary melatonin level and daily rhythm. Since then, this hormone has been closely studied, and now we can tell you more about it. The full name of this molecule is N-acetyl-5-methoxytryptamine, and it belongs to the indolamine family. Human bodies synthesize it naturally. The biosynthesis pathway starts from the amino acid L-tryptophan, which we consume with regular foods and drinks. It is metabolized into 5-HTP (a.k.a 5-hydroxytryptophan), which is a precursor to serotonin. And finally, serotonin is converted into melatonin. Thus, to have a healthy melatonin production, we need to eat tryptophan- or melatonin-rich foods, which include vegetables, fruits, nuts, meat and seafood, eggs, tart cherry, legumes, etc.

The fluctuations of the sleep hormone in humans become regular as early as three months after birth. When we go through puberty, our schedule moves a little forward, so that we go to bed and wake up a couple of hours later. Aged people normally face melatonin deprivation, and this is why sleeping problems are common in the elderly. The healthy peak of the hormone’s concentration in the blood falls on the period between 23:00 and 3:00, then it goes down and reaches levels 10-15 times lower than in the nighttime. Normally, the circadian cycle looks like this — 16 hours of activity, when melatonin is almost undetectable in our system, and 8 hours of sleep.

Melatonin Uses

The modern pharmaceutical industry created pills with synthetic melatonin. These medications are represented in the forms of tablets, capsules, gummies, lozenges, liquids, and topical preparations. They are available in most local and online pharmacies over the counter, and as with all OTC drugs, you do not need a prescription to buy them. Doctors administer melatonin as a safer alternative to tranquilizers to treat various sleeping disorders, like parasomnia or age-induced sleeplessness. It may also help people with vision loss, as their bodies lack the key element of internal clock regulating — their eyes do not signal to the brain about the day and night sequence.

Melatonin tabs are very popular among travelers. People who travel from one side of the planet to another confuse their bodies, and upset their natural sleep/wake schedule. Jet lag causes some serious problems, like fatigue and mind fog during the day, agitation, uncoordinated movements, and muscle weakness. These symptoms can be alleviated with the help of melatonin supplements, as they adjust your circadian cycles to new time zones.

Some doctors report that this drug makes the circadian rhythms of kids with certain mental impairments more orderly. For example, MT (abbreviation for melatonin) therapy helps autistic and mentally retarded children improve their sleep-wake schedules. Insomnia, which is induced by certain drugs, Alzheimer’s disease, schizophrenia, and other maladies, are referred to as “secondary.” They can all be treated with melatonin, including improving of the sleep efficiency.

At the same time, it is not that easy with primary insomnia. When the sleeping problems are not associated with medications and health issues, life circumstances, or any other external factors, this hormone decreases the sleep onset latency a little, yet it can hardly improve sleep quality. The half-life of melatonin is too short, less than an hour, so if you take it before going to bed, you can fall asleep quickly, but shortly after that the medicine wears off. Thus, it does not make you sleep longer or deeper. This is what the scientists claim, based on their research. Meanwhile, there are a lot of ordinary users who witness the opposite.

Benefits and Positive Effect

Except sleep improvement, melatonin produces various positive effects in human bodies. Among others, it eliminates the dangerous components, like free radicals. As an antioxidant, it works inside the cells and brain, and cooperates with other bioactive compounds that scavenge our organisms. Melatonin and its derivatives protect our bodies from oxygen and nitrogen radicals, and remove the products of the lipid oxidation from cells. MT is even more effective than C and E vitamins, the best-known antioxidants.

Another benefit of melatonin is its positive influence on immunity. Unfortunately, this mechanism of action of the sleeping hormone is not well-studied. There are two almost identical types of melatonin receptors in humans — MT1 and MT2, and both are involved in sleep regulation. Additionally, they are incorporated with the cells that produce the immune response. There is also evidence that the neurohormone induces another immunomodulating molecule, cytokine. Presumably, this makes melatonin a potent remedy for inflammations, infections, and viruses.

The list of the health benefits of the sleeping hormone is huge, and we would need a couple of such articles to review them all closely. Herein we will give you a brief look at the numerous curative actions of melatonin:

• this hormone promotes healthy eye functioning. It appears that some organs, including the guts and retina, also take part in MT production. MT1 and MT2 receptors are found in the eyes, and they react to light and darkness, emitting certain amounts of the neurohormone. When they fail, it can lead to various vision impairments. For instance, melatonin mediates the electrical responses of the retina cells, prevents glaucoma and degeneration of macular, and increases the viability of the cone cells — the photoreceptors that provide color vision in humans;
• it was noted that patients with drug-induced tinnitus also felt relieved after exogenous MT administration. Depending on dosages, it may prevent disorders of the vestibular apparatus;
• MT increases metabolism and promotes weight loss;
• the scientists place great store on the anti-cancer capacities of melatonin. The ongoing research encourages medical academia to assert that this hormone may be used in oncology disease treatment. First of all, medical experts noticed that most cancer patients had similar disorders in the production of the sleeping hormone. They examined both sexes with breast, colon, and prostate tumors. After a couple of tests, it was also found that evening administration of MT retarded malignant cells on the early stages of the disease. In addition, this biosubstance showed the potency to inhibit the estrogen receptor activity, which can initiate the malignant cell development. Increasing the immune protection of our bodies, it suppresses the cancer metastasizing and induces the apoptosis of the tumor cells;
• high blood pressure may be also induced by melatonin deficiency, and consequently it can be treated with the supplementation of MT drugs. The group of scientists from Slovak Republic investigated the antihypertensive action of the pineal hormone. Indolamine was found to affect the vascular and central nervous systems and decrease arterial tension;
• as well as the heart and respiratory rates, melatonin can give a tune-up to insulin fluctuations. They also depend on the day-night biorhythms, and researchers from the Indian University claim that MT receptors are directly involved in increasing and decreasing insulin. Patients with diabetes are commonly melatonin deficient, and their biological clocks are disturbed, which makes them resistant to insulin and intolerant to glucose. Medical specialists hope that further studies will prove the capacity of MT therapy to restore insulin production together with the internal clock;
• melatonin alleviates the signs of aging, e.g it reduces oxidative damage and protects skin from the hazardous impact of ultraviolet rays. MT administration stopped hair loss in men and women, and the animals tests showed the efficacy of melatonin to improve bone health in old rats;
• antioxidant action of the night hormone improves the sexual health of men and women. In males, it prolongs the life of the semen cells, and it increases the sperm number and overall quality. In females, MT dosing promotes the maturation of ova. Thus, it improves fertility in both sexes;
• melatonin may reduce seizures in children with epilepsy, though medical circles argue about that. Different studies give different results, so further investigations must be made to prove the possible effectiveness of MT in epilepsy treatment;
• melatonin may be involved in the treatment of some neurological illnesses and speed up the recovery time after brain injuries. It induces the growth of neurons and protects them from damage, enhances the natural protection of the brain against the external malicious agents (known as blood-brain barrier), helps stroke patients restore their health and normal brain performance, and decreases trauma-induced swellings. In animal and human models, melatonin mitigated the symptoms of Alzheimer’s and Parkinson’s diseases. As both maladies cause the poor performance of MT receptors, the administration of this hormone was implemented. Doctors observed better sleep and overall state of their patients;
• this indolamine helps with gastrointestinal disorders, improves the function of the thyroid and basal glands in menopausal women, works as a painkiller in certain conditions, treats chronic kidney and liver diseases, and produces many other beneficial effects.

This is not all, but it is better to stop here, otherwise this review of melatonin will turn into a medical encyclopedia. New studies are going on, and in a year or two we will know about some novel uses of melatonin drugs.

Side Effects

Melatonin is considered to be generally safe when used carefully and within the limits of the recommended dosage. There have been cases of melatonin administration for 2 years in a row with no adverse reactions.

Regardless, several side effects are possible, and you have to inform your doctor and probably discontinue the medication if you experience one of the following problems:

• nightmares and vivid dreams;
• chronic headache and dizziness;
• ingestion disorders;
• low libido;
• bad mood, tiredness, daytime sleepiness and irritation.

All drugs have strict contraindications, and so does melatonin. Avoid driving and operating machinery a couple of hours after MT administration. Pregnancy is not the right time to take any medications of which the effects that have not been fully studied. Expectant and breastfeeding mothers should not take hormonal preparations without consulting a doctor. Melatonin is contraindicated to people with restless leg syndrome and bleeding disorders.

In general, there is a good rule that fits all situations — if you have any health issue, you should talk to your health adviser before taking any medication, including melatonin. We told you already that it influences lots of processes in our bodies, and the misuse of such preparations may aggravate the problems you try to solve. Do not try to treat diabetes, epilepsy, or hypertension on your own, as you can make things worse.

Interactions with Medications

Melatonin can increase or decrease the action of certain medications, or work improperly if taken with some other preparations:

• you should never use melatonin supplements with sedatives and tranquilizers. These drugs cause similar effects, and the results of their interactions can be dangerous;
• caffeine, on the contrary, neutralizes the action of the sleeping hormone;
• taking melatonin with hormonal contraceptive medications may elevate the risk of MT overdose and side effects. The same happens with antipsychotics and antidepressants;
• anticoagulants, beta blockers, and antihypertensives taken with melatonin may dangerously increase their action;
• drugs for diabetes should not be taken together with MT as they can result in poor efficiency of the drugs.

The best advice for all occasions stays the same — seek medical help before you start taking new medicines. By the way, if you are going to have some fun and intend to drink alcohol, it is better to skip a dose of your daily melatonin. Together with liquor, it can put you to sleep in the middle of the party.

Melatonin Dosage

No matter how safe it is, melatonin can cause overdose, and you will know it by feeling constantly groggy, which is known as “melatonin hangover.” You may also face the enhanced adverse reactions of your organism on MT treatment, and in this case you should consider a lower dosage. All products have instructions included in the package, so you can read the guidelines and follow them.

The common max dose of MT for children and adults for oral administration is 5 mg per day. Usually, physicians do not recommend taking more as it can cause more harm than good to your circadian rhythm. Still, there are some exceptions. The minimum effective amount of the medicine is 0.3-0.5 mg. Between these measures, melatonin is often taken for sleeping disorders, insomnia, and delayed sleep onset. Blind people can take more, up to 10 mg 60 minutes before going to bed. If you have had your natural sleep-wake cycle disturbed with some external circumstances, you can take 2 mg in the evening daily, and increase this dose to 12 mg for a short period to have a quicker effect. Jet lag symptoms are alleviated with 0.5-3 mg of MT taken for a couple of days after the arrival in the new place. To treat hypertension, people take up to 3 mg daily for a month.

Melatonin and Mood

Melatonin receptors seem to take part in mood regulation. For instance, they perceive the feeling of anxiety and can alleviate it. A group of doctors from Spain were looking for the remedy that could help their patients discontinue other sleeping pills without severe withdrawal. Usually, people, especially senior patients, experienced anxiety and depression after they stopped using soporifics. Melatonin not only minimized problems with sleep in the examinees, but it also improved their behavior and emotional state.

The hopes for MT effectiveness for depression are also based on clinical findings that the individuals with mood disorders, in most cases, happen to have a malfunction in the melatonin production. Their daily rhythms are disrupted and this seems to exert the depressive effects. Measuring the MT concentration in saliva at night and in the morning, doctors can diagnose depression and apply necessary medication, which can be melatonin, too. It was noted that when the sleeping cycles and sleep quality are back to normal, people have better mood and overall well-being. Thus, MT drugs exert a powerful antidepressant action.

The major problem of melatonin drugs for anxiety and depression is that they can be taken only in the second half of a day, otherwise they only make the problems worse. Pharmacists wanted to create a synthetic preparation with the same effects, but longer half-life and more profound effects. It had to be the MT receptor agonist, meaning that it had to activate the MT1 and MT2 receptors and be of the same structure. In the first decade of the 21st century, one such MT analogue was developed in Israel. Neurim Pharmaceuticals Ltd. created the novel drug piromelatine, and in 2010 it was tested on rats. The researchers compared its effects to melatonin. The MT agonist performed the anxiolytic and antidepressant action regardless of the time of administration, while melatonin worked properly only if used in the afternoon.

Melatonin As a Natural Sleep Aid

For now, melatonin is mostly used as a sleeping aid. Not in vain, we must say, as it is much safer than most hypnotic drugs. Lots of people have concerns about sedatives, as they cause dependency and the info about their precautions is basically wallpaper! MT, on the other hand, is natural for our bodies, and all you need is to be careful with rates and methods of administration. This is why individuals all over the world prefer it over pharmaceutical soporifics. If you do not exceed the recommended dosage, even long-term administration will not cause any withdrawal, tolerance, or addiction, and insomnia will not come back with time.

There are drugs, like Circadin, with a prolonged-release dosage, where the active constituent gets into the bloodstream gradually. Such pills can be used in patients with primary insomnia, and they work much better than their immediate-release analogs. The daily 2 mg administration alleviates insomnia, configures the inner clock, and combats the day-time fatigue and sleepiness. This is one of the most essential benefits of melatonin — you not only can sleep better, but also feel more alert and wakeful in the morning. With the help of this drug, you get additional energy for daytime activities.

Except pills from the local pharmacy, you can buy the MT dietary supplement in various online drugstores. Some of the bestsellers are:

• Melatonin P.R. by Douglas Laboratories, 3 mg of modified-release melatonin in each pill;
• Melatonin by Now Foods, for sleep, gastrointestinal support, and protection from free radicals. Each capsule contains 3 mg of the drug;
• Natrol represents Melatonin Time Release tablets, which work all night and provide a long and restful sleep. The pills include 10 mg of vitamin B6 and 5 mg of the chief ingredient;
• the brand Puritan’s Pride offers super strong capsules with 10 mg of the immediate-release MT;
• Nature Made manufactures the capsules that include melatonin and calcium, which is also a very popular combination.

These are only the top supplements on the web, but the choice of MT preparations is huge, for every need and budget.

Alternative Treatment of Sleep Disorders

Yes, melatonin can help you feel alert during the day, but this is just its secondary impact, simply a consequence of enhanced sleep quality at night. Sometimes, it is not enough. There are a lot of people who need pills which promote vigilance and concentration. They also are meant to treat sleeping disorders, but the approach to the problem from a different angle. Eugeroics help you stay active during the day, so that when the night comes all you can think about is resting your head on a pillow. They increase dopamine (DA), an important neurotransmitter that provides motivation, alertness, and energy, and enhances brain activity. Normally, when melatonin is high — dopamine is low, and vice versa.

Thus, increasing DA during the day when you need to stay active is a good thing to normalize the sleep-wake cycle. If, for any reason, you had to stay awake at night, eugeroics will help you get through the next day without dozing off at the work table. Provigil and Nuvigil are the best-known and reputed medications for daytime sleepiness, as their effects are clinically proven, and they are certified by FDA (the Food and Drug Administration, USA). These tablets belong to the Schedule IV controlled substances, meaning that they are generally safe, but you need a prescription to buy them, which is not always convenient. Doctors prescribe drugs strictly according to their on-label indications.

In the ModafinilXL online pharmacy, you can improve your working and learning productivity, as well as enhance vigilance, memory, and thinking without undue bureaucracy. We do not require prescriptions, yet we recommend at least talking to a health specialist before starting to take the drugs. We recommend you to try the generic drugs with the same active compounds — Modafinil for Provigil and Armodafinil for Nuvigil — and with the same effectiveness. The only difference is their price, which is surprisingly wallet-friendly. One 200 mg Modvigil tablet costs less than a dollar in ModafinilXL, which is much cheaper than a branded drug. So, why pay more? In our drugstore, you can find such pills as Waklert 150 mg, Artvigil 150 mg, Modalert 200 mg, and others. If you are not sure, we suggest you consider our best offers — a combo pack with all tablets we market for the lowest price, or the free trial pack of modafinil or armodafinil tablets to see which suits you better.

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