Melatonin Supplement Facts and Effects

Sleep is one of the most important functions for humans. Sleep is often considered essential than food because it helps our body repair and heals itself. Without sleep, our energy resources get depleted, our brains fail to function normally, and our productivity suffers. Lack of sleep over an extended period also leads to various kinds of health ailments.

More important than sleep itself is the sleep-wake cycle. Although sleep is necessary, it doesn’t mean a person can sleep at any time during the day. For instance, it isn’t all right to stay awake at night and sleep at work. Feeling sleepy when the person is supposed to stay awake is a sign of lack of sleep, and may even indicate a sleep disorder. Excessive sleepiness is also one of the biggest causes of road accidents.

Lack of sleep is often caused because of a busy work schedule and lifestyle. But in some cases, it could also be because of an underlying disorder. Sleep disorders often go undiagnosed, but in order to understand sleep disorders, we have to understand the factors affecting sleep.

What Is the Role of Sleep Hormones?

The normal sleep-wake cycle in living is called the circadian rhythm. In humans, this cycle is influenced by hormones to a great extent, and also adjusted according to external cues. Daylight is often the biggest cue for the human brain to wake up and get to work. In nocturnal beings, like owls and bats, daylight indicates its time to go to sleep. These cues generate from the hypothalamus of the forebrain and naturally synchronize or reset according to the 24-hour rotation cycle of the Earth.

The most important hormones affected by this natural sleep-wake cycle are melatonin and cortisol. Melatonin is entirely dependent on the circadian rhythm. Produced in the pineal gland in the brain, this hormone lowers body temperature and causes drowsiness, indicating it’s time for sleep.

Since humans are diurnal beings, they are supposed to be naturally active during the daytime and sleep during the night. For sleep to occur at the right time, the production of melatonin is highly important. Melatonin normally is produced between 8 pm and 9 pm and stops being produced between 7 am, and 8 am in the morning. This period clearly marks the time when we should be ending the day’s work and getting ready for bed.  Melatonin is absent (or minimal) during the daytime.

How Does Melatonin Work?

Simply put, melatonin is the hormone responsible for drowsiness and sleep. It is what makes us tired and sleepy and indicates its time to rest. Melatonin is the hormone that regulates the sleep-wake cycle. Because melatonin production is absent during the day, the brains understand it has to stay awake and active. Melatonin production signals to the brain that it’s time for sleep, whether it’s day or night.

A vital factor in sleep regulation is exposure to light or darkness. When we are exposed to bright lights, a special region in the hypothalamus called the suprachiasmatic nucleus (SCN) sends a signal to other parts of the brain that it’s time to get up and be active. This includes a rise in core body temperature and the release of the stimulating hormone cortisol. During this phase, melatonin production is absent.

Melatonin is often called the Dracula of hormones because it is produced only after dark. Even artificial bright lights have been found to hinder the production of melatonin. Most sleep problems are caused because of disrupted melatonin production, although it is hardly diagnosed. In fact, the primary cause for sleep disorders is always something related to melatonin levels.

What Causes Excess Melatonin Production?

As we have already seen, normal melatonin production is what sleep depends on. A person with a healthy sleep-wake cycle has normal melatonin levels. But quite often, people may suffer from abnormal melatonin levels, leading to various sleep and hormonal disorders. Since melatonin is a hormone, it is interconnected with other hormones in the body. When melatonin production is disrupted or elevated, the rest of the hormones are also affected, resulting in various disorders of the system.

An elevated level of melatonin isn’t unusual. In fact, a lot of people suffer from naturally elevated melatonin production. This is most noticeable during certain times of the year. An increased melatonin level is characterized by sleep disturbances and extreme tiredness. Other symptoms of elevated melatonin levels include:

• Difficulty waking up in the morning
• Excess daytime sleepiness
• Fatigue and lethargy
• Low body temperature
• Depression and anxiety
• Foggy memory

What Affects Melatonin Production?

Too Little Sunlight

Spending a lot of time away from sunlight has been found to cause elevated melatonin levels. This is most noticeable in the darker months of winter when there is little sunlight around. This is when melatonin production rises because the brain thinks it is always time for sleep. An elevated level of melatonin is the biggest reason behind seasonal affective disorder (SAD), most noticeable during autumn and winter when days are shorter and darker.

Liver Dysfunction

Like all hormones, melatonin is also metabolized in the liver. If there is an excess of any hormone, the liver helps eliminate it from the system. But when the liver function is abnormal, it hinders the removal of the excess hormone from the system. This is why liver dysfunction can lead to an increased level of melatonin in the system, causing excessive sleepiness and fatigue during the daytime.

High Intake of Vitamins B3 or B6

Low levels of vitamins B3 or B6 are often responsible for lack of sleep. But when the intake of these vitamins becomes more than normal, it can lead to excess melatonin production.

Antidepressants

Certain antidepressants mimic sleep, causing drowsiness and fatigue. This is because antidepressants are supposed to calm down the brain and help the person sleep. Because depression makes the brain overworked and the nervous system overwhelmed, antidepressants make the melatonin production rise and cause sleep.

Once the root cause of the elevated melatonin levels has been found, it can be corrected by several means, such as spending time outdoors in the sun or improving the liver function.

What Causes Low Melatonin Levels?

This is a more common complaint, compared to excess melatonin. Decreased production of melatonin is often the biggest reason behind insomnia and excessive daytime sleepiness. When melatonin isn’t produced when it should be, it keeps a person awake even when it’s time to sleep. Sleep disturbances increase susceptibility to diseases, poor concentration and memory, and mood swings, among other problems.

Melatonin production decreases as people age. This is why older people sleep less than younger people. But owing to busy schedules and modern lifestyle, several people often suffer from a lack of melatonin.

Excess Exposure to Daylight: In summer when there is abundant sunshine, people often love to sunbathe or spend more time outdoors. This has a negative effect on melatonin production. Because of the excess exposure to natural light, melatonin production is reduced, and sleep is affected. Spending more time outdoors in the sun makes people more active because of the suppressed melatonin.

Excess Exposure to Artificial Light: Those who spend long hours in front of a backlight device, often complain of lack of sleep. This is because the artificial lights hinder melatonin production. Artificial light mimics sunshine and signals the brain that it should remain alert and awake. Watching late night TV, working long hours on the computer, or spending too much time on the phone are all reasons for lower melatonin levels.

Lack of Serotonin: The well-being and happiness hormone serotonin is directly related to melatonin. A neurotransmitter and the precursor to melatonin, serotonin is first acetylated in the pineal gland, and then methylated to produce melatonin. When serotonin is low, melatonin is also low.

Medications: Certain medications are known to hinder the production of melatonin. For instance, beta blockers, which control heart rhythm and reduce blood pressure, often lead to sleep disorders because of decreased melatonin levels. This is because the adrenergic beta1-receptors are inhibited by the medication. Many medications for neurological ailments also lead to sleeplessness because of lower melatonin levels.

Caffeine and Alcohol: Melatonin is produced by neurotransmitters in the brain, which can be affected by consumption of caffeine and alcohol. Excessive consumption of caffeinated or alcoholic beverages close to bedtime affects the melatonin-producing neurotransmitters and causes sleep issues. Those who suffer from sleep disorders should always avoid drinking these beverages close to bedtime.

Exercising Late in The Evening: For some people, exercising late in the evening or before bedtime has been found to cause sleep disorders. This is because exercising increases heart rate and metabolism, and hinders the melatonin level.

Stress: While stress can take various forms, one thing it always does is increase the level of cortisol. As already mentioned earlier, cortisol and melatonin are directly affected by the sleep-wake cycle. Also known as the hormone behind stress and inflammation, cortisol significantly reduces the production of melatonin. The higher the level of cortisol, the lower the level of melatonin. In people with a lot of stress, melatonin production is greatly reduced, leading to problems like insomnia, fragmented sleep, and changes in appetite and mood. If stress is the reason behind lack of sleep, then cortisol levels need to be lowered first.

What Are Melatonin Supplements?

Sleep disorders are more common than we think, and because they are uncomfortable and cause significant stress to the sufferer, people are ready to try anything that promises a good night’s sleep. Sleep aids are routinely administered by healthcare practitioners to people who suffer from sleep-related disorders. While sleep disorders can be caused by several factors, including sleep apnea, snoring, and other neurological problems, the ones caused by low melatonin levels are often treated with melatonin supplements.

When our bodies are unable to produce sufficient amounts of necessary hormones naturally, they have to be supplemented externally. For instance, those who don’t produce sufficient levels of progesterone or testosterone often need to go for hormone replacement therapy. It is quite similar in the case of melatonin. Supplements are available in the form of pills, liquids, or chewable tablets, either natural or synthetic.

How are Melatonin Supplements Made?

As mentioned above, melatonin is either natural or synthetic. Natural melatonin is what is produced naturally in the body, by the pineal gland. However, the supplements available in the market aren’t exactly natural. Melatonin supplements have been available since the 1990s. Back then, it was specifically used to treat primary cases of insomnia in those above 55 years of age. Because melatonin production drops as people grow older, melatonin supplements were seen as a natural way to keep the hormone level normal and regulate sleep. But these days melatonin is used more like a sleep aid by anybody and everybody because it’s thought to be natural.

Melatonin supplements are actually synthetic melatonin produced in the laboratory under controlled conditions. This was first done in 1958 by A.B.Lerner. In the laboratory, melatonin can be produced in a number of ways. It can be produced by reducing 5-methoxyindole-3-acetonitrile with Ethanol and Sodium. The resultant product is acetylated using acetic anhydride and glacial acetic acid. Most of the melatonin supplements sold around the world are actually from chemically produced melatonin blended with an inert carrier.

The question is: why chemically produce melatonin when it is naturally available? This is because natural melatonin is taken from the pineal glands of cows. Natural usually means “good” as opposed to chemically manufactured, but melatonin taken from natural sources is usually contaminated with bacteria, viruses and abnormal proteins called prions, which do more harm than good. It must also be noted that melatonin chemically produced in the laboratory is identical to natural melatonin in our bodies. There is no chemical difference between the two.  Synthetic melatonin is pure and free from impurities and biological contaminants.

Who Should Take Melatonin Supplements?

Melatonin supplements have become very popular these days as an increasing number of people suffer from sleep-related disorders. When melatonin was first created, it was meant to treat insomnia in those above 50 years of age, because that is when melatonin production naturally drops. But today it is used as a natural sleep aid if people have trouble falling or staying asleep. Melatonin is also sometimes taken for other sleep problems such as delayed sleep phase disorder, where it is tough to fall asleep before 2 a.m.

Melatonin supplements are used when people have jobs that disrupt normal sleep schedule, a condition known as sleep work disorder. These supplements may also be used to treat or prevent jet lag; the tired, worn-out feeling people get when traveling across different time zones.

Melatonin is available as over-the-counter dietary supplements in the US and can be purchased without a prescription. However, in certain countries like the United Kingdom, all sleeping pill, including melatonin, is available only on the prescription of a medical practitioner. Over the counter, melatonin isn’t regulated by the FDA. It must be noted that melatonin isn’t a magic sleep aid, and work differently for different people. It is advised that melatonin is taken only after consulting a doctor.

Are Melatonin Supplements Safe?

Since melatonin is a hormone naturally produced by the body, it is thought to be safe. But anything in excess is bad for health, and the same applies to melatonin. A melatonin level of 10 picograms per milliliter during the daytime and 100 pg/ml after dark is normal. Any more or less than this level can cause sleep disruption and other problems.

Although melatonin has fewer side effects compared to sleeping pills, there are few things to keep in mind before reaching for the over-the-counter melatonin supplement:

Melatonin can have side effects: Although minor, melatonin can have a few side effects, such as daytime sleepiness, headache and dizziness, digestion issues, anxiety and confusion, and depression. This is why melatonin supplements shouldn’t be taken continuously. It is hard to get addicted to it, but taking melatonin at a stretch for a long time can lead to excess melatonin in the system.

It interferes with certain medications: Melatonin supplements are known to interfere with certain drugs, such as anticoagulants (blood thinners). Melatonin makes blood thinner, so taking it along with anticoagulants will lead to excessive bruising and bleeding. Birth control pills are also known to produce extra melatonin, so taking the supplement along with it will cause excessive sleepiness. Melatonin also interferes with immunosuppressants. Therefore, it is best to take melatonin after consulting a doctor and letting him know about other medications you are taking.

It may not be entirely safe: Over-the-counter melatonin supplements are not regulated by the FDA, and therefore, may not have entirely safe ingredients. The only other ingredient in synthetic melatonin is the inert carrier, but over-the-counter melatonin supplements may also carry certain unknown additives. These additives can have unwanted side effects when taken in higher doses. The amount of actual melatonin can also vary in these supplements. In many cases, the amount of melatonin may be very low, and the amount of additives can be high. Not only do these supplements cause side effects but also fail to regulate sleep.

There is no correct dose: Since melatonin is not prescribed medication, there is no recognized dosage for people with sleep disorders. The patient must always consult a physician before taking melatonin, and then follow the instructions on the right dosage. The supplement should be made in a lab and not taken from animal sources, because these are more likely to have contaminants. If there are any side effects, the patient must stop taking the supplement and consult the physician.

It is not a miracle cure: When people start taking a sleep aid, they believe that it is the end to all their sleep issues. That isn’t often the case. While melatonin can help treat sleep disorders to an extent, it is not a magic cure for insomnia. It may help induce sleep, but it may not be able to help you stay asleep. This is the reason why melatonin supplements are most effective to treat the seasonal affective disorder, jet lag, cluster headaches, and helping people sleep after surgery. If a person responds well to the supplement, they can keep taking it without serious side effects, but depending upon the supplement all the time will de-sensitize your receptors and make them unresponsive to lower doses of melatonin. This will make you keep taking higher doses.

It isn’t safe for kids: No sleep supplement is entirely safe for children, including melatonin. Since children are in the growing stage, the supplement affecting their hypothalamus and pituitary glands can cause problems. Changing the normal system of their bodies with this unregulated substance can be potentially dangerous. Instead, children should be taught proper sleep hygiene to help induce sleep more easily. No supplement should be given to children without first consulting a physician.

It isn’t the only solution: Since melatonin supplements can be purchased without a prescription, it is easy to pop a pill whenever you cannot get to sleep. But that isn’t how it should be. Instead of reaching for supplements right away, consider altering your lifestyle and practicing proper sleep hygiene. If you must take supplements, consider starting with natural aids like essential oils and chamomile tea. Melatonin supplements should always be the last solution.

Can Melatonin Really Help Induce Sleep?

Although different people may react differently to the supplement, it has been found in several studies that melatonin positively affects the sleep cycle, including reduced sleep onset latency, increased sleep duration, and efficiency.

What Is the Appropriate Dosage of Melatonin Supplement?

It must be noted that excess melatonin supplement can be harmful. Only a single dose of 0.1 to 0.3 milligrams should be taken in 24 hours. This is the proper dosage, sufficient to bring the nocturnal plasma concentration of melatonin to the normal levels. Even though melatonin is largely non-toxic, it should never be taken in doses as high as 10 milligrams, because that will raise the plasma levels sixty times more than normal.

When Should Melatonin Be Taken?

Melatonin shouldn’t be taken earlier than 60 minutes before bedtime. If you want to sleep earlier than usual, you should take 0.1 to 0.3 mg of melatonin two to three hours before the desired bedtime.

Conclusion

Although melatonin supplements are easily available and very popular, they must always be taken with proper care, and after consultation with a physician. In all cases, a sleep aid should be taken only after all tried and tested measures to induce sleep have failed. A sleep physician is the best person to advise on the correct dosage and duration of melatonin supplements.