Why Is Melatonin Overdose Not A Prominent Risk During The Treatment Of Insomnia?

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Written by:


, Sleep Researcher
Last Updated: Sun, November 25, 2018
Fact checked by:

Marko Jevtic

, Sleep Specialist

The human body may not be a mystery anymore, but the complex biochemical reactions that regulate our metabolisms sometimes throw the scientists and doctors in frenzy. Most of our body’s functions depend on chemical messengers, also known as  hormones. They form a part of the endocrine system along with the several glands that produce these hormones.

Some of these hormones are ubiquitous among all mammals. It signifies their importance in the maintenance of homeostasis in the mammalian body. One hormone, in particular, is present in the plant system as well. Melatonin or N-acetyl-5-methoxy tryptamine is the first line of defense in plants against oxidative stress. In animals, this hormone regulates the circadian rhythm. Calling it a part of the circadian clock is an understatement since it plays crucial roles in the maintenance of blood pressure, reproduction, and the sleep-wake cycle.

Several organ systems in the human body are directly or indirectly dependent on this hormone. It elicits these responses by binding with the melatonin receptors and sometimes it mediates biochemical mechanisms by functioning as an antioxidant. In its medicinal form, it can treat insomnia or delayed sleep onset. It is a multifunctional compound that acts as a neurotransmitter and a neurohormone. Melatonin is also a neuro-protector that prevents cell damage by working as a potent anti-oxidant.  

Scientific evidence points towards a successful long-term treatment of sleep deprivation in adults and children with melatonin. In the US, Europe, and Canada, you can buy melatonin supplements over the counter. Other countries may require a prescription from a doctor.

Why is Melatonin Overdose Uncommon?

At present, medical professionals rely on melatonin for the treatment of delayed sleep phase syndrome and insomnia. It can mediate the circadian rhythm and advance the sleep onset period.

Melatonin is a hormone that occurs naturally in the human body. The level of the hormone varies from one person to another, but it is not a foreign compound our system has to encounter. Interestingly, the effective dose of the supplement differs considerably between people. It can depend on many factors including age, daytime physical activity, and other medicinal interactions. Therefore, pointing out a melatonin overdose from a blind study is quite impossible.

In short, experts often state that overdosing on melatonin is impossible. However, taking them beyond recommended levels can elicit unpleasant and disruptive side effects. Sometimes, using this supplement for an extended period can result in dependence and habituation. People are also likely to experience a hangover effect from the regular use of melatonin supplements.

How Does Melatonin work in Treating Insomnia?

Today, about 70% of adults in the US report disturbances of sleep quality and duration. Some of them report their inability to fall asleep during designated bedtime for over a few months. Insomnia is the difficulty in falling asleep or staying asleep during the night. People with insomnia do not experience restorative sleep. The symptoms include low energy, fatigue, mood disturbances and decreased productivity. Although the primary symptoms are similar, there are two broad classifications of this sleep disorder.  

Insomnia in the chronic form can be a result of co-morbidity. Understanding the cause-effect relationship between the two issues is quite impossible, leading to complexity of possible treatment options.

A person’s response to light and darkness depends on his or her circadian rhythm. Melatonin mediates the light and dark response. Light or dark information stimulates a pathway that leads to the suprachiasmatic nucleus (SCN) of the hypothalamus. As a response to light, it signals the pineal gland that switches on melatonin production and its release into the bloodstream. Serotonin, a tryptophan derivative, is the precursor to melatonin. The pineal gland is the site of conversion of this hormone to melatonin. Several theories state that the high level of biochemical activity of serotonin might depend on its ability to generate melatonin.  

The usual production of melatonin starts at around 9 pm. In case of an average metabolism rate, the level of the sleep hormone increases sharply, and you should feel sleepy by 11 pm to 12 am. The effect of high levels of this compound remains in the blood for over 12 hours, and the levels start dropping in the morning. By 9 am, the presence of melatonin in blood is barely detectable and remains so throughout the day. The activity peaks at around 3 am, which is when people have the most profound sleep. In children, melatonin levels are higher than in adults. That is one of the reasons they need more extended periods of restorative sleep.  

Melatonin is the “hormone of darkness” that promotes the onset of activity in nocturnal animals, and it fosters sleepiness in the diurnal ones. Hijacking this hormonal pathway can give us control over the amount of sleep and quality of rest. Researchers and scientists have been working for years to perfect the dosage and design of melatonin supplements that can mediate sleep pathways and suppress the symptoms of insomnia in the population.

What is the Correct Dose of Melatonin?

Young children should avoid taking melatonin unless a specialist recommends use. Doses as low as 1 milligram and 5 milligrams can cause seizures in children. People’s sensitivity to melatonin varies according to metabolism and underlying physiological conditions. Overdosing on melatonin is highly unlikely, but adverse effects start manifesting in doses in the 30 mg range.

An adult should always start with a safe beginner’s dose around 0.2 mg and 5 mg. That is the lowest dose range that is both effective and safe in adults. Determining the correct dosage can be complicated since it varies with body weight, BMI, age, and sensitivity. Although in several countries it is an OTC product, you should always consult your physician and a sleep expert before beginning melatonin treatment.

What are a Few Things About the Sleep Hormone you Should Know?

Starting sleep medication can bring a lot of changes in your lifestyle. Melatonin is a hormone and taking supplements to increase its level in your system can have many side effects. It can affect your sleeping hours, diet, productivity and daytime temperament.

There are several facts about it you must know before you start taking it. Here are the ten points about melatonin that can help you understand the treatment, contraindications and positive effects of it.

  1. Our pineal gland produces this hormone as a response to the light receptors in the retina. This pathway is present in all mammals, but it works differently for nocturnal and diurnal species. Its primary function is to mediate the sleep cycle by monitoring the activity of the clock genes.
  2. This darkness hormone is the natural pacemaker of the body. It can signal the body about the time during the day or the time of year. It regulates the internal clock of the body.
  3. Melatonin supplements adjust the internal clock of a person. It can help you fall asleep faster and stay asleep for 8 hours. People, who do not experience therapeutic sleep benefit from taking melatonin supplements.
  4. It is also a short-term treatment for shift working, jet lag and sleep deprivation. Long-term use of this compound can cause complications.
  5. Blue light from LEDs and smart devices can hamper the effectiveness of melatonin. You can think of blue wavelength light to be its arch nemesis, and the presence of this light makes it more challenging for people to fall asleep.
  6. Therapists and doctors often recommend the use of red light in the ambiance to complement the effects of melatonin. They have the least impact on shifts in circadian rhythm and changes in melatonin levels. They are the perfect choice for bedroom lighting and night lights.
  7. This hormone plays a vital role in the regulation of menstrual cycles. Increased levels of melatonin can suppress the synthesis of luteinizing hormone and delay the release of the ovum from the ovary. It can interfere with the frequency, duration, and onset of the menstruation cycles.
  8. Doctors prescribe melatonin for the treatment of developmental and learning disabilities including ADHD and autism. The efficacy of the procedure can vary considerably depending on the severity of the challenge.
  9. Melatonin and cortisol are antagonists. As the level of the former hormone declines, cortisol levels in the blood increase. It increases as the person wakes up. Therefore, in especially stressful times, people experience an imbalance of the cortisol and melatonin activities causing extended periods of wakefulness and daytime sleepiness.
  10. Blind people cannot receive light and dark signals. Therefore, it becomes necessary to modulate their circadian rhythms from the outside with the help of supplements like melatonin that can restore the circadian rhythm.

What Can Qualify as Melatonin Overdosing?

Taking too much melatonin is possible. Usually, repetitive doses above 30 mg can disrupt the sleep-wake cycle in adult individuals. While defining a standard overdose limit for this supplement is impossible since there is no usual safe dose for everyone. However, it is indeed possible to experience at least one or several unpleasant side effects of the medicine.

Doctors usually recommend a dose between 0.2 mg and 20 mg for adults. Several patients take more than the prescribed dose without any severe side effects. In case, your regular treatment of supplements has stopped working, you should speak with your doctor.

If you are thinking about taking a higher than the regular dose of melatonin to boost your sleep onset and duration, you might not get the desired results. Research shows that the half-life of this ingredient is about 50 minutes. That means it exists in the blood only for about 50 minutes before dissipating. There is no chance of improving your sleep quality or duration by increasing the dose of melatonin. Instead, you might wake up with a sullen mood and a bad “hangover.”

What are the Symptoms of Melatonin Overdose?

Studies on proven cases of melatonin overdose show that too much of the substance can have undesirable effects that are contrary to the desired purpose. Too much sleep hormone in your system can make it harder for you to fall asleep. An overdose of melatonin is rarely lethal, but it can leave you groggy and irritable the next day. It can also cause vivid nightmares and bizarre dreams that may make sleeping at night extremely difficult.

In addition to these, you might also experience the following symptoms.

  1. Dizziness
  2. Nausea
  3. Irritability or anxiety
  4. Joint pain and back pain
  5. Stomach cramps and diarrhea
  6. Headaches and wooziness

In fact, some even suffer from the sudden elevation of blood pressure. Taking a supplement without expert advice is not smart. You should always consult your GP and cardiologist if you are taking beta blockers and calcium channel blockers for your cardiac problems.

These side effects are usually ephemeral, and they go away within a day. However, the dizziness, excessive daytime sleepiness, physical pain and headaches can pose a high risk of accidents and bad decision making during the next day. It is unlikely for melatonin to cause symptoms of an overdose on its own, but consumption with alcohol and opioid can elicit severe reactions.

With which Medications and Substances do Melatonin Interact?

Naturally occurring organic compounds have a broad reactivity range. Same is true in the case of melatonin.

  1. The supplement interacts with CNS depressants aka sedative medication. Both of them cause drowsiness and dizziness. Therefore, taking the two drugs together can double the effect. Never take melatonin with clonazepam, lorazepam, zolpidem, and Phenobarbital.
  2. Caffeine elicits interactions with melatonin since the wakefulness stimulating compound can decrease the effectiveness of the hormonal supplement.
  3. Fluvoxamine also interacts with melatonin from time to time. The former increases the amount of the hormone supplement that body absorbs. Consuming them together increases the side effects of the hormone.
  4. Diabetes medication can also react with the supplement. The sleep hormone can increase blood glucose concentration by decreasing their affectivity.
  5. Birth control medication also interacts with this medication. Therefore, speak with your gynecologist and your sleep expert before starting melatonin therapy.
  6. Anti-histamines and immune system suppressants interact moderately to strongly with the natural hormone supplement. Taking it with immunosuppressant can decrease the immunity suppressing the effect of the medications.  
  7. Melatonin interferes with the blood clotting mechanism and the anti-coagulant medication that doctors prescribe for patients suffering from a high risk of thrombosis. The supplement can increase a person’s chance of bleeding and bruising.
  8. All kinds of benzodiazepine compounds react with melatonin.
  9. The medication reacts mildly with flumazenil. The latter compound decreases the effectiveness of the supplements.

How to Avoid Melatonin-alcohol Interaction?

Many of us enjoy the occasional drink after a long day at work. A little alcohol does not affect our health adversely, in fact, it helps us relax and prepare for the next day’s battle. However, is one shot of whiskey or a pint of beer as harmless when you combine it with melatonin therapy?

A combination of melatonin and alcohol is potentially dangerous since liquor can rid your body of melatonin quickly. Although alcohol acts as a sedative, it interrupts your sleep cycle. It can worsen symptoms of sleep apnea and non-restorative sleep. Here are a few of the adverse side effects you might experience if you combine the two.

Combining the two can cause swelling of your extremities, excessive sweating, flushing, and delusion, breathing trouble and fainting. In case you have consumed alcohol and melatonin together, you need to speak with your physician immediately.

To avoid all the trouble, you need to plan your evening. Spread out your socializing so that there is a 2 to 3 hours gap between drinking and your medication. Of course, the duration of wait will depend directly on the amount you have had to drink. Try to stick to 60 ml to 80 ml alcohol for the time you are on the new medication. Since melatonin is only a short-term treatment, this kind of restriction should not disrupt your social life for long.

What are the Top Benefits of the Neurohormone that are Enough to Overrule the fear of Melatonin Overdose?

The FDA does not monitor the quality standards of melatonin. Nonetheless, millions opt for this OTC nutritional supplement from time to time. Why is it so? Why do people keep going back to melatonin, if it poses many risks and threats? It is Completely Natural

Unlike the benzodiazepines and non-benzodiazepines, melatonin supplements are au naturel. Sleep trouble goes away once you bring this natural supplement into the scene. It can “fix” disrupted circadian rhythms and make up for low melatonin synthesis in the body.

It is instrumental in treating insomnia and delayed sleep onset syndrome in the ages 55 years and older. New, prolonged release formulations are ideal for the treatment of primary insomnia in adults.

It is a Potential Treatment for Prostate Cancer and Breast Cancer

By now, we know that melatonin interacts with the hormones of the reproductive system. That makes us wonder if this compound can treat diseases of the reproductive system as well. Several in vitro studies involving mammalian (human) breast cancer cells show that it can inhibit the growth of tumor cells.

The scientists reproduced the same survey in a mouse model (in vivo). That promises a potential treatment for common hormone-resistant breast carcinoma. At the same time, studies involving prostate cancer show that melatonin levels are much lower in people suffering from prostate carcinoma than in the healthy (control) population. Melatonin can actively inhibit the growth and proliferation of prostate cells in vivo.

Helps Deal with Menopause

All women go through several physiological changes in life. During puberty, the first couple of years go by trying to adjust to the monthly cycles that bring a surge of hormones, cramps, leg pain, nausea, and bleeding. 40 – 45 years after the initiation of the menstrual cycles begins the menopause phase, where an annoying period starts once again. Only this time, the cycle is more ruthless, and it brings forth hot flushes, joint pain, skin irritations, mood swings and hunger cravings.

Several studies involving menopausal and peri-menopausal women and melatonin show that it can lead to the recovery of thyroid and pituitary functions. It is a promising find since a natural compound can finally help with the restoration of post-menopausal health and redressal of menopause symptoms.

It Can help Tackle Fibromyalgia

Imagine living in pain 24/7 without any specific reason. You don’t have to imagine, in case you have fibromyalgia. This disorder involves the severe pain of connective tissues and muscles, all over the body, without any specific cause.

Research over the last few years shows patients taking melatonin supplements to experience decreasing pain and discomfort. The group that took melatonin in combination with fluoxetine (antidepressant) experienced faster improvement. Further research shows that people, who suffer from chronic migraines may benefit from melatonin treatment.

It can Strengthen the Immune System

While we have already asked you not to take immunosuppressant with melatonin, you need to know the reason. The latter increases the strength of the immune system. You can think of it as the “immune buffer” that can act as an anti-inflammatory, anti-infection and immunity boosting agent.

Research points towards the use of melatonin in the treatment of localized infections and edema. The effectiveness of this powerful anti-oxidant in the treatment of systemic infections like septicemia creates a promising future for viral and bacterial immunotherapy.

It can Effectively Reduce the Symptoms of Jet Lag

Jet lag does not fall under the category of delayed sleep or advanced sleep onset disorders or insomnia. Jet lag occurs when you have traveled from one part of the world to another, and your internal clock is not in sync with the external clock.

Documented research shows that 9 out of 10 trials for the “treatment” of jetlag with mild doses of melatonin were successful. It helps people adjust faster to the new external clock, without disrupting their inherent circadian rhythms. As per the research data, doses between 0.5 milligrams and 5 milligrams work well for re-syncing the internal clock.

Melatonin can Help children with Developmental Issues Like Autism

As per a recent publication in the Scientific American, autism levels are on the rise in the US. It may be due to the increasing levels of awareness among the parents and the evolution of better methods of diagnosis in the mainstream, but the research on developmental issues in children are also on the rise.

According to a Developmental Medicine and Child Neurology publication from 2011, 35 individual studies on the effects of melatonin on autism spectrum disorders including Rhett Syndrome and Asperser’s Syndrome show that supplementation of the “sleep hormone” can help with improvement of daytime behavior and better night-time sleep quality.

Helps with Bladder Dysfunction

Bladder dysfunction is quite common among women who have undergone a hysterectomy and in older men. People with bladder problems often suffer from elevated levels of malondialdehyde.

Melatonin helps reduce oxidative stress in the body, and it combats bladder dysfunction. This natural hormone supplement can help you deal with an overactive bladder by lowering the stress elevating hormone malondialdehyde.

It can Reduce Tinnitus

If you have been hearing an annoying buzzing or whirring noise in your ears for some time now, you must already know that modern medicine does not have too many pharmaceutical or surgical cures for it. Tinnitus is an age-old problem for all ages that can be ephemeral or quite permanent. It can even lead to depression, anxiety and constant irritability in adults or children.

Modern research in medicine and diseases shows melatonin to be effective against tinnitus in all ages. Taking 3 milligrams of melatonin for 30 nights in a row can reduce the symptom of tinnitus in adults. It also helps in improving the sleep quality in the same patients.

It is an Excellent Stress Buster

There is no better way to tackle job-related or any other stress in life than getting a good night’s rest. However, only some of the most privileged souls of the world get to sleep each night soundly. Resting has become an unachievable dream for the most of us unless you have access to the natural sleep hormone nutritional supplements.

It controls the levels of cortisol (decreases) that can relieve the stress symptoms in your body. Melatonin is an effective natural way to unwind, relax and get a good night’s rest before your body goes into a fatigue-shock.

It can Also Help Treat Heart Conditions

In 2018, you would be surprised to hear about an adult, who does not have any heart troubles. The surmounting stress and promotion of unhealthy lifestyles can take a severe toll on your cardiac health.

The lack of enough melatonin secretion in your system will increase your blood pressure and create severe pressure on the arteriolar and ventricular walls, and the heart valves. Melatonin supplements can actively reduce the blood pressure and protect the heart. It may even treat cardiovascular diseases.

Where Does Melatonin Occur Naturally?

Melatonin is a natural dietary supplement in the USA, as per the directives of the Food and Drug Administration (FDA). It is an OTC product in Canada and the US. Therefore, the restrictions and regulations applicable to medications are not relevant to melatonin (nutritional) supplement.  

There are several food items including fruits, vegetables, seeds, herbs and cereals that contain high levels of the neurohormone. For exampl, bananas, grapes, grains, malt beer, olive oil, plums, rice, and plums contain melatonin. Research shows that when we consume oranges, pineapples, bananas, and grapes our blood melatonin levels increase significantly.

Sticking to a diet of rice, rolled oats, barley, walnuts, sunflower seeds, flaxseed, mustard seeds, peanuts, tart cherries, asparagus, broccoli, tomatoes, olives, cucumber, olives, and grapes is the best way to improve your sleep quality naturally. These are natural reserves of the neuro-protector hormone. Staying away from fatty food and caffeine will help you enjoy the sleep-inducing effects of these foods.

What else Should you Know and Remember About this Darkness Neurohormone?

Earlier, scientists and pharmaceutical companies synthesized melatonin from the bovine pineal tissue. Right now, almost all pharmaceutical companies across the US and Canada produce it synthetically. It reduces any chance of cross-infection and anaphylaxis that was prominent in animal tissue-based cultures.

Several food manufacturers and beverage brands sell melatonin-rich products via grocery stores and departmental stores in different parts of the US and several European nations. Nonetheless, it remains a critical neurohormone and does not become a natural additive in your food. Always check the labels of the melatonin nutritional or dietary supplement you buy for the level of the compound present in the total quantity of food or drink.

Although you may find these supplements outside pharmacies, at your favorite departmental store, you should consult your doctor to lessen the chances of any contraindications. It is imperative in case you are consuming heart medicines, diet pills, birth control pills, anticonvulsants, antidepressant or anti-anxiety medications.

Melatonin supplements can be of various types and powers. Your doctor, psychiatrist and sleep expert can help you determine which one is the right concentration depending on your age, BMI, weight, and other health conditions. Therefore, it is neither smart nor advisable to treat sleeping disorders in children with over the counter melatonin “nutritional” supplements.

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