Formation of melatonin in the body
The body produces melatonin naturally primarily in the pineal gland (epiphysis) of the brain. Smaller amounts are also produced by the retina of the eye and the gut.

How much melatonin is formed and released in the body depends, among other things, on the intensity of the light in the environment. Darkness at night stimulates secretion. During the day, on the other hand, melatonin levels are about three to twelve times lower than at night. Light stops the production of melatonin.

What affects melatonin levels? The body's own production of melatonin naturally decreases with age. Low melatonin levels or melatonin deficiency can also be caused by excessive consumption of caffeinated beverages, alcohol or nicotine. Exercising in the evening and constant stress also lower the melatonin level. Another (very) rare cause is a lack of the neurotransmitter serotonin. 

In addition, medications such as anti-inflammatory drugs and painkillers from the NSAID group (such as acetylsalicylic acid or ibuprofen) can lower melatonin levels when taken in the evening. 
Conversely, a (persistently) elevated level of melatonin can be the result of longer periods of darkness and fewer hours of sunshine in the winter months. Experts suspect that this effect is related to the phenomenon of "winter blues" or "winter depression".

Some antidepressants and liver diseases can also increase the amount of melatonin in the body.

What are melatonin supplements? In Germany, Austria and Switzerland, melatonin sleep products are available for the following applications (indications):

Sleep disorders in people 55 and older: A doctor may prescribe melatonin to improve poor sleep when the sleep disorder has no physical or psychiatric cause (primary insomnia). The application is only temporary.

Sleep Disorders in Minors: Melatonin medications are approved to treat sleep disorders in children (2 years and older) and adolescents with autism spectrum disorder and/or Smith-Magenis syndrome (a rare inherited disorder). The preparation can be prescribed if other sleep hygiene measures have not helped in the past (e.g. regular bedtime).

Jet lag: In Germany (but not in Austria and Switzerland), prescription melatonin is also approved for the short-term treatment of jet lag in adults. Since March 2022 it has been considered a lifestyle drug and is therefore no longer reimbursed.

In addition to these prescription melatonin tablets, pharmacies in Germany and Austria also offer over-the-counter melatonin preparations (such as capsules, sprays or tablets) as sleep aids. However, foods containing melatonin are not permitted in Switzerland.

How is melatonin used? How many milligrams (mg) of melatonin you can take per day and how exactly you use it depends on its purpose.

Sleep disorders from the age of 55
Prescription drugs for insomnia for people over 55 contain melatonin in a dose of two milligrams. These are deferral tables, i. H. Tablets in which the release of the active substance is delayed.

To help them fall asleep, patients take a melatonin tablet in the evening after their last meal and one to two hours before bedtime. The tablet should be swallowed whole. When crushed or chewed, it loses its long-lasting release properties!
 
The melatonin preparation is not suitable for long-term use! Use in consultation with your doctor for up to 13 weeks. If you continue to have trouble sleeping, you should definitely talk to your doctor again.

Sleep disorders in autism and/or Smith-Magenis syndrome
  A melatonin product for minors with autism and/or Smith-Magenis syndrome also contains prolonged-release tablets. Two doses are available: one and five milligrams.

The intake is usually started with two milligrams. If this does not help enough with insomnia, the doctor can increase the melatonin dose to five milligrams. The maximum daily dose is ten milligrams.

Children and adolescents swallow the tablet(s) whole (do not crush, crush or chew) half an hour to one hour before bedtime. It should be taken after a meal or with food such as yogurt, orange juice or ice cream if you have difficulty swallowing. However, such preparations mixed into tablets should be taken immediately - the mixture should not be saved for later use.

With regard to the duration of treatment, there is information on the use of melatonin over a period of up to two years. After at least three months of use, the attending doctor assesses whether the drug really helps the little patient to fall asleep. If this is the case, the doctor will check at regular intervals whether further use is still necessary.

Stress from time difference

Adults with jet lag symptoms take one melatonin tablet, three milligrams of melatonin with a glass of water once a day at bedtime according to the local time upon arrival at the destination, but not before 8 p.m. or after 4 a.m. as a standard dose. The intake should not last longer than four days.

If the usual dose of three milligrams does not adequately relieve jet lag symptoms, a higher-dose formulation (five milligrams of melatonin at a time) can be tried.

o not eat anything for two hours before and after taking it. People with high blood sugar or diabetes should preferably take a melatonin product at least three hours after a meal.

sing an over-the-counter melatonin supplement For the use of over-the-counter melatonin preparations (capsules, sprays, etc.), read the product information and ask at the pharmacy. Hormone supplements, like melatonin medications, can sometimes have side effects — even if they're sold without a leaflet.

What side effects does melatonin have? In general, melatonin supplements are fairly well tolerated. However, side effects in the form of side effects are still possible. Therefore, preparations should not be made without hesitation.

Prescription melatonin products used to treat insomnia over 55 sometimes cause side effects such as headaches, migraines, drowsiness (upper abdominal pain), indigestion, nausea, mouth ulcers, dry mouth, dermatitis, rash, dry skin, itching, night sweats, and pain. in hands, feet or chest and feeling weak.

Menopausal symptoms and weight gain are also rare side effects of melatonin. The same goes for high blood pressure, nightmares, anxiety, insomnia, irritability, nervousness and restlessness.

These melatonin drugs rarely cause depression, aggression, increased sexual desire, prostatitis, problems with memory and attention, blurred vision, or dizziness.

Side effects of melatonin supplementation in minors with autism and/or Smith-Magenis syndrome are common: mood swings, aggression, irritability, drowsiness, headache, sudden insomnia, sinusitis, fatigue, and morning tiredness.

According to the technical data, short-term use of a melatonin supplement for jet lag can cause headaches, nausea, loss of appetite, drowsiness, daytime sleepiness, and confusion.

Is Melatonin Addictive? The body can get used to many prescription drugs, but not to melatonin. There is no risk of addiction here.

Overdose or improper timing of administration
Don't take too much melatonin! According to experts, overdose most often causes drowsiness or drowsiness. Headaches, dizziness, and nausea are also cited as possible symptoms of jet lag overdose.

 Also, taking too much melatonin can disrupt your sleep-wake cycle, as can taking it at the wrong time. For example, if you take melatonin in the middle of the night, you may still feel the sleep-inducing effects the next morning. This can be dangerous if you drive a car in the morning, for example.

How does melatonin work? A hormone can “dock” to certain binding sites (receptors) in the body. They are found in the brain, but also in the blood vessels and some cells of the immune system. When melatonin binds to these receptors, it signals the body to initiate a sleep phase.

In addition, melatonin has an effect on the thyroid gland: the production of thyroid hormones is inhibited. It slows down metabolism, lowers energy expenditure, lowers body temperature and affects the release of sex hormones.

In addition, melatonin has an antioxidant effect, which means it can neutralize "free radicals". These are cell-damaging compounds that are produced during metabolic processes in the body's cells. External factors such as cigarette smoke or UV radiation can contribute to their formation.

Benefits of Using Melatonin
Taking melatonin products to help you fall asleep or fall asleep is said to normalize disrupted circadian rhythms, reduce the time it takes you to fall asleep, and even improve sleep. But is it really true?

Review analyzes of current studies do not provide a consistent picture of the effectiveness of melatonin intake in the treatment of sleep disorders in general. For example, melatonin may objectively, or at least subjectively, decrease the time it takes to fall asleep in some, but not all, studies. The quality of sleep also improved.

The melatonin drugs approved in Germany, Austria and Switzerland are each intended for a specific area of application and a specific group of patients. For this precisely defined purpose, its effectiveness has been proven in studies - one of the requirements for approval as a medicinal product.

This does not mean that all patients respond equally to prescription melatonin tablets. After all, sleep regulation is a very complex mechanism involving many other factors besides melatonin.

Manufacturers of melatonin supplements are not required to research the effectiveness of their product before launching it on the market. Insomnia often goes away on its own when the trigger (e.g., stress) is eliminated and good sleep hygiene (e.g., bedtime) is followed. If not, you should contact your doctor. This is especially true for children who suffer from insomnia.

These interactions can occur with melatonin
Consult your doctor before taking melatonin products. Melatonin can interact with other medications. This can weaken or increase the effect of melatonin or other medications. Side effects can also increase.

Here is an overview of active ingredients that should not be taken together with melatonin and should be taken with caution:

• fluvoxamine and imipramine (medicines for depression)
• Benzodiazepines (sleeping pills such as diazepam and lorazepam)
• Z-Drugs (sleeping pills such as zolpidem and zopiclone)
• thioridazine (antipsychotics)
• methoxypsoralen (used for phototherapy in psoriasis)
• Cimetidine (heartburn medicine)
• Estrogens (e.g. in hormonal contraceptives or hormone replacement products)
• Quinolone antibiotics (such as ciprofloxacin)
• Rifampicin (antibiotic)
• Carbamazepine (anti-epilepsy medicine)

 In addition, taking melatonin should not be combined with alcohol. Beer, wine, and the like can decrease melatonin's effect on sleep.

This list is just a selection. Interactions with other active ingredients are (at least) conceivable. Therefore, it is best to consult a doctor before using melatonin products.

Melatonin during pregnancy and lactation
It is not yet known what effect melatonin tablets may have on the unborn child during pregnancy. Animal studies have shown that the hormone passes through the placenta to the unborn child. As a precaution, experts advise pregnant women not to use melatonin.

Natural melatonin can pass into breast milk. This probably applies to topical melatonin as well. The hormone can enter the baby's body through breast milk. Possible effects are not yet known. As a precaution, experts recommend not taking melatonin and breastfeeding at the same time.

Autoren:

Mag. pharm.  Christopher Waxenegger

Christopher Waxenegger studierte Pharmazie an der Universität Wien. Es folgten die erfolgreiche Fachprüfung für den Apothekerberuf sowie die freie Mitarbeit in einer Arztpraxis mit dem Schwerpunkt Medikationsanalyse. Seit 2020 widmet er sich dem Fachjournalismus und verfasst Sachtexte zu verschiedenen Gesundheitsthemen. Im Urlaub erkundet Christopher gerne die schottischen Highlands und genießt die Ruhe der Natur.