Have you bought melatonin at the pharmacy? In a few years it has gone from being a supplement that someone almost smuggled you from the United States to combat jetjag to one more remedy that can be bought without a prescription.
Unlike other sleep aids and anxiolytics, such as benzodiazepines (e.g. Lorazepam), melatonin is perceived as a safe, natural remedy for improving sleep. This coincides with an increase in awareness and prevalence of sleep disorders. The Spanish Society of Neurology (SEN) It is estimated that between 20% and 48% of the adult population have difficulty initiating or maintaining sleep, and melatonin is readily available as a first aid before resorting to prescription drugs.
But, in addition, melatonin is sold promising other benefits that are not directly related to sleep, such as its antioxidant, neuroprotective and even anti-aging capacity.
How melatonin works
Melatonin is a hormone produced primarily by the pineal gland in the brain. Melatonin production occurs in response to darkness, and its main function is to regulate the circadian rhythm, the ‘internal clock’ that synchronizes sleep and wake cycles with external signals of day and night.
This internal clock resides in an area of the brain called the suprachiasmatic nucleus, in the hypothalamus, which is the control center for the circadian rhythm. This brain circuit is responsible for us orienting ourselves in time. a famous experiment Conducted in the 1960s with a group of people who were living in a room without natural light or other external signs of the passage of time, it showed that their brain ‘knew’ that it had to sleep and wake up in a 24-hour cycle.
Under normal conditions, melatonin secretion occurs in the pineal gland when the retina detects the decrease in light. The signal from the eyes produces a chain of other signals and, from there, the pineal gland begins to release melatonin.
Within the brain, and in other parts of the body, melatonin binds to receptors called MT1 and MT2. By binding to these receptors, melatonin ‘slows down’ the central nervous system, reduces the activity of neurons and produces the sensation of drowsiness. Exposure to light at night, especially blue light from screens and mobile phonesinhibits this process by reducing the activity of the enzyme N-acetyltransferase, necessary for the synthesis of melatonin.
Melatonin supplements and insomnia
Melatonin supplements may help regulate sleep by mimicking the effects of natural melatonin, especially in people with circadian rhythm disturbances, such as jet laghe onset insomnia (difficulty falling asleep) or sleep disorders in the night workerslike health personnel who must be on duty.
In these cases, endogenous melatonin production is out of sync. It may also be insufficient, as occurs in older people. The main effect of a melatonin supplement is to shorten the time needed to achieve sleep. “It is a hormone secreted in rhythmic pulses and has a circadian rise and fall. If you saturate it with a small pill, one of 1.9 milligrams, it causes levels of melatonin in your blood that are much higher than the endogenous ones,” explains Dr. Miguel Ángel Sánchez González, a psychiatrist specialized in sleep disorders.
To date, melatonin has not proven effective in the treatment of insomnia, and especially in people under 55 years of age who still have a robust own production of melatonin.
Miguel Ángel Sánchez González
— psychiatrist specializing in sleep disorders
“To date, melatonin has not proven effective in the treatment of insomnia, and especially in people under 55 years of age who still have a robust production of melatonin,” warns Dr. Sánchez. There is studies that indicate The effectiveness is minimal, and melatonin is not effective in improving sleep quality, or maintaining sleep throughout the night. The latter is the problem suffered by people with maintenance insomnia, who can fall asleep, but wake up in the middle of the night and can no longer sleep.
The 2023 guidelines of the European Sleep Research Society They only recommend slow-release melatonin for people over 55 years of age and for a maximum of three months. The use of fast-acting melatonin is not recommended for the treatment of insomnia, nor are other widely used drugs, such as ramelteon, antihistamines or plant remedies such as valerian.
“I tell patients that we don’t have sleeping pills, they don’t exist. There are some pills that can promote sleep in some circumstances, for a time. But the number one treatment for insomnia disorder in adults is cognitive-behavioral therapy, ahead of any pharmacological treatment,” says Dr. Sánchez.
Taking more melatonin pills does not help you sleep
In Spain, melatonin supplements are considered food products and are regulated by the Spanish Agency for Food Safety and Nutrition (AESAN). Its marketing is allowed as long as the dose does not exceed 2 milligrams per pill, and that is why most contain 1.9 mg of melatonin. Even have been withdrawn from the market repeatedly supplements that exceeded that dose.
A review of studies at the University of Amsterdam recommends taking melatonin in the lowest possible dose, for the shortest possible time, between 1 and 3 milligrams. Although it is generally considered safe for short-term use, melatonin can cause side effects, such as dizziness, nausea, headaches, and drowsiness. An extensive review of studies published in the Journal of Pineal Research found that higher doses, more than 10 mg per day, could exacerbate these side effects without providing additional benefits.
Although it is generally considered safe for short-term use, melatonin can cause side effects, such as dizziness, nausea, headaches, and drowsiness.
“It makes no sense to give 20 milligrams of melatonin,” says Dr. Sánchez, especially if the insomnia problem has another origin. The doctor explains that if someone takes it and wakes up because of pain or worry, they will attribute this to a lack of effectiveness of melatonin.
The other benefits of melatonin
In 2015 the prestigious medical journal The Lancet published an editorial titled Melatonin, the new companion of aspirin? comparing these two medications for their cardiovascular health benefits when taken as a daily supplement. Beyond helping to regulate sleep when there is jet lagmelatonin supplements have shown other potential benefits due to their antioxidant, anti-inflammatory, and neuroprotective properties. A review of studies published this year corroborates its beneficial effect on the immune system, cardiovascular function, antioxidant defense and cholesterol levels, in addition to acting as an anti-cancer and anti-inflammatory.
This protective use of melatonin was tested in a study with rats published in Nature who suffered cardiac arrest and were then resuscitated. Administration of melatonin protected the brain from damage, despite being deprived of oxygen. Other review of controlled studies with diabetic patients found that melatonin is effective in reducing the symptoms of the disease and improving blood sugar levels.
Its role in protecting the brain from neurodegenerative diseases has also led melatonin supplements to be considered a possible anti aging therapy. Dr. Sánchez, who was working in the Interdisciplinary Sleep Unit of the Jiménez Díaz Foundation during the pandemic, provided 6 mg of melatonin per day to older Covid-19 patients who had sleep problems after admission. “We compared these patients with the rest of the population and saw that they had a much lower mortality,” he says. The results were published in the Journal of Clinical Sleep Medicine in 2022.
Although these findings are promising, many of them require further clinical investigations to establish their efficacy and safety in broader therapeutic applications. “Melatonin is not the Holy Grail,” explains Dr. Sánchez. “But if you are over 55 years old, try it and it helps you a little to induce sleep, then better.”
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