Overview of melatonin
How melatonin works
Uses of melatonin
- Amnesia or “melatonin hang-over” the next day
- Harder to fall asleep
- Waking after 3-4 hours, unable to go back to sleep
Some doctors also believe that high doses, prescribed long-term can negatively impact the body’s own production of melatonin, leading to dependency. Vivid dreams, particularly alarming if the patient is a child, have been reported with high doses or long-term use.
Since the body produces less than 1 mg of melatonin daily, doses in the range of 0.1 mg - 0.5 mg are known as physiologic doses. Amounts above this range are known as pharmacologic doses. Researchers from the Massachusetts Institute of Technology (MIT) in 2001 compared physiologic doses to pharmacologic doses and very low (below physiologic) doses and found the best objective data at the 0.3 mg doses of melatonin. The physiologic melatonin dose (0.3 mg) restored sleep efficiency and elevated plasma melatonin levels to normal.
The pharmacologic dose (3 mg), like the lowest dose (0.1 mg), also improved sleep; however, it induced low body temperature and caused melatonin levels to remain high into the daylight hours. While we need to lower body temperature to sleep well, doing so excessively can disrupt sleep. Melatonin’s ability to lower body temperature may give significant clues to the appropriate dosage. For example, an individual may notice a need for more covers, which together with excessive movement, may suggest too much melatonin at night.
Researchers also evaluated the 0.3 mg dose in children who suffer from Angelman’s Syndrome (AS), a rare genetic condition in which sleep is difficult to maintain and there are other symptoms including severe mental retardation. They determined that the 0.3 mg dose effectively elevated blood levels, decreased restlessness during the night, and children went to bed more willingly. What is profoundly interesting is that many of these children were taking medications which are known to deplete melatonin and AS children are thought to produce less melatonin than developmentally normal children, possibly due to their poorly formed pineal glands. These subjects likely have the most need for melatonin yet only 0.3 mg was sufficient to see clinically relevant improvements.
Dr. Paolo Lissoni’s cancer research demonstrated that 20 mg was effective in arresting tumor growth and improving quality of life markers. Subsequent studies have all mirrored this dose; however, it is important to note that 20 mg was a calculated dose. Little research to date has been conducted on lower dosages to determine if they are as effective in cancer patients or if the physiological dose of 0.3 mg can be used for prevention. In 2002 Dr. Alfred J. Lewy and colleagues found that physiologic doses (0.5 mg) may offer benefits that pharmacologic doses (20 mg) do not. These researchers observed the effects of doses of melatonin in blind humans who often have disrupted circadian rhythms due to the pineal gland not receiving appropriate light stimulation from the retina. The debate continues with uncertainty about “How much melatonin is too much?” Hormone production and timing of secretion has many variables. In addition, bioavailability of the form or product used can play a part. Many practitioners, who have regularly used higher dosages of 1- 3 mg find that when they switch forms, for example, to plant-based Herbatonin from synthetic or animal-based product, lower dosages are just as effective. Melatonin is quickly broken down by the body and a personalized dose should therefore be given daily. For example, if an individual feels best on 1 mg melatonin, giving 3 mg every third day is not a viable alternative. Off-the-shelf products containing 3-5 mg are often chosen because they are seen as a good value, but getting more medicine for your dollar is not always better value. The lowest effective dose of any product, natural or prescription is always the most prudent choice.
For this reason,
- Start at the physiological dose of 0.3 mg unless using for specific conditions where higher doses are needed short term (e.g. jet lag or shift work)
- Increase slowly if necessary over the next few days
- Take 30-60 minutes prior to bed
- Take on an empty stomach
- For difficulty maintaining sleep, take melatonin in conjunction with rest in complete darkness (avoid light stimulation from television and computers); a controlled-release formulation may be required depending upon the cause of disrupted sleep
Melatonin for children
The prescribing of melatonin for children is now well accepted, with poor sleep, attention-deficit disorder, and autism spectrum disorder all studied and reviewed, with effectiveness and safety confirmed. However, studies range widely across dosing levels and period of use. It is also important to note, as mentioned previously, that healthy children generally produce three times the level of melatonin that adults do, and that in many cases removing light (night light, computer, TV) can be enough to trigger their own production. Because of this some authorities suggest limiting melatonin to 0.3 mg in children. “The dose of melatonin applicable to each patient must vary according to multiple factors such as the child’s medical problems, the severity and type of sleep problems, or the associated neurological pathology.”
Indiscriminate dosing may lead to unnecessary dependence. Again, it is worth repeating that the least effective dose is the best dose.
Melatonin use has been studied in neonatal care with breast milk content of melatonin shown to vary during the day. This is an issue for the lactating mother who is pumping and storing her milk to be aware of and yet another reason that breast is superior to formula.
Finally, to underscore the discussion of dosing in both pediatrics and adults, it is important to understand that melatonin is metabolized via the liver. Slow metabolism by the relevant liver enzymes has clinical application. Therefore, if an individual finds decreased the effectiveness of melatonin over time, the dose should not be increased, but rather decreased.
It is best to speak with an authority on melatonin when deciding on its use. Melatonin has some strong clinically valid health benefits for specific conditions; however, dosing and form play a critical part in how effective they will be for you. Every person is different and that is why working with your primary health practitioner, who has a strong historical understanding of your health and what other medications you are taking is key. A number of conditions and medications have been shown to depress melatonin levels in the blood and your solution could be simply to stop or change from those particular options. While your doctor or pharmacist may be a good source of information regarding these interactions, even they may not be able to keep up with the volume of information so if a suggestion doesn’t sound right, make sure you also get a second opinion from an expert in melatonin forms and dosages.
Our medical team is always available to answer any of your questions and work with your primary healthcare practitioner.
Phone: 415 243 9991