Taking Melatonin, the Right Way

Dose, Form, and Other Considerations for Precise and Effective Use

Melatonin supplement sales have increased significantly in the last years. Yet often people say that it doesn’t help them as they wish. There are so many variables in using melatonin – What dose? What time? What form? What brand? Are there side effects? Should children take melatonin?

Today let’s talk about the science of how to use melatonin. We’ll go into all these considerations, so you’ll be well-informed. As always, check with your licensed healthcare provider if you want to take melatonin or any other supplement.

Finding the Right Form
On the shelf you’ll find many forms, from capsules and tablets, to gummies and drops. The most concerning is gummies. Gummies often have artificial ingredients such as food dyes, and sugars. Some food dyes are associated with childhood conditions that are often associated with sleep disruption, particularly attention difficulties (1). Because of the sugar, children may act like the gummies are candy. From 2012-2021 the number of children getting emergency care due to melatonin overdose increased by 530%, with 287 children in intensive care. The American Academy of Sleep Medicine recommends advises behavioral approaches for childhood insomnia before medications, including melatonin (2).

Melatonin drops may more easily be taken for people who have difficulty swallowing capsules or tablets. Liquid melatonin can also be more finely dosed drop by drop. Note this form will have an immediate effect.

Route
The first route that comes to mind is oral melatonin. Sleep onset insomnia can be treated with an immediate release formula. Along with immediate release, there are also options for time-released or sustained release capsules. An example of use for these could be sleep maintenance type insomnia, where a person falls asleep easily at the beginning of the night, yet wakes up after a few hours.

Other routes of melatonin administration that are used for specialized purposes include IV melatonin, transdermal, vaginal, and other methods.

Quality
Of real concern is the lack of quality standards in the melatonin products that are available over the counter. A couple studies have found significant deviation from what is listed on the label. One study pulled melatonin supplements off the grocery shelf. The amount of melatonin varied from 17-478% of the labelled amount. In addition, the lot-to-lot variability was 465%. For this reason, it’s best to get the highest quality melatonin possible, rather than that available at the grocery store.

Multiple Melatonin Source Options
Originally melatonin supplements were sourced from animal pineal glands. More recently, melatonin has been chemically manufactured. There are some concerns here about the possibility of contaminants due to the manufacturing process, which uses chemicals such as formaldehyde, and phthalidimides, among others.

Now, melatonin from plants, “phytomelatonin,” is an option. The melatonin compound it ubiquitous in Nature, and is found in most plants. This is my preferred source, as there is decreased risk of contaminants. Plus, it is a more powerful antioxidant and anti-inflammatory than synthetic forms (4).

What is the Right Dose?
There are So. Many. Doses. available. A physiological dose is 0.3mg to 1.0mg. This is in keeping with the level that’s naturally produced by the body. Three milligrams and above is a pharmacologic dose. For most sleep and circadian rhythm disorders there has been no evidence that doses above 3mg are more effective. (A few are treated with a 5mg dose).

Last week we talked about the actions of melatonin at the cellular level, and how melatonin can be used for a wide array of disorders. For medical conditions, it’s common to use the higher doses. The dose varies considerably by condition, and this is an area of active research, which has not settled on standard doses yet.

Timing Matters, a Lot
One of the most powerful actions of melatonin is as a chronobiotic, which we talked about in the last newsletter. Taken at specific times, and in specific doses, melatonin can shift our body clock, causing us to be sleepy either later or earlier than typical. It’s likely that this action is why people sometimes get different effects from the melatonin than they are aiming for. For this reason, if you are getting different effects than you wish, consult with a knowledgeable doctor who can advise on the right dose and timing for your needs.

Conclusion
I hope this series on melatonin serves you in pursuing your health. Our endogenous, intrinsic, melatonin is suppressed by the pervasive artificial light at night. That melatonin has actions beyond sleep and circadian rhythms, to impact our health at a cellular level. Awareness of melatonin’s use is growing, yet knowing the right use makes all the difference in its’ effectiveness. If melatonin isn’t getting the effect you wish, re-examine these factors, and consult with your physician.

Sleep well and Dream big,

Dr. Catherine

Selected references:
1.     Miller MD, Steinmaus C, Golub MS, et al. Potential impacts of synthetic food dyes on activity and attention in children: a review of the human and animal evidence. Environ Health. 2022;21(1):45. Published 2022 Apr 29. doi:10.1186/s12940-022-00849-9 PMID: 35484553
2.    AASM advises parents seek medical advice before giving melatonin to kids
3.    Erland LA, Saxena PK. Melatonin Natural Health Products and Supplements: Presence of Serotonin and Significant Variability of Melatonin Content. J Clin Sleep Med. 2017;13(2):275-281. Published 2017 Feb 15. doi:10.5664/jcsm.6462 PMID: 27855744
4.     Kukula-Koch W, Szwajgier D, Gaweł-Bęben K, Strzępek-Gomółka M, Głowniak K, Meissner HO. Is Phytomelatonin Complex Better Than Synthetic Melatonin? The Assessment of the Antiradical and Anti-Inflammatory Properties. Molecules. 2021;26(19):6087. Published 2021 Oct 8. doi:10.3390/molecules26196087 PMID: 34641628