Melatonin Supplement Recommendations

Melatonin Can be Your Key to a Good Night’s Sleep

There’s little argument that it’s helpful to take melatonin supplements to fend off jet lag or get back into a regular sleep pattern. There’s even some good evidence that in those who are melatonin-deficient—which is primarily those over the age of 60—it can help maintain optimal health and promote better sleep.

Every system in your body responds to circadian rhythms, set by waking and sleeping, light and darkness. If your circadian rhythms are out of sync it can interfere with the regulation of hormones and brain neurotransmitters, as anyone who has experienced jet lag can attest. Melatonin supplements can help you reset your body to a more normal rhythm so that your biochemical orchestra is playing in harmony.

If taking melatonin for a few weeks doesn’t help with sleep problems, it’s probably best to dig deeper and find out why. Here’s an article by John R. Lee, M.D. on How to Sleep Better.

If you do have a melatonin deficiency even though your “sleep hygiene” is good (See How to Sleep Better), then a regular melatonin supplement may work well for you.

GETTING STARTED IN THE MORNING
It’s about Light, Dark, Melatonin, Cortisol.

The adrenal hormone cortisol is a great example of how out-of-sync circadian rhythms can affect the entire body. Cortisol plays an essential role in regulating blood sugar, insulin, fat storage, inflammation and muscle function. The brain and the adrenal glands have their own rhythm for the release of cortisol: it’s highest in the morning, then drops gradually through the day and the evening, reaching it’s lowest point at about 2 a.m. While the body is presumably in its deepest state of sleep and rest and melatonin levels are beginning to drop, cortisol levels finally begin to slowly rise again, and really climb between 6 a.m. and 8 a.m. People who get up and stay up in the wee hours while the adrenals are busy replenishing cortisol may make the job more difficult. Cortisol and the other adrenal hormones help charge the body’s batteries for the day ahead. Have you ever tried to start a car with a dying battery? That’s what it’s like for a body asked to greet the morning without cortisol.

One way to help your body regain its biorhythms if you’re getting up early is to make sure that you go to sleep in darkness (no lighted clocks, night lights etc), and wake in bright light. Darkness turns on melatonin production and brightness turns down melatonin and turns up cortisol production. Blue light, such as from fluorescent lights, and computer and TV screens, seems to be the best at helping the body wake up. And it also works in reverse—blue light is the worst when it comes to falling asleep, as it suppresses melatonin production.

Melatonin levels also drop precipitously as we age, and many researchers believe that taking melatonin supplements is a key to living longer, healthier lives. This has been validated in rodent studies, but since they have different circadian rhythms than humans, and are nocturnal, the research may or may not apply. Nevertheless, melatonin has shown great benefit for the elderly and in Alzheimer’s patients for promoting better sleep.

Dosage: More Melatonin is Not Better
Like all hormones, taking more melatonin is not better. For help with sleep, for resetting your biological clock, and healthy aging maintenance, a dose of 0.3 to 1 mg appears to be the optimal amount recommended by most experts. Even a 1 mg dose can produce blood levels that are 100 times higher than peak levels produced naturally, which is not something to be desired if you’re aiming for a physiologic (what the body would make) dose. The time to take melatonin is at night, half an hour to an hour before going to bed.

Higher doses should be considered medicinal not supplemental. There has been much research done with higher doses of melatonin on the immune system, cancer, migraines, Alzheimer’s and inflammation, but results are inconsistent and indications are that, over time, it has both beneficial and harmful effects at high doses. Some research has shown that excess melatonin can free up bound iron to harmful levels, and deplete glutathione, an amino acid that’s essential for good liver function. It may also boost parts of the immune system to the point where allergies can go from moderate to severe, and immune system diseases become worse. Another finding with high doses is that beneficial effects wear off over time. Without good research to the contrary, I can’t see any reason to “mess” with your biochemistry with high doses of melatonin.

Forms: Tablets, Sublingual, Cream, Time Release
Melatonin is fat soluble, so using a transdermal (skin) cream will work, but it hasn’t been shown to be a particularly effective delivery system. Taking it sublingually (under the tongue) is probably an effective delivery system, but may also lead to a quick spike in levels followed by a quick drop, much like progesterone. There’s some evidence that time-release melatonin can help extend sleep, but the majority of research shows that a 0.3 to 1 mg tablet or capsule works just fine.

References

Brzezinski A, “Melatonin in humans” [a review] NEJM 1997 Jan 16;336(3):186-95.

Clapp-Lilly KL, Smith MA et al, “Melatonin acts as antioxidant and pro-oxidant in an organotypic slice culture model of Alzheimer's disease,” Neuroreport 2001 May 8;12(6):1277-80.

Osseni RA, Rat P et al, “Evidence of prooxidant and antioxidant action of melatonin on human liver cell line HepG2,” Life Sciences 2000 Dec 15;68(4):387-99.

Pandi-Perumal SR, Zisapel N et al, “Melatonin and sleep in aging population,” Exp Gerontol 2005 Dec;40(12):911-25. Epub 2005 Sep 23.

Pappolla MA, Sos M et al, “Melatonin Prevents Death of Neuroblastoma Cells Exposed to the Alzheimer Amyloid Peptide,” J Neuroscience Volume 17, Number 5, Issue of March 1, 1997 pp. 1683-1690.

Wu YH, Swaab DF, “Disturbance and strategies for reactivation of the circadian rhythm system in aging and Alzheimer's disease,” Sleep Med 2007 Sep;8(6):623-36. Epub 2007 Mar 26.