Melatonin In Perimenopause And Menopause

I can’t say enough good things about melatonin. Both what our body naturally makes and melatonin in supplement form.

So why is there so much “melatonin is bad for you” information on the internet? My best guess is this:

  1. It is a hormone, which leads people to believe it’s dangerous

  2. People are writing opinion pieces (using reasonable common sense), without looking at the scientific studies

  3. It is assumed to be addictive or that supplementation will suppress the body’s natural production of melatonin

  4. As always, more research is needed

What it is:

Melatonin is produced in the pineal gland of the brain in response to sunlight and darkness. In a healthy circadian rhythm, melatonin begins to rise as natural light diminishes late in the evening and peaks around 2 am, declining to the lowest level of the day upon awakening. Melatonin and cortisol dance in opposition so when cortisol levels are at their highest point, melatonin levels are at their lowest (after waking) and vice versa.

Although discovered as a product of the pineal gland and initially thought to be unique to that organ, it is now known that melatonin is produced in many, perhaps all, cells in the body. However, melatonin produced outside the pineal gland is not released into the general circulation in any appreciable amount.

Interestingly, melatonin levels appear to correlate with the menstrual cycle and the moon cycle. In birds, the daily variations in melatonin and corticosterone (equivalent to cortisol in humans) disappear during full-moon days. This is thought to be similar for humans, which may be why some of us don’t sleep as well on full-moon nights.

Melatonin levels seem to decline with age, and have been associated with things like poor sleep quality, osteoporosis, dementia, depression, cancer, and fibromyalgia.

The reason behind this decline may be due to calcification of the pineal gland - once thought to be a normal process but possibly due to toxins such as fluoride. Another large reason for poor melatonin levels is lack of natural sunlight during the daytime hours and overstimulation via artificial light in the evening/nighttime hours.

What is does:

Although melatonin is well known for its sleep support properties (inducing sleepiness and lowering core body temperature, a requirement for sleep onset), it has a plethora of other properties.

Melatonin is a powerful free radical scavenger, otherwise known as an anti-oxidant.

It is known as an analgesic, meaning it can reduce pain. It is a powerful anti-inflammatory and provides anti-tumor properties. It is important in reproductive health. It is produced downstream from serotonin, but also contributes to serotonin levels in a bi-directional manner.

There is a fair amount of evidence that melatonin treatment has a favorable effect on bone density and body weight. Melatonin treatment also seems to improve EEG patterns. In dose above 3 mg each night, melatonin also seems to improve hot flashes and night sweats for women in perimenopause and menopause.  

Melatonin has also shown to suppress electromagnetic frequency (EMF) induced oxidative stress.

Dosing:

  • It has been suggested that low doses (0.3-1.0 mg) are the most effective dose for sleep support.

  • Others report that a melatonin daily doses of 0.5 - 5 mg are also effective for sleep.

  • Doses higher than 5 mg do not seem to improve sleep quality any more than lower doses.

  • In a study on people who have a hard time falling asleep, 0.5 mg of melatonin was as effective as ten-fold the dose of 5 mg.

  • A comparative study on age-related insomnia, 0.3 mg was shown to be more effective than 3 mg.

  • Dosing between 10 mg and even up to 100 mg each day have been studied to provide anti-cancer properties

*There are sustained release formulas on the market, which can help those with middle of the night wakings.

Does melatonin supplementation reduce natural production of melatonin?

To date, there are no studies to suggest that supplementation will decrease the body’s natural production of melatonin.

Oral melatonin supplementation at 0.5 mg, over a one week period in shift workers, did not influence basal secretion. This has been replicated with 2 mg and 5 mg of melatonin supplementation.

When a blind person supplemented a dose of 50 mg in one case study (blind people being an example of a population with no sunlight-mediated melatonin production), this dose being 100-fold higher than the standard 0.5 mg, did not significantly influence basal secretion status after 37 days.

Although in vitro studies suggest that high melatonin doses desensitize receptors, the efficacy is maintained in humans after repeated administration. Also, no tolerance or rebound symptoms are reported after withdrawal.

Potential benefits of melatonin during perimenopause and menopause:

  • Improved sleep

  • Improved bone health

  • Improved mood and well being

  • Reduced risk of breast cancer

  • Reduced risk of endometrial cancer

  • Reduced pain

  • Reduced hot flashes and night sweats (with higher doses)

  • Reduced risk of dementia

Potential side effects:

  • Headaches

  • Dizziness

  • Vivid dreams

  • Nausea

  • Fatigue

  • Low blood pressure

Cautions:

  • Melatonin increases the effects of antidepressant medications.

  • Melatonin can increase the risk of bleeding if administered with Coumadin (warfarin). NSAIDS like ibuprofen can lower melatonin levels.

  • Melatonin enhances the effects of metformin and other anti-diabetic medicines.

  • Commercially available melatonin supplements ranged from — 83% to +478% of the labeled content!

  • 26% of the melatonin supplements studied commercially, contained serotonin, though this was not labeled.

Taking too much serotonin (referred to as serotonin syndrome) by combining medications such as antidepressants, migraine medications and melatonin can lead to a serious drug reaction. Mild symptoms include shivering and diarrhea, while a more severe reaction can lead to muscle rigidity, fever, and seizures.

As with any supplement, quality matters.

I suggest avoiding Amazon and most over-the-counter products. If you are a patient of mine, Fullscript is a good place to get high-quality brands.

In summary:

More research is needed (especially in kids, although the research is so far overwhelmingly positive), but from my clinical and research experience, the benefits of melatonin supplementation (even long-term) outweigh the risks for the majority people, especially for women in perimenopause and menopause.

💕,

Dr. Laura Neville

References:

Jehan S, Jean-Louis G, Zizi F, Auguste E, Pandi-Perumal SR, Gupta R, Attarian H, McFarlane SI, Hardeland R, Brzezinski A. Sleep, Melatonin, and the Menopausal Transition: What Are the Links? Sleep Sci. 2017 Jan-Mar;10(1):11-18. doi: 10.5935/1984-0063.20170003. PMID: 28966733; PMCID: PMC5611767.

Lewy AJ, Emens JS, Sack RL, Hasler BP, Bernert RA. Low, but not high, doses of melatonin entrained a free-running blind person with a long circadian period. Chronobiol Int. 2002;19(3):649-658. doi:10.1081/cbi-120004546

Mundey K, Benloucif S, Harsanyi K, Dubocovich ML, Zee PC. Phase-dependent treatment of delayed sleep phase syndrome with melatonin. Sleep. 2005;28(10):1271-1278. doi:10.1093/sleep/28.10.1271

Reiter RJ, Rosales-Corral SA, Manchester LC, Tan DX. Peripheral reproductive organ health and melatonin: ready for prime time. Int J Mol Sci. 2013;14(4):7231-7272. Published 2013 Apr 2. doi:10.3390/ijms14047231

Treister-Goltzman Y, Peleg R. Melatonin and the health of menopausal women: A systematic review. J Pineal Res. 2021;71(2):e12743. doi:10.1111/jpi.12743

Zhdanova IV, Wurtman RJ, Regan MM, Taylor JA, Shi JP, Leclair OU. Melatonin treatment for age-related insomnia. J Clin Endocrinol Metab. 2001;86(10):4727-4730. doi:10.1210/jcem.86.10.7901

 

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