Melatonin Sublingual

Melatonin, a naturally occurring indolamine, is produced primarily in the pineal gland but also in mammalian bone marrow, platelets, gastrointestinal tract, eyes, skin, and lymphocytes [1]. It plays a vitally important role in regulating the body’s daily and annual biological rhythms and thus the sleep/wake cycle. Research suggests that melatonin supports antioxidant activity, cardiovascular health and immune function as well [2,3].

Normal melatonin secretion is suppressed by light and stimulated by periods of darkness. Nocturnal secretion of melatonin is at its highest during childhood, and then decreases with age. Studies, including meta-analyses, suggest that supplemental melatonin supports desirable sleep patterns in certain individuals, including the elderly and those who have unusual work hours, such as night shift workers or people traveling across time zones [4-7].

Human research studies suggest that melatonin supports the quality of healthy sleep as it relates to falling asleep, sleep efficiency (percent of time asleep to total time in bed), and awakening.

Melatonin has been closely studied for its role in supporting antioxidant activity, especially since intracellular melatonin is concentrated in the mitochondria, a major site of oxidative metabolism. Melatonin has been found to support extracellular antioxidant activity, support glutathione production, and stimulate production of intracellular antioxidant enzymes—including superoxide dismutases and glutathione peroxidase [8]. As a lipophilic molecule, melatonin is able to permeate the lipid portion of low-density lipoprotein (LDL) and support antioxidant activity in cells. Research suggests that melatonin supports blood pressure already in the normal range and overall cardiovascular health [8].

Finally, research suggests that melatonin aids immune system activity by supporting T-helper cell function, immune-specific progenitor cell production, cytokine balance, and production of mediators, such as gamma-interferon and immune-supportive interleukins [1,2,4,9].

References

1. Srinivasan V, Pandi-Perumal SR, Brzezinski A, et al. Melatonin, immune function and cancer. Recent Pat Endocr Metab Immune Drug Discov. 2011 May;5(2):109-23. [PMID: 22074586]
2. Korkmaz A, Reiter RJ, Topal T, et al. Melatonin: an established antioxidant worthy of use in clinical trials. Mol Med. 2009 Jan-Feb;15(1-2):43-50. Review. [PMID: 19011689]
3. Maestroni GJ. The immunotherapeutic potential of melatonin. Expert Opin Investig Drugs. 2001 Mar;10(3):467-76. Review. [PMID: 11227046]
4. Haimov I, Lavie P, Laudon M, et al. Melatonin replacement therapy of elderly insomniacs. Sleep. 1995 Sep;18(7):598-603. [PMID: 8552931]
5. van Geijlswijk IM, Korzilius HP, Smits MG. The use of exogenous melatonin in delayed sleep phase disorder: a meta-analysis. Sleep. 2010 Dec;33(12):1605- 14. [PMID: 21120122
6. Olde Rikkert MG, Rigaud AS. Melatonin in elderly patients with insomnia. A systematic review. Z Gerontol Geriatr. 2001 Dec;34(6):491-7. Review. [PMID: 11828891]
7. Kunz D, Mahlberg R, Müller C, et al. Melatonin in patients with reduced REM sleep duration: two randomized controlled trials. J Clin Endocrinol Metab 2004 Jan;89(1):128-34. [PMID: 14715839]
8. Dominguez-Rodriguez A, Abreu-Gonzalez P, Reiter RJ. Melatonin and Cardiovascular Disease: Myth or Reality? [in Spanish]. Rev Esp Cardiol. 2012 Mar;65(3):215-218. Epub 2012 Jan 13. [PMID: 22245066]
9. Cardinali DP, Esquifino AI, Srinivasan V, et al. Melatonin and the immune system in aging. Neuroimmunomodulation. 2008;15(4-6):272-8. Review. [PMID: 19047804]