Melatonin (Controlled Release)

Melatonin is a neurohormone produced from tryptophan by the pineal gland when it is stimulated by darkness. While melatonin regulates many other hormones; its primary function appears to be regulation of the body’s daily and annual biological rhythms.*

Oral supplementation has been shown to have some benefit with regard to time to sleep onset, total sleep time, and sleep efficiency.[1] Noteworthy advantages over pharmaceutical sleep aids are improved performance upon wakening and the absence of memory impairment.[2,3] According to studies, daytime melatonin supplementation by travelers crossing time zones and/or shift workers also promotes sleep.*[4]

Research has shown that melatonin not only fights free radicals during sleep, but also stimulates the body’s own antioxidant systems. For example, it reduced harmful oxidized cholesterol (LDL) in post-menopausal women. [5] Melatonin’s antioxidant capacity also accounts for its role as a neuroprotectant. By delivering antioxidant benefits and correcting the circadian rhythm, melatonin could support cognitive function.*[6,7]

A decrease in plasma melatonin correlates with a decline in immune function in some individuals beginning around the age of sixty. Interestingly, lymphoid cells are an important physiological source of melatonin in humans.The hormone appears to stimulate production of T helper (TH) cells and their release of interleukin-2, gamma interferon and opiod peptides.[8] Considering the decline in melatonin synthesis with age, exogenous supplementation with the hormone has long been of interest in anti-aging protocols.*[9,10]

The addition of pyridoxine in this formula supports the biosynthesis of melatonin and may also enhance dream recall.*

The biphasic delivery system consists of 1mg of melatonin in the coating solution and the remainder in the tablet core. The melatonin in the coating solution is immediately released upon digestion. The melatonin in the tablet core is released over a 6-hour period. The tablet core contains a tableting agent, hydroxypropyl methylcellulose that works by forming a gel layer when hydrated. This gel layer acts as a diffusion barrier to control the rate of release of the melatonin in the tablet core. As the tablet travels through the intestine, the gel layer slowly erodes to release the melatonin, which then is available for absorption in the intestine.*

Directions

Take 1 tablet with water 20 minutes before bedtime, unless otherwise directed.

References

1. Brzezinski A, Vangel MG, Wurtman RJ, et al. Effects of exogenous melatonin on sleep: a meta-analysis. Sleep Med Rev.2005;9:41-50. [PMID: 15649737]
2. Paul MA, et al.Melatonin and zopiclone as pharmacologic aids to facilitate crew rest. Aviat Space Environ Med. 2001 Nov;72(11):974-84. [PMID: 11718517]
3. Wesensten NJ, Balkin TJ, Reichardt RM et al. Daytime sleep and performance following a zolpidem and melatonin cocktail. Sleep. 2005;28:93-103. [PMID: 15700725]
4. Srinivasan V, et al. Jet lag: therapeutic use of melatonin and possible application of melatonin analogs. Travel Med Infect Dis. 2008 Jan- Mar;6(1-2):17-28.[PMID: 18342269]
5. Wakatsuki A, et al. Melatonin inhibits oxidative modification of low-density lipoprotein particles in normolipidemic post-menopausal women. J Pineal Res. 2000;28:136-142 [PMID: 10739299]
6. Peck JS, et al. Cognitive effects of exogenous melatonin administration in elderly persons: a pilot study. Am J Geriatr Psychiatry. 2004;12:432-436. [PMID: 15249281]
7. Asayama K, Yamadera H, Ito T, et al. Double blind study of melatonin effects on the sleep-wake rhythm, cognitive and noncognitive functions in Alzheimer type dementia. J Nippon Med Sch. 2003;70:334-341. [PMID: 12928714]
8. Cardinali DP, et.al. Melatonin and the immune system in aging. Neuroimmunomodulation. 2008;15(4-6):272-8. [PMID: 19047804]
9. Armstrong SM, Redman JR. Melatonin: A chronobiotic with anti-aging properties? Med Hypotheses 1991;34: 300-9 [PMID: 1865836]
10. Rozencwaig R, Grad BR, Ochoa J. The role of melatonin and serotonin in aging. Med Hypotheses 1987;23: 337-52 [PMID: 2889131]
11. Miyamoto A, et.al. Serum melatonin kinetics and long-term melatonin treatment for sleep disorders in Rett syndrome. Brain Dev. 1999 Jan;21(1):59-62 [PMID: 10082254]
12. Arendt J. Safety of melatonin in long-term use. J Biol Rhythms 1997;12:673-681 [PMID: 9406044]
13. Voordouw BC, et.al. Melatonin and melatonin-progestin combinations alter pituitary-ovarian function in women and can inhibit ovulation. J Clin Endocrinol Metab. 1992 Jan;74(1):108-17. [PMID: 1727807]
14. Abd-Allah AR, et al. Effect of melatonin on estrogen and progesterone receptors in relation to uterine contraction in rats. Pharmacol Res. 2003 Apr;47(4):349-54 [PMID: 12644393]