Melatonin

Sleep Supplements

Melatonin

Description

Melatonin is produced naturally in the body by the pineal gland.1.2 It is a primary hormone involved in regulating the body's circadian rhythms and female menstrual cycle.1,3,4 It also plays important roles in blood pressure regulation, seasonal reproduction, immune system health, and bone and tooth health.1,5.6 Melatonin levels are higher at night, suppressed by bright light, and decline as we age. Low levels of melatonin can cause sleep disturbances, as it is a primary component in the sleep-wake cycle.1,7 Melatonin is derived from tryptophan, an essential amino acid. When tryptophan is consumed through the foods we eat, it is converted into serotonin (a neurotransmitter) and then broken down further into melatonin at night.1

Benefits

  • Has powerful antioxidant effects.1,8-11
  • Promotes brain health even under challenging conditions.1,12-17
  • Potentially beneficial in preventing abnormal cellular development.1,17-24
  • Has immune-enhancing properties.1,25-32
  • Beneficial when used peri-operatively (surrounding surgeries).1,33-41
  • Promotes better sleep.1,42-46
  • Helps avoid jet lag.1,47-50
  • Aids in the biologic regulation of circadian rhythms.1,3,51
  • Supports reproductive and follicular health in women desiring to get pregnant.4,9,52-57
  • Has adaptogenic properties.58-60
  • Promotes a healthy inflammatory response.61-66

Side effects

Adverse reactions associated with melatonin include morning grogginess and daytime hangover. Aspirin, NSAIDS, and beta-blockers may lead to decreased melatonin levels. Use of melatonin with benzodiazepenes, sedating antihistamines, sedating antidepressants, and other sedating drugs may cause additive sedation and increase incidence of adverse effects.

Administration

Those who use melatonin supplements to help with sleep disturbances or jet lag usually take about 3 mg at bed time. Morning drowsiness indicates a dose is too high. Dose can be increased under physician supervision to obtain a good night's sleep.

References:

  1. No authors listed. Melatonin. Monograph. Altern Med Rev. 2005 Dec;10(4):326-336.
  2. Srinivasan V, et al. Melatonin and melatonergic drugs on sleep: possible mechanisms of action. Int J Neurosci. 2009;119(6):821-46.
  3. Bittencourt LR, et al. Chronobiological disorders: current and prevalent conditions. J Occup Rehabil. 2010 Mar;20(1):21-32.
  4. Shi L, et al. Melatonin and hypothalamic-pituitary-gonadal axis. Curr Med Chem. 2013;20(15):2017-31.
  5. Liu J, et al. Melatonin effects on hard tissues: bone and tooth. Int J Mol Sci. 2013 May 10;14(5):10063-74.
  6. Arushanian ÉB, et al. Therapeutic potential of melatonin in oral cavity diseases. Eksp Klin Farmakol. 2012;75(6):48-52.
  7. Shechter A, et al. Nocturnal polysomnographic sleep across the menstrual cycle in premenstrual dysphoric disorder. Sleep Med. 2012 Sep;13(8):1071-8.
  8. Ortiz F, et al. The beneficial effects of melatonin against heart mitochondrial impairment during sepsis: inhibition of iNOS and preservation of nNOS. J Pineal Res. 2013 Sep 30. doi: 10.1111/jpi.12099. [Epub ahead of print] PubMed PMID: 24117944.
  9. Tamura H, et al. Melatonin as a free radical scavenger in the ovarian follicle. Endocr J. 2013 Jan 31;60(1):1-13.
  10. Farías JG, et al. Melatonin protects the heart, lungs and kidneys from oxidative stress under intermittent hypobaric hypoxia in rats. Biol Res. 2012;45(1):81-5.
  11. Pandi-Perumal SR, et al. Melatonin antioxidative defense: therapeutical implications for aging and neurodegenerative processes. Neurotox Res. 2013 Apr;23(3):267-300.
  12. Marchetti C, et al. Melatonin protects PLPC liposomes and LDL towards radical-induced oxidation. J Pineal Res. 2011 Oct;51(3):286-96
  13. Srinivasan V, et al. Role of melatonin in neurodegenerative diseases. Neurotox Res. 2005;7(4):293-318.
  14. Arushanian EB, Baida OA, Mastiagin SS. Effect of melatonin on memory, individual time perception, and anxiety in young people of different chronotype groups. Eksp Klin Farmakol. 2006 Jan-Feb;69(1):21-23.
  15. Rosales-Corral SA, et al. Alzheimer's disease: pathological mechanisms and the beneficial role of melatonin. J Pineal Res. 2012 Mar;52(2):167-202.
  16. Cecon E, Markus RP. Relevance of the chronobiological and non-chronobiological actions of melatonin for enhancing therapeutic efficacy in neurodegenerative disorders. Recent Pat Endocr Metab Immune Drug Discov. 2011 May;5(2):91-9.
  17. Rios ER, et al. Melatonin: pharmacological aspects and clinical trends. Int J Neurosci. 2010 Sep;120(9):583-90.
  18. Brzozowski T, et al. The role of melatonin and L-tryptophan in prevention of acute gastric lesions induced by stress, ethanol, ischemia, and aspirin. J Pineal Res.1997 Sep;23(2):79-89.
  19. Di Bella G, et al. Melatonin anticancer effects: review. Int J Mol Sci. 2013 Jan 24;14(2):2410-30.
  20. Wang J, et al. Melatonin potentiates the antiproliferative and pro-apoptotic effects of  ursolic acid in colon cancer cells by modulating multiple signaling pathways. J Pineal Res. 2012 Dec 8. doi: 10.1111/jpi.12035. [Epub ahead of print] PubMed PMID: 23330808.
  21. Wang J, et al. Melatonin suppresses migration and invasion via inhibition of oxidative stress pathway in glioma cells. J Pineal Res. 2012 Sep;53(2):180-7.
  22. Cui P, et al. Melatonin prevents human pancreatic carcinoma cell PANC-1-induced human umbilical vein endothelial cell proliferation and migration by inhibiting vascular endothelial growth factor expression. J Pineal Res. 2012 Mar;52(2):236-43.
  23. Bizzarri M, et al. Molecular mechanisms of the pro-apoptotic actions of melatonin in cancer: a review. Expert Opin Ther Targets. 2013 Sep 14. [Epub ahead of print]
  24. Hill SM, et al. Age-related decline in melatonin and its MT1 receptor are associated with decreased sensitivity to melatonin and enhanced mammary tumor growth. Curr Aging Sci. 2013 Feb;6(1):125-33.
  25. Cardinali DP, et al. Melatonin and the immune system in aging. Neuroimmunomodulation. 2008;15(4-6):272-278.
  26. Nasrabadi NN, et al. Expression of MT2 Receptor in Patients with Gastric Adenocarcinoma and its Relationship with Clinicopathological Features. J Gastrointest Cancer. 2013 Oct 19. [Epub ahead of print]
  27. Jung JH, et al. Melatonin Suppresses the Expression of 45S Preribosomal RNA and Upstream Binding Factor and Enhances the Antitumor Activity of Puromycin in MDA-MB-231 Breast Cancer Cells. Evid Based Complement Alternat Med. 2013;2013:879746. doi: 10.1155/2013/879746. Epub 2013 Apr 7.
  28. Maldonado MD, et al. Melatonin protects mast cells against cytotoxicity mediated by chemical stimuli PMACI: possible clinical use. J Neuroimmunol. 2013 Sep 15;262(1-2):62-5.
  29. Csaba G. The pineal regulation of the immune system: 40 years since the discovery. Acta Microbiol Immunol Hung. 2013 Jun;60(2):77-91.
  30. de Oliveira Tatsch-Dias M, et al. The concept of the immune-pineal axis tested in patients undergoing an abdominal hysterectomy. Neuroimmunomodulation. 2013;20(4):205-12.
  31. Carrillo-Vico A, et al. Melatonin: buffering the immune system. Int J Mol Sci. 2013 Apr 22;14(4):8638-83.
  32. Sokolovic D, et al. Melatonin protects rat thymus against oxidative stress caused by exposure to microwaves and modulates proliferation/apoptosis of thymocytes. Gen Physiol Biophys. 2013 Mar;32(1):79-90.
  33. Jarratt J. Perioperative melatonin use. Anaesth Intensive Care. 2011 Mar;39(2):171-81.
  34. Maitra S, et al. Melatonin in perioperative medicine: Current perspective. Saudi J Anaesth. 2013 Jul;7(3):315-321.
  35. Kurdi MS, Patel T. The role of melatonin in anaesthesia and critical care. Indian J Anaesth. 2013 Mar;57(2):137-44.
  36. Yoshitaka S, et al. Perioperative plasma melatonin concentration in postoperative critically ill patients: its association with delirium. J Crit Care. 2013 Jun;28(3):236-42.
  37. Wilhelmsen M, et al. Anxiolytical, analgesic and sedative effects of melatonin in the perioperative phase. Ugeskr Laeger. 2011 May 16;173(20):1424-7.
  38. Sultan SS. Assessment of role of perioperative melatonin in prevention and treatment of postoperative delirium after hip arthroplasty under spinal anesthesia in the elderly. Saudi J Anaesth. 2010 Sep;4(3):169-73.
  39. Ismail SA, Mowafi HA. Melatonin provides anxiolysis, enhances analgesia, decreases intraocular pressure, and promotes better operating conditions during cataract surgery under topical anesthesia. Anesth Analg. 2009 Apr;108(4):1146-51.
  40. Caumo W, et al. Preoperative anxiolytic effect of melatonin and clonidine on postoperative pain and morphine consumption in patients undergoing abdominal hysterectomy: a double-blind, randomized, placebo-controlled study. J Pain. 2009 Jan;10(1):100-8. doi: 0.1016/j.jpain.2008.08.007.
  41. Caumo W, et al. The clinical impact of preoperative melatonin on postoperative outcomes in patients undergoing abdominal hysterectomy. Anesth Analg. 2007 Nov;105(5):1263-71.
  42. Pandi-Perumal SR, et al. The effect of melatonergic and non-melatonergic antidepressants on sleep: weighing the alternatives. World J Biol Psychiatry. 2008 Jan; 4:1-13.
  43. Pandi-Perumal SR, et al. Role of the melatonin system in the control of sleep: therapeutic implications. CNS Drugs. 2007;21(12):995-1018.
  44. Sánchez-Barceló EJ, et al. Clinical uses of melatonin: evaluation of human trials. Curr Med Chem. 2010;17(19):2070-95. Review.
  45. Pallesen S, Bjorvatn B. Circadian rhythm sleep disorders. Tidsskr Nor Laegeforen. 2009 Sep 24;129(18):1884-7.
  46. Lemoine P, Nir T, et al. Prolonged-release melatonin improves sleep quality and morning alertness in insomnia patients aged 55 years and older and has no withdrawal effects. J Sleep Res. 2007 Dec;16(4):372-380.
  47. Zee PC, Goldstein CA. Treatment of shift work disorder and jet lag. Curr Treat Options Neurol. 2010 Sep;12(5):396-411.
  48. Srinivasan V, et al. Jet lag, circadian rhythm sleep disturbances, and depression: the role of melatonin and its analogs. Adv Ther. 2010 Nov;27(11):796-813.
  49. Paul MA, et al. Phase advance with separate and combined melatonin and light treatment. Psychopharmacology (Berl). 2011 Mar;214(2):515-23.
  50. Paul MA, et al. Melatonin treatment for eastward and westward travel preparation. Psychopharmacology (Berl). 2010 Feb;208(3):377-86.
  51. Gitto E, et al. Update on the use of melatonin in pediatrics. J Pineal Res. 2011 Jan;50(1):21-8.
  52. Tamura H, et al. The role of melatonin as an antioxidant in the follicle. J Ovarian Res. 2012 Jan 26;5:5. doi: 10.1186/1757-2215-5-5.
  53. Reiter RJ, et al. Peripheral reproductive organ health and melatonin: ready for prime time. Int J Mol Sci. 2013 Apr 2;14(4):7231-72.
  54. Rizzo P, et al. Effect of the treatment with myo-inositol plus folic acid plus melatonin in comparison with a treatment with myo-inositol plus folic acid on oocyte quality and pregnancy outcome in IVF cycles. A prospective, clinical trial. Eur Rev Med Pharmacol Sci. 2010 Jun;14(6):555-61.
  55. Batıoğlu AS, et al. The efficacy of melatonin administration on oocyte quality. Gynecol Endocrinol. 2012 Feb;28(2):91-3.
  56. Carlomagno G, et al. Contribution of myo-inositol and melatonin to human reproduction. Eur J Obstet Gynecol Reprod Biol. 2011 Dec;159(2):267-72.
  57. Reiter RJ, et al. Melatonin and stable circadian rhythms optimize maternal, placental and fetal physiology. Hum Reprod Update. 2013 Oct 16. [Epub ahead of print] PubMed PMID: 24132226.
  58. Arushanian EB, Beĭer EV. Pineal hormone melatonin is an universal adaptogenic agent. Usp Fiziol Nauk. 2012 Jul-Sep;43(3):82-100. Russian.
  59. Arushanian EB, Naumov SS. Comparative experimental study of the psychotropic and chronotropic activity of adaptogenic phytopreparations and melaxen. EkspKlin Farmakol. 2010 Jan;73(1):7-9.
  60. Smirnova AV, Naumcheva NN. Solar activity and cardiovascular diseases. Klin Med (Mosk). 2008;86(1):10-7.
  61. Mauriz JL, et al J. A review of the molecular aspects of melatonin's anti-inflammatory actions: recent insights and new perspectives. J Pineal Res. 2012 May 31. doi: 10.1111/j.1600-079X.2012.01014.x. [Epub ahead of print]
  62. Jaworek J, et al. Protective effect of melatonin on acute pancreatitis. Int J Inflam. 2012;2012:173675. doi: 10.1155/2012/173675.
  63. Ochoa JJ, et al. Melatonin supplementation ameliorates oxidative stress and inflammatory signaling induced by strenuous exercise in adult human males. J Pineal Res. 2011 Nov;51(4):373-80.
  64. Esposito E, Cuzzocrea S. Antiinflammatory activity of melatonin in central nervous system. Curr Neuropharmacol. 2010 Sep;8(3):228-42.
  65. Hardeland R, et al. Melatonin--a pleiotropic, orchestrating regulator molecule. Prog Neurobiol. 2011 Mar;93(3):350-84.
  66. Alamili M, et al. Melatonin suppresses markers of inflammation and oxidative damage in a human daytime endotoxemia model. J Crit Care. 2013 Oct 16. pii: S0883-9441(13)00326-2. doi: 10.1016/j.jcrc.2013.09.006. [Epub ahead of print]

These statements have not been evaluated by the Food and Drug Administration. These products are not intended to diagnose, treat, cure, or prevent any disease.


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