Melatonin

Melatonin

10 mg

180 Sublingual Tablets ( SKU: 9286, NPN: 80036635 )

Benefits

  • Sublingual tablets provide consistent melatonin bioavailability - pharmacokinetic studies indicate that 30 to 60% of an oral dose of melatonin is metabolized via the liver9 and overall gastrointestinal absorption is variable10,11
  • A singular high potency sublingual tablet is optimal for those who need higher doses of melatonin (10-20 mg)
  • Derived from non-animal sources
  • Refreshing, natural peppermint flavour

Feature Summary

Sleep is a vital part of health and many of us are not getting enough. The 2002 Canadian Community Health Survey found about 1 in 7 adults has difficulty falling asleep or staying asleep. Insomnia affects 1 in 3 seniors and is 40% more common in women. Changes in sleeping patterns are largely reflective of our circadian rhythms, which are guided by the pineal hormone, melatonin. Melatonin is also known to decline as we age, which accounts for a number of the sleep changes we experience throughout life. Additionally, jet lag and shift work can significantly alter circadian rhythms and thus melatonin secretion.1,2,3

In the face of insomnia, many people have tried prescription sleeping pills, but they can interfere with REM sleep, disrupt deeper stages of sleep and lead to confusion, sluggishness, anxiety and even drug dependency. Conversely, Melatonin has shown clinical benefit for inducing sleep or adjusting sleep cycles4 reducing sleep onset latency and improving perceived quality of sleep, without impairing daytime psychomotor performance or creating dependency.5,6 In fact, supplemental melatonin and bright light therapy are considered standard medical treatment for cases of jet lag, shift work, age-related insomnia, delayed sleep-phase disorder, advanced sleep-phase disorder, and non-24-hour sleep-wake disorder.7 Chronic sleep disturbance is a risk factor for premature aging, diabetes, obesity, cardiovascular disease and certain cancers,8 demonstrating just how important it is to maintain normal melatonin levels to enhance sleep quality.

Medicinal Ingredients

Serving Size: 1 Sublingual Tablet
Servings per Container: 180

Each Tablet Contains:
Melatonin (Vegetarian Source)............................................10 mg

Non-Medicinal Ingredients

Lactose monohydrate, microcrystalline cellulose, natural peppermint flavour, croscarmellose sodium, vegetable grade magnesium stearate (lubricant).

Allergens:

Contains no artificial preservatives, colours or sweeteners and no soy, wheat or yeast. Sealed for your protection. Do not use if seal is broken. For freshness, store in a cool, dry place.

Contraindications

Consult a health care practitioner prior to use if you have a hormonal disorder, diabetes, liver or kidney disease, cerebral palsy, seizure disorders, migraine, depression and/or hypertension, or if you are taking blood pressure or sedative/hypnotic medications. Do not use if you are taking immunosuppressive drugs and/or if you are pregnant or breastfeeding. Do not drive or use machinery for 5 hours after taking melatonin. If symptoms persist continuously for more than 4 weeks (chronic insomnia), consult your health care practitioner.12 Keep out of reach of children.

Drug Interactions

Melatonin can stimulate immune function and may reduce the efficacy of immunosuppressive drugs.13 Theoretically, concomitant use of melatonin with sedative/hypnotic or central nervous system depressants may be additive. However, benzodiazepines may also reduce endogenous melatonin levels.14 Melatonin can reduce the efficacy of blood pressure medication nifedipine GITS (Procardia XL).15 Case reports suggests melatonin may potentiate anticoagulant and antiplatelet medications, however, the mechanism and clinical significance are unknown.16 Melatonin may impair glucose utilization and increase insulin resistance in diabetic patients. However, the clinical significance of this effect on diabetics is unknown.17 Contraceptive drugs can increase endogenous melatonin levels. Theoretically, this may increase the effects and adverse effects of oral melatonin use.18 Fluvoxamine significantly inhibits the elimination of melatonin,19 which some researchers believe could be helpful in the treatment of refractive insomnia.20 However, this interaction may also cause excessive unwanted drowsiness and other adverse effects.

  1. Karasek M, Winczyk K. Melatonin in humans. J Physiol Pharmacol. 2006 Nov;57 Suppl 5:19-39.
  2. Zawilska JB, Skene DJ, Arendt J. Physiology and pharmacology of melatonin in relation to biological rhythms. Pharmacol Rep. 2009 May-Jun;61(3):383-410.
  3. Alternative Medicine Review. Melatonin Monograph. Altern Med Rev. 2005;10(4):326-336.
  4. Kunz D, Mahlberg R, Muller C, Tilman A, Bes F. Melatonin in patients with reduced REM sleep duration: two randomized controlled trials. J Clin Endocrinol Metab. 2004 Jan;89(1):128-34.
  5. Wade AG, Ford I, Crawford G, McMahon AD, Nir T, Laudon M, Zisapel N. Efficacy of prolonged release melatonin in insomnia patients aged 55-80 years: quality of sleep and next day alertness outcomes. Curr Med Res Opin. 2007 Oct;23(10):2597-605.
  6. Wade AG, Ford I, Crawford G, McConnachie A, Nir T, Laudon M, Zisapel N. Nightly treatment of primary insomnia with prolonged release melatonin for 6 months: a randomized placebo controlled trial on age and endogenous melatonin as predictors of efficacy and safety. BMC Med. 2010 Aug 16;8:51.
  7. Bjorvatn B, Pallesen S. A practical approach to circadian rhythm sleep disorders. Sleep Med Rev. 2009 Feb;13(1):47-60, Epub 2008 Oct 8.
  8. Litinski M, Scheer FA, Shea SA. Influence of the Circadian System on Disease Severity. Sleep Med Clin. 2009 Jun 1;4(2):143-163.
  9. Lane EA, Moss HB. Pharmacokinetics of metabolism in man: first pass hepatic metabolism. J Clin Endocrinol Metab. 1985;61:1214-1216.
  10. Kovacs J, Brodner W, Kirchlechner V, Arif T, Waldhauser. Measurement of urinary melatonin: a useful tool for monitoring serum melatonin after its oral administration. J Clin Endocrinology Metabolism. 2000;85 (2):666-670.
  11. Waldhauser F, Waldhauser M, Lieberman HR, Deng MH, Lynch HJ, Wurtman RJ. Bioavailability of oral melatonin in humans. Neuroendocrinology. 1984 Oct;39(4):307-13.
  12. Natural Health Products Directorate. Monograph: Melatonin – sublingual [Internet]. 2006 [updated 2006 Dec 7; cited 2012 Sep 21]. Available from:http://webprod.hc-sc.gc.ca/nhpid-bdipsn/monoReq.do?id=137&lang=eng
  13. Lissoni P, Barni S, Mandala M, Ardizzoia A, Paolorossi F, Vaghi M, Longarini R, Malugani F, Tancini G. Decreased toxicity and increased efficacy of cancer chemotherapy using the pineal hormone melatonin in metastatic solid tumor patients with poor clinical status. European Journal of Cancer. 1999;35:1688-92.
  14. Djeridane Y, Touitou Y. Chronic diazepam administration differentially affects melatonin synthesis in rat pineal and Harderian glands. Psychopharmacology (Berl). 2001;154:403-7.
  15. Lusardi P, Piazza E, Fogari R. Cardiovascular effects of melatonin in hypertensive patients well controlled by nifedipine: a 24-hour study. Br J of Clin Pharmacol. 2000 May;49(5):423-7.
  16. Herxheimer A, Petrie KJ. Melatonin for the prevention and treatment of jet lag. Cochrane Database Syst Rev. 2002;2:CD001520.
  17. Cagnacci A, Arangino S, Renzi A, Paoletti AM, Melis GB, Cagnacci P, Volpe A. Influence of melatonin administration on glucose tolerance and insulin sensitivity of postmenopausal women. Clin Endocrinol (Oxf). 2001 Mar;54(3):339-46.
  18. Wright KP Jr, Myers BL, Plenzler SC, Drake CL, Badia P. Acute effects of bright light and caffeine on nighttime melatonin and temperature levels in women taking and not taking oral contraceptives. Brain Res. 2000 Aug 11;873(2):310-7.
  19. Hartter S, Grozinger M, Weigmann H, Roschke J, Hiemke C. Increased bioavailability of oral melatonin after fluvoxamine coadministration. Clin Pharmacol Ther. 2000 Jan;67(1):1-6.
  20. Grozinger M, Hartter S, Wang X, Roschke J, Hiemke C, Rose DM. Fluvoxamine strongly inhibits melatonin metabolism in a patient with low-amplitude melatonin profile. Arch Gen Psychiatry. 2000 Aug;57(8):812-3.