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What is Melatonin?

Melatonin is a hormone (N-acetyl-5 methoxytryptamine) in the pineal (say: "pin-ee-all") gland each night to help us sleep. The pineal is a key element in the maintenance of the body’s endocrine regulation (hormone balance), immune system integrity, and daily metabolic balance. The pineal gland serves as a biological clock by secreting melatonin (along with numerous other neuropeptides) at night, and it also functions as the timekeeper of the brain, helping to manage the sleep-wake cycle. Melatonin production in the body is triggered by darkness and prevented by light, and it helps the body manage its circadian rhythm (know when it is time to sleep and time to wake up).

The antioxidant supplement Melatonin is not a herb or vitamin. Melatonin was discovered in the 1950s as a neurohormone produced in the brain by the pineal gland from the amino acid tryptophan and became available over the counter in 1994 as a dietary supplement. Tryptophan (l-tryptophan), an essential amino acid synthesized from proteins during digestion via the action of proteolytic enzymes, is converted during the day to serotonin (a brain chemical involved with mood), before getting converted ultimately to melatonin. Melatonin regulates your sleep-wake cycle and has been demonstrated to have powerful antioxidant properties. Many of Melatonin’s proposed therapeutic or preventive uses are based on this property, and because of this, aside from being used successfully to treat sleep disorders, Melatonin is also currently being studied for its effectiveness as a treatment for a variety of diseases, including AIDS, cancer, and cardiovascular disease.

What is Melatonin used for and who uses it?

Melatonin is responsible in setting the brain's internal clock, ensuring a balance between the body's hormone secretions, and generating and governing sleep-wake rhythms. The sleep-wake rhythms or circadian rhythm is an internal 24-hour time-keeping system that plays an important role in when we fall asleep and when we wake up, which is among melatonin’s key roles. The melatonin pulse controls many neuroendocrine functions, so it follows that when the timing or intensity of the melatonin peak is disrupted (as in aging, stress, jet-lag, or artificial jet-lag syndromes), many physiological and mental functions are negativey affected. The ability to think clearly, remember key facts, and make sound decisions can be profoundly hampered by these upsets in the biological clock. Melatonin is also involved in regulating the timing and release of female reproductive hormones, which means melatonin is crucial in determining when menstruation begins, the frequency and duration of menstrual cycles, and when menstruation ends (menopause).

In addition to its hormone actions, melatonin also has strong antioxidant properties and clinical evidence indicates it can help enhance the immune system. As an antioxidant, it eliminates cell-damaging free radicals, chemical constituents that have an unpaired electron, thus helping prevent or delay the onset of heart disease, cancer and other conditions. When taken or combines with certain cancer drugs, it can eliminate malignant cells. Relative to vitamin E, Melatonin is twice as potent at shielding cell membranes from lipid peroxidation, and is five times more effective compared to glutathione in neutralizing hydroxyl radicals. Because of low levels of glutathione in the brain, Melatonin and adenosine may be of particular importance in protecting brain cells. In addition to the hydroxyl radical, melatonin can also neutralize superoxides, singlet oxygens, hydrogen peroxide and hypochlorous acid. Melatonin also works synergistically with glutathione peroxidase, superoxide dismutase and catalase by improving gene expression and activity of these anti-oxidant enzymes.

Melatonin may help treat a number of sleep disorders, such as Delayed Sleep Phase Syndrome or DSPS (a condition characterized by trouble falling asleep); insomnia; and sleep disturbances that are brought about by illnesses and disorders such as dementia, depression, Alzheimer’s disease, Attention Deficit Disorder (ADHD), autism, and epilepsy. For its antioxidant, immune-enhancing, and anti-inflammatory properties, melatonin is currently being looked at as a possible treatment for cancer. Because the antioxidant effects of melatonin may enhance the effectiveness of chemotherapy drugs and reduce their side effects, melatonin supplements may prevent the unpleasant side effects of chemotherapy, such as nerve damage, mouth sores, wasting, and platelet count drops. It is also currently being studied as a treatment for high blood pressure, HIV, Parkinson’s disease, Seasonal Affective Disorder (SAD), smoking cessation, UV skin damage, and Tardive Dyskinesia (TD), a side effect of antipsychotic medications that causes involuntary twitching.

How pure is your Melatonin?

This pharmaceutical grade Melatonin is assayed by the manufacturer as 99.4% pure product (normal range 99.0% and above). You will receive a double sealed and labeled bulk polyethylene bag containing this white powder product. It contains no fillers, taste additives, or anti-caking agents. The remaining 0.6% by weight are inactive byproducts of the extraction.

To help regulate our sleep-wake cycles, our bodies produce melatonin at night. The amount of melatonin produced by our body seems to lessen as we get older. It is for this reason why scientists believe young people have less problem sleeping than older people. Melatonin supplements have also been used to aid the blind maintain a normal sleep pattern (since they lack light stimulus). Melatonin supplements may also assist in establishing new sleep patterns, and many people find them effective in preventing jet lag or adjusting to night shifts. For these reasons, it makes sense to consider taking this as a supplement.

What Is The Recommended Dosage of Melatonin?

Since the appropriate dose can vary enormously for each individual, and because there is no Recommended Dietary Allowance (RDA) for melatonin, start off small (e.g. less than half of a milligram) each night before bed-time, and gradually move up to larger doses if necessary. Since the body produces some melatonin naturally during sleep and levels of melatonin intake vary with a person's age, many doctors and experts recommend a level similar to the body's own production, typically between one to three milligrams taken two hours or one-half hour before a person wants to go to sleep. You can see the full bulk density/volumetric conversion chart for Melatonin here.

Mcg and mg are units of weight applied to tiny fractions of grams:
1 mcg = 1 microgram = one-millionth ( 1 / 1,000,000 ) of a gram
1 mg = 1 milligram = one-thousandth ( 1 / 1,000 ) of a gram = 1,000 mcg

To illustrate, a dosage of 1.5 mg is five times the dosage of 300 mcg (.3 mg). Since in Melatonin dosage we are dealing with tiny fractions of grams, accurate dosing of Melatonin can only be obtained with an accurate milligram weight scale such as those you can buy here for between $30 and $40 including shipping.

As always, if you have concerns or questions, consult a physician or a health care professional before taking any supplements. Before taking any kind of medicine, check with your doctor to ensure that the supplement you want to take is right for you. You may be allergic or you may have a sensitive stomach which may raise the need for special instruction as far as dosage goes. The information and product descriptions appearing on this website are for information purposes only, and are not intended to provide medical advice to individuals. Consult with your physician if you have any health concerns, and before initiating any new diet, exercise, supplement, or other lifestyle changes.

Safety, Precautions, and Potential side effects of Melatonin

Due to the extreme potency and the small dosing required of this product we are restricting sales to qualified health practice professionals only. Please email store@purebulk.com to prequalify your purchase of this product. Melatonin should not be taken by people using certain antidepressants, such as Prozac (a serotonin inhibitor) or Nardil (a monoamine oxidase inhibitor). Interaction between melatonin and these types of antidepressants can cause a stroke or heart attack. Preliminary symptoms include confusion, sweating, shaking, fever, lack of coordination, elevated blood pressure, diarrhea, and convulsions.

Keep in mind that melatonin can make you really sleepy, and should only be taken before sleep and not during the day or before driving. Melatonin has side effects, but much less compared to that of pharmaceutical sleeping pills. Vivid dreams and next day morning grogginess are common melatonin side effects on daily dosages greater than 0.5 mg. Those with high blood pressure can use melatonin without a major contraindication since melatonin may slightly lower blood pressure. Pregnant or breast-feeding women should not take it though. People taking blood thinners, antiseizure drugs, blood pressure medications, diabetes medications, or hormone replacement therapy should avoid melatonin supplements, as they may interfere with the effectiveness of these medications.

The information at Purebulk.com is NOT a substitute for medical advice. ALWAYS consult your doctor or pharmacist. Do not use any dietary supplement as a replacement for conventional care, or as a reason to postpone seeing a doctor about a medical problem. Tell all your health care providers about any complementary and alternative practices you use. Give them a full picture of what you do to manage your health. This will help ensure coordinated and safe care.

Melatonin is used in the following Brand names and Proprietary Formulas

Optimum Melatonin, Fountain Of Youth HGH Complete, NOW Melatonin, Pharmaceutical Alternatives SomaRest, SciVation Knockout, Accurate Release®; Appleheart Melatonin®; Circadin®; Inspired by Nature®; Mel®; Melatonin-BioDynamax®; Melatonin Controlled Release®; Melatonin-Metabolic Response Modifier®; Melatonin-New Hope Health Products®; Melatonin Olympian Labs®; Melatonin-Optimum Nutrition®; Melatonin Tablets®; Melatonin Time Release®; Melaxen®; Nature's Bounty®, Puritan's Pride®; Rozerem®; Twinlab® Melatonin; Valdoxan®.

Combination product examples: Melatonex® (vitamin B6); Melatonin Forte® (Piper methysticum, kavalactones, valeriana); Melatonin PM Complex® (vitamin B6, vitamin B2, vitamin B3); Melatonin spray® (Gamma Aminobutyric Acid, Pyridoxal-5-phosphate); Super Snooze with Melatonin® (valerian root, hop, scullcap, chamomile, passion flower).

References & Further Research

Prolonged melatonin administration decreases nocturnal blood pressure in women
The nocturnal decline of blood pressure (BP) is almost coincident with the elevation of melatonin, which may exert vasodilatating and hypotensive effects. In this study it was investigated whether prolonged nocturnal administration of melatonin could influence the daily rhythm of BP in women. Overall data indicate that prolonged administration of melatonin may improve the day-night rhythm of blood pressure, particularly in women with a blunted nocturnal decline.

Melatonin and bright-light treatment for rest-activity disruption in institutionalized patients with Alzheimer's disease
Fifty subjects (mean age 86) with Alzheimer's disease were divided in three. One group received 1 hour of natural morning light exposure (> or = 2,500 lux in gaze direction) Monday to Friday for 10 weeks and 5 mg melatonin, anther group had natural light therapy alone. Control subjects received usual indoor light (150-200 lux). Light treatment alone did not improve nighttime sleep, daytime wake, or rest-activity rhythm. Light treatment plus melatonin increased daytime wake time and activity levels and strengthened the rest-activity rhythm.

Melatonin Improves Sleep in Asthma: A Randomized, Double-blind, Placebo-controlled Study
Disturbed sleep is common in asthma. Melatonin has sleep-inducing activity and reportedly affects smooth muscle tone and inflammation. The aim of this study was to evaluate the effect of melatonin on sleep in patients with mild and moderate asthma. This was a randomized, double-blind, placebo-controlled study. Melatonin treatment significantly improved subjective sleep quality, as compared to placebo. No significant difference in asthma symptoms, use of relief medication and daily PEFR was found between groups. We conclude that melatonin can improve sleep in patients with asthma. Further studies looking into long-term effects of melatonin on airway inflammation and bronchial hyperresponsiveness are needed before melatonin can be recommended in asthmatic patients.

Melatonin for International Customers

We have the most economical shipping costs & labeling practices for International orders. You can see our shipping costs here. Also, please note, that anything in a 1.5kg package can be shipped within a single flat rate envelope, however our shopping cart mistakenly displays 2 envelopes. Go ahead and ship the order, and you will notice that it only charges you the cost of 1 anyway. Look at the shipping costs tab above to see for yourself how you can calculate these charges.

Buying Melatonin Bulk or Wholesale

If you need Melatonin in bulk or wholesale quantities, please feel free to contact us with sourcing/shipping/fulfilment questions. If you have any questions about shipping or would like to arrange a shipment to an excluded country please use the contact page!