Melatonin

What Is It?

Melatonin is a hormone manufactured and released into the bloodstream by the pebble-size pineal gland nestled deep within the human brain. Surprisingly, scientists only became aware of melatonin’s presence in 1958. Children tend to excrete large amounts of this hormone, while older adults produce relatively little. But individual levels of melatonin vary widely. About 1% of the population naturally has quite low levels, while another 1% has levels 500 times above the average.

Melatonin is intimately involved in synchronizing the body’s hormone secretions, setting the brain’s internal clock and generating circadian rhythms (daily biorhythms). These patterns govern the release of hormones that regulate such body functions as reproduction and digestion. Significantly, melatonin also works around the clock to signal the body, which is sensitive to light cues, when to sleep and when to awaken. Typically, the pineal gland begins excreting melatonin around dusk, rapidly increases its output between 2 A.M. and 4 A.M., and then decreases its output again as daylight appears.

Most melatonin supplements on the market are pure synthetic versions of the hormone, and are practically identical to that which humans produce naturally. Although sold as a dietary supplement in the United States, melatonin is available by prescription only in France and a number of other countries.

Health Benefits

Melatonin is widely used to relieve insomnia and the symptoms of jet lag, two common problems of modern life. Unlike many other sleep aids, melatonin isn’t addictive. The hormone may promote health in other ways as well. As an antioxidant, it hunts down and eliminates cell-damaging free radicals, possibly helping to prevent or delay the development of heart disease, cancer and other conditions. When combined with certain cancer drugs, it may destroy malignant cells. Other preliminary findings suggest a possible role in lessening the nerve damage associated with Parkinson’s and Alzheimer’s diseases, and an ability to prevent strokes and heart attacks by reducing high blood pressure.

Specifically, melatonin may help to:

Treat insomnia. The ability to fall asleep and stay asleep may get a boost from melatonin supplementation. Some studies of young and elderly adults have shown that taking a small amount of melatonin before bedtime helps to both hasten sleep and improve its quality. These benefits were seen in insomniacs as well as in individuals who struggle with only occasional sleep problems.

Ease sleep problems caused by pain or stress. Frequent night-time awakenings can occur as a result of chronic pain or stress. In such situations, melatonin may help by encouraging sounder slumber.

Fight jet lag and restore normal sleep patterns. If you’re working a night shift or are traveling across time zones, melatonin supplements may help your body to overcome any disorientation and quickly reestablish a normal sleep pattern. Recent studies of airline personnel and others who travel long distances found that melatonin supplements significantly relieved jet lag symptoms. This was true regardless of whether they were flying eastbound or westbound. However, not all studies have found melatonin to be superior to a placebo for such jet lag symptoms as fatigue, daytime sleepiness and impaired alertness.

Slow the aging process. Animal research indicates that melatonin may be of value in extending life–elderly mice administered the supplement lived 25% longer than their cohorts in one study–although much more investigation is needed before firm conclusions can be made about its value for humans in this regard. Melatonin’s antioxidant properties may help to stave off illnesses commonly related to aging, such as heart disease and cataracts. The hormone may boost immune-system function as well, which can weaken with age.

Combat SAD-related depression. A number of people who feel quite normal and energetic in summer become depressed and sluggish in winter, when sunlight is weaker and less abundant. Low melatonin levels may also be present in individuals who react in this way. According to a handful of preliminary studies, such individuals are said to be suffering from SAD (seasonal affective disorder) and may experience a significant improvement in mood if they take several tiny doses (0.1 mg) of melatonin in the afternoon. Study participants who failed to improve took either a large single dose in the morning or no melatonin at all. More studies are needed in this area.
Note: Melatonin has also been found to be useful for a number of other disorders. For information on these additional ailments, see our Dosage Recommendations Chart for Melatonin.

Forms

tablet
spray
softgel
lozenge
liquid
cream
capsule

Dosage Information

For insomnia: Take 1 to 3 mg immediately before going to bed between 9 P.M. and 11 P.M. Start with the lower dose and gradually increase it over time, if needed. (Older adults may want to start at an even lower dose of 0.3 to 0.5 mg.) In general, the lower dose (1 mg) may prove effective if you have trouble falling asleep, but a higher dose (3 mg) may be necessary if you have difficulty staying asleep.

To prevent jet lag when flying from west to east:
–On the day before the flight, take a small dose (about 0.5 mg) of melatonin in the middle of the afternoon.

–The day of the flight, take 3 mg two hours earlier than you took the melatonin dose the previous day.

–Upon arrival at your final destination, spend some time in natural sunlight as soon as possible.

–For the first three or four nights of your stay, take 3 mg before bedtime.
To prevent jet lag when flying from east to west:
–On the day before the flight, take a small dose (0.5 mg) in the morning, and the same amount again on the morning of your departure.

–Upon arrival at your final destination, wait until morning to take another small dose (0.5 mg, for example) and continue to do so for the next few mornings.

–In the late afternoon of the day that you land, try to spend at least half an hour outside without wearing sunglasses.

For overnight shift work: If you are on a consistent schedule that involves retiring in the morning, take 1 to 3 mg just before going to sleep. If your work hours tend to change, however, consult a health expert for guidance on how and when to take melatonin.
Be sure to check out our Dosage Recommendations Chart for Melatonin, which lists therapeutic dosages for specific ailments at a glance.

Guidelines for Use

To relieve insomnia, it’s important to take melatonin at the same time every day.

Because precise dosing is so important with a hormone such as melatonin, it’s probably not wise to use melatonin in topical (cream or sublingual spray) forms. With repeated applications–and depending on how efficiently your skin absorbs the product–you may end up absorbing more melatonin than you intended.

General Interaction

Check with your doctor before using melatonin along with a conventional antidepressant. Adverse drug reactions may result.

Excessive drowsiness may occur if the hormone is taken along with sedatives, sedating antihistamines, muscle relaxants and narcotic pain relievers.

Consult your doctor before considering melatonin if you take prescription corticosteroids. An adverse reaction is likely.
Note: For information on interactions with specific generic drugs, see our WholeHealth Chicago Drug/Nutrient Interactions Chart.

Possible Side Effects

Most people feel drowsy within 30 minutes of taking melatonin, an effect that can persist for several hours.

The development of side effects appears to depend on how much you take and how sensitive you are to the hormone.

No major problems have been reported in individuals taking relatively conservative doses (3 mg or less).

Minor side effects have been observed in some people taking up to 8 mg. These include headache, stomach upset, lethargy and disorientation. Some users report a lack of clear-headedness upon waking, and vivid dreams or bad bouts of insomnia. Lower the dosage if any of these reactions occur.

Still under investigation is whether high doses of melatonin alter the menstrual cycle and can adversely affect a woman’s fertility.

Other risks associated with prolonged use (longer than six months) at any dosage are still being explored.
• Preliminary research in test tubes indicates that melatonin supplements may react with chemicals in the body to alter behavior, such as mood, in unwanted ways. More research is needed to determine if this occurs in humans as well.

Cautions

If you take any prescription medication, check with your doctor before starting on melatonin supplements, as potentially hazardous interactions could result.

When buying melatonin supplements, check the label to confirm that they’re synthetically produced and not made from animal glands; these pose the risk of exposure to contaminants.

Because melatonin can cause drowsiness, avoid driving or handling heavy machinery for several hours afer taking it.

Don’t take melatonin if you’re pregnant or nursing.

Women trying to conceive should not take melatonin; at high doses, it appears to work as a contraceptive.

Children and teenagers produce copious amounts of melatonin and should not take melatonin supplements.

Don’t take melatonin if you suffer from kidney disease, epilepsy, diabetes, depression, any autoimmune disease, severe allergies, heart disease, leukemia or multiple sclerosis.

Ailments-Dosage

Arthritis 1-3 mg at bedtime for insomnia. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
Chronic Pain 1-3 mg at bedtime. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
Depression 1 mg at bedtime. Doses lower than 1 mg may also work.
Fibromyalgia 1 mg at bedtime. Doses lower than 1 mg may also work.
Insomnia 1-3 mg at bedtime. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
Menopause 1-3 mg at bedtime to improve sleep. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
Migraine 1-3 mg at bedtime to improve sleep. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
Perimenopause 1-3 mg at bedtime. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
PMS 1-3 mg at bedtime. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
Stress 1-3 mg at bedtime. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.
Tinnitus 1-3 mg at bedtime, as needed. The lower dose should be tried first. If necessary, gradually increase the dose. Doses lower than 1 mg may also work.

Doctor Recommendations
David Edelberg, M.D.

Melatonin has proven to be remarkably helpful for insomnia, and for some people, it’s as potent as any prescription sleeping pill. Which is why a prescription is required for melatonin in most European countries.

HOW IT HELPS INSOMNIA

Normally, the pineal gland at the base of your brain sends out a burst of melatonin in the late evening in response to increasing darkness, and this makes you sleepy. If you’ve got an adequate natural supply of melatonin, taking an additional melatonin supplement probably won’t help all that much. (As a sidelight, blind individuals with no light-dark perception can have terrible problems with sleep and do in fact benefit nicely from melatonin supplements.) If you’re finding it’s getting harder and harder to fall asleep the older you get, it just may be that the level of melatonin in your pineal gland is declining. Here, extra melatonin can be a godsend and no shortage of studies confirm this. By the way, melatonin will have an additive effect as a sleeping agent if used with other sleepy-time herbs such as 5-HTP or valerian.

WHAT TO LOOK FOR

Although melatonin is produced by the brain’s pineal gland, store-bought melatonin is strictly a synthetic product—and not a puree of dehydrated cow pineals.

Forms

Melatonin comes in several forms, and all of them work well. Capsules or tablets are the original form; they take effect in about an hour. Time-release capsules and tablets allegedly work longer, mimicking the body’s own melatonin levels during the night. (These pills may also be marked “extended-release” or “sustained-release.”) In fact, one study showed that although regular and time-release forms were equally effective at initiating sleep, the time-release form was better at maintaining sleep. Liquid drops are placed undiluted under the tongue (they’re orange-flavored), so they are directly absorbed through the tissues of the mouth and race into the bloodstream. Sprays are also absorbed very quickly, so you’re better off if you tuck yourself in before spraying. Lozenges should be allowed to gradually dissolve under your tongue.

OTHER SUGGESTIONS

Adjust amounts gradually. The capsule size ranges from 1 to 3 mg. I’d start at the lower end first and slowly increase the dose, if needed. You certainly can get a hangoverlike feeling the next day if you take too much late at night. Take melatonin at the same time each evening to get the full effect from your supplement. It’s a hormone, not a sleeping pill, and it works much the way your body does. (In fact, it is the regular release of your own natural melatonin that makes you feel sleepy at the same time each evening.) Important tip: This supplement works for sleep problems only if your blood levels of melatonin are low. While you can get tested, melatonin measurements fluctuate so much that the tests are generally of little use. You’d probably do better simply trying the supplement to see if it works for you.

Posted in Knowledge Base, M, Mental Health, Nutrition, Nutritional Supplements, Vitamins, & Herbal Remedies Tagged with: , , , , , , , , , ,