Take Two Melatonins and Call Me in the Morning

What Dosage is Best?

Melatonin supplements are currently available in 0.2 mg, 0.3 mg, 0.5 mg, 0.75 mg, 1 mg, 1.5 mg, 2 mg, 3 mg, 5 mg, 10 mg, and 20 mg tablets or capsules. Some bottles list dosages in mcg (micrograms); 1 mg (milligram) equals 1000 mcg. Lozenges, which are dissolved in the mouth, are available in 0.5 mg, 1 mg, 2 mg, 2.5 mg, 3 mg, and 5 mg. In the summer of 1995, a slow release form of melatonin became available. Soon after, a liquid preparation came on the market with 1 mg per cc. In March of 1996, a clever company came out with melatonin tea, 0.5 mg per tea bag.

Melatonin cannot be patented for exclusive sale, so a number of companies manufacture and distribute it. A wide range of doses works for people. Each person has a unique physiology, hence, no blanket statements can be made. A person may also require a higher dose during nights when he or she is extremely alert, upset, preoccupied, or had a caffeinated evening drink.

It may be best to swallow a melatonin pill on an empty stomach or with a small meal. Melatonin taken on a full stomach does not seem to be as consistently effective. This may be because the pill is not fully absorbed, or simply absorbed too slowly.

After swallowing a pill, peak levels in the blood are found in about 1 hour. An interesting finding in a previously discussed study referred to in Chapter 1 (Waldhauser, 1990) was that the amount of melatonin present in the bloodstream of different volunteers sometimes varied by a factor of 300! This shows the uniqueness of each individual’s absorption and metabolism.

Melatonin in the range of 0.1 mg to 5 mg is effective in inducing a natural yawn and maintaining a deep sleep in most people.

An article published in the May, 1995, issue of Clinical Pharmacology and Therapeutics (57:552-8) and titled “Sleep-inducing effects of low doses of melatonin ingested in the evening” gives us a good idea on appropriate dosages. Drs. Zhdanova and Wurtman, from MIT, gave volunteers 0.3 mg of melatonin and found it to be effective. This low dose was able to raise blood melatonin levels above 120 picograms per milliliter, a level present at night in children while in deep sleep (a picogram is one millionth of a milligram).

If you are planning to take melatonin for the first time, start with a dose in the range of 0.1 to 0.5 mg. Most tablets come in doses much higher than this so you may need to break them in small pieces. Capsules can be opened and a portion used. If these low doses are not effective, then you can take more the following nights.
If there is no response to pills, sublingual lozenges can be tried. Lozenges seem to be more consistently effective in inducing sleep than pills since they are not absorbed from the stomach and metabolized by the liver— which can greatly reduce the amount reaching the bloodstream. Instead, the melatonin dissolves in the mouth and directly enters the bloodstream. Some individuals find that a small dose from a lozenge may be as effective as a large dose from a pill.

There are some people who respond weakly even to high doses. Ted, a 23 year old student, informs me, “I took what I believe was an overdose, two 3 mg pills and two 5 mg lozenges, a total of 16 mg. It did seem to induce in me that sleepy state right before one falls asleep, but the feeling wasn’t overwhelming. In fact, I only felt sleepy when I laid on my bed; otherwise I think I could have stayed up longer.”

Wayne, a 24 year old computer programmer from Seattle, asserts, “I have severe chronic insomnia and I’ve used melatonin twice. Neither time did it seem to improve my sleep. (My body is amazingly good at resisting sleep.) Both were 3 mg doses taken just a few minutes before bed.”

Keep in mind that melatonin is subtle compared to the effects of prescription sleeping pills. It doesn’t have their knockout punch. Matthew, a 26 year old teacher, tells me, “I am impressed at the similarity between melatonin and natural sleep. As someone who has suffered periodic bouts of insomnia, melatonin provided natural sleepiness without the drowsiness of some prescription medicines that I’ve taken in the past.” Heather, a 24 year old massage therapist, nods, “Sleep comes on naturally and peacefully.”

Some individuals do very well with small doses. A survey respondent wrote, “I’m 57 years old and have been taking melatonin regularly for insomnia for a year. Previously, I would sleep 4 or 5 hours, then wake up and not be able to go back to sleep. With 1 mg of melatonin I sleep through the night. If I do happen to wake up, I am able to easily fall back asleep. I’ve had no side effects at all and wake up refreshed.”

For most people melatonin is effective the very first night. Some of my patients report feeling an effect after the first week. However, some may take up to a month before noticing a difference. MacFarlane and colleagues also noted this: “Improved sleep is in evidence from the first treatment night, but an increased efficacy is observed with repeated treatments.”

When is the Best Time to Take Melatonin?

People vary widely in their response times. Pills are effective for most people when swallowed about half an hour to 90 minutes before bed. Lozenges dissolved in the mouth seem to work more quickly. You may take them between 10 minutes and an hour before going to bed. Most people notice a natural yawn within half an hour of dosing.

I, personally, do well with 0.25 mg taken 45 minutes before bedtime. When I put my head on the pillow, I’m out! I have found that a low dose is more effective when taken at least an hour or two before bed while a high dose can be taken closer to bedtime. One of the most common mistakes people make with melatonin is taking it too close to bedtime. This is not a prescription sleeping pill and doesn’t work as quickly. For the most part, a good hour is required for best results. Let’s also keep in mind that tablets and lozenges from different manufacturers may be absorbed at different rates.

Leona, a 42 year old social worker, tells me, “I took a 1 mg lozenge right before bed. I didn’t feel any effects from it and had trouble falling asleep. I tried it again a few nights later right before bed. Still no effect. I was almost going to give up on melatonin until you suggested I try it at least 1 hour before bed. This seemed to make all the difference; I went to sleep within a couple of minutes of putting my head on the pillow.”

One survey respondent wrote that he has chronic insomnia and takes 10 mg of melatonin an hour before bed. He wakes up at 3 or 4 am and takes another 10 mg. This works for him; he feels fine the next day. Another user noted that he once woke up at 3 am and couldn’t fall asleep. He hadn’t taken any melatonin the night before. After an hour of tossing in bed, he took two 3 mg pills at 4 am and had trouble getting out of bed the next day. He felt groggy most of the morning. It’s best to take melatonin to accentuate our natural sleep rhythm avoiding the use at a late hour where it could shift our cycle to an undesired time.

One friend has found that breaking a pill in small portions and taking about 0.2 mg 90 minutes before bed and taking another 0.2 mg 30 minutes before bed gives her a better sleep than taking it all at one time. This is a good option for some since melatonin is gradually produced by the pineal gland at night. One could therefore take small doses maybe 2 hours, 1 hour, and 30 minutes before bed. I tried this approach recently, using tiny doses, and it worked well. I must have taken a total of less than 0.3 mg.

These anecdotes indicate the importance of trial and error in finding out the best dose and the best time for your unique self. If melatonin doesn’t work for you initially, don’t give up. Experiment with varying doses and times. You may also try another brand if the first is not effective. As a rule, if you have trouble falling asleep, consider sublinguals. If you have no trouble falling asleep but wake up in the middle of the night or early morning, consider taking a pill just before bed with food, or the slow release form, which stays in your system longer. If you have difficulty in both falling asleep and staying asleep, you could combine low doses of sublinguals and the slow release.

Slow-release (also known as sustained, time, or controlled-release) melatonin will likely become more popular in the future. A 1995 study published in The Lancet found a 2 mg slow release pill to be very helpful in older insomniacs, especially after regular use for 3 weeks (Garfinkel). It is possible that smaller doses, such as 0.5 mg, may also be just as effective.

Those who are used to taking prescription sleeping pills may require a few days or weeks before noticing the subtler effects of melatonin.

Is Melatonin Addictive?
Since no studies in humans have yet been published specifically addressing this question, I can’t make a definitive statement about melatonin’s addictive potential. I can only state my own experience and the experience of my patients who feel melatonin not to be physically addictive. Those who take it for its anti-aging effects use it regularly and aren’t concerned with addiction. The majority of users who take it for improved sleep only do so when they really need it. A few mentioned that they liked the improved quality of sleep so much that they wanted to use melatonin often— almost like a weak psychological addiction.

It is possible that for some insomniacs melatonin can be habit forming. Stuart, a regular user for 4 months, is one example: “I don’t have a strong urge to take it but I can tell the difference in the quality of my sleep when I do use it. At night, when its getting close to bedtime, I sometimes think to myself, you know, I really want to sleep well tonight. So, often I pop a pill.”

Dennis, who is 52, writes, “I have been a vegetarian and meditator for 20 years. Anything I take routinely I make a practice of not taking for 1 day a week, 1 week per month, and 1 month per year. With melatonin I have noticed no withdrawal, no feeling of addiction, and no noticeable effect other than natural restful sleep when I take it. Honestly, it feels like something my body is missing and should have, and welcomes it when I take it. I feel no ‘impact’ like I do with pharmaceuticals. Great stuff.”

For the past year and a half I’ve taken about 1-5 mg of melatonin three or four nights a week. With time, I discovered that a lower dose, such as 0.25 mg, was also effective. My sleep has been extremely deep and restful. I recently stopped taking it for a week and have noticed no withdrawal symptoms. I personally find that there is a slight habit forming tendency, and, as Stuart reported above, it is tempting to use melatonin regularly since the sleep it provides is so soothing.

Some users find that they initially sleep an hour or two longer. After a few weeks, they sleep fewer hours but more efficiently.

What About Tolerance?

No formal studies have been done in humans regarding this issue. The use of most pharmaceutical sleeping medicines is known to lead to tolerance. Higher and higher doses are often needed.

Tolerance to melatonin is infrequent. Less than a tenth of my patients or survey respondents felt the need to take higher doses. Jerry, a 67 year old chiropractor from Miami, tells me, “I’ve been using 1.5 mg of melatonin regularly for 7 months. It seems to be as effective now as the first few nights.” Tolerance is even less frequent in those who do not use melatonin every night, but take breaks once in a while.

I have, though, come across individuals who became tolerant to melatonin. Loretta, a 46 year old insomniac from Portland, Oregon found that melatonin stopped working for her when she took 9 mg every night for 10 months. Were melatonin receptors in her brain downregulated? A 1993 study in rats found regular supplementation decreased the number of melatonin receptors in the brain (Gauer). Will regular, high dose melatonin desensitize our brain to this hormone? I tell all my patients and melatonin users to use this supplement at most every other night, and in low doses, until we learn more about the question of tolerance.

Are There Withdrawal Symptoms?

Abruptly stopping prescription sleep medicines after chronic use can often result in sleep disturbances for a week or two. For some it takes longer. Data from my surveys suggest that withdrawal symptoms from the abrupt discontinuation of short-term melatonin use are uncommon. There is little or no insomnia the night following discontinuation, and any disturbances are corrected within a few days.

A few of my patients have noticed that they sleep just as well, or even better, the night following the use of melatonin. It seems that sometimes there is a slight carry-over effect.

Steve Dyer, 38, a software engineer from Cambridge, Mass., writes, “I find that melatonin is very effective at helping me get to sleep. Originally, a single lozenge was all that I needed, but I found that 4 lozenges worked better. I go to bed on time, and wake up on-time, refreshed.

“I used 10 mg of sublingual melatonin, four 2.5 mg lozenges, for several months. Upon stopping it, I had no rebound insomnia at all.”

It’s still too early to tell whether suddenly stopping melatonin after a few years of regular, nightly use will lead to withdrawal symptoms.

Many of our current uncertainties about the use of melatonin will no doubt be answered by the high interest in this supplement which is generating a great deal of research. Marilyn Elias, who wrote the December 20, 1995 article in USA Today, reports that the National Institutes of Health is spending $5 million a year on 57 melatonin studies, mostly about sleep and the body clock.

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Written by Ray Sahelian MD

Explore Wellness in 2021