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."