Melatonin Serotonin Level - Sublingual or Time Release

Melatonin, the pineal hormone, became available over the counter in 1994. Melatonin is a hormone released each night to help us sleep. In addition to sleep, melatonin has many other benefits. Melatonin is available as a capsule to swallow and as melatonin sublingual under the tongue. Melatonin is made from serotonin. A melatonin level is not necessary to know before using a melatonin product. A sublingual melatonin may work quicker but time release melatonin may sustain sleep longer.

Melatonin Source Naturals
Melatonin supplement sustained release form of melatonin provides a slower, more physiological absorption.

Suggested Use: 1/3, 1/2 or a full melatonin supplement one to 4 hours before bedtime. Melatonin works best if used only a few times a week as opposed to nightly.

Supplement Facts:
Melatonin 1 mg timed release

Benefits of Melatonin:
1. Lessens the effects of jet lag. Daily doses of melatonin, at 1 to 5 mg, taken an hour or two before bedtime at the new destination for 2 to 4 days may be helpful in reducing symptoms of jet lag. It's very difficult to know exactly the dosage of melatonin that would be effective. There is a wide range of individual response to melatonin.

2. Is a strong antioxidant. Evidence continues to accumulate regarding the antioxidant benefits of melatonin. In laboratory studies, melatonin has been found to stimulate natural antioxidant systems in addition to offering protection to the DNA present within cells. While these effects have been observed primarily using pharmacological (very large) doses of melatonin, in a small number of experiments melatonin has been found to have antioxidant properties in small, physiological doses as well. The ability of melatonin in inhibiting oxidative damage has been tested in a variety of neurological diseases where free radicals have been suspected as being in part causative of the condition. Thus, melatonin has been shown to reduce amyloid protein toxicity of Alzheimer's disease, to reduce oxidative damage in some types of Parkinson's disease, to reduce brain injury when exposed to low blood or oxygen flow, and to lower brain damage due to a variety of toxins.
        Low dose melatonin treatment in mice enhances the body's natural anti-oxidant system, and this may have anti-aging properties. This study has convinced me to take 0.1 or 0.2 mg of melatonin a couple of nights a week. I have a melatonin pill of 0.5 mg and I take a portion of it about an hour to three hours before bed.

3. Melatonin may enhance the immune system. The details are fuzzy.

4. May have anti-tumor abilities. There's been quite a few studies with melatonin and cancer, most of them done in Italy. Most of the studies have shown benefits using 10 to 40 mg of melatonin nightly. However, much is yet to be learned about this approach, and hardly any oncologists in the US are familiar with the use of melatonin as an anticancer agent. Therefore, at this point, the use of melatonin is still experimental. However, since cancer is ultimately a fatal disease in most cases, it may be worthwhile to try melatonin. Your physician can easily access all the research on Medline.

5. Melatonin may have anti-aging potential due to its anti-oxidant properties. We won't know for sure for many years to come if melatonin increases longevity, nor will we know in the near future the ideal dosage, timing, and frequency.

6. Melatonin enhances dreams. This could lead to vivid, enjoyable and memorable dreams or, on the flip side, vivid nightmares. Melatonin enhances REM sleep.

Melatonin and serotonin relationship
Serotonin converts to melatonin at night in the pineal gland to help us sleep. Taking a serotonin precursor such as 5-HTP can lead to more melatonin production.

Less is More
MIT scientists confirm that melatonin is an effective sleep aid for older insomniacs and it appears that only a small dose of melatonin (about 0.3 milligrams) is necessary for a restful effect. Taken in that quantity, melatonin not only helps people fall asleep, but also makes it easier for them to return to sleep after waking up during the night. However, the amount in most melatonin products on the market ranges between 1 to 5 mg. At this high dose, tolerance can develop and the melatonin receptors in the brain become unresponsive. Thereafter, melatonin becomes less effective.    

Melatonin level
Is it necessary to have a blood test for melatonin level? We don't think so. A melatonin level is not necessary to know before taking a melatonin pill. As we age, it is possible that some people have a lower blood melatonin level at night.

Sublingual melatonin. Should I take the regular melatonin pills, sublingual, or the time release? Can melatonin be taken with food?
Most of the melatonin presently on the market is the regular 3 mg pill to swallow or as sublingual melatonin. You may want to cut this pill into a fifth or even a tenth and use this dose your first night, about an hour or two before bed without food in your stomach. Alternatively, you can also purchase melatonin pills at 1 mg or sometimes even lower dosages are sold. If this low dose is effective, then you may keep using it as needed for sleep. If you don't feel any effect, then take a little more the following nights.
   If your main problem is falling asleep, then try the melatonin sublingual form, in the range of 0.3 to 1.0 mg, about an hour or two before bed. Sublingual melatonin could work quicker and is a good option if you already have food in your stomach since if you take a melatonin pill with food, it may not absorb as well or as quickly. However, some people wake up in the middle of the night, or early morning, feeling alert. Most of these people would want to sleep a couple of hours longer. Melatonin has a short half-life and therefore is metabolized very fast and will be out of the body soon. This explains why many people wake up early.
   In order to stay asleep longer, a good option is slow-release melatonin, which is released consistently throughout the night. Slow-release (also known as sustained, time or controlled-release) melatonin will likely become more popular in the future. Another form that is useful is melatonin tea. The tea is drunk about an hour before bed. One company has added half a mg of melatonin to their tea bag. We are not clear yet on how supplementation influences snoring.

Melatonin Research Update
Melatonin: An Anti-Aging Hormone Supplement? -- Ever since melatonin became available over the counter in 1994, it has created a lot of controversy. The medical establishment has been quite uneasy with this hormone being available without a doctor's prescription, and I remember back in the mid 1990s quite a number of articles were published in journals read by doctors warning them of potential serious side effects. This surprised me since my evaluation of the research did not indicate that melatonin was dangerous. It has been a decade since melatonin has been freely sold to the public, and to my knowledge there have not been any published studies to indicate that this hormone has caused any serious harm. In fact, more research continues to be published regarding its benefits. Numerous studies now indicate that melatonin has powerful antioxidant properties, in addition to its known hormonal activities which includes sleep inducement . A recent study published at the University of Rajasthan in Jaipur, India investigated the influence of low-dose chronic administration (0.10 mg/kg body weight/day for 3 months) of melatonin against age-induced oxidative stress in mice tissues, namely brain, liver, spleen and kidney. Sixteen-month-old mice were supplemented with melatonin for three months and then autopsied (at the age of 19 months). The results indicated that melatonin was able to significantly reduce the age-induced decline in the body's natural antioxidant system. The researchers state, "These findings indicate that low-dose chronic administration of melatonin acts as a free radical scavenger and anti-aging agent."
     Comment: Research thus far is convincing that melatonin has many beneficial properties. However, it is difficult to determine the ideal dosage and frequency of melatonin use in humans. At this time it would seem safe and prudent to take a low dose, such as 0.1 to 0.5 mg of melatonin a few nights a week, particularly for those who suffer from insomnia. Melatonin is best taken on an empty stomach about 1 to 3 hours before bedtime. Since most pills come in dosages ranging from 0.5 to 3 mg, you could bite off a small portion of the pill.

Melatonin Pharmacotherapy for Nocturia in Men With Benign Prostatic Enlargement.
Drake MJ, Mills IW, Noble JG. J Urol. 2004;171:1199-1202.
Nocturia is a common condition often attributed in aging men to benign prostatic enlargement. Older adults are prone to nocturnal sleep disturbance, of which disturbed circadian rhythm may be a component since it improves with nighttime administration of melatonin. This study was designed to investigate melatonin as a potential treatment for nocturia associated with bladder outflow obstruction in older men. A total of 20 men with urodynamically confirmed bladder outflow obstruction and nocturia were entered into a randomized, double blind, placebo controlled crossover study assessing the effect of 2 mg controlled release melatonin at night on nocturia. Symptoms were assessed at baseline and after each 4-week treatment period using a frequency volume chart, the International Prostate Symptom Score and symptom problem index. Maximum urinary flow rate and post-void residual urine volume were also assessed. Baseline frequency of nocturia was 3.1 episodes per night. There were 7 men (35%) with detrusor overactivity and 10 (50%) had nocturnal polyuria. Melatonin and placebo caused a decrease in nocturia of 0.32 and 0.05 episodes per night (p = 0.07) and a decrease in the nocturia bother score of 0.51 and 0.05, respectively (p = 0.008). Nocturia responder rates (a reduction from baseline of at least -0.5 episodes per night) differed between the active medication and placebo groups. Daytime urinary frequency, International Prostate Symptom Score, relative nocturnal urine volume, maximum urinary flow rate and post-void residual were unaffected by melatonin treatment. Melatonin treatment is associated with a significant nocturia response rate, improvement in nocturia related bother and a good adverse effect profile. However, it is uncertain whether the observed changes in this study are clinically significant.

Long term Melatonin Safety
Melatonin has been recommended for the treatment of insomnia and jet lag, yet little is known about its long term effects on the body, and some in the medical community have questioned its safety. Researchers at the University of Lodz in Poland. evaluated the effects of melatonin administration on sleep and routine blood chemistry in elderly women. The study was performed on 14 women aged from 64 to 80 years. Melatonin 2 mg was given at 7 pm nightly for 6 months. Before and after melatonin treatment blood samples were taken in the morning after an overnight fast. The total blood count, glucose, total cholesterol, LDL, HDL, and triglycerides were measured by routine laboratory methods. Thirty-six percent of those on melatonin had an improvement in general sleep quality. Melatonin treatment did not influence significantly either total blood count, glucose or blood lipids levels. The researchers conclude that on the basis of this preliminary open study it seems that melatonin administration may be safe for elderly subjects.
     Comments: It’s reassuring to know that blood chemistry was not affected in any significant adverse way by 6 months therapy with melatonin. On the basis of this preliminary study, it seems that elderly individuals should be quite safe if they use melatonin one to three times a week at a dose of 0.1 or 0.5 mg.

Melatonin in patients with reduced REM sleep duration: two randomized controlled trials.
Department of Psychiatry and Psychotherapy, Charite Campus Mitte-Universitatsmedizin Berlin, 10117 Berlin, Germany.
J Clin Endocrinol Metab. 2004 Jan;89(1):128-34.
Recent data suggest that melatonin may influence human physiology, including the sleep-wake cycle, in a time-dependent manner via the body's internal clock. Rapid-eye-movement (REM) sleep expression is strongly circadian modulated, and the impact of REM sleep on primary brain functions, metabolic processes, and immune system function has become increasingly clear over the past decade. In our study, we evaluated the effects of exogenous melatonin on disturbed REM sleep in humans. Fourteen consecutive outpatients (five women, nine men; mean age, 50 yr) with unselected neuropsychiatric sleep disorders and reduced REM sleep duration (25% or more below age norm according to diagnostic polysomnography) were included in two consecutive, randomized, double-blind, placebo-controlled, parallel design clinical trials. Patients received 3 mg melatonin daily, administered between 2200 and 2300 h for 4 wk. The results of the study show that melatonin was significantly more effective than placebo: patients on melatonin experienced significant increases in REM sleep percentage (baseline/melatonin, 14.7/17.8 vs. baseline/placebo, 14.3/12.0) and improvements in subjective measures of daytime dysfunction as well as clinical global impression score. Melatonin did not shift circadian phase or suppress temperature but did increase REM sleep continuity and promote decline in rectal temperature during sleep. These results were confirmed in patients who received melatonin in the second study (REM sleep percentage baseline/placebo/melatonin, 14.3/12.0/17.9). In patients who received melatonin in the first study and placebo in the second, the above mentioned effects outlasted the period of melatonin administration and diminished only slowly over time (REM sleep percentage baseline/melatonin/placebo, 14.7/17.8/16.2). Our findings show that exogenous melatonin, when administered at the appropriate time, seems to normalize circadian variation in human physiology. It may, therefore, have a strong impact on general health, especially in the elderly and in shift workers.

Products
Natrol melatonin
Source Naturals melatonin - Source Naturals melatonin 5 mg may cause side effects.
Jarrow melatonin
GNC melatonin
Melatonin 300 mcg is available, this would mean it is melatonin 0.3 mg. We think 300 mcg is a good option for many people.
Schiff

emails
Q. I read a report on melatonin that recommends to take it only 3 times a week and in low dosages. However,
does this refer to all age groups? I am 66 years old (female) and certainly low in melatonin. I sleep very badly.
   A. The guidelines on melatonin use are general and flexible, and we suggest reading about how to get deeper sleep at this website.

Q. Is melatonin a vitamin since it is over the counter?
   A. Melatonin is not a vitamin but classified as a hormone.

Q. Can I take melatonin if i am on Prozac?
   A. Some people find Prozac to cause insomnia or sleep disturbances, melatonin may not work as well for those taking Prozac or other SSRIs since the serotonin system may be disturbed.

Q. Does supplementing with melatonin increase the levels of serotonin either in the brain or peripherally? Also, would taking melatonin be contra-indicated for someone who has exhibited symptoms of serotonin syndrome in the past?
   A. We don't think melatonin taken as a supplement in a dosage of less than 3 mg will have much of an influence on serotonin levels in the brain or peripherally. Melatonin does not seem to be involved in serotonin syndrome.

Q. I am a 64 year old woman who until the age of 55 never had a sleep problem, as soon as i started menopause i start having insomnia, my doctor prescribe me 0.5mg Ativan and i have been taking it every night for about 2 years, then the 0.5mg stop working my doctor doubled the dose, after a while that also stop working it takes hours to fall asleep, i read the article about melatonin on your web site and i said to myself it's worth the try. My question is shall i stop the Ativan while i am taking the melatonin i decided to take a low dose 2 times a week.
   A. Natural sleep pills such as melatonin are not recommended to be taken the same night as a pharmaceutical sleeping pill. It is best to take melatonin on a night that a person is not taking prescription sleep meds. However, there is sometimes a rebound effect on sleep when a drug is stopped. The rebound effect means that it is difficult to sleep since the brain is used to getting the sleep drug. Thus, when a natural sleep pill such as melatonin is taken, it may appear that it is not working since it has to overcome the rebound effect. It is best to follow all suggestions for a deeper sleep as mentioned at sleep web page.

Q. In the past, I have purchased 3mg chewable lemon flavored melatonin. This is for a 5 year old child with medical problems. The place we purchased it from is no longer in business and I can not seem to find this anywhere. Is there anything you can do to tell me if this is offered.
   A. We don't carry lemon flavored chewable melatonin pills. The 1 mg sublingual melatonin pill we link to is peppermint flavored.

Q. Could melatonin cause burning mouth, that is the only thing that I can think of that may cause this as I do not take meds. I just hate this problem and have had it for years now. Could it be long term effects of taking melatonin? I already take R- alpha lipoic acid and that is not helping.
   A. We have had no reports from anyone that melatonin causes burning mouth. We know people who have given us feedback on long term effects of taking melatonin and no burning mouth has been reported.

Q. I have been reading and researching the benefits of melatonin on your site as well as other internet sites. There seems to be many benefits to at least some level of melatonin supplementation. However, some information that has alarmed me regarding the artificial increase of melatonin through supplementation is that increased melatonin can decrease the amount of serotonin in your body (more importantly, the brain). Couldn't this reduction in serotonin lead to depression? Can you shed some insight on this?
   A. We don't know exactly what influence melatonin supplements have on serotonin levels when used for prolonged periods, but we do have reports of mild depression with high dose regular melatonin supplement use.

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