19 replies to this topic

[hani]

There's very little information on the internet concerning what's better, time release or immediate. I take melatonin for sleep AND its numerous benefits as an antioxidant. I found a couple on iherb:

Natrol, Melatonin TR, Time Release
http://www.iherb.com...0-Tablets/22708

This one lasts for 8 hours and comes with 10mg Vitamin B6.

Source Naturals, Melatonin, 3 mg
http://www.iherb.com...60-Tablets/4304
Immediate release, 1mg B6 plus calcium.

Now Foods, Melatonin, 1 mg
http://www.iherb.com...250-Tablets/702
Two stage release, some immediate some time release. Also comes with B6, Niacin and Magnesium citrate.

Source Naturals, Melatonin, Orange Flavored Sublingual, 2.5 mg
http://www.iherb.com...40-Tablets/1309

What do you think is better

[maxwatt]

If you want to mimic the body's natural hormonal cycle of melatonin levels don't use time release. It's a good way to disrupt your circadian rhythms which shortens lifespan in rodent studies. OF course if you have electric lights and watch TV or use a computer at night, they are probably already disrupted.

Lower doses are better if you want to sleep. 2, 3 and 5 mg doses send blood levels much higher than anything that occurs naturally withing an hour, and in about four hours levels plunge well below daytime baseline. Most people wake up and can't get back to sleep at this point. It's a good way to disrupt your circadian rhythms. (If I have time, I'll try to find the post from several years ago with a summary and link to the pharmokinetic study where I am getting this information.)

Depending on body weight, if one wants to restore or reinforce one's circadian rhythm, and get 'natural' sleep, doses between 300 and 600 micrograms would be ideal. The Life Extension Foundation (LEF) makes a 300 mg pill, as does Rexall Sundown - the latter is available in many pharmacies, or online at Amazon and elsewhere. An additional advantage to this one is it can be taken sublingually, hence faster acting. There are also one milligram tablets from different vendors, which can be cut with a pill-splitter.

If you are looking for other effects than reinforcing your natural circadian rhythms, then there is no generic answer which is best: you're on your own. You have to infer a dose from whatever study deals with the effect you are seeking. Melatonin is supposed to be a super anti-oxidant and to have cancer preventing properties, and the marketers of melatonin pills make these claims repeatedly, but there is no established protocol for such use that I am aware of, and other substances are also said to have such properties. Carbon-60 in olive oil for anti-oxidant action in the lipid layer of one's cells, or reishi spoor oil for anti cancer properties, to name two (not claiming efficacy, just mentioning two that are currently popular for such purposes.)

In short, time release melatonin is a bad idea.

[hani]

Has there been studies that show melatonin levels throughout sleep?

[Andey]

If you want to mimic the body's natural hormonal cycle of melatonin levels don't use time release. It's a good way to disrupt your circadian rhythms which shortens lifespan in rodent studies.
In short, time release melatonin is a bad idea.

Why do you think so ?
If you look at natural melatonin levels they look completely different to the large peak that you will receive from standart release melatonin

here is for example same type of graph for Circadin ™, time released type of melatonin
It looks similar to natural occuring graph

Edited by Andey, 20 June 2013 - 01:44 PM.

[maxwatt]

the two graphs are different scales, not compatible for comparison to endogenous levels.

Edited by maxwatt, 20 June 2013 - 02:13 PM.

[maxwatt]

While 0.5 mg initially was higher than endogenous secretion, toward morning the levels were consistent with natural levels;
Eyeballing the time release graph in the previous post, it seems the levels from the time release were higher than one might want toward waking, and after waking.

Perhaps one could develop a time release without the sudden early peak, but it would be hard to control the downward side of the curve, if not impossible to avoid higher levels than one might want in the morning. In most people this might contribute to daytime drowsiness. I would think one would want to avoid high levels when one wants to be awake and alert.

[Andey]

While 0.5 mg initially was higher than endogenous secretion, toward morning the levels were consistent with natural levels;
Eyeballing the time release graph in the previous post, it seems the levels from the time release were higher than one might want toward waking, and after waking.

Perhaps one could develop a time release without the sudden early peak, but it would be hard to control the downward side of the curve, if not impossible to avoid higher levels than one might want in the morning. In most people this might contribute to daytime drowsiness. I would think one would want to avoid high levels when one wants to be awake and alert.

I conclude completely opposite looking at the same graphs.
Time release melatonin didnt give unnatural 10 folds plasma level peaks, graph is much more similar to endogenious one. For TR melatonin you can adjust waking levels by lowering dosage or different brands could have different time release part lasting for example 6 hours. But you cant adjust these peaks for plain melatonin, and if something could harm and destroy circadian rhythms as you wrote in first answer than its more probably will be this peaks.

[maxwatt]

You cannot use that graph comparing a 2mg time-release to 2 mg regular to conclude anything with precision; the units are percent of AUC, which does not translate to plasma levels. I suspect the manufacturer chose that sort of graph to make their product look better. The other graph showing 0.5 mg vs. endogenous levels shows at most a three fold increase in plasma level over peak endogenous, and a near match on the down-slope of the curves after about four hours. When melatonin levels should be declining toward the end of the sleep period, blood levels from a time-release will be higher by a few fold, which I would expect would lead to grogginess and difficulty waking. Time release formulations are tricky things, usually an outer coating of the substance being delivered surrounds a wax coating that is slowly digested, hopefully slowing the remaining dose. Or it is all embedded in the wax. I am suspicious of the technology for delivering a steady or even an intentionally timed dose. Even big pharma sometimes gets it wrong, and their technology and resources are much better than supplement manufacturers.

So we have a choice of a level perhaps three times normal initially, versus a similarly too high level after about four hours, lasting well into the next morning. Take your choice.

[Andey]

Thanks for explanation. Cant argue because you are definitely more informed on this subject.
To back your idea about increased level at the morning I can say that I feel little bit groggy first few minutes after awaking while taking TR Melatonin. It doesnt last long but I definitely didnt experience such thing without melatonin.

[Kevnzworld]

I think there is also an issue with age. Older middle aged people like me (56) secrete less melatonin. I have experimented with various doses of regular, sublingual and time release melatonin. My circadian rhythm is a little screwed up given my evening computer/ TV habits.
I've concluded that 3 mg 6 hour time release taken an hour before bed works the best for me. I sleep 7- 8 hours and I don't experience any hangover effect.

[Luddist]

There are also liquid melatonins available. Supposedly they can act faster by sublingual absorption and the dose can be varied easily by the number of drops. I plan on trying some liquid myself. I haven't ordered yet but the Solgar brand looks like the best option for price/concentration (just don't use a full dropperful as they recommend).

[spirilla01]

I´ve had great succes moving from Source naturel 2mg timed releaseto Life extension 750mcg timed released.
I´m not waking up anymore during night time, but I have to admit, that I´ve cut back on my red wine consumtion from 3-4 glasses to 1-2 at the same time.

I´ve had great succes moving from Source naturel 2mg timed releaseto Life extension 750mcg timed released.
I´m not waking up anymore during night time, but I have to admit, that I´ve cut back on my red wine consumption from 3-4 glasses to 1-2 at the same time. Also , I´ve added 1g of glycine too. Seems to work perfectly.

[pone11]

While 0.5 mg initially was higher than endogenous secretion, toward morning the levels were consistent with natural levels;
Eyeballing the time release graph in the previous post, it seems the levels from the time release were higher than one might want toward waking, and after waking.

Perhaps one could develop a time release without the sudden early peak, but it would be hard to control the downward side of the curve, if not impossible to avoid higher levels than one might want in the morning. In most people this might contribute to daytime drowsiness. I would think one would want to avoid high levels when one wants to be awake and alert.

 

It might be useful to this discussion to show the endogenous pattern of melatonin release in humans at different ages:

 

 

A 300 to 500 mcg dose does appear to crudely simulate the release pattern of a 15-to-35 year old person.   There is a nice summary of melatonin effects here:

http://www.benbest.c.../melatonin.html

[Nate-2004]

It's best to ramp up the dose over time I think. 3mg is probably fine till you're 50.

 

The kind I buy is the spray bottle version by source naturals, if in the US you can get a 3 pack of those pretty cheap on Amazon and they last a long time. Each spray is a dose of 1.5mg so two squirts over 35, 1 squirt under, 3 over 50, under the tongue, try to keep it there but it's not that important if you swallow it.

 

The dreams I get from it are wack but the sleep comes quickly which for me is great because I'm insomnia prone. If you combine it with L-theanine you can get some pretty good sleep quality. Be sure to get tested at a university sleep center to be sure you don't have sleep apnea. I have it and CPAP changed my life. I must have had sleep apnea way back as a kid and not even known it. Also kids are kept from getting enough sleep by the establishment, mostly government schools. It's pretty sickening just how stunted they are by this.

Edited by Nate-2004, 02 August 2017 - 07:11 PM.

[Multivitz]

Vanadium is needed to get the Tyrosine through the blood brain barrier, Tyrosine is used to make Melatonin in the brain. Boron is key, but Zinc, Mganesium, and other minerals are essential for everything. Never take drugs, ever.

[Daniel Cooper]

What kind of Melatonin should you buy?

 

The one that says "Boron" on the label.  Duh!

 

 

 

 

 

 

[Shemp999]

Is it possible to own stock in elemental Boron?

[Multivitz]

You are obviously stupid enough to imbalance yourselves with drugs that work short term lol
No one needs Melatonin, it works as a sleep agent because it demands Magnesium from the bloods electrolytes, thus dulling the electricity potential of the CNS. What a pair of media zombies lol
I believe in the men in white coats, they look serious and know more than me.......

Edited by Multivitz, 06 October 2017 - 12:56 AM.

[Daniel Cooper]

Magnesium?  Don't tell me you've given up on Boron ..........

 

 

 

 

 

 

 

[Kalliste]

One odd thing about Melatonin (3mg Natrol) is I notice a sharp IQ drop the last minutes Before falling asleep. Thoughts become insanely stupid. Wonder whats happening.