26 replies to this topic

[ZRTMWA]

Has anyone tried taking a megadose of melatonin? This quote from Wikipedia piqued my curiosity:

"Extremely high doses of melatonin (50 mg) dramatically increased REM sleep time and dream activity in both people with and without narcolepsy."
(http://en.wikipedia.org/wiki/Melatonin)


The quote is cited from the book "Melatonin and the Biological Clock" by Alan Lewis (1999). There's no way of knowing how the melatonin was administered without talking to the author but I'm assuming it was orally. Oral melatonin is only 35-50% bioavailable so if the author did perform the experiment intravenously, much more melatonin would be needed to be taken orally.

I'm thinking about taking 10 5 mg pills one night when I have at least 12 hours to kill, just in case it knocks me out. For now I just break a 5 mg pill into quarters and take one quarter when I don't feel tired (2 nights a week on average).

[RTSW]

I'd love to hear about it. I've been taking 3mg melatonin daily for over 6 months now, and it's been helping me. 50mg is quite a dose... but a dramatic increase in REM is quite an effect as well. If you report positive results, I just might try it myself, just once

[impdaddee]

3 mgs before bed sets off my dream cycle while I'm still awake. Not REM sleep, but minutes of flowing, disconnected images and leisurely mind's-eye fantasy drifting until sleep sets in.

5-HTP does the same, but the internal images flash by at lightning speed.

[thedevinroy]

I thought melatonin has a bell curve of effectiveness. The more you take, the longer you have to wait for it to kick in. That way for me and my sister. But when it does hit... bang, out for hours.

[evodude]

when i'm sleep deprived i take one pill of 10mg. Works in about a half hour and i sleep really well. In the morning all my muscles are super relaxed. And yes, it enhance my conscious dreaming.

Edited by evodude, 25 October 2011 - 07:58 PM.

[hamishm00]

My experience with melatonin over the last 15 years is that 50mg won't be any more 'noticeable' than 5mg.

[RTSW]

My experience with melatonin over the last 15 years is that 50mg won't be any more 'noticeable' than 5mg.

Maybe we have to take into account the limited bioavailability when administered orally, then? That would mean over 100mg... sounds insane.
What's the maximum dosage you've experimented with?

[thedevinroy]

My experience with melatonin over the last 15 years is that 50mg won't be any more 'noticeable' than 5mg.

I tend to agree and disagree. I agree that there isn't much difference with onset (maybe a higher dose increases onset in some people by half hour or hour, does for me), but I disagree that there isn't some difference in effect. When I take a lot of melatonin, my muscles don't want to move in the AM... it's like moving dead weights.

[m00k0w]

MY first forays with melatonin were at 3mg, and then I tried quickly escalating dosages of up to 42mg. These did nothing but make me too energetic and overheated while trying to fall asleep. I slept probably one hour of the entire night.

Some research says .3mg is a better dose than 3mg, giving full sleep inducing effect without side effects. Remember this is a hormone, not like another serotonin agonist. It doesn't act harder the more you take.

[thedevinroy]

MY first forays with melatonin were at 3mg, and then I tried quickly escalating dosages of up to 42mg. These did nothing but make me too energetic and overheated while trying to fall asleep. I slept probably one hour of the entire night.

Some research says .3mg is a better dose than 3mg, giving full sleep inducing effect without side effects. Remember this is a hormone, not like another serotonin agonist. It doesn't act harder the more you take.

Funny you say that. I actually tried 10mg one time with the same results: more energy. I did get the usual relaxation, but it wasn't until 1.5 to 2 hours later.

[ZRTMWA]

Last night I took 50mg of melatonin around 11 PM. I slept until 1:45 PM. It's the most I've ever slept at once. I woke up for about 10 minutes at 3AM and 11:30 AM. I never ever remember my dreams when I wake up. Same thing happened at 3 and 11:30 but when I awoke at 1:45, I woke up out of a dream which I still remember. I chewed up all of the melatonin into a mushy paste in my mouth before I swallowed it, to ensure that the effects would come on quickly. I felt very tired/relaxed as I lay in bed. I probably fell asleep in under 10 minutes.

Confounding Variables to this experiment:
I used MJ twice yesterday, the second time around 8PM. MJ is said to hinder REM sleep but actually increase melatonin levels (contradiction?). I also had a sip or two of alcohol an hour before I went to bed, but that was so little I can't see it really messing with my sleep at all. Also, I had only slept a combined 15-16 hours the three nights before last night. The two nights before were probably 5 hours and then 4 hours. I know getting a short amount of sleep causes a REM rebound (increase of time in REM sleep) the next night you sleep. Also because I chewed up the melatonin, the effects could've come on quicker but not last as long.

I plan to repeat this experiment next Wednesday night, without any other substance use and get a good night sleep Tuesday night to ensure there are no REM rebound effects. Also, I might chew up 25mg and swallow the other 25mg to get a sort of instant but also "time release" effect. In conclusion, taking 50mg of melatonin at once is really a waste of your melatonin.

Edited by ZRTMWA, 27 October 2011 - 06:50 PM.

[manic_racetam]

Last night I took 50mg of melatonin around 11 PM. I slept until 1:45 PM. It's the most I've ever slept at once. I woke up for about 10 minutes at 3AM and 11:30 AM. I never ever remember my dreams when I wake up. Same thing happened at 3 and 11:30 but when I awoke at 1:45, I woke up out of a dream which I still remember. I chewed up all of the melatonin into a mushy paste in my mouth before I swallowed it, to ensure that the effects would come on quickly. I felt very tired/relaxed as I lay in bed. I probably fell asleep in under 10 minutes.

Confounding Variables to this experiment:
I used MJ twice yesterday, the second time around 8PM. MJ is said to hinder REM sleep but actually increase melatonin levels (contradiction?). I also had a sip or two of alcohol an hour before I went to bed, but that was so little I can't see it really messing with my sleep at all. Also, I had only slept a combined 15-16 hours the three nights before last night. The two nights before were probably 5 hours and then 4 hours. I know getting a short amount of sleep causes a REM rebound (increase of time in REM sleep) the next night you sleep. Also because I chewed up the melatonin, the effects could've come on quicker but not last as long.

I plan to repeat this experiment next Wednesday night, without any other substance use and get a good night sleep Tuesday night to ensure there are no REM rebound effects. Also, I might chew up 25mg and swallow the other 25mg to get a sort of instant but also "time release" effect. In conclusion, taking 50mg of melatonin at once is really a waste of your melatonin.

I remember hearing that melatonin has very poor oral bio-availability. So chewing it up and leaving it in your mouth for a while would be a good idea if you're trying to increase the amount being absorbed (most things are better absorbed sublingually). Keep us posted on the effects on dream quality. Always looking for ways to enhance my dreams.

[RTSW]

Great report! I'll be waiting for the next one, with less variables involved. I'm hoping the tweaking of melatonin intake will lead to a more restful sleep (I've had issues with fatigue for many years now). A longer sleeping period could be problematic, though.

[ZRTMWA]

I decided to finally revisit this thread.

Trial #2:
The night before this I got 7-8 hours of sleep. At 1:05 AM I chewed 25mg of melatonin, held the powder in my mouth for 1 min, swallowed and swallowed 25mg unchewed. I had a lot of trouble falling asleep and went in and out for about two hours. I woke up around 11:15. I did remember one of my dreams which almost never happens. For some reason, I usually wake up most mornings not remembering any of them.

Overall, I'd say it's definitely a waste of melatonin. Splitting the 5mg pills into quarters usually works in 15-30min for me.

[hippocampus]

I usually take about 0,5 mg and it's enough to knock me out and even make me sleepy in the morning sometimes. 3 mg is way too much anyway, at least for young people, imo. it's best to take care of sleep hygiene :\

[Thorsten3]

Take B6 or P5P everyday that should help dream recall. AChEIs such as Galamantine should also help.

The craziest dreams I have ever experienced have been through using GHB and Piracetam. Never in my life I have come across anything so life like and detailed. There were actually plots behind everything and everything seemed to have a purpose despite the bizarre nature of what i saw. I mean when you first start taking Piracetam the dreams can be pretty cool but GHB just took it somewhere else. I won't even begin to explain what world I was in! I don't take G anymore BTW and I certainly don't advocate it use to anybody. If you are interested in becoming a drug addict with severe withdrawals, sure give it a whirl!

With respect to the Melatonin I notice the dead weight sensation first thing in the morning but this is with the timed release version (I tried 3mg). But it also ruins the following day because I feel like that for hours and it also feels pretty dysphoric.

With normal Melatonin it knocks me out (3mg) and then when I wake up the following day I feel fine.

I figure hyperdosing normal Melatonin and having the dead weight sensation first thing in the morning may be due to the fact that you've taken far too much and your body is still trying to get rid of it.

For those who are noticing worse effects for sleep initiation by hyperdosing your Melatonin maybe your M1,M2 and M3 receptors are going to become less sensitized by bombardment of the extra Melatonin? I'm not currently on it but I have always got similar effects with the antidepressant Agomelatine. I'm not sure how strong of an agonist it is at some of those receptors but after a while it seems to loose its effectiveness at inducing sleep. It is possible to the receptors could become desensitized or your body could downregulate its own supply of Melatonin.

A recent good addition to my sleep routine has been ashwagandha. I find it an extremely sleepy herb even at low doses. Maybe it's how it interacts with GABA but it seems to give me deeper sleep and along with melatonin my sleep is pretty good right now. Taurine, Arginine and Magnesium are also useful if you want to add an extra punch for your bedtime cocktail.

Edited by Thorsten2, 24 January 2012 - 11:15 PM.

[blood]

Anyone experimented with taking 50-100 mg/ day melatonin over an extended period?

High dose melatonin apparently suppresses visceral fat... in mice... at a human-equivalent dose of around 50mg/ day:

http://www.lef.org/m...-Factors_02.htm

While no human weight-management trials using melatonin have been published thus far,95 preclinical trials are encouraging. In middle-aged rodents, daily melatonin administration was found to suppress abdominal fat, plasma leptin levels, and insulin levels, while also reducing body weight and food intake.96,97 Other researchers reported that melatonin was associated with decreased intra-abdominal fat, decreased plasma insulin and leptin levels, and the absence of age-related weight gain.95,98

Furthermore, laboratory investigations discovered melatonin's ability to activate brown adipose tissue, which encourages your body to burn fat instead of storing it.99-101In recent years, brown fat has increasingly become a target for halting the global obesity epidemic.102 In a rat model of pre-diabetic, diet-induced obesity, supplementing obese rats with 4mg/kg/day of melatonin resulted in reductions in body weight, belly fat, serum insulin levels, and triglycerides.103 In humans, the equivalent dose is 48 mg for a 165 lb adult, which is a very high dose that could produce next day drowsiness. Typical human doses for melatonin range from 300 micrograms to 10 milligrams at bedtime.

Edited by blood, 14 May 2013 - 05:26 AM.

[blood]

"Daily melatonin administration at middle age suppresses male rat visceral fat, plasma leptin, and plasma insulin to youthful levels"
http://www.ncbi.nlm..../pubmed/9927336

"In a clinical safety study, chronic high-dose (300 mg/day) rectal melatonin was well tolerated during an observation period of up to 2 yr..."
http://www.ncbi.nlm....pubmed/17014688

"Daily melatonin supplementation in mice increases atherosclerosis in proximal aorta... Even though high melatonin doses inhibit LDL oxidation in vitro, the effect of melatonin on atherosclerosis has never been studied. We have demonstrated that the feeding of hypercholesterolemic mice with an atherogenic diet supplemented with melatonin highly increases the surface of atherosclerotic lesions in the proximal aorta... This study suggests that caution should be taken as regards high melatonin dosage in hypercholesterolemic patients..."
http://www.ncbi.nlm....pubmed/12051775

[BLimitless]

I have a lot of Melatonin lying around. I take up to 250mg at a time.

3mg is the dose I would take to induce sleep. But I do not really take that anymore, much preferring to take at least 50mg. There are two bizarre coinciding deficiencies induced by modern living & bright lights - Vitamin D3 and melatonin, due to the way our sleep schedules have been shifted by late night light exposure. So why take 3mg of what is a very safe substance already part of the brain and easily metabolised if needed when you can take 50mg+ and get some amazing health benefits from perhaps one of the most powerful antioxidants found in the brain!



Funnily enough Melatonin is also vaporisable, which leads to very interesting effects when an MAOI-A is co-administered. Melatonin is sleep inducing and also crucial for quality sleep. I feel very calm and satiated the days after administration. Co-administration of melatonin with L-tryptophan and L-tyrosine makes me feel really great, sharp and lucid. The effect on the dream state is that it amplifies awareness of/in dreams but also enabling the rest required to get into deep sleep stages.

It is observed that L-tyrosine has a colour enhancing effect and creates a sensation of an "internal sunny day" so to speak; this is brought out by dosing in the above regimen.

Perhaps the effects on dreaming and sleep arise from two key metabolites; Mexamine (5-Methoxy-Tryptamine) and Pinoline (6-MeO-THBC). The latter is an MAOI inhibiting type A and perhaps B also; the prior is an endogenous hallucinogenic tryptamine thought to be implicated in dream awareness & dream perception. Specifically the deacetylation of Melatonin produces 5-MT and supposedly this process coincides with entering REM/dream stages of sleep; the Mexamine is broken down upon cessation of dream phenomena. Pinoline is also secreted throughout the time to inhibit the breakdown of the 5-MT and perhaps many other endogenous hallucinogenic alkaloids.




The Tryptophan Metabolic (Kegg) pathway should be of interest here -





Personally I would say that it is better to supplement further up the chain with L-tryptophan. But there are times you will want to preferentially push towards the Melatonin direction but even then I would consider administering Tryptophan in combination. It has such a good effect on your well-being and mood, relaxation and sleep; and decent doses of it (6g) feel very safe.

Edited by BLimitless, 14 May 2013 - 03:47 PM.

[renfr]

I have some melatonin laying around, I already took up to 15mg all it did is increase very vivid dreams for a few days but that's all.

Concerning the risk of atherosclerosis the study mentions that it was caused fundamentally not by melatonin but by the atherogenic diet so that isn't much of a problem if you have a good diet and doesn't have hypothyroidism.

[LexLux]

Could melatonin offset the nitric oxide inducing effects of pramiracetam?

 

Melatonin and nitric oxide.

www.ncbi.nlm.nih.gov/pubmed/16682846

 

Melatonin regulates nitric oxide synthase expression in ...

www.ncbi.nlm.nih.gov/pubmed/18685253

 

Melatonin counteracts inducible mitochondrial nitric oxide

www.ncbi.nlm.nih.gov/pubmed/16313501

 

Edited by LexLux, 18 May 2014 - 02:18 AM.

[KimberCT]

I've taken 50mg nightly for over a year. I've "quit" a couple times as an experiment. There was a couple days of insomnia until my normal sleep pattern returned.

Unlike 0.3-3mg, the larger dose improves my sleep quality and seems to have antidepressant effects (cheap agomelatine?).

If anyone plans to try it, I'd suggest ramping up to 50mg. Jumping straight to a high dose actually caused me insomnia.

[Kewell357]

>6mg of melatonin gives me the most severe brain fog the next day.

[Jeff McJackoff]

I've taken 50mg nightly for over a year. I've "quit" a couple times as an experiment. There was a couple days of insomnia until my normal sleep pattern returned.

Unlike 0.3-3mg, the larger dose improves my sleep quality and seems to have antidepressant effects (cheap agomelatine?).

If anyone plans to try it, I'd suggest ramping up to 50mg. Jumping straight to a high dose actually caused me insomnia.

 

[Jeff McJackoff]

I have a lot of Melatonin lying around. I take up to 250mg at a time.

3mg is the dose I would take to induce sleep. But I do not really take that anymore, much preferring to take at least 50mg. There are two bizarre coinciding deficiencies induced by modern living & bright lights - Vitamin D3 and melatonin, due to the way our sleep schedules have been shifted by late night light exposure. So why take 3mg of what is a very safe substance already part of the brain and easily metabolised if needed when you can take 50mg+ and get some amazing health benefits from perhaps one of the most powerful antioxidants found in the brain!



Funnily enough Melatonin is also vaporisable, which leads to very interesting effects when an MAOI-A is co-administered. Melatonin is sleep inducing and also crucial for quality sleep. I feel very calm and satiated the days after administration. Co-administration of melatonin with L-tryptophan and L-tyrosine makes me feel really great, sharp and lucid. The effect on the dream state is that it amplifies awareness of/in dreams but also enabling the rest required to get into deep sleep stages.

It is observed that L-tyrosine has a colour enhancing effect and creates a sensation of an "internal sunny day" so to speak; this is brought out by dosing in the above regimen.

Perhaps the effects on dreaming and sleep arise from two key metabolites; Mexamine (5-Methoxy-Tryptamine) and Pinoline (6-MeO-THBC). The latter is an MAOI inhibiting type A and perhaps B also; the prior is an endogenous hallucinogenic tryptamine thought to be implicated in dream awareness & dream perception. Specifically the deacetylation of Melatonin produces 5-MT and supposedly this process coincides with entering REM/dream stages of sleep; the Mexamine is broken down upon cessation of dream phenomena. Pinoline is also secreted throughout the time to inhibit the breakdown of the 5-MT and perhaps many other endogenous hallucinogenic alkaloids.




The Tryptophan Metabolic (Kegg) pathway should be of interest here -





Personally I would say that it is better to supplement further up the chain with L-tryptophan. But there are times you will want to preferentially push towards the Melatonin direction but even then I would consider administering Tryptophan in combination. It has such a good effect on your well-being and mood, relaxation and sleep; and decent doses of it (6g) feel very safe.

 

 

 

+rated you.

thanks for post. good post.
 

[baslangicnoktasi]

I've taken 50mg nightly for over a year. I've "quit" a couple times as an experiment. There was a couple days of insomnia until my normal sleep pattern returned.

Unlike 0.3-3mg, the larger dose improves my sleep quality and seems to have antidepressant effects (cheap agomelatine?).

If anyone plans to try it, I'd suggest ramping up to 50mg. Jumping straight to a high dose actually caused me insomnia.

 

Did you experience any change in your weight? 

[KimberCT]

Yes, however I've attributed to my shitty diet lately. When I ate well for a month, I noticed the weight coming off rapidly.