Melatonin megadoses?

The person to ask is Russel Reiter, Ph.D.

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Many interesting articles here:
https://www.melatonin-research.net/index.php/MR

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In the end you can either decide to take something or not take it. The dose has an effect. The timing has an effect. With melatonin there is a lot of scaremongering, but the body produces it for a reason.

For sure.

I’m interested in melatonin due to couple of reasons.

  1. I have a reflux disease, and there are some data suggesting that melatonin could help (e.g. The potential therapeutic effect of melatonin in gastro-esophageal reflux disease - PMC)
  2. from the longevity perspective, especially ASCVD risk perspective (I have high Lp(a))

However, I believe that exercise is the best “medicine” for longevity. Particularly Zone 1 - Zone 2 endurance training which increases the number and efficiency of mitochondria. I have read that Q10, metformin and vitamins C and E can blunt some exercise adaptations. So I’m a little bit cautious for antioxidants / supplements.

P.S. Sorry for the poor English.

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I provided a link to the research. I take a lot of melatonin always during the night.

Yep, thanks. I’ll take a look at tomorrow.

TJ - my partner had a bad case of reflux. It was cured by her naturopath who prescribed nightly melatonin. Each week the dose was increased. As I remember, her dose only reached 10 mg per night before seeing the healing effect. It seemed a pretty miraculous cure at the time. My understanding is the melatonin tightens the sphincter between the stomach and the esophagus, thus reducing reflux. Good luck.
.

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I can’t take it. It gives me very vivid, violent, disturbing nightmares.

Wow, could you give more details? Is she still taking melatonin?

When did you take it and how much?

I took 5 mg just before bed time.

I tend to take it when I wake up during the night sometimes after 5 hours sleep to extend sleep. It is, however, gabaergic and it may encourage dreaming even if you take it during the night.

Ideally I am for enough sleep so that I am not tired during the next day. Measured on a fitbit sometimes that is as little as 5 1/2 hours. Generally 6 hours actually asleep will do this although more recently I have been sleeping 7 and 8 hours (with the assistance of melatonin after 5 hours and following a large number of interventions) - which I am quite pleased with. I tend to take quite a bit, however. I record how much and for the last 7 days it was 170, 270, 420, 490, 220, 250 and 70mg. I rarely take less than 100mg. I mainly use 10mg pills, but also 60mg pills and there are suppositories at 200 and 400mg. I am not sure about how bioavailability varies, however.

Topping up the mitochondrial melatonin has a broad range of anti-inflammatory effects.

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@John_Hemming does the ingested melatonin get into mitochondria? I understand the mitochondria exposed to sunlight makes its own melatonin to protect against damage.

I reviewed with my partner: Note - this isn’t medical advice

  1. Started with 1 mg melatonin and increased by 1mg melatonin weekly till she reached 6mg. Then stayed with that 6mg dosage for a month at least as she remembers

  2. Took bitters as a way to stimulate digestion juices in stomach

  3. Took aloe juice - “inner filet” was the type of juice

She noted it was a combination of things - avoid triggers that bother your gerd. Hope this helps - report your experience

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You are right that the mitochondria make melatonin from serotonin and sunlight exposure (longer wavelengths) help for generation of serotonin. However, also pineal (and other serum) melatonin get into the cells and then the mitochondira. I did a quick search and found this (I was aware of this thesis and from personal experience):

However, new transport systems, namely GLUT/SLC2A and PEPT1/2, have been shown
to have an active role in facilitating melatonin transport
across membranes. Furthermore, the localization of these
two transport systems in the mitochondria strongly suggests
the participation of both in mitochondrial transport of melatonin. The role of these and other transporters in diferent
cell types as well as their use as potential therapeutic targets
for diferent diseases should be further investigated

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Eventually the nightmares stop… wish I could remember how long it took.

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How much do you take when you wake up? I’ve been using this strategy with some sleep promoting herbs, with weak results, so I’d like to try melatonin instead and see if I can sleep longer…

ive used life extension brand time release and it seems to work.

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It varies. What I find is that it is likely when I wake during the night that I will not be able to get back to sleep until the next ultradian cycle (HPA axis cycle). If my sympathetic nervous system is in wake mode (sympathetic rather than parasympathetic - Cortisol Awakening Response (CAR)) then getting back to sleep will probably not be practical. Melatonin has about a 30 minute half life. The sleep cycles last about 90 minutes. Hence I take time release melatonin 45 minutes to an hour after waking and then a number of immediate release pills after an hour with a view to getting back to sleep. If you are not used to melatonin a relatively small dose may do the job (10s of milligrams). However, last night I swallowed 90mg at an hour and 100mg in ten mg pills (which I store in my cheeks so I can suck one at a time).

I then got back to sleep around 15 minutes later.

However, if you try this start small. If you get the timing wrong you can end up having another sleep cycle where the cortisol awakening response is strong and you won’t sleep.

The main thing is to have some patience for the body’s ultradian cycle to operate. Your ultradian cycle may be shorter or longer than mine.

I use a fitbit to find out precisely when I woke.

Last night I had about 5 hours sleep before waking with a CAR and melatonin gave me about 2 hours more sleep. (but with 90 mins awake)

An important side effect of sucking dissolvable melatonin pills is a reduction in gum infection.

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3mg works for me.
Back to sleep quickly if I wake up and feel wide awake.

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