High Dose Melatonin Therapy

[Oxajil]

Um, does this mean that if you have light sensitivity (or damage to retinal photoreceptors) that taking melatonin makes it worse?

That's a reference to this study (poor rats!): Link

Abstract:

Melatonin increases photoreceptor susceptibility to light-induced damage.

Melatonin is an indolamine hormone synthesized in the retina and pineal gland. It is thought to act as a paracrine neurohormone in the mammalian retina. Pinealectomy has been shown to protect photoreceptors from light-induced damage, and melatonin treatment has been reported to increase the degree of photoreceptor damage in albino rats. To determine how melatonin influences photoreceptor survival, the effect of melatonin administration on light-induced retinal damage was studied. Melatonin was administered to albino rats by intraperitoneal injections at various times before or after light exposure. The rats were exposed to high-intensity illumination (1600 lux) for 24 hr to induce photodamage, then returned to cyclic lighting for 12 days. After this, they were killed, and their eyes were removed and examined histologically. Measurements of the outer nuclear layer (ONL) thickness were taken at 12 different loci around the circumference of the retinal sections. The animals that received daily melatonin injections (100 micrograms) in the late afternoon (3 hr before lights off) for 1-3 days before photodamage showed an approximate 30% greater reduction compared with sham control animals in ONL thickness in the superior quadrant, the area most susceptible to light damage. Melatonin injections given after the photodamage did not affect ONL thickness. Although retinal susceptibility to light damage varied with time of day, the degree to which melatonin increased the degree of damage appeared unaffected by the time of day. These results suggest that melatonin may be involved in some aspects of photoreceptor sensitivity to light damage.

So, if I understand correctly, in simple terms, melatonin injections before the rats were exposed to a lot of light, led to additional eye damage. But melatonin injections after the exposure of light led to no additional eye damage. Which may translate to: Don't take melatonin in the morning or maybe even early afternoon (but midafternoon is okay as mentioned earlier). Or: If you're planning to look straight at the sun or staying in a very bright place, you might want to take melatonin later! It can be tricky translating such studies.

FWIW: I have corneal scar tissue, and I used to be very sensitive to light, leading me to wear sunglasses most of the time, but that went away at some point and now I only have to do it on some summer days when it's very light out there. I'm saying this because I regularly took/take melatonin for periods of time one to several hours before sleep, and it never affected my sensitivity in a negative way. I doubt that a high concentration of melatonin would. Though perhaps (just a guess though!) taking it late afternoon and/or evening (if single dose; evening) would be the safe route if you have high sensitivity to light.

Hope this helps!

 

[s1mpleman]

So, if I understand correctly, in simple terms, melatonin injections before the rats were exposed to a lot of light, led to additional eye damage. But melatonin injections after the exposure of light led to no additional eye damage. Which may translate to: Don't take melatonin in the morning or maybe even early afternoon (but midafternoon is okay as mentioned earlier). Or: If you're planning to look straight at the sun or staying in a very bright place, you might want to take melatonin later! It can be tricky translating such studies.

FWIW: I have corneal scar tissue, and I used to be very sensitive to light, leading me to wear sunglasses most of the time, but that went away at some point and now I only have to do it on some summer days when it's very light out there. I'm saying this because I regularly took/take melatonin for periods of time one to several hours before sleep, and it never affected my sensitivity in a negative way. I doubt that a high concentration of melatonin would. Though perhaps (just a guess though!) taking it late afternoon and/or evening (if single dose; evening) would be the safe route if you have high sensitivity to light.

Hope this helps!

Good points, and I was under a similar understanding.

I also suffer from Anterior Uveitis (a lot less now thanks to diet changes) and have taken melatonin on a night with no adverse effects on my eyes sensitivity FWIW.

 

[Gaby]

I just finished reading "Extreme Dose Melatonin - The Miracle Anti-Aging Hormone, Anti-Alzheimer's Hormone, Anti Baldness Hormone, Menopause Reversal Hormone" by Jeff T. Bowles:

Melatonin - Jeff T Bowles

Melatonin Case Studies and results - Jeff T Bowles

jefftbowles.com

Is the fastest reading ever! Jeff T. Bowles is also the author of "Miraculous Results - Extremely High Doses of Vitamin D3" which we discussed elsewhere in this forum. Or at least I remember reading it and several members experimenting with his recommendations.

Bowles theorizes that one of the most important functions of the luteinizing hormone (LH) is to drive the destruction of tissue as we age (as opposed to when we are young). So LH attacks the brain in Alzheimer's disease. He quotes research pointing to the fact that an LH suppressing drug stop Alzheirmer's disease on its track, in women only. He explains, at least theoretically, why it didn't work in men and it has to do with the rest of the hormones. More specifically, he argues that men will only be protected by increasing their progesterone levels. This is where melatonin comes in.

He quotes research of melatonin's protective effects in Alzheimer's disease (AD), and he highlights how melatonin suppresses LH. He quotes his own blood tests which show how his LH levels dropped by 30% by taking 300mg of melatonin at night for two months. Not only that, his progesterone levels rose by 15%.

He argues that progesterone is one of the best neuroprotective substances on earth and himself takes 100mg of pregnenolone a day, which is a precursor for DHEA, progesterone, etc. He explains the levels of LH, progesterone and other hormones as we age and tells the story of how women delayed menopause by taking melatonin in high doses. Some women who already had menopause, started menstruating again.

His advice for people with initial stages of AD: for women, 75mg melatonin at night, and might even boost to 500mg. The same advice goes for men, except it would be 125mg of melatonin. He also suggests 200 to 400mmg of pregnenolone. However, he highlights the following:

It would be best to boost your melatonin doses gradually -- get used to 3mg, over a week or so, then go to 6mg, for a week, then 12mg, etc, doubling the dose every time you get used to the old dose. Why?

Because some of his friends started with 100 mg and didn't notice anything. On the 3rd day, it hit them: they got a bad case of dizziness or vertigo. He speculates that it is like fasting, some people get dizzy after several days of fasting.

After 12mg are reached, he suggests 24, then 48, then 75mg. For men, 96, then 120. He quotes results of members of his yahoo group where loved ones seemed to have recovered short-term memory despite the initial stage of AD. Anecdotally, he says that one member who only took coconut oil for one month, had pregnenolone levels increased by 250%!

Melatonin increases most of the "good" hormones and decreases most of the "bad" hormones, and it decreases all reproductive hormones regardless if they are good or bad.

Bowles also confesses to bad effects of melatonin among his members: higher chance of shingles, further thinning of hair if your father had thin hair, further thickening of hair if your father had thick hair. There was a case of recurrence of Lyme's disease.

He also quotes most of the papers on the protective effects of nicotine and smoking in AD, but he argues that it is due to the fact that smoking causes LH suppression. Same with smoking benefits in endometrial cancer, Parkinson's disease, Tourette's syndrome, etc.: smoking reduces LH.

LH levels go from 60% to 1100% increase in males by age 80. In females, +2600%. He speculates that progesterone protects women at some point, but that these levels might explain why AD is more common in elderly women than in elderly men.

So the above is the short version. He is fond of speculating very creatively. Furthermore, he has published papers. For instance:

The Evolution of Aging: A New Approach to an Old Problem of Biology - PubMed

Most gerontologists believe aging did not evolve, is accidental, and is unrelated to development. The opposite viewpoint is most likely correct. Genetic drift occurs in finite populations and leads to homozygosity in multiple-alleled traits. Episodic selection events will alter random drift...

pubmed.ncbi.nlm.nih.gov

This theory suggests that the protective effect of smoking and ibuprofen for Alzheimer's disease is caused through LH suppression.

 

[Anamarija]

It would be best to boost your melatonin doses gradually -- get used to 3mg, over a week or so, then go to 6mg, for a week, then 12mg, etc, doubling the dose every time you get used to the old dose. Why?

Thank you Gaby, great info.

This is from book Ronald Ross Watsona - Melatonin in the Promotion of Health:

In the past 50 years since the discovery of MEL, we have witnessed an emergence of a plethora of information from studies on a wide group of animals, including vertebrates and invertebrates, and plants subjected to MEL, the most unique and wonder molecule among all the known substances in areas covering endocrinology, pharmacology, physiology, psychology, chronobiology, and environmental biology. The most remarkable feature of this pineal hormone is its synthesis in the synchronization with the environmental light/dark (LD) conditions. In all the animals investigated so far, irrespective of their habit, MEL synthesis in a 24-hour cycle reaches peak during the dark phase. As a hormone, MEL afforded the first opportunity for its use as a chronobiological marker, particularly for those who are engaged in circadian studies. It plays a central role in primary circadian pacemaker (suprachiasmatic nucleus, SCN) to synchronize the body functions to LD cycle of the environment. Accordingly, this hormone is considered as a “chronobiotic molecule,” or the “hormone of darkness.” Molecular biology study dealing with its biosynthetic enzymes and their genes, molecular regulators, degradation byproducts, and the mechanisms of signaling in a cell has opened up a new chapter in circadian research. Carefully controlled studies in different animals, including the human, have implicated MEL in the control of a wide variety of body functions ranging from aging to aggression,
hibernation to hypertension, jet lag to seasonal affective disorders, sleep to stress, and reproduction to tissue regeneration. More recent studies revealed that MEL, because of its lipophilic nature, can cross the plasma membrane of any cell and thereby has free access to all the tissues, organs, and systems in the living body and by acting as a potent scavenger of free radicals may play an important role in combating oxidative stress in a metabolically active cell [7]. Moreover, MEL is known to be involved in complex processes of cellular protection and apoptosis. A rapidly expanding body of literature suggests that MEL as a biomarker of circadian dysfunctions may play pivotal roles in various neurodegenerative or neurological diseases. As a result, MEL has become a potent candidate for investigation in several disciplines of experimental biology and pathophysiology signifying its importance in clinical and therapeutic research. The aim of this review is to track the progress in research from discovery of MEL to its potential use in therapy by focusing the most fascinating, and arguably important, data gathered in recent past. We emphasize mostly on recent review articles, including ours, as they included many original findings that contributed to the current state of knowledge.

 

[Laura]

This is really starting to sound like a potential rejuvenating/life extending therapy.

I guess we should note that the mice that had eye issues were albinos and albinos in general have eye issues to begin with so I don't think Mrs. Peel has anything to worry about.

Also, the protocol for building up to the high doses sounds better. Obviously, starting too big too fast is what I did wrong and I sure did have vertigo and feel half drunk for a few days!!! I'm going to go at it again in the right way!

 

[liam1310]

I'm using melatonin for years now, never anymore than 3mg, most of the time I use liquid or Swanson Melatonin capsules, other ingredients are rice flour and gelatin. 3mg 120 capsules, it also comes in 10mg 60 capsules.

I took 6mg last night, first time taking more than 3mg, didn't notice much of a difference, just a good night's sleep, l will experiment with increasing the dose.

Thanks for the info guys.

 

[s1mpleman]

Also, the protocol for building up to the high doses sounds better. Obviously, starting too big too fast is what I did wrong and I sure did have vertigo and feel half drunk for a few days!!! I'm going to go at it again in the right way!

Wow, if that's how you felt from your staggered attempts I can only imagine what the 100mg intravenous study participants experienced after that dose.

 

[Laura]

I just finished "The Melatonin Miracle" by Walter Pierpaoli, MD. etc and William Regelson, MD. It's pretty much about the basics of melatonin, where it is produced, what it does, interactions with body systems, that sort of thing. The book talks about how they came to the idea that it can reverse aging and also that it is an anti-cancer element in the body. The solution presented is supplementation.

There are no real details about any cases that tell you how much of anything was given, for how long, etc, so don't get it expecting that. I only took a few notes as follows:

Pineal gland senses and reacts to other types of EM fields besides light; this can interfere with the production of melatonin which may be one factor behind the increase in cancer since the beginning of the widespread use of electricity, artificial lighting, appliances, etc. It may not be just light... EMFs may trigger the growth of cancer cells by blocking the anti-cancer action of melatonin.

Melatonin helps normalize cholesterol levels and blood pressure.

Zinc supplements are needed by older people; melatonin is closely involved in zinc transport, so the fall of levels of one is associated with the other.

For insomnia or restless, broken sleep:

Tak 1 mg melatonin. If you are not asleep in 30 minutes take another 1 mg. If in 30 min, not asleep, repeat with another 1 mg, up to 5 mg. (I guess if 5 doesn't work, you could start higher the next night with 2 mg, then another 2 mg in 30 min, and so on.)

Anyway, after you finally do get a night's sleep (having found the amount that does the job), continue taking that amount every night for 2 weeks for a reset, and then, if you are in the "anti-aging" set, go to your normal supplementation amount.

Anti-aging:

Age	Dose 30 minutes before sleep time
40-44	.5 to 1 mg
45-54	1 to 2 mg
55-64	2 to 2.5 mg
65-74	2.5 to 5 mg
75 plus	3.5 to 5 mg

If groggy next day, reduce your dose by 1/2 mg. Try that, if still groggy, reduce again. Obviously, if the suggested amounts don't do the job, you can try upping it by 1/2 mg at a time.

Now, this book says that everyone in the above age brackets should be taking melatonin in these amounts or something close because it is by that much that the pineal's ability to produce it declines at those ages. Book says if you do this, you can reverse aging and prevent cancer and a host of other problems.

Synthetic melatonin is preferred.

 

[zhenqing]

This is all very fascinating!

I've been using melatonin for years as well, but only for my insomnia. I've started taking 1mg dose back in 2011 or so, after I saw melatonin mentioned here on the Forum, but 1mg didn't do much for me, so I increased to 5mg, and that worked wonders for quite a while, until I had to increase to 10mg a few years back (because my life got more and more stressful).

It takes around half an hour to an hour for me to get sleepy, and then I sleep like a baby, and I never feel groggy in the morning (assuming I went to bed at a reasonable hour and slept a reasonable amount, which for me is not less than 7 hours and no more than 8 hours).

If I skip even one day of taking melatonin, my insomnia returns. So it's been a godsend for me, because the usual prescribed drugs for sleeplessness are awful.

 

[Laura]

This is all very fascinating!

I've been using melatonin for years as well, but only for my insomnia. I've started taking 1mg dose back in 2011 or so, after I saw melatonin mentioned here on the Forum, but 1mg didn't do much for me, so I increased to 5mg, and that worked wonders for quite a while, until I had to increase to 10mg a few years back (because my life got more and more stressful).

It takes around half an hour to an hour for me to get sleepy, and then I sleep like a baby, and I never feel groggy in the morning (assuming I went to bed at a reasonable hour and slept a reasonable amount, which for me is not less than 7 hours and no more than 8 hours).

If I skip even one day of taking melatonin, my insomnia returns. So it's been a godsend for me, because the usual prescribed drugs for sleeplessness are awful.

Do you live in a high EMF environment? People who do, probably have worse sleep and will need more.

I'm just wondering if people who do will have to take higher doses than the book recommends. Of course, it is going to be very individual and people will have to find their proper dosage.

Anyway, everything I've been reading is very positive for this therapy. And let's face it, sleep is very important in these times, and repairing DNA damage too. We are simply bombarded with evil frequencies and it's only going to get worse with that 5G business. We need all the help we can get.

 

[zhenqing]

Do you live in a high EMF environment? People who do, probably have worse sleep and will need more.

I'm not sure, Laura. I live in a city, not the biggest (population a little more than 100k), but it's a city nonetheless. I'm afraid I don't have much knowledge in the matter of EMF yet (i.e what constitutes as high EMF environment) . I've always thought that my sleeplessness was caused by my chronic stress/anxiety, but of course the real cause may be more complicated than that.

I'll be changing my environment for a few weeks in a couple of days (sort of vacation time) - it's going to be interesting to observe if/how my body and mind is going to react.

 

[Laura]

I'm not sure, Laura. I live in a city, not the biggest (population a little more than 100k), but it's a city nonetheless. I'm afraid I don't have much knowledge in the matter of EMF yet (i.e what constitutes as high EMF environment) . I've always thought that my sleeplessness was caused by my chronic stress/anxiety, but of course the real cause may be more complicated than that.

I'll be changing my environment for a few weeks in a couple of days (sort of vacation time) - it's going to be interesting to observe if/how my body and mind is going to react.

Might be a good time to experiment with some higher doses just for a reset.

 

[seek10]

Thank you for sharing the information. Normally I tend to take Melatonin before sleep .5 mg to 1 mg depending on the day. When I take it, dreams are more clear, but i have tendency to sleep drowsily for more time. I think one more experiment to try with large doses ( I don't mean 120 mg) probably max 10 mg slowly for me.

 

[Stoneboss]

Do you live in a high EMF environment? People who do, probably have worse sleep and will need more.

I'm just wondering if people who do will have to take higher doses than the book recommends. Of course, it is going to be very individual and people will have to find their proper dosage.

Anyway, everything I've been reading is very positive for this therapy. And let's face it, sleep is very important in these times, and repairing DNA damage too. We are simply bombarded with evil frequencies and it's only going to get worse with that 5G business. We need all the help we can get.

I took 10mg of melatonin every night for several years in the past with no ill effects, just a good night's sleep and lots of vivid dreaming. But then for whatever reason I stopped taking it. Then, 16 months ago, we (my wife and I) moved to a different house. We now have wifi again and I'm not able to "hardwire" the internet like I did at our previous house. Also, it's a duplex so there's just a wood framed wall partition between us and our neighbor, who also has wifi. To make matters worse, both hydro meters are "smart meters". So it's no wonder I've had terrible sleep and insomnia since we moved here... until about a month ago. That's when I started taking melatonin again, 10mg every night. It took about 4 or 5 days before I got re-adjusted to the melatonin, but now I'm sleeping very well again, and lots of vivid dreaming. I didn't realize until now, since reading this thread, on the effectiveness that melatonin can have with combating EMF. I'm probably going to experiment and increase the dosage. Thank you for starting this thread Laura!

 

[nicklebleu]

We now have wifi again and I'm not able to "hardwire" the internet like I did at our previous house.

Have you tried internet over the power lines, along the lines of this? It’s pretty much plug and play and if you don’t have any fancy wiring it should work. The connection is also encrypted if you are not the only one on the power line network (eg multistory building).