' The bioavailability of oral melatonin was only 3%, but a considerable variability between the volunteers was noticed. '
The other problem with oral melatonin is that the effects are short lived, lasting only about five hours.
On the other hand, topically applied melatonin lotion accumulates in the many layers of the stratum corneum and is more slowly released into the circulation over a period of approximately 24 hours as discussed here :
' In a clinical study, the skin penetration properties of melatonin 0.01% in a cream and 0.01 and 0.03% in a solution were investigated by evaluation of the serum melatonin levels over a 24-hour time course in 15 healthy volunteers. Blood samples for melatonin measurements were taken at 9.00 a.m. before applying the test preparations and 1, 4, 8 and 24 h after application. The measurements were carried out by radioimmunoassay for melatonin. In 15 volunteers, the serum levels of melatonin before application of the topical preparations were between 0.6 and 15.9 pg/ml. After application of the 0.01% melatonin cream, there was a steady increase starting from 9.00 a.m. up to a mean serum value of 9.0 pg/ml at 9.00 a.m. the next day. The solution of 0.01% melatonin also showed an increase, starting from 5.00 p.m., up to a mean melatonin level of 12.7 pg/ml 24 h after application. The solution containing 0.03% melatonin resulted in elevated melatonin levels 1 and 8 h after application. The values were 18.1 and 19.0 pg/ml. The cumulative melatonin values for each preparation were 7.1, 8.6 and 15.7 pg/ml, respectively. This study shows that the strongly lipophilic substance melatonin is able to penetrate through the skin and leads to dose- and galenic-dependent melatonin levels in the blood. '
Given the above data, I have been testing topical melatonin lotion (ML) for the past year and a half in myself, family, friends and acquaintances. The results seem to show that ML improves the length of time ML is active in the body, but it also had an effect that I suspected it would, but was not sure that it would. That effect, was pain relief.
In one friend with collorectal cancer that had metastasized to the liver that was testing very high dose oral melatonin at 360 mg/day, melatonin lotion could offer pain relief in the area of the liver that 360 mg of oral melatonin could not.
It is worth mentioning that , in studies, melatonin has shown the ability to help multiple spinal issues which I have not previously discussed on this forum.
WHAT TYPE OF PAIN RELIEF DID MELATONIN LOTION OFFER
The following list of 40 items is what was reported to me by everyone that tested ML.
1. Neck pain from multiple causes.
2. Lower back pain.
3. Shoulder pain.
4. Migraine headache relief.
5. Head and neck pain relief from a neck injury after falling backward onto the rim of a plastic bucket.
6. Eczema of the scalp.
7. Scalp pain.
8. Completely relieved jaw pain from two jaw fractures and helped to get to sleep. Based on studies may also help the fractures to heal faster.
9. Synergy pain relief with the Hyaluronic Acid / Stopain remedy for degenerative disc disease (DDD) which I have not discussed on this forum.
10. Headache relief
11. Muscle pain
12. Eliminated nerve tingling in feet caused by stage IV cancer with Lepto Menengeal.
13. Ankle pain
14. Knee pain
15. Swelling of the neck caused by injury
16. Calf pain of unknown cause
17. Nerve pain
18. Hand and finger pain
19. Back pain that required a cane to walk was relieved enough that no cane was needed after regular twice daily applications.
20. Relieved sciatic nerve pain
21. Relieved thyroiditis and swelling with pain + sore throat pain that made even swallowing saliva very painful and of unknown origin and eliminated it in about a week eliminating the need for further application of melatonin lotion to the area. My friend thought it might have been caused by a recent endoscopy.
22. Relieved hip pain
23. Relieved bulging disc pain
24. Relieved Atopic Dermatitis
25. Stomach discomfort relief after applying to the surface of the stomach.
26 Relieved thumb joint pain
27. Helped a person to alleviate pain and muscle tension prior to her chiropractic appointment allowing her chiropractor to make what they both described as very good adjustments to her spine, which he had previously been unable to do because of muscle stiffness caused by the pain.
28. Helped two people with arthritic hand pain, one that was unresponsive to Borax and one that was only minimally responsive to Borax.
29. Helped a person with pain from liver cancer in the area of the liver to temporarily effectively relieve the recurring pain.
30. Helped a friend to sleep well when applied in the early evening.
31. Relieved pain in sore toes
32. Stiffness and discomfort of the hands without pain present was eliminated.
33. Improves wound healing.
34. Adds to the effectiveness of certain topical psoriasis medications.
35. Relieved toe cramps.
36. Alleviates spinal stenosis pain.
37. Much more effective pain relief than 360 mg of oral melatonin per day.
38. The very significant pain relief in multiple areas of the body caused high blood pressure to decrease, allowing for a halving of the hypertension medication dose by one friend.
39. Reduced the swelling of swollen arthritic finger joints.
40. Healed trigger finger in four days for one tester.
It is worth mentioning that the people who tested ML generally felt that ML had a cumulative effect for the first 2 to 3 weeks. In other words, pain relief seemed to increase for the first 2 to 3 weeks of regular use. At 2 to 3 weeks, the benefit was generally more than it was on the first 3 days of regular use.
WHAT IS MISSING
Only one person with PD tested the lotion, but they weren't testing it for the type of pain often seen in PD, so I have no idea if it will help with that type of pain, but I am doubtful if it would because that type of pain seems to be tied to the various medications used to treat PD.
HOW I MAKE MELATONIN LOTION
Gather The Ingredients
1. Melatonin bulk powder - 1/4 level full measuring spoon (This is roughly 750 mg)
2. Cetaphil Lotion - 1.5 ounces
3. Gin - 1.5 ounces
4. Three ounce bottle
I Add the melatonin powder to the bottle and then I add the 1.5 ounces of gin to the bottle. Replace the cap and shake the bottle until the melatonin powder is fully dissolved in the gin. It is important to fully dissolve the melatonin in the gin before adding the lotion in order to get maximum effectiveness. Now top the 3 ounce bottle off with Cetaphil lotion and shake very well. I often use this mix right after making it. I apply this lotion SPARINGLY up to twice a day.
SIDE EFFECTS
A couple of people who tested this lotion said that if they applied too much lotion or too often, it could make them feel tired, but if they applied in the later afternoon and before bed it wasn't bad. As with oral melatonin, some people are more sensitive to feeling tired and it seems that ML may have similar effects. Applying sparingly also helped prevent tiredness.
WARNING
Please get your doctor's approval and supervision before testing this lotion and to make sure it will be compatible with all medications you are taking, as melatonin has shown not to be compatible with certain medications.
Interesting! My HWP also has RLS and melatonin aggravates his RLS. This slow absorption method might be worth a try. Did the folks using the ML for pain apply it to the specific areas of their body where they had pain?
Yes, it should avoid that problem since little of the melatonin will reach the digestive system, but will definitely make it into the blood circulation and the brain since it easily crosses the blood brain barrier.
I wonder if it's the melatonin or what else they pack into the pills. Meanwhile this whole idea solves the riddle I have always had which is when you take two or three or five melatonin for sleep, who in the world and how in the world can they tolerate claiming they're doing well taking it better taking 50 60 80 mg who in the world could tolerate that? 3% bioavailability sure answers that one, finally.
wow, interesting. I tend to break open a melatonin capsule and sprinkle under my tongue. It does send me to sleep quickly but I often do wake about 5 hours later
I have tried one but we are quite restricted in NZ and can’t buy over the counter and have to get prescription to be allowed to import it. I used to be able to get the dual spectrum nature bounty but last time I tried to buy it none of the ones that would sell to NZ had it so I ended up with 10mg caps from them. 10 mg is too much and gives me psychedelic dreams so I started just taking a sprinkle and that worked so one cap lasts me about 4 days.
I included instructions on how to make ML, but I also included this safety warning :
' Please get your doctor's approval and supervision before testing this lotion and to make sure it will be compatible with all medications you are takin, as melatonin has shown not to be compatible with certain medications. '
This is how my friends who tested ML described sparingly :
Take an approximate pea sized amount of lotion and apply to the back of the neck from just below the shoulder line up to the top of the neck. Note that the top of the neck is above the hairline, all the way to the base of the skull. Several people mentioned to me that applying all the way up to the base of the skull offered more pain relief than just going to the hairline. They said that once you did this, you will "have a feel" for applying sparingly.
Some people, such as myself, have a high tolerance for melatonin and can apply as much and as often as I want.
In testing ML, I found that substituting Aloe Vera gel for the Cetaphil lotion allows application to the face and close proximity to the eyes without eye irritation. Why would you do this? Because both aloe vera gel and melatonin are good for the skin and will offer protective effects to the facial skin. If you try doing this with the lotion mix, it will be irritating to the eyes. The gel caused little if any irritation to the eyes.
Very helpful, thanks! I am absolutely going to try this. I've wanted to take melatonin anyway, but at oral doses above 5 mg, it makes me restless at night. I have a back pain issue that started about 10 years before my PD diagnosis. It's probably PD-related (can't identify any structural or nerve issues), and it's the bane of my existence. Currently, it limits me much more than my Parkinson's.
I am really interested in whether it can help with the PD pain that many forum members have mentioned that occurs when transitioning from on time to off time as the medications are wearing off. If it does, that could be quite useful on this forum. In any case, it seems like a good and effective option for getting melatonin.
Meanwhile this whole idea solves the riddle I have always had which is when you take two or three or five mg melatonin for sleep, who in the world and how in the world can they tolerate claiming they're doing well taking it better taking oral 50 60 80 100mg who in the world could tolerate that? 3% bioavailability sure answers that one, finally.
Well, I was at 132 mg/day and since adding ML to my regimen, I have reduced my dose of oral melatonin to 60 mg/day to maintain my melatonin gut level since it is thought that normal melatonin gut level is second only to mitochondrial melatonin level.
In order for the topical melatonin to work, it has to be dissolved and the gin dissolves melatonin. That is the reason why you can not add the lotion until you first dissolve the melatonin in the gin. Once the melatonin is fully dissolved in the gin, then you add the lotion. If you try to mix all three at the same time, the mix will be too weak to be fully effective.
Thank you for these details. I want to run by my concoction with you. I was unable to get the bulk powdered melatonin, and tried grinding up pills but they needed way too much gin to dissolve which I am assuming is because the pills have a lot of filler. My solution was to use liquid (cherry flavoured) melatonin and mix it with lotion.
I am starting with 0.5 ml of liquid melatonin from the dropper which has 5mg of melatonin and two ‘pumps’ of lotion, and mixing them together in my hands, before massaging into the skin - and just mix it up every night before applying.
I am wondering how my mixture’s concentration (5mg/application) compares to a pea sized application of your recipe. If 3 ounces contain 750 mg of melatonin, where 1 liquid ounce = 6 teaspoons, and if one pea sized amount = 1/4 teaspoon, then 750 mg/3 ounces/6 teaspoons/4 peas per teaspoon = 10.4 mg per pea sized application. So if these calculations are reasonable, it looks like I am starting with half strength (more or less) with the 5 mg application.
Sorry for the delayed reply, I just now saw your question as I did not receive a notification.
Please let us know how your mixture works out for you. I'm wondering what country you are in that you can get the melatonin formulation you described, but can't get the bulk powder form?
I am in Canada, and probably could get it via the US (like I did for Piping Rock B complex) but would rather get it from the local store. Here is the 10mg/ml Liquid Melatonin by Sisu (natural black cherry flavour - even though we are using it topically), that I mix with lotion 🧴 in my palms. No results to report yet, but it was easy to incorporate into HWP’s nightly foot massage (lucky guy) to help with mild (and hoping to stay mild) neuropathy. Certainly no bad side effects (😅). This liquid form is probably much more expensive than the bulk powder, but at least it does not require gin, lol.
With the mix I described, each ounce contains 250 mg of melatonin and the breakdown looks somewhat like this :
3 oz. = 750 mg melatonin
2 oz. = 500 mg
1 oz. = 250 mg
3/4 oz. = 187.5 oz.
1/2 oz. = 125 mg
1/4 oz. = 62.5 mg
1/8 oz. = 31.25 mg
1/16 oz. = 15.625 mg
Seems like a pea sized amount would be around 1/16 oz or slightly more. If you are diluting 10 mg of your flavored melatonin dropper fluid with lotion, you are significantly below the amount of melatonin in the lotion I described.
It might be easier to check eBay Canada for melatonin powder. As to the gin, it very likely improves transdermal absorption for the brief period that it rapidly evaporates right after application :
Thank you, Art. That is very helpful. Until I track down the powder - thank you for the link- I will increase the concentration of my mixture.
We notice that compared to the usual lotion, the lotion with melatonin makes his feet feel a warmth and a pleasant tingly sensation after it has been applied. Do you notice similar short term effects?
I have not heard such reports previously so that is new information for me, but I have to consider it with a grain of salt as there may be other ingredients in your melatonin liquid that are causing those sensations. Reports I have gotten were mainly pain relief, but a few others as well.
As to that link, I selected ebay Canada, but I did not see any clarification that it took me to ebay Canada.
It may be better for you to go to ebay Canada using your browser and make certain they actually have the melatonin powder.
You are brilliant. Thank you so much. I'm going to make some as soon as I get the ingredients. Very hopeful I can help friends who experience a lot of pain, and maybe myself, who experiences a little. Plus my face could always look better.
Thank you Art for all this wonderful information, your research, your testing, sharing this, and your time!!
I ordered the melatonin and lotion this morning and will mix it up as soon as I get it. My HwP has excruciating back pain which is from working hard and playing hard his whole life and I suppose, now, increased from PD. I am hoping this will help him tremendously!!
After looking over your list of what it can help I will be smearing the stuff on many places on both of us. I am very excitedly hopeful for great results. We’ll apply it at night just in case we get too sleepy from it!!
I have been using the melatonin cream per your recipe. I use it on both shoulders & low back. I have not been applying it twice daily, usually only once. Yes, it has been helping!!! I also have been using my HwP’s Well Red helmet on my right shoulder & the Well Red pad on my back once a day.
I am sure the combination of Melatonin cream & Red Light is greatly improving my pain. I don’t think I’d get as good of results with just one or the other.
This morning I was very impressed., though. When I got up this morning my back was really hurting so I put the cream on & I was so amazed that my pain was very negligible in a very short time. My back & shoulders are extra troublesome right now since I am having to do extra heavy lifting.
So all in all I am very pleased with the results & will continue to keep it on hand.
I'm glad the melatonin lotion (ML) is helping you with pain relief for your back and shoulders caused by the heavy lifting! Is it also helping you with migraine headaches, as that is what #4 is about? My friends, family and acquaintances who tested ML reported that the benefits, when used daily, seemed to increase for the first 2 to 3 weeks and then plateaued.
You are now the fourth forum member to report pain relief from ML!
I know that ML can help relieve many forms of pain in multiple areas of the body from head to toe, but am very interested if it can help relieve pain in PwP during medication transition periods, when the meds are either wearing off or kicking in? Some forum members have reported pain during these periods and I do not yet know if ML can help relieve that type of pain? That could be useful information for forum members who are affected by that type of pain.
Btw, it is worth mentioning that a main method of action of red light therapy (RLT) is that it is thought to increase local melatonin levels in mitochondria where the RLT is applied. ML seems like a somewhat cheaper and easier way to increase those melatonin levels, but not just locally as ML will increase melatonin in the blood also.
I forgot that you originally intended to use the melatonin lotion for your husbands "excruciating back pains". Has he tried it yet and did it help him? From feedback I have gotten from others, it seems to have a cumulative effect for the first two to three weeks when the benefit levels off.
Hi Art ~ Yes, I did try it on my husbands back pain area. It didn’t seem to help him too much. But maybe I should give it another try since he had a cortisone injection last week. We don’t know if that has helped yet. But maybe the ML would work better now.(?)
Thank you for the feedback Gail. Something that all three of the first people that tried ML said to me, not including myself, is that initial pain relief was less that Stopain roll on, available at most drug stores, but after a week of 2x a day application, pain relief exceeded Stopain roll on, noticeably.
I will say that nobody who I had test ML described their pain as "excruciating" and that may be a level beyond what ML can help quickly, but given the beneficial effects of melatonin to the spine and muscles, a one month or longer trial period of 2x day applications may be worth considering for your husband?
' Melatonin is a highly evolutionary-conserved ancient molecule that was only recently rediscovered as a safe dietary supplement in muscle disorders and in exercise. This review attempts to shed light on potential and promising therapeutic roles of melatonin to limit muscle deterioration, mainly mitochondrial function, and sarcopenia. Main pathways activated by melatonin in skeletal muscle are drawn in Figure 2. '
' However, the utility of melatonin in athletes to obtain the best physical performance is strictly time-dependent, dose-dependent, and exercise-dependent. '
The following gives information on one way of several that melatonin helps the spine :
Topical melatonin, beyond its more efficient absorption and pain relieving effects is also a potent skin protectant as described in the following link :
Here is a relevant quote from the review article :
' In our view, endogenous intracutaneous melatonin production, together with topically-applied exogenous melatonin and its metabolites, represent two of the most potent defense systems against external damage to the skin. '
Interestingly, melatonin in the blood, has very limited potential to reach the skin, but melatonin absorbed from the skin can readily reach the blood.
If you are in the UK, I suggested a UK supplier of bulk melatonin to a forum member and they said they were able to order the powder from them with reasonably quick shipping and they said it worked for 4 different issues once they made the lotion. Here is the link :
I have always felt that oral melatonin was a very poor way to deliver melatonin and that is why I have always looked for a better way to deliver melatonin where we could get more benefit from it. Then I came across the study describing the absorption of melatonin through the skin and have been testing that method for about 1.5 years now and finally felt comfortable with posting that information on this forum after that testing. Having melatonin active in your system all the time is much more beneficial than just a 5 hour useful window that oral melatonin offers.
The actual absorption rate of melatonin varies by individual, but the point being that oral melatonin is very poorly absorbed and in some people at a rate even lower than 3% . I don't know what measure of picograms of melatonin in the blood that the 360 mg oral dose achieves in humans because there are no studies that I am aware of that define that number at that dose, but it may still be 3% or thereabouts , but not enough to surpass the local tissue level that ML easily reaches. I do know that melatonin lotion can reach very significantly higher local tissue levels before it moves on to the blood stream though. The other consideration is that an even higher oral dose such as 360 mg may have an even poorer percentage absorption rate than a lower dose. With only a 5 hour window of opportunity for oral melatonin to perform in humans, this is another significant obstruction to oral melatonin usefulness. I think the majority of oral melatonin does its work in the gut microbiome and that is why I still take oral melatonin as well as topical melatonin.
Topically applied melatonin accumulates in the layers of the stratum corneum where it is released over an approximate 24 hour period, somewhat like a patch. Based on what I have read in the literature, I feel that oral melatonin does its major work in the gut, while topically applied melatonin does its main work in the skin and then moves onto the blood circulation and ultimately the brain since melatonin readily crosses the blood brain barrier (BBB). If melatonin crosses the BBB and it does, then that means it very likely gets into the cerebral spinal fluid (CSF), which would be very important for PwP, as melatonin in CSF is protective of the brain. PwP are thought to have lower melatonin level in the CSF. Topical melatonin also avoids the first pass loss and gut microbiome loss. The combination of delivery methods seems better than either one alone. The pain relieving effects are just a bonus.
In symptom # 4, a friend told me that melatonin lotion alleviated their migraine headaches faster than anything else they had tried and also mentioned their migraines used to last a week, but now are over in less than a day with very reduced symptoms during that initial period. This new (May, 2024) randomized, placebo controlled trial (RCT) adds further confirmation to the idea that melatonin significantly relieves migraine headaches with a very good safety profile :
' Our study shows that melatonin was more efficacious than the placebo in the reduction of frequency and duration of migraine attacks. It was equally safe as the placebo and might be effective in the preventive treatment of episodic migraine in adults. '
This is a copy and paste from a post by forum member MarionP that is relevant to this post on the pain relieving effects of melatonin lotion as well as my reply :
MarionP profile imageMarionP in reply to chartist
4 hours ago
Art, melatonin by ingestion versus melatonin cream which is topical: what basis to think either would work? (PS I used your formula to make melatonin cream and my perception has been that it helps with pain for sure, many thanks for that one!)
My Reply :
chartist profile imagechartist in reply to MarionP
5 minutes ago
Marion, thank you very much for the feedback as feedback is very useful! As far as I am aware, you are only the third forum member to have given feedback on actual use of melatonin lotion (ML) and all three are positive and add further confirmation to what I have reported on this forum regarding ML. I will copy and paste your post into the original ML thread.
If you look at the last link about melatonin lotion ( healthunlocked.com/cure-par... ), in that link, I link to the studies which answer your question. As to pain relief, my thinking on that aspect of ML is based on multiple studies suggesting that melatonin, through its direct and indirect antioxidant and radical scavenging activities as well as its well described anti inflammatory effects in the literature, should definitely have pain relieving qualities and my testing confirmed that response. The oral dose required to reach the pain relieving effects of ML have to be astronomical. The potential of ML for benefit to human health, imo is far greater than equivalent dosing of oral melatonin. Imo, the combination of both is even more so.
I tested ML in myself, family, friends and acquaintances for over a year and a half to confirm that aspect of ML. Of note is that most testers using ML daily suggested that continued daily use seemed to have a cumulative effect for the first two to three weeks or to say that a little differently, the benefit seemed to increase when compared to the first application, for about two to three weeks and then it leveled off .
This is another copy and paste of a post by forum member MarionP regarding this topic and my reply :
MarionP profile imageMarionP in reply to chartist
7 hours ago
You know there is a very nice side benefit, which is that one does not have to rely on the traditional NSAID medications with their side effects and risks... Such as ibuprofen, acetaminophen, aspirin, naproxen, and even diclofenac... Not to mention the ones which one must have a prescription and carry higher risks too. I think that is not a small benefit so I would encourage other people to take your little topical concoction here very seriously. Also, you know it is really doggone cheap.
chartist profile imagechartist in reply to MarionP
6 hours ago
You are absolutely correct regarding the NSAID side effects when compared to melatonin lotion (ML). Another point is that because of the multiple methods of action of melatonin, ML also has the potential to offer healing effects to multiple areas of the body such as the spine, as discussed here :
ncbi.nlm.nih.gov/pmc/articl...
Here is a relevant quote :
' Preclinical studies suggest that melatonin may exert neuroprotective effects and promote the restoration of neurologic function after SCI (Figure 1). Multiple mechanisms are potentially involved, including antioxidant effects, regulation of iNOS, inhibition of proinflammatory cytokines, blood vessel repair, restoration of the blood-brain barrier, inhibition of cell apoptosis, edema resistance, inhibition of cell autophagy, and regulation of MMP, p38, JNK, ERK1/2, and MAPK pathways. '
Given the fact that melatonin can traverse the human body with relative ease, you can see where ML suggests potential to be effectively applied on top of the spine for benefit in that location.
I will copy and paste these posts into the original thread for continuity.
I prepared melatonin lotion by measuring out one gram of powdered melatonin from Bulk Supplements into 2 oz of vodka. I had to stir it for a little while but it did fully dissolve. I then added the solution to 2 oz of Ceravie Lotion, which is quite thick on its own. The resulting combination had a satisfactory consistency.
I then applied this liberally to my arms which have been quite sore, and to my lower back and to my neck, which have been stiff and painful, once a day, for 3 weeks straight. The good news is no adverse effect. As you know I'm not able to tolerate oral melatonin. The bad news is no effect on the pain, stiffness and soreness. No harm done, at any rate.
Also for the last few days I've been using infrared heat on my arms.
Thank you for the feedback, p_b! Well it sounds like you made it correctly. Since you are tolerating it very well, maybe you can try the twice a day application. If you do that, please let me know if it helps.
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