• N&PD Moderators: Skorpio | thegreenhand

  • Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

sublingual bioavailability of melatonin

T

thesomoan

Bluelighter
Joined
Aug 7, 2010
Messages
97
Pretty much as the title says, what is the sublingual bioavailability of melatonin? is it significantly better than oral, and is there any scientific backing for melatonin supplements?
 
From what I've read the sublingual BA is higher than oral BA for melatonin, but have been unable to find any numbers.
 
Presumably, higher bioavailability / faster onset of action.
 
IME, it's A LOT more bioavailable. An eighth of a pill under the tounge feels like the full (3 mg) pill eaten.
 
That's probably true.

Still, melatonin is hardly the most sound supplement. It's efficacy seems to be backed by research, but whatever benefit it gives is pretty minor. Ramelteon, which I have some experience with, seems significantly more effective, but it's still a worthless sleep aid, IMHO.

I'm interested in how effective they might be at resetting the sleep disturbances from mania though.

edit: small sample, but PMID: 2086173 says no benefit.
 
I have experience with sublingual melatonin. I does work faster but i am not sure if the bioavailability increases.

//blazR
 
@Hammilton

Melatonin works very well for people with circadian rhythm sleep disorders. For regular insomnia it is pretty damn worthless.

Melatonin works wonders for my delayed sleep phase disorder.
 
yup, melatonin works great for me when my circadian rhythm gets jacked up... i.e. last week i got black out drunk one night, then pulled an all nighter the next night... the third night i had a hard time falling asleep, then i took melatonin (3mg sublingual btw :) ), and sleep came pretty easily afterwards.
 
I take 3-6 mg every night.. I have been trying it sublingually and it does seem to work better. I don't know if it's more effective though.
 
I've experienced surprising efficacy for my part. My doc recommended it to because of my asperger's, but never gave any rationale for the connection. However, 5 mg sublingually gives me a minor drowsiness 30 minutes after administration. It's not much, but sure helps me to place myself in bed rather than getting stuck in front of the computer. I had expected either pure placebo (of course it's hard to tell) or very very minor help.
 
Seattle_Stranger said:
Why exactly would you want to take it sublingually? I don't see any benefit in this.
Click to expand...

because it's pretty expensive in Australia.

Anyhow i was looking for an answer and found only this thread for sub melatonin n thought i'd bump it.

just an extract from this http://www.life-enhancement.com/magazine/article/307-wake-up-call-for-melatonin (is a pretty interesting read in itself)

DIVIDING LINE
From reviewing the literature it becomes clear that a dividing line must be drawn between what is a physiologic and what is a pharmacologic dose. The total amount of melatonin produced in the human body is not known (at least four other areas other than the pineal gland are thought to produce melatonin also), but most researchers agree that the pattern of concentration in the blood stream during the nighttime peak is reflective of systemic production and availability. It is important to note that bioavailability of melatonin varies depending on a number of factors but primarily whether it is ingested orally or sublingually. In the former instance perhaps only 33% gets absorbed through the average gastrointestinal tract.1 Therefore, a 1 mg capsule of melatonin may only deliver 333 mcg of melatonin, or within the range of 100 to 600 mcg. There is a wide difference when melatonin is sublingually absorbed. The amount delivered to general circulation may be much higher, perhaps 50% or more. This means that a 1 mg sublingual tablet (the equivalent in sublingual drops) will deliver 500 mcg or more. Sublingual delivery is faster too.

So i have been taking melatonin for 4 nights so far and have had very interesting results. I've recently had to take some time off work to get my head straight. was smoking cannabis like it was going out of style and got to the point where i was using 3grams per day. joints in the day and bongs at night. in the space of around 6 months i went from half a gram to out of control, but didn't have the crazy cold sweats i was expecting, just vivid mood swings.... in hindsight it was only 6months as opposed to years. well my sleep cycle was hammered and after 2 weeks i had the pattern of a vampire.

so almost 3 weeks into abstaining from the green buds and naturally my dreams have come back, but maletonin has turned them from vague to vivid instantly, and had my first lucid dream for a long time last night. so much fun! Anyway, where i am it can only be prescribed by a gp in it's pure form, and that is in the form of 2mg sustained release tablets. i'd taken them as prescribed only to wonder about doing a sub dose, and so it seems more efficient for me to so it make sense. well all i can say is that i really look forward to going to bed even though i might not feel tired, it means the difference between lying awake for hours to falling asleep within 30mins for me. it's close relation to tryptamine interests me also, along with a vast number of other benefits, i'm sure i will look at importing this from the states one day if it continues to work so well for me. early stages yet.

currently subbing one 2mg tablet at night. must look further into dosages coz of mixed reports, some say less is better while others say more the merrier.
 
Word of warning, daily dosing of Melatonin will cause my depression to become very severe within 7 days.

Bro, just order the Melatonin from OS, customs or AFP aren't going to call you up on ordering some Melatonin in.
 
Melatonin has got to be up near the top sellers in terms of placebo effects. Aside from those that "feel better" from taking multivitamins, or 9/10 amino acids, providing you eat more than shit for breakfast. Melatonin is however usual for resetting circadian rhythms. I got good milage when I travelled around the globe a lot, helped with jet lag.

It does have an interesting effect on dreams for me for the first few nights (Insert worthless subjective bullshit disclaimer here)
 
amanitadine;11089374 Melatonin has got to be up near the top sellers in terms of placebo effects.[/B said:
Aside from those that "feel better" from taking multivitamins, or 9/10 amino acids, providing you eat more than shit for breakfast. Melatonin is however usual for resetting circadian rhythms. I got good milage when I travelled around the globe a lot, helped with jet lag.

It does have an interesting effect on dreams for me for the first few nights (Insert worthless subjective bullshit disclaimer here)
Click to expand...

care to back that up with some data? and also in what context?..... I'm very interested.
 
amanitadine said:
Melatonin has got to be up near the top sellers in terms of placebo effects.
Click to expand...

lol no, no not even remotely close (not just because it actually *DOES* work, but it's just not even that popular to begin with when compared to the rest of the OTC health supps)


anyway i'll take up to 6mg nightly (increasing dosage doesn't make too big a difference in subjective sleepiness, but the stuff's incredibly cheap here). sometimes sublingual, where i'll notice quicker onset but don't notice any bioavail changes. +1 on vivid dreaming, upon starting anyways; seems to subside after a couple days' of routine usage
 
amanitadine said:
..................It does have an interesting effect on dreams for me for the first few nights
Click to expand...
and
BMXXX: "..... +1 on vivid dreaming, upon starting anyways; seems to subside after a couple days' of routine usage"

As a psychotherapist I'm very interested in this aspect. I don't have personal experience of Melatonin, but with 5HTP, taken occasionally, I have vivid dreams relating to events from my past. The outcomes - if you can call them that - are that at the end of the dream there is a progression. A sort of "working out" has occurred. For example if I am transported back to a vignette from a time spent in a stressful situation, the outcome will be me transcending the situation and dealing positively with the stressor - usually a person who was causing me concern.

A fellow practitioner told me recently of his understanding that Melatonin was useful in inspiring dreams, although he did not comment on the potential for meaningful insights. So my curiosity has been aroused and this long overdue visit back to Bluelight and this page has sparked my interest.

I would be fascinated to hear if any of the dreams you guys have experienced left you thinking that some life issues had been partially or fully resolved.

Also, if there was a tendency to a regressive process then there could be great potential for this substance in psychodynamic psychotherapy!

E
 
Last edited:
I believe the ratio of oral vs sublingual melatonin is 10 : 1 , meaning 10 mgs orally equals 1 mg sublingually. I take about 1.5 mgs of melatonin sublingual once every few days .Seems to build up in the body.

There is a big melatonin-cannabis relationship.Melatonin taken in the dark and then smoking cannabis afterwards is EXTREMELY effective...seems to cause melatonin to be basically metabolized more. Melatonin is the best damn thing if you feel burnt out from cannabis usage - I have a sneaking suspicion that the melatonin depletion from heavy cannabis use contributes to a lot of mental fogginess. Pub med studies say up to 3000% increase in endogenous melatonin release from cannabis...A good sign that melatonin will help is if you consistently don't dream. I think you can smoke enough to inhibit R.E.M. cycles, causing ya to not get the restful sleep you need.

Does anyone else with HPPD (or not) get increased tracers , patterns, whatnot from melatonin? It can get pretty ridiculous if I take like 10 mgs. Methinks melatonin being in the serotonin cycle probally gets metabolized to all sorts of serotogenic relatives pretty easily . Nice little serotonin mood boost the next day a bit, thats for sure.

It would be wise to not take huge doses of melatonin. The doses sold are way to high IMO. I was quite out of whack from a 1 year 10-20mg sublingual melatonin binge(lulz) for a while . Too much will lead to lots of stomach weirdness ,nausea, and grogginess for way too long. The liver does not take kindly to large doses of melatonin!

Taking melatonin at night and not exposing yourself to light lowers levels of a liver protein called tumor necrosis factor(TNF), while melatonin and exposure to light increased levels of TNF. Point being, take your melatonin when its dark and don't go exposing yourself to light.A half hour of bright light after melatonin will pretty much make it not work at all, and makes you feel fucking WEIRD.

Melatonin at like 2 in the afternoon does not work on speed comedowns either aaaaagh!

-lenses
 
You must log in or register to reply here.
Top