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  • BDD Moderators: Keif’ Richards | negrogesic

Melatonin receptor agonists & antagonists + I tried all (most) other options so you don’t have to

SpiralusSancti

Bluelighter
Joined
Feb 2, 2023
Messages
2,301
Tiny background about me & sleep. I suffer from insomnia since childhood but actually never really got (mucho) medical help for it. My first sleep-aid was cannabis and it worked remarkably good for years, for a long time… But it’s not a simple to accept it as real sleep-aid for me as it was in fact insomnia cure for me that many times worked by causing me not to give a fuck I don’t sleep and often not helping me at all to sleep during “normal folks hours”.

My opinion is that neither benzos, z-drugs, antihistamines (“pure” & anti-psychotics), antidepressants are for frequent use and silver bullet for insomnia is still far away. And not just in a way as opiods are not acceptable for long term treatment of medium level pain but some are truly unacceptable for chronic insomnia and can cause a lot more problems than insomnia alone! Do I have to go into depth why? I don’t think so but I’ll say a word or two about each and why to NOT USE them as regular or even semi-regular use. I wont include technical details why it’s that way.

Benzos – not (that) effective in treating many types of insomnia, fucking addictive, fucking up your REM, rather good at fucking up brain.
Personal experience: Even with ungodly tolerance nitrazepam worked for me. Any idea how? As none other benzo I tried worked anywhere nearly as good even when I had no tolerance and I needed stupid high doses to use them as sleep aid. Two other exception being etizolam and oxazepam. Etizolam being highly effective in medium – high doses but that effect was because of how good anxiolitic it is, not sleep aid per se. But I wouldn’t use it again even if I could as it’s only truly recreational benzo I tried and that turned out catastrophic. Oxazepam works in normal doses surprisingly good (still nowhere near nitrazepam) but not with severe insomnia and not really without something with it. So oxazepam works but in combo with something.
Diazepam, alprazolam, diclazepam never worked as a sleep-aid for me in normal doses. What might work but I never tried for that is lorazepam and reason I think it might be is cuz it’s only benzo that reminded me of etizolam in it’s axiolitic quality, but a lot more subtle.

Z-drugs – obviously carrying many of the same problems as benzos but they are overall more effective sleep-aid and better option for insomnia than benzos.
Personal experience: tried zolpidem a few times and found it relatively effective, on par with nitrazepam but using effectiveness very fast and I wouldn’t play with it by pushing dose so it remains effective. So overall not something I would use regularly and even I can get it, same as with benzos, medium and long term it’s not worth risks that brings.

Antihistamines (and anti-psychotics) – inherent toxicity of stuff like dramine even at normal doses alone makes them pure choice. Arguably even a lot worse than benzos and Z-drugs; possibly somewhat worse than low-doses of second gen anti-psychotics or some of antidepressants that can be used for insomnia. Yeah, I know some anti-psychotics are good for sleep because they act as antihistamines.

Personal experience: dramine works as “dirty” sleep-aid, looses efficacy rapidly and to use it more than on very rare occasions is on par as choosing alcohol as a sleep-aid. Arguably a if a drink or two helps with insomnia even with effects on REM etc. it’s still probably safer than dosing something as dramine regularly. Quentiapine might be most off-label sleep-aid and arguably least damaging in low doses, hardly addictive at all compared to benzos. Staying under anti-psychotic dose is tricky and no matter how many time you read 25 – 100mg is under ant-psychotic dose that IS NOT TRUE if used daily. As with half-life of 7 hours (parent compound) and 9–12 hours (active metabolite, norquetiapine) you’ll end up accumulating enough of a drug to act like/for what it was designed originally. Therefore you’ll end up risking side-effects associated with anti-psychotics and that should be enough to deter you from any but a very rare use cuz even it’s not addictive as benzos it can have even more fucked up side-effects. Other anti-psychotics may be even worse. Even if highly effective for many people in low dose like olazapine is. General conclusion is, fuck ant-psychotics and avoid them if you are not getting them for their real use and avoid off-label use even if you react good to them and don’t get prolonged sedation or any other intimidate side-effect.

Antidepressants – some SSRI, SNRI and atypical antidepressants work very well as sleep-aid. Often used off-label and sometimes they are even intended for curing insomnia too. Most of logic why it’s best to avoid them as sleep-aid if you don’t have them prescribed for depression or other metal issues is similar to reasoning against using ant-psychotics as a sleep-aid.
Personal experience: Some antidepressants work relatively good as sleep-aid but usually loose efficacy even before they start helping with depression. Even occasional use will lead to side-effects tied to prolonged use so they are also out of question as sleep-aid for me. Reasons are countless and range from affecting libido to blocking (blocking) action of psychedelics. Notable example are mirtazapine and trazodone as they work much better (for most people) as sleep-aid. Mirtazapine looses efficacy quite fast as sleep-aid but if not used often and with spacing use enough can be effective for a long time. Trazodone was more of a stimulant for me because of mCPP metabolite, bordering on recreational but I met people swearing by as a sleep-aid. I think both have more prosperity in turning out to be okish drugs compared to most of SSRIs and SNRIs, both for intended and off-label use but that’s just my hunch.

Antimuscarinics & antinicotinics – way too obvious why to not use them but I have a hunch that prosperity of finding a good sleep-aid is rather fine within scope of those substances. Effective sleep-aids for sure, safe one?, that I’m not so sure.
Persona experience: plant containing scopolamine&antropine are really effective sleep aid but have low therapeutic index and sleep-aid dose is as close to tropane alkaloid high are as close as delirium causing and deadly dose. They loose efficacy as sleep-aid rapidly but not as rapidly as many of above examples. Rapid antidepressive effects are strong with this one too. Finding out for how long, ain't gona go that road, maybe with pure alkaloids after more scientific research is done. I find them almost as effective as NMDA antagonist in rapid action of removing depression but find none of lasting effects like with NMDA antagonists. Is it dose? Is it needed to use them for some time to get lasting effects? Ain’t gona go that road either until a LOT MORE research is done and neither anyone should except in life-threatening situations.

Other gabanerics – newer ones that could be a good sleep-aid still can turn out as bad or worse than benzos and old one like GHB are potentially very dangerous because of misuse
Personal experience: pregabalin and phenibut and barbital and GHB/GBL are more stimulating than typical benzo for me and I don’t find them a really useful as sleep aid. Obviously I won’t go down the road of using GHB/GBL or barbiturates or even older gabanerics in doses enough for sleep. Except in life-threating situations and in case it’s only option for you to have aceptable quality of life I would highly advise against use of those as a sleep-aid even GHB is sometimes prescribed as such as not many (poly)drug (ab)user could handle having daily dose of GHB above recreational dose and use it as prescribed. Other relatives or ancient stuff with such a big knock-out straighten are usually as bad idea or worse.

Herbs & supplements – way too many of them with way too big variables in pharmacology and pharmacodynamics to have any all round conclusion but many are a lot more safe than most if not all of mentioned above but some are as dangerous or even more because of lack of real scientific research
Personal experience: many are almost as effective, short term sometimes even more effective than many substances mentioned above. But they also generally loose efficacy very fast, don’t work on certain types/intensities of insomnia etc. I wont mention anything that can be used relationally and/or having significant, really noticeable high but can be used as a sleep-aid in a kinda off-label use, in fact I’ll mention just one, so you know what I mean – kratom/weed combo.
Melatonin, passionflower, valeriana, mexican poppy, black seed oil and many other can be rather effective at least at first, at least for mild insomnia, at least for portion of population and sometimes you can hit a jackpot with some combo and wonder why something like that, arguably very harmless, isn’t first line of defence but rather opposite. I hardly encourage you to do your own research and see for yourself, especially before trying stronger stuff, in cases of mild insomnia and in all cases to afford yourself some tolerance break with other stuff that works fine for you but it’s either unsafe or ceases to work after some time. In last case it’s very important to understand action of whatever you are using because of potential dangers with some combos (and sometimes because of half-life of substance and being on it for a long time you would actually do a combo even if you stop for a few days so have that in mind).


I will go for a melatonin receptor agonists next when I get chance, I have a hunch they could be a winner. I find melatonin surprisingly effective, but fails to work after just a few days (not at first but after you go trough some amount after that almost total tolerance tend to develop in a matter of days), and than works fine again after days or weeks of a break. That and some other properties (and rather surprising lists of side effects which I‘m lucky to non’t experience them) makes me wonder if UK decision to make it prescription drug maybe isn’t that stupid, well still just a big maybe… Only thing is idk how easily available are they in general but I’m excited about r&d of both M1, M2, M3 agonists and antagonist and will get my hands on some whenever I get a chance.

I’ll also keep exploring other emerging new options, herbal stuff and “light” substances.



Good Luck & Sleep Safe
 
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