A new case to add to the ongoing research, plus some personal reflections on the situation.
Since last Friday (9 days ago) I started suffering intense and continuous cluster headaches. I didnt know until 3 days later when i rang the doctor. I got an immediate prescription of Sumatriptan. It worked. I was grateful beyond words. But only for about 8 hours. Then I needed another. And another. In no time at all I was at the absolute dosage limit. I'm still there.
Yesterday I awoke with immediate need to take another pill. But before I did that, my thoughts from the previous days came together to try a different approach. After a day or so of realizing just how important this medicine was to me, I naturally got a little curious and did some online research into the molecule. What I saw stunned me. I had been prescribed some 5 sub DMT! WTF! That wasn't on the label. Ok lets look around and look for the chemical names, as there always is with compounds. Nothing. Not on wikipedia which usually discloses chemical names. None of the chemical suppliers. I found one distinct chemical name for it:
1-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-methylmethanesulfonamide
Would not something like (i'm no chemist) 5-sulfoxy-DMT be a bit easier to say and swallow?
I didn't research too deeply, but nowhere seemed to want to admit this. That was enough to get me suspicious.
>>
I had read and seen a couple of videos that LSD and in particular psilocybin (effectively psilocin) had been reported to be effective for cluster headache and migraine treatments. Normally, by now I would at least have had a summer LSD trip, and as such may have avoided this whole cluster headache episode. But due to lockdowns cancelling festivals and poor health, I hadn't done anything this year.
And then a burning question entered my mind. Why on earth would the pharmaceutical industry in a psychedelic adverse culture choose to doubly methylate tryptamine unless they absolutely had to?
Now I don't claim any expertise, I have only the cards to play with that I have laid in front of me. And some of those cards are the same one's we here at the Nexus share. Namely a grasp of the shapes of the different tryptamines and their subjective and functional differences.
So lets play. We have the backbone tryptamine. In the body the addition of the hydroxy group at the 5 position gives us serotonin, our feel good but not so trippy molecule. If we doubly methylate tryptamine we get out familiar friend DMT. Psychedelic AF. Doubly methylating the 5-sub serotonin gives us bufotenin, which most evidence suggests gives an attenuated visual experience at best. A methoxy at the 5-sub position gives us 5-Meo-DMT which definitely has attenuated visuals.
But they still are psychedelic, and still have some visual element. Once tryptamine is doubly methylated, it seems quite hard to disable the psychedelic effect completely. Is that the only purpose of the sulfoxy (whatever, i need a name haha) group on Sumatriptan?
This 5 sulfoxy doesnt even help with getting through first pass MAO in the stomach. Most of it is rapidly destroyed just like DMT. The medicine itself admits 85% loss to first pass MAO A metabolization. A 4-sub like Psilocin would dramatically improve this efficiency, but then that would seem to improve the psychedelic potential while reducing the chances of attenuating at the 5 position.
Is sumatriptan simply frankenstein DMT with need to disable psychoactivity placed above desire to heal people with this terrible condition?
The night before I awoke that Saturday morning I saw a video by a nice german chap who was behind the development of 2-bromo LSD as safer and more effective medicine for migraines and cluster headaches. He mentioned a couple of times that he faced some funding difficulties and alluded to more that he was not willing to discuss. The clear implications was there's lots of money being made from these Triptans, and a couple of US Nexus members indicated costs of around $40 a pill.
Evidence of big pharma being a bit Mafia like? Perhaps. But this day (yesterday) I thought fuck it, the sumatriptan isnt fixing the problem, just buying a little time, and embarassingly armed with most of the alternatives, decided to try one of the alternatives. Due to its long lasting effect and
need to avoid MAO inhibitors I decided to go for LSD.
It was a good idea i think, but here's where i just got unlucky. I awoke noticing i had a bad tooth infection starting up, very much like an abcess. I never trip with mouth/tooth pain, and especially not with an abcess. So maybe i should stick to the sumatriptans today. But then if i microdose the LSD, that surely cant do any harm. If its the best medicine it might work at below psychoactive dose, a factor that was critical today.
So swallowing my pride about scoffing about microdosing, i prepared a bottle with 2 drops of 100ug LSD added to 18 drops of spiced rum using same size pipette. 10ug a drop right? So after a little consideration, and wanting to balance need to find alternate medicine with not wanting to trip with an abcess I went for a reasonable 3 drops for a 30ug dose of LSD.
It came at me like it was 200ug.
I really didn't want to trip with an abcess, and how can this be, i definitely did not get my bottles mixed up, but i started to have doubts. What if a cluster came at me while tripping hard? The set and setting couldn't have been worse, well known in advance which is also why i didn't want to trip.
Well as usual with questions relating to should i have dropped this or that, it doesn't take long before the same answer comes back in all cases..... The immortal 'Its too late now'
As it happens, the world didnt explode into visual splendour, with beautiful geometric animations of my evolving abcess pain, but there was definitely way more effect than there should have been.
I had taken no MAOIs. They are contra-indicated with sumatriptan. I had of course taken a small amount of an ergotamine derivative that was also contra-indicated but at 12 hours after my last sumatriptan dose, which is was longer between doses than i had managed before. I bought a couple of hours from waking with a small line of coke which can hold off a headache for a short while till i got the diluted LSD prepared.
So either sumatriptan has potentiated this diluted LSD or the cluster headache chemistry itself potentiates it. That is currently unknown. Things got messy at this point as the need to neutralize the tooth pain meant i had to start chucking too many drugs down neck and nose to draw any meaningful conclusions and in the end i had to go to hospital for some stiff antibiotics for the abcess.
But one thing was salvaged from the wreckage. That 'micro' (ahem) dose did indeed chase off the cluster headache for the whole day. Until I did something that i had tried unsuccessfully for two other nights during this cluster period, which was to drop a valium to get some sleep. Just as the valium was coming on, the cluster headache started to ring behind my eye. This is exactly what happened the other two times i dropped some valium to try to get to sleep before having to take that third and at-the-limit sumatriptan for the day. It seems valium undoes the good work. The pattern was clear now, wont be trying that again.
Not exactly ideal clinical conditions, but real life is what it is. There is definitely scope for LSD to and the other doubly methylated tryptamines to work, and it could be that the 5HT2a agonism could be a requirement for the full medical effect required. Sumatriptan seems to be a miracle drug, but it feels like its just missing the mark. The 5HT2a mark. The psychedelic effect.
And now, for me, this has got personal. Thank you for reading.
The nice german chap video:
https://www.youtube.com/watch?v=FNonSMghN40And the 5 sub frankenstein DMT that no-one will admit: