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Cause of psychedelic effects when IVing megadoses of Ethylphenidate?

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JimRaynor

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I do not administer my drugs IV so I have never experienced any psychedelic effects from Ethylphenidate myself, but I have read countless reports from people claiming they do. The same people claims that this is something unique to ethylphenidate and megadoses of other stimulants, even methylphenidate, does not produce something even remotely similar.

You may label this as simply stimulant psychosis from overdosing, but isn't stimulant psychosis in general unpleasant and something people try to avoid? The psychedelic trip on EPH on the other hand is, in general, regarded as highly euphoric and pleasant. The effects are also more often compared to a regular psychedelic trip than stimulant psychosis/hallucinations on dopaminergics. When all the reported experiences are taken together and accounted for there seems to be something truly special about EPH. Is it possible that it has affinity for the 5-HT2A receptor in megadoses? Any other possible explanations? Maybe NMDAr antagonistic activity? Are there any other known stimulant that gives pleasant hallucinations in large doses?

From what I gather the psychedelic effects starts from 200 mg IV'ed, and gets stronger as the dose goes up. The trip seems to last 30 - 60 minutes after dosing too.
 
Need more details on these reports Jim. Very curious. If it is a source board, well, PM me. Not enough details here.
 
amanitadine said:
Need more details on these reports Jim. Very curious. If it is a source board, well, PM me. Not enough details here.
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The board I have read the reports on is in swedish so I guess that's no use for you. The effects seems pretty consistent though, in that everybody who IV 200+ mg experiences them so some testimonials about it should exist on this board too. Though very few on this board is reckless enough to IV such doses. For some reason only the somewhat responsible seem to hang out here on bluelight.
 
Maybe wierd 5-HT/NE action? Methylphenidate has affinity for 5-ht2b as an antagonist. (possibly 1abd too, maybe, I'm not sure) Perhaps ethylphenidate binds to 1a/2a/2c as agonist?

Of course the very premise of shooting a 200mg+ ball of what is essentially synthetic cocaine is a truly absurd idea if you don't want to end up on the floor having a cardiac episode or stroke. At that level the eventual comedown would be amazingly rough too.

I think if you want a psychedelic, just do a psychedelic... don't megadose stimulants...
 
That's crazy. WHo would want to take mushrooms when you can IV 200mg of what is basically ritalin?
 
200mg i'v would, i imagine, leave most people either in the hopsital, or in a state of psychosis, and i'd imagine the cardiovascular side affects would make one not want to repeat the expirence. You can call the latter a trip (stim psychosis), but its only similarity is the distortion of reality, and none of the good elements of a psychadelic, at the cost of a brutal comedown.

To be frank, i would think anyone who claimed to trip off a megadose of ethylphenidate is having a psychotic episode. I doubt it has anything in common pharmacologically with the action of psychadelics. And judging by the size of those doses, i'd wager a good # of the people reporting psychadelic action are abusing eph heavily, not getting very much sleep, and that alone will cause trippy psychosis, and thats not very fun at all either.
 
Pharmacologically speaking, ethylphenidate causing psychedelic effects is "not surprising" in that it has very high affinity for the dopamine system over the NE system. Dopamine is what causes stimulant psychosis.
 
TCMVegas said:
Pharmacologically speaking, ethylphenidate causing psychedelic effects is "not surprising" in that it has very high affinity for the dopamine system over the NE system. Dopamine is what causes stimulant psychosis.
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So are those claiming that this is something unique with EPH wrong? Are there other selective dopaminergic stims known to have this effect?
 
MDPV is well known for psychotic reactions in overdose, and has a very similar pharmacological profile...
 
TCMVegas said:
Pharmacologically speaking, ethylphenidate causing psychedelic effects is "not surprising" in that it has very high affinity for the dopamine system over the NE system. Dopamine is what causes stimulant psychosis.
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Psychadelic is usually a term saved for hallucinations caused by serotonin agonism. Dopamine overload, stimulant psychosis, or sleep deprivation psychosis, hell any other type of hallucinogen like salvia or tropane alkaoids usually aren't called psychadelic.

Personally, i think psychadelic is a term that should be specific to serotonin agonism, they cause hallucinations through that mechanisim. stimulant psychosis/sleep deprivation psychosis, or other types of hallucinations imho aren't psychadelic, at least in the classically accepted usage of the term, or that they share the same pharmacological explanation for the visual/auitory/perceptional distortions. Not to start a semantics cicle jerk or anything =D.

To summarize, psychadelic is a stretch when describing anything other than serotonin agonists, relatively speaking imho. Not that all psychadelic affects are caused by serotonin agonism/agonists, just theres a big difference between dopamine overload induced hallucinations from stimulants, and psychadelic "hallucinations" from serotonin agonism. Especially when one is not a significant releasing agent/re-up inhibitor (psychadelics), and the other is largely caused by re-up inhibition/release of dopamine (stimulants), not to say they don't have affinity for dopamine receptors, or vice/versa for serotonin (o other monoamine) release/re-up inhibition with some psychadelics.

Its definately not cut/dry, but i think theres a significant relative difference between hallucinations from dopamine agonism/release/re-uptake (or sleep deprivation when determining the cause of hallucinations from stimulants), and classical psychadelic hallucinations caused by agonism of a few select serotonin receptors.

Saying hallucinations from stimulants is psychadelic, is a bit misleading, semantically speaking imho.
 
Its either psychedelic of a psychotic episode, unless you tripped before you wont be able to tell what it is, since ritalin acts on sero its possible this one does too wich could explain psychedelic effects, altough it would be unlikely it activates 5HT2A like psychedelics, probably more like serotonin wich doesnt induce the second cellular pathways and is therefor not psychedelic.
 
I ment 1A, i know its not very strong but ethyl may be stronger, for us to gues and for the brains receptor to know

Adding a methyl group to amp makes it a mild serotonin releaser, so its possible that a close rit analogue also has alot more sero activity.

What neuro-chemical causes the hallucinations from sleep deprivation? Serotonin?
 
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(apologies for merging you guys' posts - slip of the hand)

It's not any one chemical, it's a generalised dysfunction caused by a variety of factors (substance P, histamine etcetera)

And simple extension of the methyl ester to an ethyl ester is much different than putting substsitutions on the phenyl ring. You forget that ethylphenidate has actually had receptor affinity tests done!
 
I didn't know that substance P was involved in producing hallucinations. I'll look into it, thanks.
 
It may not be - all I know is some neuropeptides are elevated with sleep deprivation. It's a complex multifaceted issue
 
I thought that it may be like 'the bends' - where nitrogen becomes toxic; maybe serotonin becomes 'hallucinogenic' under 'extreme' conditions - whatever they may be (maybe a change in metabolism?).

I could look into it though, rather than pontificate!
 
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