O-acetyl Loperamide

[MaxiTot13]

I read quite a bit about Loperamide the last few days. A few things first. Loperamide crosses the BBB at very high doses. The dose varies per person, meaning a dose that does nothing for one kills another. It is very dangerous in opiate naive folk, and it is very dangerous with long time use. The drugs is useful on its own for withdrawal. It does cause mild euphoria, according to numerous users, and analgesia equivalent to codeine.

Apparently, there has been some talk on this forum of converting Loperamide into O-acetyl Loperamide since it has an active OH group, a prerequisite for acetylation. The thought was this could allow the drug to cross the blood brain barrier more effectively. There have been some preparations of the drug for scientific testing, though nothing in humans and only as a comparison drug.

Someone on these forums said they reacted Loperamide with glacial acetic acid and shot up 17 mg. Had they actually created O-acetyl Loperamide and done that, they'd be dead.

Based on my experience with the chemical in laboratories, contact to skin causes numbness and tingling for about five minutes then general analgesia for up to six hours with a similar effect to 20 mg oral Norco. This is as little as you'd get on your arm from a small spill, probably 1/8-1/4 of a teaspoon.

Do not try to make this, and if you do, go incredibly slow. If you don't feel anything, don't assume it's just Loperamide and down it, assume you have high tolerance and act cautiously, if you want to even experiment with this.

My best advice is do not try at all, but I know that won't happen. It's incredibly potent and dangerous.

 

[Ligaturd]

This honestly sounds like a junkies wet dream. People are going to start looking up how to acetylate opioids and trying this. Usually how it works.

 

[Bagseed]

I believe that acetic acid won't be sufficient to get the desired product.

 

[Slow_Mobius]

I believe that acetic acid won't be sufficient to get the desired product.

I think you would need an acyl halide... not recommended

 

[Bagseed]

yeah, or acetic anhydride, but since this is close enough to synth discussion, I didn't want to get more specific

 

[szuko000]

Part of me is thinking this should be closed because it appears to be more of a synthesis discussion however, as there are a few tricks like this perhaps its best the community learn about their existence now. It can remain open provided its a discussion of these analogs and not how to create them... I'll leave it open to see where it goes but no more synthesis discussion or it will have to be closed.

 

[Slow_Mobius]

To clarify, o-acetyl is refering to an ester instead of a hydroxyl? I'm not too familiar with this kind of nomenclature.