Trigger Warning Canadian Journal of Anesthesia Editorial Labels Carfentanil (note spelling) as a Weapon of Mass Destruction

[4DQSAR]

FYI

Carfentanil: a weapon of mass destruction - Canadian Journal of Anesthesia/Journal canadien d'anesthésie

link.springer.com

So when I pointed out that highly potent opioids could realistically see a defendant charged under anti-terrorism laws, I wasn't the first by a significant margin. Think about it from the perspective of law enforcement agencies. Yes, you might find some new highly potent opioid that isn't implicitly controlled as a drug in your nation, but they could make the reasonable case that your intention was to use it as a WMD. No matter what the format. Put it on blotters? Yeah - easy to wash back off blotters so I see that as no defence whatsoever.

I can't speak of the anti-terror laws in anywhere but the UK but anyone charged with such crimes loses a LOT of their rights as compared to someone charged with other crimes - even violent crimes. Now what your intentions will certainly be well demonstrated by a decent defence barrister, but it could take months or even years to end up in a court room and all the while, you will be sat in a Catagory-A prison and almost certainly on a wing reserved for those charged with terrorist offences.

I do not recommend anyone ever break the law but I especially recommend people don't put themselves in a position where they could be inprisoned for terrorist offences (unless they are guilty - in which case, they deserve it).

 

[ChemicallyEnhanced]

Hmmmm...personally, I consider opioids to be more of a Weapon of Mass Consumption

 

[ChemicallyEnhanced]

FYI

Carfentanil: a weapon of mass destruction - Canadian Journal of Anesthesia/Journal canadien d'anesthésie

link.springer.com

So when I pointed out that highly potent opioids could realistically see a defendant charged under anti-terrorism laws, I wasn't the first by a significant margin. Think about it from the perspective of law enforcement agencies. Yes, you might find some new highly potent opioid that isn't implicitly controlled as a drug in your nation, but they could make the reasonable case that your intention was to use it as a WMD. No matter what the format. Put it on blotters? Yeah - easy to wash back off blotters so I see that as no defence whatsoever.

I can't speak of the anti-terror laws in anywhere but the UK but anyone charged with such crimes loses a LOT of their rights as compared to someone charged with other crimes - even violent crimes. Now what your intentions will certainly be well demonstrated by a decent defence barrister, but it could take months or even years to end up in a court room and all the while, you will be sat in a Catagory-A prison and almost certainly on a wing reserved for those charged with terrorist offences.

I do not recommend anyone ever break the law but I especially recommend people don't put themselves in a position where they could be inprisoned for terrorist offences (unless they are guilty - in which case, you deserve it).

For serious, I don't get why anyone would even WANT that shit anywhere near them. NOBODY needs that, no matter how crazy-high your tolerance may be. Isn't Carfentanyl to Fentanyl what Fentanyl is to Morphine?

 

[4DQSAR]

For serious, I don't get why anyone would even WANT that shit anywhere near them. NOBODY needs that, no matter how crazy-high your tolerance may be. Isn't Carfentanyl to Fentanyl what Fentanyl is to Morphine?

It's turning up in samples of street fentanyl, apparently.

I've concluded that the market model being forced on US opioid users is to get them so tolerant and dependent on the products that substitution won't work, cold turkey likely extremely severe.

I've said it before. I've known five chemists who broke rule 1. Of that five, two are dead, one is still in prison 20 years later and two were still suffering abstainance syndrom a full year after they stopped using. I meen, they all ended up whacking up increasingly crazy doses every 20 minutes night and day. How did they THINK it was going to end?

So cut to something two orders of magnitude more potent... see where I'm going?

 

[ChemicallyEnhanced]

It's turning up in samples of street fentanyl, apparently.

I've concluded that the market model being forced on US opioid users is to get them so tolerant and dependent on the products that substitution won't work, cold turkey likely extremely severe.

I've said it before. I've known five chemists who broke rule 1. Of that five, two are dead, one is still in prison 20 years later and two were still suffering abstainance syndrom a full year after they stopped using. I meen, they all ended up whacking up increasingly crazy doses every 20 minutes night and day. How did they THINK it was going to end?

So cut to something two orders of magnitude more potent... see where I'm going?

Terrifying thought, but yeah. I've actually HEARD of that happening with high-dose fent users where methadone and bupe just DON'T WORK.
I know a guy on Fent and they had him on 200ml Methadone a day and he was STILL so sick he had to keep using fent on top of it (which was REALLY bad)

 

[4DQSAR]

Terrifying thought, but yeah. I've actually HEARD of that happening with high-dose fent users where methadone and bupe just DON'T WORK.
I know a guy on Fent and they had him on 200ml Methadone a day and he was STILL so sick he had to keep using fent on top of it (which was REALLY bad)

The acetylmethadol derivative of R-4066 is some x212 more potent than methadone and has a T1/2 of 20.8 hours (compared to 8.4 hours in methadone). So it's not like we don't know of a medication that may well substitute. But it's out of patent, complex to make (although the potency means tiny doses are sufficient) and I think most importantly, nobody seems to think it's needed. I think it is. Only time will tell.

That long duration means that it may be possible to dose patients on alternate days - so that would be a saving.

What can I say. Methadone is established and is crazy cheap. Unless and until someone patents the R-4066 derivative it on the basis of it's USAGE (opioid detoxification) which I think would be possible, we won't see it happen. But if I had the money, I would actually invest in trials. The patent holder could make a lot of money and more importantly, save a lot of lives.

Sci-Hub | Synthesis and analgesic activity of some long-acting piperidinospiro derivatives of methadone. Journal of Medicinal Chemistry, 21(5), 474–476 | 10.1021/jm00203a014

Compound 1C is the one I feel useful to medicine.

 

[ChemicallyEnhanced]

The acetylmethadol derivative of R-4066 is some x212 more potent than methadone and has a T1/2 of 20.8 hours (compared to 8.4 hours in methadone). So it's not like we don't know of a medication that may well substitute. But it's out of patent, complex to make (although the potency means tiny doses are sufficient) and I think most importantly, nobody seems to think it's needed. I think it is. Only time will tell.

That long duration means that it may be possible to dose patients on alternate days - so that would be a saving.

What can I say. Methadone is established and is crazy cheap. Unless and until someone patents the R-4066 derivative it on the basis of it's USAGE (opioid detoxification) which I think would be possible, we won't see it happen. But if I had the money, I would actually invest in trials. The patent holder could make a lot of money and more importantly, save a lot of lives.

Sci-Hub | Synthesis and analgesic activity of some long-acting piperidinospiro derivatives of methadone. Journal of Medicinal Chemistry, 21(5), 474–476 | 10.1021/jm00203a014

Compound 1C is the one I feel useful to medicine.

I think in SOME people (only some because they definitely have a higher abuse potential than Methadone) could benefit from high-dose Fentanyl patches for maintenance, simple because you get 72hrs of cover from them.

 

[4DQSAR]

A few years ago a US pharmacutical company was developing sufentanil patches. It's not a terrible option because sufentanil actually has a much bigger TI than plain vanilla fentanyl.

But the fentanyl epidemic hit the US and as far as I can tell, development was abandoned.

They were intend to be smaller and last for 7 days. But I'm sure I don't need to point out that if someone can chew up patches, such a large amount of such a potent opioid would represent a serious risk.