Back in the 1990s Roxane Laboratories introduced Levacetylmethadol (ORLAAM) but due to a lack of research, they failed to notice that while dinormethadone forms a cyclic metabolite which is inactive and removed by the body quite easily. ORLAAM did not &form bisnormethadol, a metabolite that frequently caused Long-QT and quite a few people died until it was removed from the market in 2003. The plus point of the drug was that it was several times more potent than methadone and could be given orally every 48 hours. Due to typical medicinal chemistry (what is most profitable, how can we avoid being liable if anyone is harmed), an existing agent developed by Janssen in the 1970s.
The image is of the acetyl ester (the methadol) of R-4066 (Spiridone). It very potent, The (D) isomer is some x212 M in potency with a T½ Something like 3.2 days. Since the FDA is now offering naltrexone implants that last for 6 months, it would seem practical to produce an implant that releases 0.1 (21mg methadonea day) to 1mg (212mg methadone a day) of the drug constantly and equally over 24 hours. Of course a client would need to be stabilized on oral doses of RM-4066 (the acetyl methadol 4066) which may take several weeks but then it would supply a constant level of the drug into the bloodstream 24 hours a day.
While implants are not cheap, I would have thought having to visit a clinic every day for months or years would cost significantly more.
Of course, careful engineering could see the implant slowly reducing the dose released. Now this would need to be carefully trialed and it is important to have a plan in case a client finds that the implant isn't working or that the reduction of the dose isn't too swift. But since the reduction goes on all day and all night, it isn't like someone getting 40mg of juice is suddenly being told that they have to reduce suddenly. Not only is it unnecessary suffering but it would be very difficult to attempt to top the dose up.
But all told, if you found the maintenance dose that works for you, do you think that an implant would offer a much more measured reduction since the drug isn't being given once a day, it's constantly being reduced.
I've just lost another friend to H and I am seriously considering taking this further.
Oh, and for the nerds, the potency is mainly due to the piperidine is at a 90° angle to the cyclohexane (the quaternary carbon is very rigid) and thus the position of the C-ring aromatic so that benzene is in a fixed position to the tertiary amine, the 2 other benzenes and the ester.
I have never been prescribed heroin but this stuff means 1 visit every 6 months (or maybe they want to check on you more frequently) then it improves the clients life. The affinity of this drug means that it will blockade H, M, OxyC, ,OxyM & even fentanyl.Of course, if you need emergency anesthesia then K or possibly sufentanil would be needed.
Does this interest you? Is this something you would consider? What logical faults have I made. Please let me know.
Sean
The image is of the acetyl ester (the methadol) of R-4066 (Spiridone). It very potent, The (D) isomer is some x212 M in potency with a T½ Something like 3.2 days. Since the FDA is now offering naltrexone implants that last for 6 months, it would seem practical to produce an implant that releases 0.1 (21mg methadonea day) to 1mg (212mg methadone a day) of the drug constantly and equally over 24 hours. Of course a client would need to be stabilized on oral doses of RM-4066 (the acetyl methadol 4066) which may take several weeks but then it would supply a constant level of the drug into the bloodstream 24 hours a day.
While implants are not cheap, I would have thought having to visit a clinic every day for months or years would cost significantly more.
Of course, careful engineering could see the implant slowly reducing the dose released. Now this would need to be carefully trialed and it is important to have a plan in case a client finds that the implant isn't working or that the reduction of the dose isn't too swift. But since the reduction goes on all day and all night, it isn't like someone getting 40mg of juice is suddenly being told that they have to reduce suddenly. Not only is it unnecessary suffering but it would be very difficult to attempt to top the dose up.
But all told, if you found the maintenance dose that works for you, do you think that an implant would offer a much more measured reduction since the drug isn't being given once a day, it's constantly being reduced.
I've just lost another friend to H and I am seriously considering taking this further.
Oh, and for the nerds, the potency is mainly due to the piperidine is at a 90° angle to the cyclohexane (the quaternary carbon is very rigid) and thus the position of the C-ring aromatic so that benzene is in a fixed position to the tertiary amine, the 2 other benzenes and the ester.
I have never been prescribed heroin but this stuff means 1 visit every 6 months (or maybe they want to check on you more frequently) then it improves the clients life. The affinity of this drug means that it will blockade H, M, OxyC, ,OxyM & even fentanyl.Of course, if you need emergency anesthesia then K or possibly sufentanil would be needed.
Does this interest you? Is this something you would consider? What logical faults have I made. Please let me know.
Sean
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