adder
Bluelighter
- Joined
- Mar 28, 2006
- Messages
- 2,851
The lower the dose, the worse it is, that's my experience at least and I've got a theory. Buprenorphine's effects are all about buprenorphine/norbuprenorphine levels ratios. Norbuprenorphine being a secondary amine is more hydrophilic than buprenorphine, so it will have a harder time going past the blood-brain barrier. It doesn't necessarily have a lower affinity to MOP receptors, actually some research found norbupe to have affinity almost as strong as bupe does, but norbupe concentration is always going to be higher peripherally than centrally. For the same reason it's got a lower therapeutic index than popular full agonists like morphine. Also, I've noticed that even when buprenorphine does produce some pronounced opioid effects for me, the high doesn't last so long as weaker opioid effects linger in the background and I'm free from withdrawal anyway, so I'm guessing it's norbupe that got to your brain wearing off.
For some time I had terrible problems with constipation when I was at 8mg a day, but usually there's a short period of time when it's actually much easier to pass stools. This is right after you take your dose, I guess this is because buprenorphine you've just taken is forcing out norbuprenorphine bound in your intestines. But after 15-30 minutes my muscles were contracted again. Recently I've been at 2-4mg a day and I was much more constipated at 2mg than at 4mg, so it must be all related to bupe/norbupe ratios in different parts of your body.
Buprenorphine is a weird opioid IMO and the lower the dose (with proper tolerance of course), the more effects come from norbuprenorphine and although you take a partial agonist, when you taper off, you actually feel almost like you're quitting a full agonist. I don't find it a bad thing that I can get slightly high from norbupe at lower doses of Suboxone, but honestly, purely for maintenance purposes a true partial agonist would be much better than buprenorphine when it comes to quitting. With the long half-life of buprenorphine it's hard to get high from it every day unless you're on a very low dose, 2mg or less, I guess.
For some time I had terrible problems with constipation when I was at 8mg a day, but usually there's a short period of time when it's actually much easier to pass stools. This is right after you take your dose, I guess this is because buprenorphine you've just taken is forcing out norbuprenorphine bound in your intestines. But after 15-30 minutes my muscles were contracted again. Recently I've been at 2-4mg a day and I was much more constipated at 2mg than at 4mg, so it must be all related to bupe/norbupe ratios in different parts of your body.
Buprenorphine is a weird opioid IMO and the lower the dose (with proper tolerance of course), the more effects come from norbuprenorphine and although you take a partial agonist, when you taper off, you actually feel almost like you're quitting a full agonist. I don't find it a bad thing that I can get slightly high from norbupe at lower doses of Suboxone, but honestly, purely for maintenance purposes a true partial agonist would be much better than buprenorphine when it comes to quitting. With the long half-life of buprenorphine it's hard to get high from it every day unless you're on a very low dose, 2mg or less, I guess.
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