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N&PD Moderators: Skorpio | someguyontheinternet
Clonazepam
- Thread starter Zeketgw
- Start date
AlsoTapered
Bluelighter
Do you have access to reasonable quantities of pure clonazepam?
The minimum solubilities of clonazepam (0.00010 M) and diazepam (0.00007 M) are observed for aqueous solutions, and the maximum solubilities of clonazepam (0.055752 M) and diazepam (0.087868 M) for the solvent mixtures studied are observed in PEG 200.
If it was utterly insoluble in water, it couldn't be used in pill form. It would require your digestive tract to contain something that would dissolve it allowing it to enter the body.
The minimum solubilities of clonazepam (0.00010 M) and diazepam (0.00007 M) are observed for aqueous solutions, and the maximum solubilities of clonazepam (0.055752 M) and diazepam (0.087868 M) for the solvent mixtures studied are observed in PEG 200.
If it was utterly insoluble in water, it couldn't be used in pill form. It would require your digestive tract to contain something that would dissolve it allowing it to enter the body.
Thanks
I just re-read this and...you do know that your stomach contains hydrochloric acid not water, right? Pills are made to be dissolved in hydrochloric acid, not water. That's why you can't swallow sublingual pills / films.
AlsoTapered
Bluelighter
If you mean buprenorphine - the liver, not the stomach that's the problem.
Buprenorphine: clinical pharmacokinetics in the treatment of opioid dependence - PubMed
Buprenorphine is a semi-synthetic opioid derived from thebaine, a naturally occurring alkaloid of the opium poppy, Papaver somniferum. The pharmacology of buprenorphine is unique in that it is a partial agonist at the opioid mu receptor. Buprenorphine undergoes extensive first-pass metabolism...
pubmed.ncbi.nlm.nih.gov
I believe the exact amount varies but <10% bioavailability is often quoted. Even films seem to be quoted at 30-55% which is a heck of a range if you ask me, but then oral methadone is just as variable.
It's worth reading about the history of buprenorphine. The discoverers suggested it might be useful for 'opiate detoxification' but I read if implants that last for months and multiple people saying they have been on it for months or even years. It was only envisioned as something to help people through the acute phase...
But I guess they will make more money if they just 'park' people on buprenorphine as they do with methadone. KW Bentley would surely known better than anyone, but he died, I presume, since he was publishing books in 1954.
If you're talking Subutex, which doesn't contain naloxone then you're right. But with Suboxone swallowed, does not get absorbed into the blood stream via the stomach or intestines. This is the reason the manufacturers combined naloxone with buprenorphine. It is to prevent people from crushing the tablets and swallowing them.If you mean buprenorphine - the liver, not the stomach that's the problem.
Buprenorphine: clinical pharmacokinetics in the treatment of opioid dependence - PubMed
Buprenorphine is a semi-synthetic opioid derived from thebaine, a naturally occurring alkaloid of the opium poppy, Papaver somniferum. The pharmacology of buprenorphine is unique in that it is a partial agonist at the opioid mu receptor. Buprenorphine undergoes extensive first-pass metabolism...
I believe the exact amount varies but <10% bioavailability is often quoted. Even films seem to be quoted at 30-55% which is a heck of a range if you ask me, but then oral methadone is just as variable.
It's worth reading about the history of buprenorphine. The discoverers suggested it might be useful for 'opiate detoxification' but I read if implants that last for months and multiple people saying they have been on it for months or even years. It was only envisioned as something to help people through the acute phase...
But I guess they will make more money if they just 'park' people on buprenorphine as they do with methadone. KW Bentley would surely known better than anyone, but he died, I presume, since he was publishing books in 1954.
AlsoTapered
Bluelighter
I didn't just make a statement, I did provide reference for you to read. The specific bioavailability data I had to sort of average out because different sources give different figures.
And naloxone has <1% oral bioavailability. It's added to stop people from injecting the drug.
And naloxone has <1% oral bioavailability. It's added to stop people from injecting the drug.
You’ve correct, you did provide reverences, thanks. I did read them - very interesting. I too looked up swallowing Suboxone vs swallowing buprenorphine alone and found different i info on Suboxone (bupe+naloxone) vs bupe alone and just cut and pasted the info - didn't copy the links. I love the trustworthiness of the internet <rolling eyes>.
Thanks for the info!
S.
Oops, I forgot to include the following: I'm well aware of the point of using naloxone to avoid injecting Suboxone.
Naloxone dosage for opioid reversal: current evidence and clinical implications
Opioid-related mortality is a growing problem in the United States, and in 2015 there were over 33,000 opioid-related deaths. To combat this mortality trend, naloxone is increasingly being utilized in a pre-hospital setting by emergency personnel and ...
www.ncbi.nlm.nih.gov
The same abstract also shows that use of bupe is quite effective for pain management, even in individuals who are opioid dependant. I am one of those people and my addictionologist has me on 6mg of Sub 5X/day. I know everyone is different but for me it is completely useless. I still have extreme pain as well as trouble walking normally after sitting at work all day - even if I get up a few times a day and try to stretch or walk a little. In addition, doing things like bending over or even kneeling to clean or get something out of the fridge for instance is extremely painful. Sometimes my back will go out to the point where I'm stuck in bed for 2 days.
My point is I'm not sure how much you can trust these abstracts or info. You can also find sites where users claim they inject Suboxone with no problem with the euphoria. Sites like bluelight.org and reddit are two examples.
I stay on Suboxone for the opioid maintenance effect which is amazing but I could and probably should be on a much lower dose since my doctor said several smaller doses several times /day are used for pain management.
The internet can be an amazing source of info but it's not always so easy to know if what you're reading is true or not.
Good conversation, thanks.
S.
AlsoTapered
Bluelighter
The funniest thing is that the affinity of naloxone has a Ki of naloxone at the mu receptor is about 8. Different sources give slightly different values.
www.guidetopharmacology.org
And buprenorphine has a Ki of about 8.4
www.guidetopharmacology.org
THAT isn't a huge difference.
People have told me they injected Suboxone, felt 'a bit rough' for a few minutes and were then high (if you can call it as such) on the buprenorphine for hours.
With fentanyl on the street, we need a more potent antagonist. The N-allyl homologue of nalmefene has sub-nM affinity. But naloxone is off-patent thus CHEAP. Since carfentanil is turning up, we should be funding development of a more powerful antagonist (like the one I suggested) because an ML takes 8-14 years, usually.
naloxone | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY
The IUPHAR/BPS Guide to Pharmacology. naloxone ligand activity charts.
And buprenorphine has a Ki of about 8.4
buprenorphine | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY
The IUPHAR/BPS Guide to Pharmacology. buprenorphine ligand activity charts.
THAT isn't a huge difference.
People have told me they injected Suboxone, felt 'a bit rough' for a few minutes and were then high (if you can call it as such) on the buprenorphine for hours.
With fentanyl on the street, we need a more potent antagonist. The N-allyl homologue of nalmefene has sub-nM affinity. But naloxone is off-patent thus CHEAP. Since carfentanil is turning up, we should be funding development of a more powerful antagonist (like the one I suggested) because an ML takes 8-14 years, usually.