resorcinol
05-29-2008, 02:44 PM
Well - there is oxycodone, which is moderately strong. However, it's weaker than even morphine when the two are compared administered intraveinously, and morphine isn't all that strong when compared to the range of opioids we have now. Many many opioids are far stronger than morphine is..
Thinking about opioids... I've noticed, in general, they're not the greatest drugs to take orally for anyone with a serious tolerance, with the exception of oxycodone. But even with OC, the doses can get MASSIVE when somebody starts to experiment with stronger opiates via IV, just to get a light buzz, because on the whole oxycodone isn't a very strong opioid.
Of the opioids that are reasonably avaliable, we can say the following:
1. Excellent oral bioavaliability: codeine, dihydrocodeine, hydrocodone, oxycodone, methadone
2. Moderate to poor oral bioavaliability: morphine, hydromorphone, oxymorphone, levorphanol, heroin, fentanyl and it's analogs
What one can quickly notice is that all of the heavyweight opiates that will get someone with a sizeable tolerance off are in the group with poor oral bioavaliability, with the modest exception of oxycodone. This is part of the reason that so many opiate lovers compared to other drug users are self coerced into gravitating towards the needle. Sure, the opiates in group two can give a STRONG buzz orally but you have to take so much more than IV, IM, SC, or plug, that you're left with the feeling that you tragically wasted drugs, and anecdotal evidence suggests that the buzz from even a great opioid is lackluster if taken orally if it's oral bio-a is low, even if you take enough according to charts, when compared to an opioid like oxycodone which is rapidly and completely absorbed orally, and gives a great euphoric buzz orally almost as good as if it was insuffulated or banged. This might be because drugs with poor oral bioavaliability aren't just poorly absorbed, but also erratically absorbed to a varying extent, not allowing that highly euphoric spike in brain levels to occur in one big whoosh.
You'll notice methadone is on the good oral bioavaliability list and is pretty strong. However, methadone is just not really well suited for daily abuse, because it accumulates and clogs the u receptors, essentially blocking it's own euphoric spike. For a chipper it's a darn good choice, but not for most of us here.
So I looked at oxycodone and thought. Oxycodone is the one common opioid that is strong enough to get off a tolerant person and can be taken orally without waste and with a nice buzz by a tolerant person. But it's not without lacking. Taken by IV, it has a weaker rush than other IVable opies, and a VERY tolerant person will need massive, expensive doses to get off, because it's just not THAT strong, and street prices are so marked up.
Clearly, a methyether at position 3 GREATLY improves oral bioavaliability, but sadly, it also weakens the drugs potency. The solution I see?.... keep the 3-methylether and modify the molecule at another spot that can enhance potency to compensate.
Since oxycodone is the most potent of the codone bunch, we start with that. Clearly, a hydroxy substitution at carbon 14 position quite nicely enhances potency... a hydroxy group there is the only difference oxycodone has when compared to hydrocodone.
If we look at oxymorphone research, we find out that esterification of that 14 -OH group greatly increases u receptor affinity and potency. This would work for oxycodone too. cinnamic acid is a great choice as it seems to boost the potency the most of the acids that were studied on oxymorphone.
So the oxycodone ester, 14-cinnamyloxycodone, is the drug I'm looking at (or rather, dreaming of). I predict that 14-cinnamyloxycodone will have a nice solid rush when IVed, have a speedy edge like it's parent drug oxycodone, have a decent duration of action, and have a GREAT ORAL BIOAVALIABILITY allowing doses the same as ones for IV administration to get one off minus the rush. No waste with oral use!
This, my opiophile friends would be a versatile opioid, and this is the one I want to see made, tested, and marketed next (yeah, in my dreams, considering the abuse [aka fun] potential would be TREMENDOUS because of exactly the properties I just described). It would be an amazing, just amazing painkiller for oral use though - I'm sure the CP patient community would root for it.
What do you guys think of 14-cinnamyloxycodone. It'd likely be made as the hydrochloride salt. Hmm, I'd give the pharmaceutical preparation this name:
CincoContin
cinoxycodone HCl
:D:cool:
Thinking about opioids... I've noticed, in general, they're not the greatest drugs to take orally for anyone with a serious tolerance, with the exception of oxycodone. But even with OC, the doses can get MASSIVE when somebody starts to experiment with stronger opiates via IV, just to get a light buzz, because on the whole oxycodone isn't a very strong opioid.
Of the opioids that are reasonably avaliable, we can say the following:
1. Excellent oral bioavaliability: codeine, dihydrocodeine, hydrocodone, oxycodone, methadone
2. Moderate to poor oral bioavaliability: morphine, hydromorphone, oxymorphone, levorphanol, heroin, fentanyl and it's analogs
What one can quickly notice is that all of the heavyweight opiates that will get someone with a sizeable tolerance off are in the group with poor oral bioavaliability, with the modest exception of oxycodone. This is part of the reason that so many opiate lovers compared to other drug users are self coerced into gravitating towards the needle. Sure, the opiates in group two can give a STRONG buzz orally but you have to take so much more than IV, IM, SC, or plug, that you're left with the feeling that you tragically wasted drugs, and anecdotal evidence suggests that the buzz from even a great opioid is lackluster if taken orally if it's oral bio-a is low, even if you take enough according to charts, when compared to an opioid like oxycodone which is rapidly and completely absorbed orally, and gives a great euphoric buzz orally almost as good as if it was insuffulated or banged. This might be because drugs with poor oral bioavaliability aren't just poorly absorbed, but also erratically absorbed to a varying extent, not allowing that highly euphoric spike in brain levels to occur in one big whoosh.
You'll notice methadone is on the good oral bioavaliability list and is pretty strong. However, methadone is just not really well suited for daily abuse, because it accumulates and clogs the u receptors, essentially blocking it's own euphoric spike. For a chipper it's a darn good choice, but not for most of us here.
So I looked at oxycodone and thought. Oxycodone is the one common opioid that is strong enough to get off a tolerant person and can be taken orally without waste and with a nice buzz by a tolerant person. But it's not without lacking. Taken by IV, it has a weaker rush than other IVable opies, and a VERY tolerant person will need massive, expensive doses to get off, because it's just not THAT strong, and street prices are so marked up.
Clearly, a methyether at position 3 GREATLY improves oral bioavaliability, but sadly, it also weakens the drugs potency. The solution I see?.... keep the 3-methylether and modify the molecule at another spot that can enhance potency to compensate.
Since oxycodone is the most potent of the codone bunch, we start with that. Clearly, a hydroxy substitution at carbon 14 position quite nicely enhances potency... a hydroxy group there is the only difference oxycodone has when compared to hydrocodone.
If we look at oxymorphone research, we find out that esterification of that 14 -OH group greatly increases u receptor affinity and potency. This would work for oxycodone too. cinnamic acid is a great choice as it seems to boost the potency the most of the acids that were studied on oxymorphone.
So the oxycodone ester, 14-cinnamyloxycodone, is the drug I'm looking at (or rather, dreaming of). I predict that 14-cinnamyloxycodone will have a nice solid rush when IVed, have a speedy edge like it's parent drug oxycodone, have a decent duration of action, and have a GREAT ORAL BIOAVALIABILITY allowing doses the same as ones for IV administration to get one off minus the rush. No waste with oral use!
This, my opiophile friends would be a versatile opioid, and this is the one I want to see made, tested, and marketed next (yeah, in my dreams, considering the abuse [aka fun] potential would be TREMENDOUS because of exactly the properties I just described). It would be an amazing, just amazing painkiller for oral use though - I'm sure the CP patient community would root for it.
What do you guys think of 14-cinnamyloxycodone. It'd likely be made as the hydrochloride salt. Hmm, I'd give the pharmaceutical preparation this name:
CincoContin
cinoxycodone HCl
:D:cool: