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Opioids Effective insufflated dose of naloxone?

Zandra

Greenlighter
Joined
Aug 16, 2012
Messages
33
So, I was hoping I could find a little more information about this. I'm aware that naloxone has an incredibly low oral bioavailability, but what about with insufflation? The reason I ask is because I recently came into some 50 mg/0.5 mg pentazocine/naloxone pills (Talwin NX) which I'd like to be able to test the dissociative/psychotic effects of. This means I'm only interested in the kappa-opioid and sigma receptor activity, I really couldn't care less about its mu-opioid affinity. Until now I was thinking I would just eat them because I didn't want to risk pushing the naloxone's efficacy too high and negating the effects, but after some reading I've found that naloxone actually has a high affinity for mu- and a low affinity for kappa-opioid receptors. Honestly, my only significant concern with using these pills was respiratory depression, because even though pentazocine is limited in that sense I have no opioid tolerance whatsoever (other than an admittedly high natural tolerance) and I'm aware that the effects I'm going for will likely require a high dose, so I still need to be cautious. If it would be possible for me to insufflate these and have a much higher effective naloxone dose in me that could reverse the narcotic effects without stopping the hallucinations, that would be pretty great. Stretching out my supply would certainly be nice as well. The only thing that gets me is that I've heard that pentazocine is also much more bioavailable when insufflated, though I'm not sure of the figures and I'm not sure what the ratio of difference with routes of administration is between pentazocine and naloxone.

Can anybody help me out here?
 
Naloxone has a really short half life and is essentially only b/a through injection. It will have a slight but very mediocre effect if insufflated, rectally admin., or sublingually/buccally admin, but the half life in the blood is still going to be like 7 minutes compared to pentazocine's hour or whatever
 
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