Bupe Buprenorphine / Subutex IV. Why no rush??

[R117329]

Can anyone explain this mystery to me? Why does it not produce a similar IV effect as Heroin, Oxy, Morphine etc? I remember a rush from Temgesic many years ago.

 

[Jekyl Anhydride]

Buprenorphine is not a full agonist and at higher doses is said to have more antagonistic properties, either way the onset of action is far longer than with more conventional full agonist opioids. While norBupe is a full agonist, it's inhibited by bupe itself. It's the combination of the two that make up Bupe's total effects. Bupe actually decreases the effects of NorBupe making up a complex pharmacological profile...that is a poor choice for a rush, and far better at being a ORT drug. Some postulate that with small amounts of Bupe, like the 200mcg in Temegesics, make for a slight change in the amount of NorBupe activity. Being opioid naive is a requiem imo.

Heroin, Oxy, Morphine, etc are full agonists with very short onset of action.

Comparison of Pharmacological Activities of Buprenorphine and Norbuprenorphine: Norbuprenorphine Is a Potent Opioid Agonist At the δ-receptor, norBUP was a potent full agonist, yet BUP had no agonist activity and antagonized actions of norBUP and DPDPE.

At μ- and κ-receptors, both norBUP and BUP were potent partial agonists, with norBUP having moderate efficacy and BUP having low efficacy.

http://jpet.aspetjournals.org/content/297/2/688

 

[kleinerkiffer]

^This
Plus the protein binding is rather high with 96% (from wikipedia)

 

[<3HairOwen]

All that above...

Also want to throw in, from experience shooting buprenorphine has no benefit besides satisfying the needle addiction, but it hardens your veins and continued use will only fuck your veins up more than necessary.

 

[RandomClean3]

Can anyone explain this mystery to me? Why does it not produce a similar IV effect as Heroin, Oxy, Morphine etc? I remember a rush from Temgesic many years ago.

Buprenorphine will be euphoric for people with little opioid experience. However, if you have used full agonists for a while, you simply won't feel the effect as a traditional opioid. Bup binds extremely tightly to the mu-opioid receptor, but the stimulation of the receptor is only 30% (100% for any full agonist like morphine, oxy, heroin, demerol, fentanyl, etc) so while for opioid naive people this still will result in opioid-like effects, for people who are tolerant, it can only have about 30% of the effects of a full agonist, so they don't feel it.

 

[Lorne???]

It also takes awhile to fully penetrate the CNS, and has a slow receptor dissaccotation and binding

It just isn't a drug to get a rush from, it is ORT for for a reason