Bupe Buprenorphine Rush IV

[Megalum]

I've been searching to find an answer to this. I wish to know the pharmacology behind why it does not provide a rush. Any information is appreciated. I'm a bio-molecular chemistry major, so please be as detailed a possible. Other answers are welcome like theories and anecdotes etc. I just need to clear this up, its been bothering me. Thank you to all responses.

 

[Animoe]

you know I don't really know exactly why either.. I mean, I know why it would give no rush if you were dependent on opiates or already have buprenorphine in your system.. But if there's no buprenorphine/opiates/opioids/etc. in your system, and you're completely clean, why does it get you high, but not have a rush?
is it due to maybe too slow of an onset even when administered via IV?

 

[Mr.Scagnattie]

It's only a partial agonist and doesn't release the same amount of dopamine as a full agonist like heroin, and what it does release, it crosses the blood brain barrier very slowly. That's why it works for maintenance. It has the ability to fill your receptors, thus preventing withdrawal, but it being only a partial agonist, it can not simulate those receptors as much as full opiates.

 

[Psychedelic Jay]

Accept the drug for what it is, not what you want it to be.

 

[sekio]

the partial agonism of bupe only explains why it has a less intense effect for most opioid users.

a big part of the drugs percieved effects is influenced by how lipophilic (fat soluble) it is. generally, the less lipophilic a compound is, the faster it hits. and the more lipophilic, the slower and more prolonged the effects. (excluding the effects of metabolism)

logD7.4 (fat solubility at physiological pH) correlates well with reported "rushiness" of opioids. buprenorphine is really lipophilic when compared to drugs lime morphine or oxycodone, so it takes a long time to reach peak brain concentrations.

the rushiness/abusability/onset time of most other drugs (benzos, stimulants, psychedelics) also correlates with logD like this pretty well.

 

[Megalum]

Incredible chart Sekio, that really puts it into perspective. Also PJ, I do love and accept buprenorphine for the wonderful tool it is, as I have been tapering with it for quite sometime-- I am going for the usage style CaptainHeroin employs. Your sentiment is very true, though.

Also, i thought it had to do with the level of agonist activation, but I figured that was only part of the reason, speed of BBB crossing hadn't crossed my mind.

I also didn't look this up, so I'm sure it's common knowledge, but wouldn't VoD have an effect on the "rush" as well (I.e methadone)? Or is that in correspondence with the lipophilicity. Thanks for the quick answers! Iappreciste it.

 

[Toz]

Fentanyl at 2.61 makes no sense, it definitely has a heavy rush and a fast onset of effects...

 

[Psychedelic Jay]

Fentanyl at 2.61 makes no sense, it definitely has a heavy rush and a fast onset of effects...

Yes it does.

The sheer potency of fentanyl makes up for it's fat solubility. The fat solubility is the only reason why it last as long as it does even as short the duration of it is...

Metabolism also plays a major role as well.

The more potent ones metabolize faster.

But strangely, Half-Life has has very little to do with activity in a lot of cases.

Edit: Due to active metabolites.

 

[Tryptamite]

I thought bupe did produce a light semi-rush? Although nothing compared to H I imagine it could be nice for a non tolerant individual?

 

[sekio]

I thought bupe did produce a light semi-rush? Although nothing compared to H I imagine it could be nice for a non tolerant individual?

Essentially all opioids when injected will produce some sort of "rush", just due to the nature of a rapid rise in opioid receptor activation. I'm sure even IV pethidine is quite nice if you're not a regular opiophile. But I've never heard someone say that shooting methadone is a "better rush" than morphine, even if it is way more potent!

I also didn't look this up, so I'm sure it's common knowledge, but wouldn't VoD have an effect on the "rush" as well (I.e methadone)? Or is that in correspondence with the lipophilicity.

It corresponds to the lipophilicity, generally.

 

[Survival0200]

Dihydromorphine and O-Desmethyl-Tramadol have negative (-) LogD pH7.4 - what does that mean?

 

[Psychedelic Jay]

Dihydromorphine and O-Desmethyl-Tramadol have negative (-) LogD pH7.4 - what does that mean?

They are more hydrophilic compounds

 

[StartedHydro]

I haven't touched an opiate in 11 days, other than lopermide. I caved in and went to the sub doc, and when I got home I prepped up a shot of 3 mg of bupe. I felt nothing. It took a solid 15-25 mins after IVed after almost two weeks off opiates to feel some sort of relief from bupe. I was even hoping for some mild energy, brightened mood, anything.... But nothing. It was as if I had been doing bupe then entire time the last two weeks.

Still, it took a solid 15 mins after IVed to start to sense WDs easing.

 

[joeburden]

I haven't touched an opiate in 11 days, other than lopermide. I caved in and went to the sub doc, and when I got home I prepped up a shot of 3 mg of bupe. I felt nothing. It took a solid 15-25 mins after IVed after almost two weeks off opiates to feel some sort of relief from bupe. I was even hoping for some mild energy, brightened mood, anything.... But nothing. It was as if I had been doing bupe then entire time the last two weeks.

Still, it took a solid 15 mins after IVed to start to sense WDs easing.

usually takes about 5 for me. you sure you didnt miss the shot?

 

[Megalum]

Ya it's about 5 for me as well, it does seem like witt that low tolly youd feel it sooner. Off topic..and this could be placebo but the white half moon activist generics really do seen to work better than strips. I have both and been waiting extra time between doses, and the whites last longer and tend to be more euphoric. After 1 year on sub, I actually nodded. I take Xanax too, but just the same dose i take with bupe everyday..