Why doesn't buprenorphine not block tapentadol?

[CrushTram]

I have tried to research this but never found any clarification as to why suboxone does not block tapentadol. Has anyone else had this occur?

Buprenorphine is deservedly a God send for everyone. But it can't dull the triggers to at least attempt a previous poison. But Buprenorphine once again is the literal wonder drug with a trigger because it blocks the effects making the alternative to be pointless.

So with that said I have tried oxy and tramadol whilst under the subcolade (100mg) program. But those abusive drugs I can't really feel, which is pointless to bother with.

But this Tapentadol irregularity is intriguing. The mechanism is too similar to tramadol yet tap with bupe is at the full blissful high. So does this happen to others? Does anyone know what it's pharmacologic action that explains it?

 

[Jen X]

I didn't find oral bupe to block much. probably the dose i was on , 4mg. When i switched from bupe to morphine 20 hours after taking bupe 160mg of morphine got me high. I got awful anxiety from bupe.
Sorry, can't answer your question, just rambling

 

[AlsoTapered]

I didn't find oral bupe to block much. probably the dose i was on , 4mg. When i switched from bupe to morphine 20 hours after taking bupe 160mg of morphine got me high. I got awful anxiety from bupe.
Sorry, can't answer your question, just rambling

Bupe caused anxiety at 4mg and the HR agency was adamant that I go up to 16mg when 2mg [BID] worked perfectly. Actually, my counselor quietly said 'just do what works' so even she recognized that 16mg of buprenorphine was inappropriate for someone who was just taking codeine for pain.

As for tapentadol, it's actual mechanism of action is primarily NOT mediated by the opiate receptors. But what opiate activity in possesses is as a partial agonist - just like buprenorphine. That's why.

 

[Smuck_Hey_Dee_Hewitt]

Bupe caused anxiety at 4mg and the HR agency was adamant that I go up to 16mg when 2mg [BID] worked perfectly. Actually, my counselor quietly said 'just do what works' so even she recognized that 16mg of buprenorphine was inappropriate for someone who was just taking codeine for pain.

As for tapentadol, it's actual mechanism of action is primarily NOT mediated by the opiate receptors. But what opiate activity in possesses is as a partial agonist - just like buprenorphine. That's why.

That is interesting, very interesting actually. I´m the type of person who, without a tolerance to Tramadol (which grows ridiculously fast for me ) ,takes 2mgs Bupre + 1 single 50mgs capsule and I feel like I´m on some other drug other than the sum of both drugs (potentiation I suppose ). Had never heard of Tapentadol before ...so is it a cumulative effect to that of Bupre ,or does it also synergise as I described above with Tramadol ?

 

[Tryptamite]

Never got much from tramadol or tapentadol but felt them to be both similar in MOA. Suppose opioid tolerance was always too high to feel any of that side of it.

 

[Smuck_Hey_Dee_Hewitt]

Never got much from tramadol or tapentadol but felt them to be both similar in MOA. Suppose opioid tolerance was always too high to feel any of that side of it.

Same here ...I actually never got anything off of Tramadol alone (and I used to take them sporadically at a time when there were still no Methadone/buprenorphine substitution programs for Heroin -Tramadol was the most prescribed pain pill for that in the 80s/early 90s. Haven´t got a clue what Tramadol does on its own basically. Reading people put on Buprenorphine for Tramadol withdrawals is bordering Malpractice imho. )
What is curious is how ridiculously high I get when (this is without a Tramadol tolerance which skyrockets in the space of a couple of days here ) I combine relative low dose bupre (0.5- 4mgs tops ) + (even ) the 1 x 50 mgs instant release on the 1st day.
I (like many )´ve always made a huge distinction between accumulation of effects from various substances and potentiation -the aforementioned combo is one of the few mixes where I feel a pretty pronounced effect which is very dissimilar from the two substances alone. Of course , by day 4 -5 I already need to enter 200 -400mgs Tram territory to feel anything ...it´s odd how fast tolerance grows with this combo.
Was just wondering if Tapentadol + Bupre works in a similar way as it does with Tramadol, and if so ,how does tolerance work ?

Apologise for going somewhat offtopic but I´m basically looking for sth to combine with Buprenorpine which makes the taper easier whilst still maintaining mood stability.

 

[Tryptamite]

I tapentadol and tramadol work in similar SNRI shady lanes and bupe is probably standing down that lane as well, acting shifty.

 

[Smuck_Hey_Dee_Hewitt]

I tapentadol and tramadol work in similar SNRI shady lanes and bupe is probably standing down that lane as well, acting shifty.

Cheers mat!e ...nothing can be worse than what I´m doing during the day ...alcohol and rock to feel alive during the day is unsustainable ...Bupre and a benzo alone no longer satisfy ...I´m just going to get some Tapentadol from one of my kind psychiatrists and take it with Bupre ...it might prevent me from these binges ...might not ...at the time , couldn´t care less one way or another to be quite honest ...alcoholism and crack is such a defeat after all the work I´ve put into this ...cheers ! I know Burial´s "Antidawn " Ep distract me from crack cravings ...some should try it ...good med ...

 

[Skorpio]

Burial´s "Antidawn

A man of taste I see. You may like Andy Stott and Actress. Both have similarities to Burial in that they do headphones oriented re-imaginations of UK club genres (kind of a post-punk tinged techno by Andy stott, and crystalline lo-fi house by Actress). Hope that can keep your mind occupied next time you need distraction.

For the people talking about tramadol and buprenorphine being a good combo, have any of you taken a single dose of effexor on burpenorphine? That would be a good way to confirm/rule out the SNRI hypothesis that seems popular in this thread.

Alternatively it could be a G-protein bias type deal where buprenorphine and tramadol differ in the G/beta arrestin ratio of an activated mu opioid receptor.

Or it could be a totally different mechanism. Even with something as thouroughly studied as opioid pharmacology, we could be missing some key facet in how these drugs work, that once revealed will illuminate these spots where simply knowing the binding affinity and efficacy values of these compounds fails to provide an adequate explanation.

 

[Tryptamite]

I think the venlafaxine and bupe route would be a good one to go down if bupe and tramadol are working.
Because the relief or effect so to speak surely aren't coming from mu agonism are they??

Effexor is maybe not addictive or habit forming but certainly it can form a physical dependence, just for people to be aware of this and other SSRI/SNRIs

 

[mygreenbic]

tapentadol has mu opioid agonism along with ne reuptake inhibition. tramadol has weak and partial agonism to my opioid receptors and inhibits reuptake of both Seratonin and NE making it less effective, less euphoric and less compatible with most other psych drugs. These are two completely different profiles. tapentadol has strong mu opioid agonism. 200mg ir tapentadol is compared to huge amounts (70mg ir) of oxymorphone when asked to ai ... so I'm about to grab 200mg tapaday from my mail box and hopefully i can feel them over my 120mg daily methadone

 

[meeer]

Bupe caused anxiety at 4mg and the HR agency was adamant that I go up to 16mg when 2mg [BID] worked perfectly. Actually, my counselor quietly said 'just do what works' so even she recognized that 16mg of buprenorphine was inappropriate for someone who was just taking codeine for pain.

As for tapentadol, it's actual mechanism of action is primarily NOT mediated by the opiate receptors. But what opiate activity in possesses is as a partial agonist - just like buprenorphine. That's why.

... 16mg Bupe to someone who was using codeine for pain is wildly fucking irresponsible. I'm glad you and your counsellor saw through that.

Ik this is a late ass response

 

[meeer]

tapentadol has mu opioid agonism along with ne reuptake inhibition. tramadol has weak and partial agonism to my opioid receptors and inhibits reuptake of both Seratonin and NE making it less effective, less euphoric and less compatible with most other psych drugs. These are two completely different profiles. tapentadol has strong mu opioid agonism. 200mg ir tapentadol is compared to huge amounts (70mg ir) of oxymorphone when asked to ai ... so I'm about to grab 200mg tapaday from my mail box and hopefully i can feel them over my 120mg daily methadone

I'm sorry but if you mean AI as in artificial intelligence, please never EVER use that for medical advice or dosing, it is a sure way to a real bad situation real quick, or at the very least a total waste and underdosage.

I have extensive knowledge on these medication types and very specifically Tapentadol as one few staples over the last 5 years. I can promise you now that a 200mg Tapentadol slow release will be a potent opioid no doubt, I once took 4-600 at a time when out of oxy and it was still fresh to me, it was certainly potent and enjoyable when not in withdrawal or anything of the sort especially at such dosages. However taken IR the bio availability drops dramatically, like down to 30 something% if i remember correctly, due to first-pass phenomenon, and that isn't locked down to just IR formulations it just seems less likely ime. Now furthermore, Tapentadol 200mg is equivalent to roughly to 80mg MME (Morphine Milligram Equivalent) as significant as it is, that is certainly less than 70mg of oxymorphone.

70mg of Oxymorphone is 210MME or 210mg of morphine. To finish up Tapentadol here in Australia is assigned depending on state with a strength of .3-.4 the strength of morphine.


If I got anything wrong someone do please correct me.

 

[ChemicallyEnhanced]

Sorry, I can't help, but I have a similar question.
In an episode of A&E's Intervention, in one episode this woman who is addicted to prescription meds (including some unusual ones that I would NOT call recreational, like Seroquel and Trazodone*), including taking both Suboxone and Opana (Oxymorphone) and she definitely got high.
So, are there certain opioids that are NOT blocked by it?


*I HATE the feeling of Trazodone, and it gives me horrible dreams

 

[ChemicallyEnhanced]

Never got much from tramadol or tapentadol but felt them to be both similar in MOA. Suppose opioid tolerance was always too high to feel any of that side of it.

Feel free to not answer if it's too personal, but are/were you on an anti-depressant at the time? I'm on a high-dose SSRI and even with no opioid tolerance (like 7 months of ZERO opioid use once) I never got anything whatsoever out of Tramadol. I think BECAUSE they're also an SNRI, that the reason some people LOVE them is because they're getting both a mild opioid affect AND an anti-depressant affect. So I think whether people enjoy them lies partially in their opioid tolerance and mostly whether they are on any type of SSRI/SNRI or MAOI.

 

[ChemicallyEnhanced]

Cheers mat!e ...nothing can be worse than what I´m doing during the day ...alcohol and rock to feel alive during the day is unsustainable ...Bupre and a benzo alone no longer satisfy ...I´m just going to get some Tapentadol from one of my kind psychiatrists and take it with Bupre ...it might prevent me from these binges ...might not ...at the time , couldn´t care less one way or another to be quite honest ...alcoholism and crack is such a defeat after all the work I´ve put into this ...cheers ! I know Burial´s "Antidawn " Ep distract me from crack cravings ...some should try it ...good med ...

Psych's can prescribe pain meds?

 

[meeer]

Feel free to not answer if it's too personal, but are/were you on an anti-depressant at the time? I'm on a high-dose SSRI and even with no opioid tolerance (like 7 months of ZERO opioid use once) I never got anything whatsoever out of Tramadol. I think BECAUSE they're also an SNRI, that the reason some people LOVE them is because they're getting both a mild opioid affect AND an anti-depressant affect. So I think whether people enjoy them lies partially in their opioid tolerance and mostly whether they are on any type of SSRI/SNRI or MAOI.

First of all mixing SSRI's with things such as tramadol is not the safest move and I can only suggest against it, due to tramadol especially having SNRI effects could lead to serotonin syndrome and this is absolutely no fun. You do not want this! Overall please try to avoid this. A more classical opioid would be far safer, in combination.

Secondly please keep in mind a good 15% of the population on average cant digest codeine and tramadol correctly due to a few issues but namely non functioning alleles or poor CYP 2D6 metabolisers, specifically with the tramadol and codeine.

 

[ChemicallyEnhanced]

First of all mixing SSRI's with things such as tramadol is not the safest move and I can only suggest against it, due to tramadol especially having SNRI effects could lead to serotonin syndrome and this is absolutely no fun. You do not want this! Overall please try to avoid this. A more classical opioid would be far safer, in combination.

Secondly please keep in mind a good 15% of the population on average cant digest codeine and tramadol correctly due to a few issues but namely non functioning alleles or poor CYP 2D6 metabolisers, specifically with the tramadol and codeine.

My doctor had me on an SSRI, Tramadol AND Trazodone at the same time once.
I take Codeine and Morphine for pain now (and Gabapentin). I metabolize Codeine fine, but maybe I'm in the % that can't metabolize Tramadol. I HAVE tested negative for opioids in drugs tests while taking Tramadol every day (it was legit prescribed and the place doing the drug testing knew I was on it).

 

[Smuck_Hey_Dee_Hewitt]

Psych's can prescribe pain meds?

Definitely (at least in most European countries ) ...:"Psychiatrists " for the scripts and "Psychologists " for verbal gymnastics and such. I thought it was like that everywhere.

 

[smokeymcpot42088]

... 16mg Bupe to someone who was using codeine for pain is wildly fucking irresponsible. I'm glad you and your counsellor saw through that.

Ik this is a late ass respo

^Yea chiatric = pez despenser cologist = belongs in a classroom. Yes Im a dick. (My father had a PhD in psychology i can make that joke. i.e I sware I have a black friend) Ooh dont get ancy.

16 seems like THE dose in US. That is what they sstarted me and everyone I know got started on. Including a kid that just did coke. Idk how sub is suppose to help him but hey hey heyy welcome to amerrika. That said id rather start at 16mg than idk 1mg; and realistically the latter is closer to what is necessary; but too much is better than not enough as long as you have control over your own input (if that made sense).