Bupe Bupe reverse naltrexone blockade?

[spider1165]

I've been told by a person with first hand experience that buprenorphine can reverse the opiate blockade from naltrexone. Logically it seems plausible. Bupe has a ridiculously strong affinity for opiate receptors. The naloxone in the pill is useless because it cant compete with the bupe, so naturally naltrexone would follow the same logic. But I cant find any medical data to confirm this theory. I participated in a naltrexone study 3 yrs ago and none of the Dr.'s had a clue (although they agreed it has merit). Anyone heard of this or have first hand knowledge? Yes; I know I can try it myself but thats easier said than done, and frankly I'm not trying to reverse my block. Just wondering if its possible...

 

[caseface99]

bupe has a higher binding affinity than naltrexone, but, what, are you asking if bupe will kick naltrexone out so you can do dope or something?

Because it will block the dope itself so the point is moot. Unless I am confused.

 

[amapola]

OP is asking if somebody on naltrexone, a longer lasting opioid antagonist used in treatment of opioid addiction, can still get high by taking buprenorphine. The answer is yes though I suspect there will still be some competition at the mu receptor.

Buprenorphine overdose is hard to treat due to only partial effectiveness of naloxone.

 

[spider1165]

OP is asking if somebody on naltrexone, a longer lasting opioid antagonist used in treatment of opioid addiction, can still get high by taking buprenorphine. The answer is yes though I suspect there will still be some competition at the mu receptor.

Buprenorphine overdose is hard to treat due to only partial effectiveness of naloxone.

Where did you find the info regarding binding affinity? My question is purely academic; not a veiled attempt to sneak around my nalterxone dosing (if I wanted to get high I would just stop taking it). I've looked all over I can't find any medical studies directly comparing the two drugs. As you point out there will be competition at the mu receptor. Also the half life of naltrexone makes me wonder if its possible in real-world experience...

 

[caseface99]

OP is asking if somebody on naltrexone, a longer lasting opioid antagonist used in treatment of opioid addiction, can still get high by taking buprenorphine. The answer is yes though I suspect there will still be some competition at the mu receptor.

Buprenorphine overdose is hard to treat due to only partial effectiveness of naloxone.

True, which is why it's a good thing overdosing on bupe alone is extremely difficult because of the cieling effect, in people with any sort of tolerance at least.

And OP hopefully someone with specific knowledge on the binding affinity will see this thread. I just did a search and I couldn't find anything remotely helpful.

Do doctors use a phrase other than 'binding affinity'? Because searching for "buprenorphine/naltrexone binding affinity" Literally doesn't come up with anything.

 

[Cane2theLeft]

Buprenorphine overdose is hard to treat due to only partial effectiveness of naloxone.

True, which is why it's a good thing overdosing on bupe alone is extremely difficult because of the cieling effect, in people with any sort of tolerance at least.

Dokomo has access to more resources than I do and he checked the respective binding affinities and found buprenorphine's is substantially higher. Hopefully when he's around later he'll be able to expound on this.

Regarding buprenorphine overdose, you really can't overdose on buprenorphine alone because of the ceiling effects... its not just that its hard; its essentially impossible. Really the only danger of overdose is when buprenorphine is combined with CNS depressants or other drugs.

 

[amapola]

My question is purely academic; not a veiled attempt to sneak around my nalterxone dosing (if I wanted to get high I would just stop taking it).

I didn't assume you were trying to break the blockade and honestly it's none of my business if you do

Let me see... I looked this up a while back during a discussion on if Naloxone could help with bupe overdose. I remember seeing it had twice the affinity. I'll see if I can't find an article for you.

In rats using 3h markers showing bupe displace naloxone (twice affinity) and hydromorphine.
http://www.sciencedirect.com/scienc...8d3dad16f5339697cdfc41b8bb81c10f&searchtype=a

Bupe stronger affinity than fent in humans.
http://bja.oxfordjournals.org/content/57/2/192.abstract

Naloxone limited effectiveness in bupe overdose.
http://www.journalofsubstanceabusetreatment.com/article/S0740-5472(10)00014-0/abstract

There's a ton of stuff out there. The abstracts should shed some light if you don't have access to university proxy servers :D

 

[caseface99]

Dokomo has access to more resources than I do and he checked the respective binding affinities and found buprenorphine's is substantially higher. Hopefully when he's around later he'll be able to expound on this.

Regarding buprenorphine overdose, you really can't overdose on buprenorphine alone because of the ceiling effects... its not just that its hard; its essentially impossible. Really the only danger of overdose is when buprenorphine is combined with CNS depressants or other drugs.

I thought so, i just wasn't 100% sure so i didn't wanna throw out false info. Thanks for clarifying.

I've taken upwards of 5 times my daily dose of bupe on occasion, and suffered no ill effects much less an overdose. Take 5 times your usual dose of many if not most other drugs and see if you don't OD..

I'm interested to hear what dokomo has to say as well.

 

[BlueLightBeam]

My buddy just got a naltrexone implant (them beads man!) and he asked the Doctor about suboxones, and was told that he would get sick if he tried. I didn't push it, but it sounded like bullshit.

 

[spider1165]

I didn't assume you were trying to break the blockade and honestly it's none of my business if you do

Let me see... I looked this up a while back during a discussion on if Naloxone could help with bupe overdose. I remember seeing it had twice the affinity. I'll see if I can't find an article for you.



There's a ton of stuff out there. The abstracts should shed some light if you don't have access to university proxy servers :D

Thanks a bunch...this is the kind of stuff i've been looking for. And I only mentioned the "academic" nature of mu question because of Caseface99's snide remark...I really apreciate the info its one of those questions thats been bugging me for a while. Spanks a bunch!!

 

[spider1165]

True, which is why it's a good thing overdosing on bupe alone is extremely difficult because of the cieling effect, in people with any sort of tolerance at least.

And OP hopefully someone with specific knowledge on the binding affinity will see this thread. I just did a search and I couldn't find anything remotely helpful.

Do doctors use a phrase other than 'binding affinity'? Because searching for "buprenorphine/naltrexone binding affinity" Literally doesn't come up with anything.

I was casing through the responses and didnt notice you'd actually gone outta your way to search "bupe/naltrexone bind affinity". thanks for the extra effort...i did the same thing, on this forum and others and came up with jack-shit as well. I think its info thats being kept under the table because naltexone (Vivitol by brand) has just recently been approved for treatment of opiate addicition. So i'm sure those Dr's and Pharm's dont want the fact that bupe has a higher binding affinity to get out to the general public because Vivitrol is now being hailed as the absolute "cure" for opiate addiction.

 

[amapola]

Hey spider1165,

Looking up information on pharmacy drug sites and other basic google indexed websites such as answers.com etc. is almost never going to get you any information that isn't heavily biased and based for general public informational purposes. If you want to look for something scientific like "bupe/naltrexone bind affinity" your best bet is journal articles and studies which can be better found on somethine like google scholar.

 

[spider1165]

Hey spider1165,

Looking up information on pharmacy drug sites and other basic google indexed websites such as answers.com etc. is almost never going to get you any information that isn't heavily biased and based for general public informational purposes. If you want to look for something scientific like "bupe/naltrexone bind affinity" your best bet is journal articles and studies which can be better found on somethine like google scholar.

Thanks again for the info and advice. Obviously im a noob so you're input is greatly appreciated