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Bupe Is it possible?

J

Jktm

Bluelighter
Joined
May 19, 2012
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I know that narcan (naloxone) doesn't fully block the effects of buprenorphine, but it does to some extent, but my question is, if one were to IV a large enough dose of buprenorphine (from suboxone pills with a 4:1 ratio bupe:narcan), would it actually be possible for one to overdose?

I know that naloxone wears off fast, but would it keep someone from fatally overdosing?
 
There was an example where someone took a bunch of 8mg tablets sublingually. What happened is they went into withdrawal because the buprenorphine antagonized the receptors at that high of a dosage.

Naloxone doesn't block buprenorphine's effects at all because buprenorphine has a higher affinity for the mu opioid receptor.
 
So really, if someone were to IV enough buprenorphine, regardless of present naloxone, it could result in a fatal overdose?

edit: Why is it though, that naloxone, administered to patients overdosing on fentanyl, is effective? fentanyl has a much stronger affinity than buprenorphine...
 
Jktm said:
So really, if someone were to IV enough buprenorphine, regardless of present naloxone, it could result in a fatal overdose?

edit: Why is it though, that naloxone, administered to patients overdosing on fentanyl, is effective? fentanyl has a much stronger affinity than buprenorphine...
Click to expand...

No, it doesn't. Buprenorphine has a higher affinity than fentanyl; because you can go into precipitated withdrawal taking Suboxone after fentanyl.

Fentanyl is more potent, but that doesn't mean it has a greater affinity for the receptor.

You could overdose on IV buprenorphine, especially if you have certain health problems or combine it with a lot of benzos/CNS depressants. For the average healthy adult such as myself, IV buprenorphine with or without naloxone, in itself, is not going to cause a fatal overdose.
 
Is this because it's only a partial agonist? I just fail to see how when something as potent as buprenorphine is administered IV especially in higher doses than one would normally take, it couldn't cause a fatal overdose.

It's still an opioid, albeit, a partial agonist, but it has the full agonist metabolite norbuprenorphine (which I realize is more prominent in lower doses of buprenorphine).
 
I'm pretty sure it's due to the partial agonist activity as well as its ability to become an antagonist at a high enough dosage. There was an example in the case studies thread about this... let me see if I can pull it up.... for some reason I'm not finding it.

At an overdose type dosage, the full agonist metabolite won't have any receptors to effect.
 
You cannot overdose on buprenorphine alone because of the ceiling effect. Naloxone has nothing to do with it. Add another CNS depressant and then it's possible.
 
It would be possible for a child or maybe an extremely opiate naive person to od...but i sincerely doubt its PLAUSIBILITY. The average healthy adult... no way. Ive seen a case study on this... I really doubt it.
 
^this.

It's possible for an extremely sensitive person to overdose on suboxone or subutex but it's unlikely for that to be fatal. There have been cases of small children accidentally ingesting suboxone and they pretty much just required monitoring in the hospital for 24 hours.

Buprenorphine being a mixed agonist-antagonit (or often, partially-correctly cited as a partial-agonist) means that the increase in agonist effects is linear up to a point and then they top off and no matter how much you take beyond that, you won't get stronger agonism. This ceiling effect to the agonism is equivalent to about 30mg of oral methadone which, while being far too high of a dose for the opioid-naive, rarely will produce a fatal overdose. There will certainly be respiratory depression, likely vomiting, profound sedation and other side effects but it's not likely to be substantially dangerous.

Really the only time buprenorphine is implicated in fatal overdoses is when it is combined with other CNS depressants such as benzodiazepines, alcohol, etc.
 
Here's one example of a *2 year old* ingesting an 8mg suboxone -

Suboxone (buprenorphine/naloxone) toxicity in pediatric patients: a case report.
Schwarz KA, Cantrell FL, Vohra RB, Clark RF.

Source
California Poison Control System, San Diego Division, University of California, San Diego Medical Center, San Diego, CA 92103, USA. [email protected]

Abstract
BACKGROUND:
Suboxone, a combination of buprenorphine and naloxone in sublingual tablet form, was recently approved in the United States for management of opioid dependence. Little information exists regarding the potential for opioid toxicity after Suboxone exposure in the pediatric population. We report a case of opioid toxicity after exposure to Suboxone in a pediatric patient and a review of other cases of pediatric Suboxone ingestion in the literature.

CASE:
A previously healthy 2-year-old boy was found with 1 tablet of Suboxone (8 mg buprenorphine/2 mg naloxone) in his mouth. Remnants of the partly dissolved tablet were immediately removed from the child's oropharynx. The child experienced 1 episode of spontaneous emesis and became drowsy en route to the emergency department 30 minutes after the exposure. The patient was observed in the emergency department; no interventions were necessary, and the child was discharged asymptomatic and stable 6 hours post ingestion.

CONCLUSION:
Suboxone, a combination of buprenorphine and naloxone, may produce opioid toxicity via sublingual absorption or ingestion by children. We present the case of a child with mild central nervous system depression after exposure to Suboxone. Pediatric case reports that demonstrate more significant central nervous system and respiratory depressant effects from Suboxone ingestion are emerging.
http://www.ncbi.nlm.nih.gov/pubmed/17876257
 
yea i dont think it would be lethal. but if it was someone with a say a methadone habit which is a long lasting opioid, it is pure hell. i accidentaly did a line of a subutex and that 110mgs a day of meth was gone, i was sickr than i can remember even coming off dope. twicthed all night and it basuically took a week back at the clinic to feel normal. its strong stuff but only in the wy for a person with a habit. from what ive read, most opiate naive ppl cant telll the diff btwn moprihne and bupe blind study.

bupe is some strong shit, i knew ppl that would buy it to get high off it. but unlike fent it has a long ass half life and isnt a full agonist, so no i dont think you can OD on it. plus the addition of the narcan is to "discourage" users from trying to IV it, thats why moer orften or not ppl get suboxone and not subutex bc derr ppl think you can slam it. will make you just as sick as a suboxone, no point.

some opiates given in a high enough dose will requuire multiple shotsd of narcan, esp dope and morphine. im oretty sure therer are just as many antagonists as there are agonists....there are a ton ive never heard of.
 
Yeah before I got serious into opiates I use to take an 8th of a Suboxone 8mg and be uncomfortably high. Some people love it, to me I found it to be a dirty high. But once I caught a habit oh my god it became an angel sent from above to take away my withdrawals lol. Very interesting chemical, thats for sure.
 
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