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Harm Reduction BIMU-8 to offset respiratory depression?

BrokedownPalace

BrokedownPalace

Bluelight Crew
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Feb 26, 2005
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I was perusing the vast pipelines of the internets, and while reading something about opiate induced respiratory depression, I stumbled across something interesting.

There is a drug called BIMU-8, which is a drug which acts as a 5-HT4 receptor selective agonist. BIMU-8 was one of the first compounds of this class. The main action of BIMU-8 is to increase the rate of respiration by activating an area of the brain stem known as the pre-Botzinger complex.

There seems to be some success in combining this substance with opioids/opiates, to reduce the respiratory depression caused by them. It can apparently do so, without negatively effecting the analgesic and therapeutic values of said drugs. This would mean one could hypothetically take larger doses of opiates without having to worry about the risk of increased respiratory depression, potentially leading to respiratory arrest.

Does anyone have any information about this or links to other studies done about this? I don't have very much time right now but I will continue to do some more research this afternoon. I hadn't heard of this until today, but it sounds very interesting and could be quite beneficial.

Mike
 
I don't know anything about the drug you are mentioning, but in regards to taking higher doses of opiates without having to worry as much about respiratory depression, you would definitely have to look at the half-life of BIMU-8 to see if it will be active during a similar time frame as your opiate/oid of choice is. If it lasts too long the increased respiration and corresponding heartrate might be uncomfortable. If it doesn't last long enough, then obviously if you take too many opiates you might be in for trouble. Also check out the active metabolites, it could create something nasty or that interacts with other things you take.

Thank you for posting this, it sounds very interesting!
 
Yeah. Unfortunately there haven't been any human trials even done so anecdotal reports would be non-existent. Interestingly, other 5-ht4 agonists which are approved for human use do not offer any effect on respiratory depression. In trials done on rats, bimu-8 has shown very positive results in regards to counter-acting the respiratory depression experienced from fentanyl.

I am not sure about the half-life, there seems to be very limited information about this compound. I am going to do more research and see what else I can find.
 
BrokedownPalace said:
Interestingly, other 5-ht4 agonists which are approved for human use do not offer any effect on respiratory depression.
Click to expand...

True, but thats because 5HT4 agonists like tegaserod were developed for the treatment of irritable bowel syndrome and similar gastrointestinal disorders, so they weren't concerned about CNS activity. Some other 5HT4 agonists like zacopride do share the anti-respiratory depressant effect, and zacopride is probably somewhat easier to find than BIMU-8 given its wider uses in research.

The ampakine drugs like CX-546 and CX-717 also happen to block respiratory depression without affecting analgesia. CX-717 is comparably effective against fentanyl induced respiratory depression as BIMU-8, and is the first drug to have gone through to human trials for this application.
 
mad_scientist said:
True, but thats because 5HT4 agonists like tegaserod were developed for the treatment of irritable bowel syndrome and similar gastrointestinal disorders, so they weren't concerned about CNS activity. Some other 5HT4 agonists like zacopride do share the anti-respiratory depressant effect, and zacopride is probably somewhat easier to find than BIMU-8 given its wider uses in research.

The ampakine drugs like CX-546 and CX-717 also happen to block respiratory depression without affecting analgesia. CX-717 is comparably effective against fentanyl induced respiratory depression as BIMU-8, and is the first drug to have gone through to human trials for this application.
Click to expand...

Cool, thanks for the info. I noticed that BIMU-8 hasn't had any human trials, and I can't seem to find anything regarding potential future human testing. I have a feeling that this isn't going to go too far for human use, atleast not anytime soon.

Thanks for pointing out the ampakine compounds that have had human trials so far. If I can get my act together this morning I am gonna do some serious researching regarding this stuff. Last night I was practically useless.
 
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