I need some help with methylnaltrexone relationg to binding efficiancys and bupe

[cj]

Like the title says Methylnaltrexone is an opiate antagonist that does not cross the blood brain barrier. Its used to treat severe opiate constipation. My question is will it outcompete buprenorphine for the receptors in GI tract. My doc is willing to write the script its just expensive and I need to know if it will work. My GI doc has no clue. he looked at a freaking Iphone app on drug interactions and said its fine 8). I have googled like hell you guys are smart as shit show me a little love please?

 

[Hammilton]

It'll be very dose sensitive. If you take a high enough dose you'll be good, I'm sure. If you're physically dependent, though, you're going to experience some significant withdrawal. It'll be like quitting heroin (I don't say Suboxone because you're gonna have it hit all at once, not slowly building for a week) without any of the CNS-mediated effects of withdrawal. I dunno what that would be like, to be honest, but I guarantee that it'll be very unpleasant the first day, and probably for a week or so.

 

[ebola?]

too tired and lazy to hunt down methylnaltrexone's binding affinities right now, but I'd do a lit search (it's not in the PDSP database). If it has mu affinity similar to naltrexone's, and you take a high bupe dose, I'd expect the methylnaltrexone to work poorly. Otherwise, who knows (edited to add: hammilton probably does )?

ebola

 

[cj]

Thank you guys soo much! The info on the internet is very limited I am thinking about calling the pharmaceutical company directly? Unfortunately I haven't had a bowel movement in 15 days so this is turning into a very serious situation. Withdrawal is the least of my concern honestly. I take around 1.5mg of bupe a day.

 

[Hammilton]

You can probably take a high enough dose to break through it. I mean, you can with heroin, so if imagine you could with this as well. 15 days is definitely serious, but I doubt it is the opiates. At that level it's almost gotta be something else, diet, water and fiber consumption... probably need to look into Senna or something else.

 

[cj]

Yeah I am under care of a GI doc. I have been on amitiza and now linzess which are supposedly the two best drugs on the market so I don't know what the deal is honestly. I think dehydration played a part probably as well as lack of fiber. But yeah I am going to continue the drugs. I haven't had a sub dose in around 30 hours so I am going be in withdrawal soon anyway. So I am thinking something is going to give in the next 15 hours otherwise I have an impaction. But I still might get the methylnaltrexone tomorrow. I will let you guys know how it turns out. Thanks for your response Hammilton!

 

[Bigazznugz]

Sorry to bump this old thread.
I got 1 question about methylnaltrexone.
Am one methadone snd its a high dose 100mgs+ so i have heard this can cause withdrawals similar to naltrexone.
So is it a bad isea for me to get this medicine or are the side effects to risky fot me? I have been on the done for at least 10 years now. :-/ But at least i get takehomes and i have no desite to use opiates plus it saves me soo much $$$.
Good idea or bad idea?
Thanks all,
Nugz