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suboxoneeater
01-18-2007, 08:13 AM
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list_uids=16837625&query_hl=19&itool=pubmed_DocSum


There is somebody on this board who was very interested in p-glycoprotein inhibitors for making loperamide have acute effects.

Apparantly, if you take these medications then take methadone you will make it more active. I never new that methadone worked via p-glycoproteins. Hell, maybe all opiates work this way?

To make all opiates more subjective would you want to first take p-glycoprotein inhibitors?

Hammilton
01-19-2007, 06:30 PM
Sure, but in this respect, you may be playing with fire. I found a study that gave a P-GP inhibitor and then Loperamide (and found no psychoactive effects) and the blood concentration of it went up 141%- that's an enormous increase.

If Loperamide would have had CNS-Depressant properties, they might have needed to have the Naloxone on hand.

Except, even when this was done, at very high doses of loperamide, Naloxone-test shows that it has no opiate-like effects. Obviously Naloxone wouldn't have saved their lives.

However, it did significantly reduce *all* withdrawal symptoms in morphine addicts. Even dysphoria. That's interesting.

There was another study that tried this combo with drug abusers (like many AIDS patients are/were- patients most likely to be on a P-GPi). They found the drug to have "very, very little abuse potential.
Considering the tendency to overstate these sorts of things (was not a drugCo funded study), I gotta think they hit the nail on the head.

Everyone makes this mistake of assuming that "Hey- all it's gotta do is get into the brain"-- no, not at all. Definitely a good start, but "not all it's gotta do" -- Once it's in the braint, then it has to choose a receptor. If it's a Mu-agonist, great, but who's to say it isn' tgoing to be a delta agonist? or show partial agonist/antagonist properties?

I have no idea if you can tell these things by looking at it or what.