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Opioids Does loperamide have a blockade effect?

V

velocity92c

Bluelighter
Joined
Jun 29, 2009
Messages
82
A friend of mine (not trying to dodge the rules, it seriously wasn't me) recently told me that while withdrawaling he took 48mg of Loperamide to try to help with it as it was all he could get his hands on. 3 hours later he was able to score 4mg of Dilaudid. After IV'ing it he says he felt no better and got absolutely no rush, compared to the very intense rush you normally get from it. I was just curious if Loperamide actually had a blockade effect? I didn't even realize it would work for withdrawals, as I didn't think enough of it crossed the BBB to make a difference. Perhaps a little clarity on both points for me?
 
For those curious, I found this thread which seems to back what my friend was saying. Kind of sucks for him but good to know loperamide can actually help withdrawal symptoms.
 
No, loperamide is a mu agonist with (generally) exclusively peripheral activity. So even if the drug had some mechanism by which to block opioid activity induced by other drugs, this would be limited to the periphery.

As for loperamide used for withdrawal -- loperamide could theoretically help, but it wouldn't affect CNS withdrawal symptoms like mental depression as it doesn't cross the BBB.
 
^I very recently thought that but I have seen learned it actually can cross the BBB if ingested in large enough amounts (also if taken with certain other chems but that's irrelevant). I don't know if lopermide has blockade action but it is fairly potent in the gut. I'd say the friend's experience is more likely he was deep in withdrawal and the dilaudid just helped a bit and he didn't really notice. Hard to say for sure but we'll see if anyone else has found loperamide out-competing other opiates or if it's affinity is definitely that low that it's impossible.
 
So that link claims that it does have a strong enough affinity to blockade the Dilaudid in the PNS and if enough crossed the BBB have a limiting effect on the CNS as well. Probably a combination of things including being in withdrawal.
 
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