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  • BDD Moderators: Keif’ Richards | negrogesic

Opioids How is Loperamide metabolized?

E

evo4ever

Bluelighter
Joined
Jun 14, 2016
Messages
1,113
Location
United Kingdom
Hey all.

Just a quick one.. Does anyone know how Loperamide is metabolized? You'd think it would be via the Cytochrome P450 pathway but I can't find any info to suggest this. Also does anyone know which protein is involved in hindering Loperamide's absorption into the bloodstream in the GI tract? Cheers guys.
 
^that should answer most of your questions.

not sure if this was included but,
When taken therapeutic doses, loperamide Does not cause euphoria or analgesia. It has poor oral bioavailability and does not readily cross the blood-brain barrier due to p-glycoprotein efflux.
P-glycoprotein (P-gp) is a transporter that removes agents from cells once they have crossed the cell membrane. It protects the organism from potentially harmful substances as it excludes them from systemic absorption in the gut and penetration into the brain. P-gp acts as a “bouncer” at the blood-brain barrier, keeping loperamide out of the CNS.
 

Loperamide-COVID-19: Loperamide is a Potent inhibitor of SARS-cov-2, COVID-19 virus in vitro

Quite interesting Belgium-Dutch and Chinese studies: de Wilde A, Jochmans D, Posthuma CC. et al. Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture. Antimicro Agents Chemother.2014...
www.bluelight.org www.bluelight.org

And it may have anti Covid-19 if this in vitro research has any weight to it. Although taking massive doses of loperamide isn’t wise on many levels.

-GC
 
PrincessDiz said:
^that should answer most of your questions.

not sure if this was included but,
When taken therapeutic doses, loperamide Does not cause euphoria or analgesia. It has poor oral bioavailability and does not readily cross the blood-brain barrier due to p-glycoprotein efflux.
P-glycoprotein (P-gp) is a transporter that removes agents from cells once they have crossed the cell membrane. It protects the organism from potentially harmful substances as it excludes them from systemic absorption in the gut and penetration into the brain. P-gp acts as a “bouncer” at the blood-brain barrier, keeping loperamide out of the CNS.
Click to expand...

Quinine inhibits Pgp resulting in upto 3-fold higher exposure to Loperamide, and according to my research the Cytochrome P450 does play a major part in the BA of Loperamide so good old Grapefruit would increase BA. I can imagine co-administering Quinine and Grapefruit would significantly increase ur exposure to Loperamide resulting in central effects at lower doses of Lope.

I would like to test this but Quinine is quite hard to get hold of. I definitely know Grapefruit juice inhibits CYP3A4 and CYP2D6 because I've tested it on Oxycodone which resulted in a more profound Histamine response and a longer half-life.
 
Last edited:
evo4ever said:
Quinine inhibits Pgp resulting in upto 3-fold higher exposure to Loperamide, and according to my research the Cytochrome P450 does play a major part in the BA of Loperamide so good old Grapefruit would increase BA. I can imagine co-administering Quinine and Grapefruit would significantly increase ur exposure to Loperamide resulting in central effects at lower doses of Lope.

I would like to test this but Quinine is quite hard to get hold of. I definitely know Grapefruit juice inhibits CYP3A4 and CYP2D6 because I've tested it on Oxycodone which resulted in a more profound Histamine response and a longer half-life.
Click to expand...
Honestly though, is lope really worth it?! I wouldn’t waste my time on lope.
 
G_Chem said:

Loperamide-COVID-19: Loperamide is a Potent inhibitor of SARS-cov-2, COVID-19 virus in vitro

Quite interesting Belgium-Dutch and Chinese studies: de Wilde A, Jochmans D, Posthuma CC. et al. Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture. Antimicro Agents Chemother.2014...
www.bluelight.org www.bluelight.org

And it may have anti Covid-19 if this in vitro research has any weight to it. Although taking massive doses of loperamide isn’t wise on many levels.

-GC
Click to expand...

May be a coincidence, but I use a of Loperamide when I run out of opioids and I had a mild version of Corona. Maybe it was milder because I was on all that Lope?
 
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