Embutramide and related cmpds

[sekio]

loperamide is indeed a substrate for the P-glycoprotien or whatever you want to call it, the multidrug transporter that diffuses stuff out of the BBB. hence there seems to be a fairly large variability in effects.

some people seem to get opioid effects off as little as a few tens of milligrams. some need large doses but still get some effects, some can only get mild effects even with large doses, and some can't get anything no matter how high they dose.

my buddy would take so many blue-green loperamide gels his urine was black (4g a day). i cannot imagine it did anything good for his kidneys, sometimes i wonder how his heart made it through all that

 

[clubcard]

That much loperamide is a disquieting thought. As for embutramide, well it's 'a riddle, wrapped in a mystery, inside an enigma'. I wonder if the N: & O: overlay BDPC? I have a terrible feeling that it will end up being used a drug used in capital punishment. Well, starting with https://patents.google.com/patent/US3045043 , I looked at all the patents by Hennig Ingeborg and there are DOZENS related to your candidate. I admit, I haven't read them through in any detail because it's very depressing. First time patents have made me feel uncomfortable.

 

[polymath]

Looks like loperamide can cause hypopituitarism and low hormone levels even at therapeutic doses in long-term use:

Case Report: Loperamide-induced hypopituitarism

Loperamide is the most commonly used antidiarrhoeal medication in the UK. We report a serious and hitherto undocumented adverse effect of chronic use in a 45-year-old man with inflammatory bowel disease. He presented to the endocrine clinic with fatigue ...

www.ncbi.nlm.nih.gov

Drugs that can't cross the BBB can still affect the pituitary gland, and megadoses of loperamide will make a disproportionately high concentration affect it.

 

[clubcard]

I have to admit that I am surprised at how cheap and easy it is to obtain huge amounts of loperamide in certain nations. In the UK it's a [P] and I think that a maximum of 16 x 2mg caps can be sold at once. Loperamide will cross the BBB but the body will actively remove it.

 

[sekio]

If you don't mind employing petty criminals it would be entirely possible to have them "five finger discount" 10,000 or more 2mg loperamide doses in an afternoon by visiting pharmacies around the city....