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reduction and dehalogenation of OTC loperamide, from thread.
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nubee
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Wed Apr 20, 2005 10:26 am
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stratosphere wrote:
apparently a quinidine/loperamide cocktail is cns active Drug Transporters Revisited

apparently quinidine is a P-gb inhibitor and P-gb is resonsible for blocking loperamide from crossing the BBB

while quinidine is prescription only, it is an isomer of quinine, both are found in chinchona bark which is readily available from herbal stores. from one source the quinine content is quoted as (2-9%) and the quinidine as (~1%).
im not sure if quinine is a P-gb inhibitor itself, but raceimization could be attempted if one wanted to improve the quinidine:quinine ratio.

this seems to indicate experimenting with chinchona extract and loperamide combos might be fruitful, although i imagine slightly dangerous.


http://rapidshare.de/files/1346562/Drug_Transporters_Revisited.pdf.html

stratosphere wrote:
in the original study Increased drug delivery to the brain by P-glycoprotein inhibition. the dosage used was 16mg loperamide and 600mg quinidine.

while i don't have access to the full article, in the abstract it only mentions resperatory response and has no mention of subjective effects. I would be interested what if anything thay say about subjective effects

i came across this thread http://opium.poppies.org/index.php?act=ST&f=15&t=1222& and unfortunatly one person found no effects from a 900mg Q, 24mg L combo besides accute constipation, although if they are a heavy user of other opiates i would imagine tolerance could be a variable.

another person noticed minimal effects but used 750mg quinine instead of quinidine and didn't specify loperamide dosage or route of delivery.


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http://rapidshare.de/files/1346565/Increased_drug_delivery_to_the_brain_by_P-glycoprotein_inhibition.pdf.html
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