negrogesic
Bluelight Crew
"Loperamide is an opioid, a piperidine similar to fentanyl, yet it is not addictive in the traditional sense, as it does not permeate the blood brain barrier. Loperamide is also known as immodium.... "
Isnt that what I said? I said that it does not go through the BBB, which makes it not addictive in the traditional sense.....
Loperamide, which was once a schedule 5 drug, is READILY available OTC at all drug stores under the brandname Immodium. Most places also sell a generic loperamide tablets, which are the same, and both are manufactured in the same factory. Although it doesnt permeate the BBB, it does significantly help with opioid withdrawal.
And its possible if you made loperamide in a polystirex like form (which are tiny plastic particles binded to the drug that help it cross the BBB, it was used with DXM in the brand name "desylem"), and in doing this it may result in a CNS active substance, a potent opioid agonist.
Also p-glycoprotein inhibitors like quinidine, or its fellow optical isomer quinine, has been used in the following pubmed study to make loperamide a poteny CNS active opioid agonist. The last sentance of the following qoute is particularly alluring ("can be reversed by a drug causing P-glycoprotein inhibition, resulting in serious toxic and abuse potential")......
When i read the above, i was quite interested, especially about the "serious toxic and abuse potential". I have used quinine to see if it works, in varying doses, as well as varying doses of loperamide, and though i definately noticed potentiation, there was VERY little CNS activity. But quinidine is a stronger p-glycoprotein inhibitor than quinine, so maybe if i had used quinidine, i would have experienced better results. If we could someone way figure out how to make loperamide cross the blood brainbarrier, we could convert a relatively cheap, legal, easily obtainable OTC medication into a potent opioid. I think the polysterix may be the best solution, or perhaps a stronger p-glycoprotein inhibitor combined with a polisterix verision of loperamide might work. If this did actually materialize and someone figured out the way and it starts circulating as a recreational drug, loperamide would become scheduled once again, or watched like ephedrine/pseudoephedrine.
It does not permeate the BBB, therefore does not get you high.
Isnt that what I said? I said that it does not go through the BBB, which makes it not addictive in the traditional sense.....
Loperamide, which was once a schedule 5 drug, is READILY available OTC at all drug stores under the brandname Immodium. Most places also sell a generic loperamide tablets, which are the same, and both are manufactured in the same factory. Although it doesnt permeate the BBB, it does significantly help with opioid withdrawal.
And its possible if you made loperamide in a polystirex like form (which are tiny plastic particles binded to the drug that help it cross the BBB, it was used with DXM in the brand name "desylem"), and in doing this it may result in a CNS active substance, a potent opioid agonist.
Also p-glycoprotein inhibitors like quinidine, or its fellow optical isomer quinine, has been used in the following pubmed study to make loperamide a poteny CNS active opioid agonist. The last sentance of the following qoute is particularly alluring ("can be reversed by a drug causing P-glycoprotein inhibition, resulting in serious toxic and abuse potential")......
BACKGROUND: Although the antidiarrheal loperamide is a potent opiate, it does not produce opioid central nervous system effects at usual doses in patients. On the basis of in vitro studies demonstrating that loperamide is a substrate for the adenosine triphosphate-dependent efflux membrane transporter P-glycoprotein, we postulated that inhibition of P-glycoprotein with quinidine would increase entry of loperamide into the central nervous system with resultant respiratory depression. METHODS: To test this hypothesis, a 16-mg dose of loperamide was administered to eight healthy male volunteers in the presence of either 600 mg quinidine, a known inhibitor of P-glycoprotein, or placebo. Central nervous system effects were measured by evaluation of the respiratory response to carbon dioxide rebreathing as a measure of opiate-induced respiratory depression. RESULTS: Loperamide produced no respiratory depression when administered alone, but respiratory depression occurred when loperamide (16 mg) was given with quinidine at a dose of 600 mg (P < .001). These changes were not explained by increased plasma loperamide concentrations.
CONCLUSION: This study therefore demonstrates first the potential for important drug interactions to occur by a new mechanism, namely, inhibition of P-glycoprotein, and second that the lack of respiratory depression produced by loperamide, which allows it to be safely used therapeutically, can be reversed by a drug causing P-glycoprotein inhibition, resulting in serious toxic and abuse potential.
When i read the above, i was quite interested, especially about the "serious toxic and abuse potential". I have used quinine to see if it works, in varying doses, as well as varying doses of loperamide, and though i definately noticed potentiation, there was VERY little CNS activity. But quinidine is a stronger p-glycoprotein inhibitor than quinine, so maybe if i had used quinidine, i would have experienced better results. If we could someone way figure out how to make loperamide cross the blood brainbarrier, we could convert a relatively cheap, legal, easily obtainable OTC medication into a potent opioid. I think the polysterix may be the best solution, or perhaps a stronger p-glycoprotein inhibitor combined with a polisterix verision of loperamide might work. If this did actually materialize and someone figured out the way and it starts circulating as a recreational drug, loperamide would become scheduled once again, or watched like ephedrine/pseudoephedrine.
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