opiateconnect369
Greenlighter
- Joined
- Oct 4, 2022
- Messages
- 6
Apparently, there is an OTC opioid that just has shitty permeability into the CNS. I didn't even know.
Loperamide Potentiation - Increasing BBB and Intestinal Wall Absorption
Efflux via P-glycoprotein can be inhibited. MDR1 inhibitors (MDR1 is a gene relevant to P-glycoprotein expression) have a stub section on the P-glycoprotein wikipedia article. However, above it a section contains this:
DANGERS - Cardiotoxicity, Arrythmia, Neurotoxicity?
Maybe lower doses, facilitated with potentiation via PPIs, could avoid these scary side effects?
Conversion to Fentanyl?
Is it possible to easily convert this substance using kitchen chemistry? It seems pretty similar.
Loperamide Potentiation - Increasing BBB and Intestinal Wall Absorption
Efflux via P-glycoprotein can be inhibited. MDR1 inhibitors (MDR1 is a gene relevant to P-glycoprotein expression) have a stub section on the P-glycoprotein wikipedia article. However, above it a section contains this:
So, Lansprazole and omeprazole would be the go-to potentiators. These are "proton pump inhibitors", so they come with some side effects of their own. But, all three of these are available OTC in just about every pharmacy in America.Some common pharmacological inhibitors of P-glycoprotein include: amiodarone, clarithromycin, ciclosporin, colchicine, diltiazem, erythromycin, felodipine, ketoconazole,[32] lansoprazole, omeprazole and other proton-pump inhibitors, nifedipine, paroxetine, reserpine,[33] saquinavir,[32] sertraline, quinidine, tamoxifen, verapamil,[34] and duloxetine.[35] Elacridar and CP 100356 are other common[citation needed] P-gp inhibitors. Zosuquidar and tariquidar were also developed with this in mind.[clarification needed] Lastly, valspodar and reversan are other examples of such agents. ABCB1 is linked to the daily dose of warfarin required to maintain the INR to a target of 2.5. Patients with the GT or TT genotypes of the 2677G>T SNP require around 20% more warfarin daily.[36] Concurrent administration of P-glycoprotein inhibitors such as quinidine potentially allows loperamide to cross the blood–brain barrier and produce central morphine-like effects. Loperamide taken with quinidine was found to produce respiratory depression, indicative of central opioid action.[37]
DANGERS - Cardiotoxicity, Arrythmia, Neurotoxicity?
High doses may result in heart problems such as abnormal heart rhythms.[18] Loperamide metabolizes into an MPTP-like compound, but is unlikely to exert neurotoxicity.[34] Since 2015, several reports of sometimes-fatal cardiotoxicity due to high-dose loperamide abuse have been published.[68][69]
Maybe lower doses, facilitated with potentiation via PPIs, could avoid these scary side effects?
Conversion to Fentanyl?
Is it possible to easily convert this substance using kitchen chemistry? It seems pretty similar.