Ok. I have read (and re-read) EVERY post about loperamide on the internet. Here's my opinion based on experience.
I took 60mg of omeprazole (a php-inhibitor) 1 hour prior to taking loperamide. I drank a Monster Energy Rehab drink which contains quercetin, which reportedly helps lope cross the blood brain barrier. Also, I took 2 garlic supplements (another pgp-inhibitor). I did not see the point in drinking tonic water, as it is quinidine, not quinine, that is a pgp-inhibitor. Then, I took 60mg of generic loperamide.
I should also add that I am prescribed morphine oral, 90mg a day. My tolerance is much higher than that, but I've avoided becoming overly physically dependent on it by tapering and skipping days every so often. Some days I take more, some days less. It takes at least 90mg for analgesia, and to get a "buzz," I would need to take at least 120mg all at once, but can also handle over 200mg. When I do take breaks, the only withdrawal symptoms I get are a mild case of "the runs," and some cold sweating & heat sensitivity.
So, last month, I ran out of my script a few days early (except for a few pills I had to save to take before the urine test at my pain clinic). I was in pain, obviously, and experiencing some gastrointestinal discomfort and some cold sweats. I decided to give the loperamide thing a try. I knew from past experience that taking 3x's the normal dose would stop the runs, so I was curious to see if, in higher doses, it would help with the sweating and mild craving, or perhaps even the pain. I did not expect to "feel" them other than that, so the bar was set very low. A few hours went by, and I had pretty much given up on any effects, although my stomach was better and my body temperature seemed more regular. Then, about 3 hours later, I was in my car, and all of the sudden, I started feeling a bit of that opiod glow. Nothing SUPER intense, but definitely there. I would describe it as similar to the way tramadol makes me feel. Kind of comes in little waves, but you feel content, and a bit of a body buzz. I also noticed I was in less pain. I am pretty confident this was not a placebo, as at that point, I had given up on feeling any CNS effects and was not even thinking about it at all. After that, I did decide to take only 15mg of instant release morphine, which normally would do absolutely nothing for me other than prevent diarrhea of a few hours. Again, to my surprise, this very small amount of MS seemed to have a synergistic/potentiating effect with the loperamide.
I repeated this experiment again a few days later, this time, taking tramadol a few hours after. Once again, it certainly seemed that that pgp inhibitors definitely allowed some of the lope to cross the BBB, and the lope definitely potentiated tramadol, which by itself, does absolutely nothing for me. Normally, on days where I skip or take very little of my pain meds, I am not able to do much at all, as I have degenerative disc disease with herniated discs, permanent nerve damage, and severe arthritis in every joint (and I'm only 34!). I was astonished that I was able to do a little grocery shopping, and even socialize with a friend for a little while without being in agony. Again, I HIGHLY doubt this was placebo, as I had extreme doubt about the whole thing. In fact, I've actually done experiments with friends in the past to see if placebos worked on me (I won't get into specifics, but I took a pill knowing that it might be real or not). Each time I ended up with the "sugar pill," I felt absolutely nothing.
Today, I have done this whole thing again, and getting the same results. I know everyone's system is different, but I do believe there is definite validity. One should be very careful, however, not to do this too often, or to take ridiculous amounts of lope because there are reports of overdoses & heart failure when taken in extreme amounts.
I've also taken buprenorphine for pain management in the past, and in a way, doing lope with this method kind of reminds of that.
