Opioids Loperamide--->Suboxone. How to?

[radiodog]

I've been on ~100 mg's of loperamide a day for quite a while now (couple years). I started it because at high doses like that it kept me completely WD free from heroin and I eventually got off heroin with it. So no matter how stupid it sounds that I'm addicted to poop pills, I don't give a shit because they got me off of heroin. Anyways, I'm wondering if anybody has ever gone from Lope onto suboxone. I'm currently trying it, and not exactly sure whether I need to still taper off the lope, or if i would be comfortably able to just cut it off immediately. I'm perscribed two 8 mg subs per day.

I'm really curious if anyone here can give me a little schooling on some of the science behind how these two opioids work on the brain. Neither of them show up on drug tests, which confuses me. Am I wasting my time trying to get on subs from the lope because they just work on different receptors or what? I really want to know more about how these work on the brain, if somebody would kindly explain. Thank you.

 

[Ohbedee]

I've been on ~100 mg's of loperamide a day for quite a while now (couple years). I started it because at high doses like that it kept me completely WD free from heroin and I eventually got off heroin with it. So no matter how stupid it sounds that I'm addicted to poop pills, I don't give a shit because they got me off of heroin. Anyways, I'm wondering if anybody has ever gone from Lope onto suboxone. I'm currently trying it, and not exactly sure whether I need to still taper off the lope, or if i would be comfortably able to just cut it off immediately. I'm perscribed two 8 mg subs per day.

I'm really curious if anyone here can give me a little schooling on some of the science behind how these two opioids work on the brain. Neither of them show up on drug tests, which confuses me. Am I wasting my time trying to get on subs from the lope because they just work on different receptors or what? I really want to know more about how these work on the brain, if somebody would kindly explain. Thank you.

First off, I'm biologist with extensive pharmaceutical development experience. I'm trying to make the following answer as accessible as possible to non biologists...

Loperative was originally being developed to be a potent opiate pain killer, but there are complications. Lope can't cross the blood brain barrier, a systemic filter that prevents numerous compounds, chemicals, infectious agents, etc. from entering the central nervous system and causing damage. The brain barrier can be over ridden by increasing systemic concentrations of a substance to a level that it essentially pushes through or spills over, you pick your metaphor. Also, there are some medicines and OTC supplements that suspend the activity of the blood brain barrier, but I'll not list them here for fear the info will get distributed.

Suboxone is an opiate and an opiate blocker, although the blocker is there only to prevent i.v. Abuse and has little to no effect orally. Suboxone has a long half life, and high binding affinity, therefore redosing in the short term will not likely increase effects, known as a ceiling effect. It it's highly effective at eliminating withdrawals while not very effective at getting users high. the opiate in suboxone does cross the blood brain barrier effectively, as do most all opiates.

The effect you are currently experiencing is the stimulation of your opiate receptors by a potent opiate that has flooded your system so completely that a miniscule volume makes it through to the cns. If you take suboxone, your likely to get a similar effect, but with increased motility in the bowels, which is a good thing. The lope. you're currently taking is paralyzing your bowels by stimulating the opiate receptors in your bowels, which is what causes constipation in all opiate users.

Hope this helps

 

[Keif' Richards]

I know that this is a little bit old at this point, but I definitely feel compelled to give my opinion. This whole Loperamide (Immodium) has definitely blown up significantly over the past couple of years. Keep in mind, everything that I'm saying is coming from an individual who has done the same thing, so no judgement. I never actually started a maintenance regime with the stuff as you have, but I've definitely done it a couple dozen times at dosages similar to what you're using. Everybody knows certain wholesale outfits in which you can buy an infinite amount of the stuff for nothing. I saw a guy at rite aid the other day buying 2 of the 200 count boxes. It's definitely become more widespread.

As we all know by now, Loperamide is an Opioid chemically similar to Fentanyl that does not, in theory, effect the central nervous system. This means you get the gastrointestinal effects of the Opioid without the psychological effects, however, it would seem that Loperamide is indeed centrally active to a certain extent, especially when taken in massive dosages such as this, the average dose being 2mg - 4mg every 4-6 hours. It would be a really great resource if it weren't for the drug's potentially dangerous effects upon the heart. There are other Opioids, like Methadone for instance, that also effect the heart's QT interval. This can and has lead to documented cases of death resulting. So, Loperamide maintenance is not something we can condone.

Anyway, I had to provide my disclaimer, but the issue at hand is essentially that you must withdraw from a pretty significant level of Opioid dependence. I have experienced and have known others who also have experienced a pretty severe withdrawal from the stuff. I'd say the only thing you can do is wait until you are very sick and then begin administering the Buprenorphine in very small dosages, monitoring your reaction closely. You have to treat this as if you are dependent upon any other Opioid.

 

[axe battler]

Keif.hit the nail onm the head. It has a loooong half-life, so you want to wait until you are in quite severe withdrawal. Look up the COWS scale and there is a certain score you need to reach before taking bupe.
It is better to start slowly though, because precipitated withdrawal is fucking horrible!
Be careful!

 

[Hodor]

Suboxone has a long half life, and high binding affinity, therefore redosing in the short term will not likely increase effects, known as a ceiling effect.

The reason for the ceiling effect isn't just the high binding affinity, it is the partial agonism.

Basically, a molecule of buprenorphine cannot fully activate an opioid receptor in the same fashion that a full agonist like morphine or your body's endorphins can.

Instead, it only partially acitvates the receptor, but makes up for this with an extreme level of binding affinity - if the bupe grabs onto a receptor, it's not letting go easily, whereas morphine will bind to a receptor, and drift away moments later.
This means that at low doses - when there are still plenty of unoccupied receptors to go around - buprenorphine actually produces intense effects. However, as you try to compensate for your increased tolerance by increasing the dose, the buprenorphine molecules will start competing with each other for the remaining receptors, leading to diminishing returns from dosage increases, to the point where you reach a "ceiling" where virtually all the receptors are occupied, but only partially activated.

This also means that buprenorphine is effective at preventing the simultaneous use of other, more recreational opioids: As long as your receptors are occupied by the tightly-bound buprenorphine, other opioids can n longer bind to and activate them.