Bupe Concurrent administration of Buprenorphine with other full agonists

[ziritt]

Is there a threshold dose of Buprenorphine below which a significant number of opioid receptors will be unbound and available for full agonism? (assuming a opioid tolerant person who is taking buprenorphine for maintenance) The math is obviously important, as steady-state plasma concentrations of buprenorphine may be several times the daily dose due to the long elimination half-life. So for example, someone who takes 0.5mg of buprenorphine every 12 hours, assuming a SL bioavailability of 30% and a half-life of 52 hours, would reach a steady-state of 1.014mg buprenorphine after ~23 days (and would have reached 90% of the steady-state amount -- 0.907mg -- after 7 days):

1. T=0h: +30% x 0mg = 0.000mg (no dose at 0h, this is the base case)
2. T=12h: +30% x 0.5mg = 0.278mg
3. T=24h: +30% x 0.5mg = 0.387mg
4. T=36h: +30% x 0.5mg = 0.480mg
5. T=48h: +30% x 0.5mg = 0.559mg
6. T=60h: +30% x 0.5mg = 0.626mg
7. T=72h: +30% x 0.5mg = 0.684mg
8. T=84h: +30% x 0.5mg = 0.733mg
9. T=96h: +30% x 0.5mg = 0.774mg
10. T=108h: +30% x 0.5mg = 0.810mg
11. ... (days 4, 5, 6, ... - ramping up to 90%)
12. T=168h: +30% x 0.5mg = 0.907mg
13. ... (1w ... 22d - ramping 90% to 99.9%)
14. T=528h: +30% x 0.5mg = 1.014mg
15. T=540h: +30% x 0.5mg = 1.014mg
16. ... (steady state achieved, will remain at ~1.014mg forever)

So my question is - in this hypothetical opioid-tolerant individual who has stabilized at 1.014mg total buprenorphine, how would you figure out the occupation percentage of receptors to see the effect that could be had by concurrently taking a full opiate? Is there a magic number of "mg's buprenorphine"? does it vary by weight? by tolerance? etc. If so, titrating the dose down to reach a desired occupation percentage should be possible, to allow some experience of full agonists (obviously not a FULL experience) - but what is the magic number? Thanks!

 

[DeathIndustrial88]

This post is a few years old now and I doubt the OP needs the answer to this question anymore but I figured I'd say something in case anyone comes across this post and also wants an answer but doesn't see one.

I don't have a precise magic number, but from my years of experience I have come to believe that around 1-2mg of bupe (either sublingual or nasal), you can take full agonists along side it and still feel about 70% of it's effects. Enough to stop cravings for me. It depends on the dosage of said full agonist though as well.

Once you get up to 4mg and beyond (regardless of ROA) is when the blocking effects really come into play and can have you thinking an entire batch of your heroin is completely bunk. Of course if you are dosing even at 2mg sub a day for awhile, this will build up to about 4mg or beyond.