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