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Old 13-12-2008, 23:10
Herbal Healer 019's Avatar
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Buprenorphine potentiation via Grapefruit Juice..Is it worth it?

SWIM uses buprenorphine recreationally & often potentiates it using GrapeFruit Juice (a CYP3A4 enzyme inhibiter) knowing that buprenorphine is metabolized by the CYP3A4 enzyme via the liver.

I've just come across some info (wikipedia_buprenorphine) that the CYP3A4 enzyme metabolizes buprenorphine into norbuprenorphine, & (norbuprenorphine) has a slightly diff. binding profile to the opioid receptors and is a stronger partial agonist at the mu-receptor & is a potent agonist in the nociceptin receptor.

With this info SWIM is starting to doubt that potentiating buprenorphine via GFJ is even worth it seeing as norbuprenorphine seems to be stronger.

Any thoughts?

Is it really worth inhibiting the enzyme that metabolizes buprenorphine into norbuprenorphine or not?
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