How is buprenorphine metabolised?

[Tialis]

Is bupe broken down by the enyzmes in liver? Would taking grapefruit juice potentiate bupe through changing the metabolism in the liver?

Exactly what enzymes are involved in the metabolism of opiates in general?

How do the liver enzymes work? What are they called?

I would appreciate it if someone could actually post some information in this thread, rather than giving me a link to some other site. Unfortunately, because of the filter I have on this computer, I can only access Bluelight (don't ask).

 

[D_DOOD]

I would like an answer as well

 

[BilZ0r]

Well, I'll answer this is an odd direction.

Firstly, How do the liver enzymes work? What are they called? They're called various things, there was an effort to standardise a lot of the names, so all "cytochrome" containing enzymes are called "cyptochrome P 450 XXX" or just "CYP XXX" where the XXX refers to genefamily-type-subtype I believe, so one common enzyme is called CYP2D6. Back in the day, that enzyme used to be called "Debrisoquine hydroxylase" because it was the only enzyme which 'hydroxylased' (adds an oxygen and a hydrogen) the chemical debrisoquine, but now it's called CYP2D6. How they work is quite complicated, because there are lots of other enzymes besides cytochrome p 450s. In general, most of these enzymes have reactive metals in their centers (iron in the case of CYPs) which add or remove electrons or hydrogens and then add something else in, like water in the case of CYPs.

Exactly what enzymes are involved in the metabolism of opiates in general? As far as which enzymes metabolise which opioids, generally, cyp3a4 and cyp3a5 metabolise opioids to inactive products. CYP3A4/5 are the enzymes that grape fruit juice inhibits to a large extent. CYP2D6 metabolises some opioids to their active forms, as review in this post on bluelight here.

Is bupe broken down by the enyzmes in liver? Would taking grapefruit juice potentiate bupe through changing the metabolism in the liver? Buprenorphine, like other opioids is a substrate for CYP3A4, theres evidence that it is metabolised by CYP2D6 and CYP2C8. So it would seem grapefruit juice can increase the amount of buprenorphine absorbed.