I know that swallowed suboxone has a very low B/A but is it because its metabolized very quickly or just because its destroyed by stomach acid? One of the metabolites of buprenorphine is norbuprenorphine a full agonist. I was wondering if it gets metabolized in to norbuprenorphine and you take a pgp inhibitor would you get the full agonist effects?
Opioids Oral Suboxone with pgp inhibitors?
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sekio
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Wiki sez: "The active metabolites of buprenorphine are not thought to be clinically important in its central nervous system effects. [...] relative to buprenorphine, norbuprenorphine has extremely little antinociceptive potency (1/50th that of buprenorphine), but markedly depresses respiration (10-fold more than buprenorphine). This may be explained by very poor brain penetration of norbuprenorphine due to a high affinity of the compound for P-glycoprotein."
In principle if you took a PGP inhibitor, that would remove one barrier, however if the binding affinity for buprenorphine @ the mu opioid receptor is higher, then bupe will prefer to bind rather than the norbuprenorphine!
In principle if you took a PGP inhibitor, that would remove one barrier, however if the binding affinity for buprenorphine @ the mu opioid receptor is higher, then bupe will prefer to bind rather than the norbuprenorphine!
Thats why I I said doing it orally, with a B/A of only 10% that leaves only .8mg of buprenorphine which leaves plenty of receptors unoccupied. That is only if the other 90% will be metabolized, or is it only the 10% that gets metabolized into norbupe?