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Morphine: Do CYP2D6 Inhibitors Increase Oral Bioavailability?

MurphyClox said:
There is some reason why one shouldn't consume grapefruit juice together with certain pharmaceuticals, just to quote the probably most famous example.

Murphy
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Does this apply to any opiates besides the loss of potency found in codeine? I was unaware of any major toxicity issue with opiates and opiods.

Also the simple answer is cimetadine which inhibits both 450 and d26 or white GF juice which is highly effective for many individuals.

Also can anyone comment on why DPH imediately inhibits enzymes but GF Juince and Cimetadine take about an hour to be effective?
 
I'm not really aware of any serious grapefruit-juice/opioid-interactions at the moment. The statement was meant in general...

The longer onset of action could be attributed to necessary metabolism: Maybe (not sure here) it's not the compound itself but rather a metabolite that causes the CYP-inhibition. Pharmacokinetics could also play a role (prolonged uptake into the blood stream).
Apart from this I don't see a reason why one compound should need more time than another one; as soon as it hits the liver, the CYPs get inhibited.

One last thing:
theWorldWithin said:
...cimetadine which inhibits both 450 and d26 or...
Click to expand...
I assume that "d26" equals "2D6"?! The 2D6-isoform IS actually a CYP-enzyme. So, both terms describe somehow the same.

Peace! Murphy
 
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...also, some CYPs are constitutionally expressed (i.e. always present) and some have to be induced. And that takes some time of course. Don't ask me, which isoform does what, no idea here.
 
sorry for bumping an old thread, but this seems unresolved

So, will CYP enzyme inhibtion increase the BA/reduce the rate of metabolism of morphine to an increased effect? It seems that from what I can tell, most every other opioid is affected by the CYP system in some way (all the codone derivatives, fentanyl, propxyphene, morphones, if i'm correct) that leads to either an increased or extended duration, is this the same for morphine? Yes, or no, and to what degree compared to the CYP systems inhibition on the peak/extended plasma levels of drugs like oxycodone?

And, as far as glucuronidation, is there a way to manipulate that aspect in order to increase effectiveness of morphine? If so, what are some examples of OTC/RX aids in that process?/////

Should both of these measures be taken if practical to boost a dose of morphine sulfate?
 
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