Codeine slowing Naloxone metabolism?

[Raihiar]

Hi fellow bluelighters!

I recently thought back a few years, that codeine- and Tilidine+Naloxone pills don't really mix too well in my personal experience.
Is it possible that the codeine hogged all the enzymes that usually inactivate naloxone via first-pass-metabolism, causing effects not unlike WDs when taking my then usual dose of 600mg Tilidine/48mg Naloxone and adding some (400mg) codeine to it?

Hope this is the right subforum for this question, but if it fits another better, then feel free to move it.

Raihiar

 

[theGirlWithBlueHair]

Codeine is weird drug for people for two reasons: 1) Either the first group of people will of people will metabolize it too quickly and not feel anything, or 2) will not metabolize it at all and not feel anything.

This has to do with CYP2D6.

What's happening is that you're probably not metabolizing the codeine, leaving it all inactive - getting no effects - what you said about the naloxone...so what would be going on is your receptors are clogged by essentially two antagonists...

 

[Raihiar]

Thanks for the fast answer!
but i should have added that codeine on its own works extremely well! even when i had a 1200mg Tilidine (rel. potency 0.2) tolerance, 400mgs of codeine (0.1) still had me nodding, itching and generally feeling awesome.
Only the combination of the two, or more precisely ingesting both sorts of pills at the same time, caused dysphoria and RLS and so on.. codeine after the tilidine-peak works, as does tilidine after codeine-peak.

This has to do with CYP2D6.

What's happening is that you're probably not metabolizing the codeine, leaving it all inactive - getting no effects - what you said about the naloxone...so what would be going on is your receptors are clogged by essentially two antagonists...

if i got no effects at all, i'd say you're right, but well.. i was physically addicted at the time - and i sure as hell felt like i was in WD.. not because of a long time since my last dose, i know THAT feeling.

Raihiar

 

[theGirlWithBlueHair]

Tilidine has to be metabolized as well, though. And if I am not mistaken, it is an somewhat phencylicine and ketamine, correct?

I think what you might be experiencing is that by ingesting them both at the same time you are not going to be metabolizing them both to their active metabolites to an appreciable extent.

Remember with drugs that are prodrugs, such as codeine and tilidine, with big dosages, you want to to stagger for maximum absorption and conversion, for the codeine into the morphine and the tilidine into the nortilidine.

Especially the tilidine. I wouldn't want to waste that. A mu agonist, NMDA antagonist, and DOR? That's an interesting substance.

And adding the naloxone in, as soon as your converting your codeine and tilidine, all you're doing is blocking it at the mu site.

Trying staggering the dosages, by taking smaller dosages every half hour, like you would with tramadol or gabapentin.

 

[Raihiar]

thats good advice, thanks again
just too bad i can't leave the naloxone out of the mix though.. the tilidine pills have 8mgs of naloxone for every 100mg of tilidine (so you don't need a narcotics-script, a normal one is sufficient - even the most laid-back docs are very reluctant to give anyone a narcotics-script) and i can't really think of a way to seperate the two, these pills are ER and make a hell of a mess when soaked in water or something. i guess, with a bit of trial and error i could find a way eventually but tbh i don't really have the patience to do that atm.