Misc quinine and tramadol (tonic water)

[mike.vick]

Tonic water has about as much quinine as soda has caffiene - 83mg/L - does it potentiate the opiate effects of tramadol by giving more o-Desmethyltramadol metabolite- the potent MU-opiate agonist.

 

[Slow_Mobius]

What's your rationale for using it as a potentiator? The only reason that I can think of would be if it's inducing whatever enzymes are metabolizing tramadol to its demethylated metabolite.

 

[mike.vick]

What's your rationale for using it as a potentiator? The only reason that I can think of would be if it's inducing whatever enzymes are metabolizing tramadol to its demethylated metabolite.

It acts as a weak pg-p inhibitor, about 1-30th the strength of quinidine.

 

[Slow_Mobius]

I didn't think tramadol had a problem crossing BBB. I also think you would need to take a ton of quinine to get a significant amount of PGP inhibition

 

[mike.vick]

Oh, I got you. Thanks. Grapefruit-juice maybe? CYP-inhibitor, I don't know if you want an inhibitor or an inducer in order to get more o-desmethyltramadol in-vivo.

 

[Slow_Mobius]

Oh, I got you. Thanks. Grapefruit-juice maybe? CYP-inhibitor, I don't know if you want an inhibitor or an inducer in order to get more o-desmethyltramadol in-vivo.

You would want an inducer. An inhibitor would give slow down metabolism to o-desmethyltranadol so you'd probably end up with less opioid and more SNRI effect

 

[mike.vick]

You would want an inducer. An inhibitor would give slow down metabolism to o-desmethyltranadol so you'd probably end up with less opioid and more SNRI effect

Thank you, sir!

 

[kleinerkiffer]

You would want an inducer. An inhibitor would give slow down metabolism to o-desmethyltranadol so you'd probably end up with less opioid and more SNRI effect

This
And by taking a PGP inhibitor you'd let more than just the drug reach your neurons and imo it's not worth the side effects

 

[Lorne???]

This
And by taking a PGP inhibitor you'd let more than just the drug reach your neurons and imo it's not worth the side effects

You are gonna, at least ideally, want a selective CYP3A4(and also 3A5, probably and again, preferably) Erytrhimycin fits this bill, and I think(?) telithoromycin is even more potent inhibitor( though Z pack, whichever mycin it is, is pretty much useless and should be avoided)

Erythromycin is a moderate- strong, and it is more selective for CYP3a4, opposed to grapefruit juice(100% white, although Ocean Spray no longer makes pure white grapefruit juice, instead a mixture which is primarily (or would seems to be) White GFJ, with some Red GFJ mixed in(15-30% is fair enough guess, but just that, a guess).

Tonic water is useless as mentioned and pure quinine would be counter-productive.

Cimetidine is a well known inhibitor, but, although primarily effective against CYP3a, it also inhibits other enzymes, in particular CYP2D, which you do not want, of course.

Since potent and selective inhibitors are RX only, and some simply impractical, you are stuck with WGJ, or the more common hybrids.

WGJ itself is a potent 3A4 inhibitor at high amounts, but also inhibits other enzymes, including 2D(though weak-moderate, depending upon dose) and I think 1A, or 1A2.

Overall, WGJ THAT IS PURE I your only practical OTC option, and 3A4 inhibition beats out 2D, especially if your not consuming ridiculous amounts.

But honestly, unless you're a poor or intermediate CYP2D metabolizer, Tramadol works fine on its own, and if this is Sone attempt to beat a high tolerance, won't work.

And M1 has a similar binding affinity to oxycodone, but this does not make it a potent MU agonist, albeit probably underrated.

I would take it on its own, Tramadol does lower the seizure threshold, and has a typical TMAX of 2-4h. Of course, it also has 3 or maybe even 4 metabolites.

If you get Erythrymycin, and safely confirm you are not allergic, a double dose would work just fine(might need an anti-emetic though)

And finally, forget 2D inducers, they practically don't exist, and the very few are RX only, sometimes dangerous, and unlike inhibitors, which have an almost immediate effect(but are still more effective daily), inducers require 2-3 days to really start working fully. Sorry, limited options. Now, methadone is a different story

 

[mike.vick]

^^^^ WOW, thanks.
If only I could get some Glutethimide I'd be rollin' - 2d inducer and barbituate... The good ole days.