Sweet UGT enzyme chart (inhibitors/inducers)

[Naggers]

Found this a couple days ago and posted it in a thread of mine over in OD but thought I'd share it with my EADD peeps too as I've been looking for a chart like this for ages.

http://www.pharmacologyweekly.com/content/pages/ugt-enzymes-medications-herbs-substrate-inhibitor-inducer

Here's a breakdown of the metabolism of codeine and morphine to help make use of the chart, though ofcourse it is useful for many more things! According to the footnote at the bottom, it is a work in progress and inhibitors/inducers are being added as they are made known to the authors. Apparently quinine and naproxen also inhibit UGT2B7 (source: bluelighter), which among other things will delay metabolism of hydrocodone and oxycodone and prolong the effect.

What I found interesting was that nicotine is an inducer of UGT1A1 which is responsible for converting morphine to M3G and M6G, though I haven't looked at whether or not those are particularly active metabolites yet. Anyone?

Also interesting is that Silybum marianum (milkthistle) is an inhibitor of a number of UGT isozymes including UGT2B7.

Anyone know any other inhibitors/inducers of UGT isozymes?

 

[Poodles!]

Nice!

Morphine is metabolised by UGT2B7 into M6G (~10%) and M3G (~60%). Of these only M6G is active as a μ receptor agonist and is much more potent than morphine with some studies suggesting it is responsible for the majority of morphines pain relieving effects. I remember one studying stating that it was between 45 and 800 times more powerful than morphine...

Unfortunately, M3G is evil. EVIL. It's a convulsant and causes hyperalgesia (increased sensitivity to pain). If you want to get hooked on opiods, don't go for morphine or heroin... M3G will build up in your system and hyperalgesia cannot be good for withdrawals. Niether are seizures if you're prone to them. (I guess for many people this is easier said than done)

It maybe worth noting that I usually take a fair bit of Milk Thistle (250+mg silymarin) with my pods (it's also a CYP3A4 inhibitor) and I've noticed NO potentiation. Grapefruit is still king. Shame it doesn't work with morphine by itself, although I usually use straight morphine to top up my pods (too expensive otherwise).

 

[Mental Kenny]

Milk thistle works wonders as a potentiator for ketamine and methoxetamine, scaringly so, actually, especially with the MXE, when taken at least an hour before, if you take more than 200 mgs of the extract you will definately notice an increase in effects, especially in lenght.

It also enhances kratom, doesn't make it stronger or more euphoric but it definately makes it last longer.

Word of note before you try it with dissociatives, as it knocked me off my ass on several occasions.

 

[monstanoodle]

Nice find
Just a thought - Over in Advanced Drug Discussion you will most definitely get many more educated replies (not to say that you're not getting them here!) but just that if you would like it to be moved over there then let one of the mods know
It purely seems the most logical place for such a topic - And I am a Vulcan so I'm all about that logic n shit n shtuff

Note on Milk Thistle - I remember reading many posts on here in the past that it potentiates Methadone by quite an amount, possibly on either it's Opioid agonist or NMDA antagonist action or both, but yes you should be careful if you're planning on using it in such a way.

 

[Naggers]

Sound logic my noodly friend!

I'm never sure if things are 'advanced' enough for ADD. Whenever I go for a browse over there I come away with my head hurting, I'm still a noob when it comes to chemistry.

Send this bad boy on its way!

 

[monstanoodle]

Eeee yes I know what you mean, they're all a bunch of pretentious arseholes over in ADD, smoking pipes of Lavender and drinking Chardonnay - speaking of it's zesty camphor flavours
(I jest, good people of ADD ) I'm reeling this badbwoi over to you as you will likely be able to help more
Hope yer all good over there folks!


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