• 🇬🇧󠁿 🇸🇪 🇿🇦 🇮🇪 🇬🇭 🇩🇪 🇪🇺
    European & African
    Drug Discussion

    Welcome Guest!
    Posting Rules Bluelight Rules
  • EADD Moderators: Shambles

News Severe Co-Codamol Shortage in the UK

4DQSAR said:
Well, technically there are two classes of compound in grapefruit juice (and orange peel - so Seville marmalade will also work) that blocks the action of CYP3A4.

So It stops N-demethylation. But the result is the same - more morphine (the active metabolite of codeine).

It certainly does make things like codeine act for longer as N-demethylation is an important pathway.

If anyone finds a CYP-2D6 inducer (the enzyme that performs the O-demethylation) which is safe and well-tolerated, that would likely win a Nobel Prize.
Click to expand...
I read so many conflicting opinions about whether white or pink grapefruit juice must be used, and whether it should be taken before, with, or after codeine. The same also applies to other things that block the action of the relevant enzymes. Things like cimetidine-tagamet, which I guess is mainly theoretical now, since it's no longer incredibly easy to import a vast range of POMs like this from online pharmacies based in India.

Perhaps now it's long since defunct I can mention 4NRX (or something like that). What an amazing website that was for ordering a vast array of POMs from India. Never any bother from UK Border Force either. How much things have changed! :(

Perhaps @4DQSAR could comment on my first sentence?
 
@Bleaney - I'm sorry but I don't know. I just drink pink grapefruit juice because that's all that's available in the two shops that sell it that I can physcally get to.

I can go look into it for you if it matters.

Always happy to help a friend.
 
Last edited:
Temperature (°C) Approximate Solubility (g/L) Parts of Water required per 1 part Codeine Phosphate
0°C ~230 – 250 g/L ~1 in 4 to 4.3 parts
5°C ~270 g/L ~1 in 3.7 parts
10°C ~310 g/L ~1 in 3.2 parts
15°C ~350 g/L ~1 in 2.8 parts
20°C 400 g/L (Official Standard Point) 1 in 2.5 parts
25°C ~430 – 450 g/L ~1 in 2.2 parts
30°C ~480 – 500 g/L ~1 in 2.0 parts

I don't know how to make neat tables on BL. I spaced it all out but I'm sure people can manage that for themselves.

The KEY part is that codeine phosphate is VASTLY more water-soluble than paracetamol in dH2O. If a buffer is added e.g. soluble tablet formulations, the solubility of paracetamol goes up a lot hence should be avoided and one of the above references just shows how shifting the pH a little to the basic can result in vast changes to underline why soluble formulations are verboten.
 
Last edited:
4DQSAR said:
@Bleaney - I'm sorry but I don't know. I just drink pink grapefruit juice because that's all that's available in the two shops that sell it that I can physcally get to.

I can go look into it for you if it matters.

Always happy to help a friend.
Click to expand...
No it doesn't matter very much right at this moment, as I'm using quite a lot of kratom r/n anyway, and that completely blocks all good effects from lighter opiates such as codeine for a week or more, in my experience.

I just wondered if you knew off the top of your head. No need to look into it if not, as I probably wont be using codeine for some time.

(Barring any unforseen hospital admissions and enforced kratom abstinence, or any other injuries or pain conditions etc.)
 
Bleaney said:
No it doesn't matter very much right at this moment,
Click to expand...

As far as I know, in all of the human experiments I've read, no mention of the specific type of grapefruit juice is given (which on reflection it possibly should have been) but both contain furanocoumarins and be it 4 x 100mL in the elderly of 3 x 200mL in adults, the results were almost total inhibition of N-demethylation. Probably less would work but the experiments were aimed at real-world cases.

Do people drink grapefruit juice in smaller quantities than 100mL? I don't know...
 
Shambles said:
I’ve always been under the impression that white grapefruit juice is more effective.
Click to expand...

It could well be. But if 200mg [TID] or 100mg [QID] of an unspecified colour of grapefruit juice is sufficient to essentially irreversibly (non-competitively) block 100% of CYP3A4 enzymes, that's a real-world scenario.

I seem to recall in the dim and distant past grapefruit juice concentrate used to be a retail product. Even now with few exceptions anywhere from 60-85% of the water is removed as shipping water is kind of wasteful.

Niche but true - After Kenneth Halliwell murdered Joe Orton, he washed down 22 x 100mg Nembutal capsules with a can of undiluted grapefruit juice. Now why isn't clear but I have it on reasonably good authority that long before the action of the furanocoumarins was understood, if alcohol was unavailable, it was lore at the time that the juice was some sort of 'booster'.
 
Well, having successfully detoxed from my extremely mild codeine habit, I then stumbled upon 100 x 50mg tramadol HCL tablets.

That shit is weird.

First couple of days were great, felt like going up on MDMA during the day, followed by proper gouching at night.

Quickly turned to shit thereafter.

That stuff hits hard. After only a week at approx 500 - 600mg/day, the nightime leg shennanigens have been horrendous, and i've been mitigating it with yet more codeine.

A harsh reminder of why I never liked tramadol...
 
F.U.B.A.R. said:
Well, having successfully detoxed from my extremely mild codeine habit, I then stumbled upon 100 x 50mg tramadol HCL tablets.

That shit is weird.

First couple of days were great, felt like going up on MDMA during the day, followed by proper gouching at night.

Quickly turned to shit thereafter.

That stuff hits hard. After only a week at approx 500 - 600mg/day, the nightime leg shennanigens have been horrendous, and i've been mitigating it with yet more codeine.

A harsh reminder of why I never liked tramadol...
Click to expand...
There seems to be lots and lots of 30mg dhc not on the street but not to hard to find
I don't move in opiate circles and I know users will use them sometime for withdrawal
My wife has tennis elbow and she is in awful pain ,they gave her amatriptyline which didn't help
Without enquiring to hard I managed to get her 30mg dhc
 
4DQSAR said:
Niche but true - After Kenneth Halliwell murdered Joe Orton, he washed down 22 x 100mg Nembutal capsules with a can of undiluted grapefruit juice. Now why isn't clear but I have it on reasonably good authority that long before the action of the furanocoumarins was understood, if alcohol was unavailable, it was lore at the time that the juice was some sort of 'booster'.
Click to expand...
Now there's a whole other debate: is it best to take the grapefruit juice before, at the same time, or after the variety of different substances it appears that g/f juice can potentiate?

I've read so many conflicting accounts and experiences regarding this.
 
The answer is almost certainly 'no'.

It seems quite specific to non-competitive inhibition of CYP3A4 i.e. the one responsible for N demethylation. But it's a fluid with plenty of sugar and likely dilutes barbiturates so vomiting doesn't occur UNTIL the person is unconscious.
 
Bleaney said:
Now there's a whole other debate: is it best to take the grapefruit juice before, at the same time, or after the variety of different substances it appears that g/f juice can potentiate?

I've read so many conflicting accounts and experiences regarding this.
Click to expand...

I was always under the impression that you should down the grapefruit juice approximately an hour before taking the pills.

That’s what I’ve always done and works fine for me. YMMV and all that, naturally.
 
The oxycodone isnt a green tablet is it Perkins? That's the nitazenes that have killed about 250 across the UK - I got 5 "40mg oxycodone" for £35. Scraped a tiny bit off it under my thumbnail and licked it and was very ill for about 24 hours.
 
Shambles said:
I was always under the impression that you should down the grapefruit juice approximately an hour before taking the pills.

That’s what I’ve always done and works fine for me. YMMV and all that, naturally.
Click to expand...

There's bioperine you can buy in health shops - think it does the same thing as grapefruit juice. Supposed to be safer than grapefruit juice cos it wears off in a few hours while grapefruit leaves your liver fucked for 3 days and needing to manufacture new enzymes I vaguely recall
 
Cream Gravy? said:
That's sadistic as fuck (amatryptaline for pain)
Click to expand...

Worked for me - but in both cases it's anecdotal evidence.

But for neuropathic pain specifically, it can be very effective.

Amitriptyline for neuropathic pain in adults - PMC

This is an updated version of the original Cochrane review published in Issue 12, 2012. That review considered both fibromyalgia and neuropathic pain, but the effects of amitriptyline for fibromyalgia are now dealt with in a separate review. ...
pmc.ncbi.nlm.nih.gov pmc.ncbi.nlm.nih.gov
 
You must log in or register to reply here.
Top