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Codeine Extraction

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I don't understand the cimetidine. You say it inhibits metabolism, so the drug stays in the system longer. Isn't this what happens with promethazine? Or is the idea that promethazine is only a weak inhibitor, whereas cimetidine is a strong inhibitor?
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They inhibit two different enzymes. Promethazine inhibits CYP2D6, whilst cimetidine inhibits CYP3A4.

Codeine is a prodrug; it's converted into morphine by the liver via CYP2D6. So promethazine would stop as much codeine being converted into morphine.

CYP3A4 metabolizes opioids into less useful substances. By inhibiting that, less of the drug is initially metabolized and goes into the blood stream, and it takes longer for your liver to metabolize what is in your body.

You've got the idea in your edit: that the morphine that codeine is converted to is increased in half-life and blood concentration somewhat. Except that CYP2D6 only demethylates codeine into morphine, CYP3A4 is what then metabolizes both of those into useless things.

I'm very tired and out of it right now so I will have to come back to this and see if it makes sense in a few hours. :)
 
^Yeah makes sense, thanks. Actually after I wrote that I checked out cimetidine on MIMS, it lists a bunch of enzymes it inhibits and one of them was CYP3A4. Grapefruit juice inhibits CYP3A4 as well, doesn't it? In a sense making it more of a true 'potentiator' than promethazine.

I think that's why I didn't get much from codeine the first few times - I was always taking 50mg promethazine beforehand :P

I always thought it was great that we could get promethazine here but you can't in the USA. But you can get cimetidine there whereas its Rx only here. I think I'd rather have the cimetidine and take another anti-histamine.... having said that though, if all cimetidine is doing is increasing efficacy then one could just take more codeine, as that is available here, and enjoy the synergy with promethazine taken at t+10 ;)

Ah, the vagaries of OTC meds... :)
 
^ Yes, that's exactly what I was about to point out as well... that cimetidine is Rx only here whilst it's OTC there, but we have OTC promethazine and they have to get it Rx'd. :D

Using GFJ to mess around with the half-life has never really done much to opioids I've found, I tend to get harder hit by them though then others and codeine effects me for hours after dosing anyway. Promethazine is great to add on though. :)
 
^Reading through the GFJ FAQ you mention that GFJ may also be a 2D6 inhibitor, and link to an article. The link times out on me though - do you have a copy of that article or can you summarise what it said to lead you to that conclusion?

Kind of keen to try GFJ next time with codeine, not expecting wonders though. Will definitely keep using promethazine though, I find 50mg is enough to keep the itches at bay but will probaably try 75mg next time for added sedation. I've also found that breaking the tabs up with your front teeth brings on the promethazine quicker, which is great because as soon as you feel the come up from the codeine you can take the promethazine and get the effects pretty quickly. :)

EDIT: Btw, this is the article that was linked to.
 
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Mr Blonde, what are the effects of repeated use of a drug on the CYP2D6 enzymes. What I mean is do the enzymes play any part in tolerance and addiction?? Can you deplete your enzymes from over-use? Would liver damage or hepatitis change your absorption of drugs?
 
Hi all,

I was wondering how much water everyone uses for their pills? ie how much water to use per 8/500 pill for a CWE?

Thanks,

SS
 
I generally use 50ml to initially dissolve the pills, then another 20ml or so just to wash out the cup and make sure I get all of the gunk into the filter. I found once I got up into the 30+ pills range I needed an extra 10 or 20ml to dissolve the pills, otherwise it wasn't viscous enough.
 
^ Thank you.

I'm using 64 pills at 8/500. I didn't quite understand your answer though. I read somewhere that 2 ml per pill was a good guide. Would you/others agree with that?

I think its important since too much water could be in excess of whats needed to dissolve the codeine adequately, therefore leaving 'excess' water to dissolve more of the APAP. The correct balance would in theory allow all the codeine to dissolve while limiting the amount of APAP left to the absolute minimum.
 
Well I read (on erowid I think), that 70ml of water will absorb 1 gram of APAP at 31 degrees celcius, so I figure if I keep it around that I should be A-ok. 64 pills might be a bit trickier, but if you do 100ml or so you should be fine.

And uh, I'm gonna assume you already have an opiate tolerance, if not that dose is wildly excessive.
 
Yeah 2ml per tab would be about right I would think. If you're particularly worried about paracetamol maybe get a stronger brand next time. AFAIK the strongest OTC brand is 15/500, and there are several with 12.8/500. Using 12.8mg tabs you would only need about 2/3 of the tabs for the same codeine content, meaning less water and therefore less paracetamol.

Crankinit, I think that solubility data is from the chart that you see on a few sites that lists the solubility of codeine, paracetamol and aspirin:

Solubility at 31C:
Aspirin 1g/100 ml
Acetaminophen 1g/70 ml
Codeine 1g/2.3 ml

Solubility at 21C:
Aspirin 1g/300ml
Acetaminophen 1g/150 ml
Codeine 1g/0.7 ml

So you can see that cooling that water down to 21C will reduce the solubility of the paracetamol by about half! So, serotonin_system, definitely use refrigerated water to dissolve/filter!
 
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Yeah that looks like the one I saw, I always refrigerate my water because of that, never hurts to be safe.

I've found most places give 8/500, I've yet to find anywhere that gives higher than 10/500 except one store that kept boxes of nurofen plus with 12.5mg on the shelf.

On that note, has anyone had any experience with stores asking for name/address when you buy large boxes? I know one guy who says the store asked for his details when he bought a 48 box of nurofen plus. Could just lie I guess, but thats kind of sketchy.
 
It may be different in different states; when I was doing the unsafe OTC list, I noticed that some products were schedule II in some states but schedule III in others (meaning they would have to take name/address). I am in SA and only once have been asked for name and address, and that was when buying a box of 96x10/500. Buying 12.8mg or 15mg is not a problem and can generally get in whatever size you want. Sometimes the sales assistants will even try to sell you the 96 boxes because it's better value :)

I have to say I was very surprised when asked for name/address for that box, I didn't think codeine was schedule III in SA. Maybe it's because they only had the 24's on the shelf and I asked for the bigger box!
 
Yeah maybe they only do it if it seems suspect. I'm in SA and have never had issues, but I've never bought more than a single 24 pack from one pharmacy.
 
Crankinit said:
Well I read (on erowid I think), that 70ml of water will absorb 1 gram of APAP at 31 degrees celcius, so I figure if I keep it around that I should be A-ok. 64 pills might be a bit trickier, but if you do 100ml or so you should be fine.

And uh, I'm gonna assume you already have an opiate tolerance, if not that dose is wildly excessive.
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Thanks a lot for your reply everyone, very helpful.

Re your comment about opiate tolerance, I have zero tolerance. I didnt think 512mg codeine was a huge amount, especially considering you likely lose some of that during the extraction...

I did it last night and felt pretty buzzing! However I am on 40mg citalopram which as i understand it inhibits the enzyme responsible for converting codeine to morphine, so maybe that's why I 'need' a larger dose.

Also, some1 mentioned getting tabs with more than 8mg codeine in them. Im in the UK and as far as I know thats all i can get from the pharmacy. Somebody correct me if Im wrong.
 
Crankinit said:
Yeah maybe they only do it if it seems suspect. I'm in SA and have never had issues, but I've never bought more than a single 24 pack from one pharmacy.
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You're in SA and have never seen above 10mg in a pharmacy? They are in every single pharmacy I go into!
 
serotonin-system said:
Thanks a lot for your reply everyone, very helpful.

Re your comment about opiate tolerance, I have zero tolerance. I didnt think 512mg codeine was a huge amount, especially considering you likely lose some of that during the extraction...

I did it last night and felt pretty buzzing! However I am on 40mg citalopram which as i understand it inhibits the enzyme responsible for converting codeine to morphine, so maybe that's why I 'need' a larger dose.

Also, some1 mentioned getting tabs with more than 8mg codeine in them. Im in the UK and as far as I know thats all i can get from the pharmacy. Somebody correct me if Im wrong.
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512 is a pretty huge dose, in fact most sources consider somewhere between 400mg - 500mg to be the ceiling dose, after which the body cannot convert any further codeine to morphine because all of the enzymes are inhibited.

I've never used above 350mg, and both times I took 350 it felt rather excessive, and I went through a 3 month period of daily codeine use which I'm sure at least contributed something of a tolerance. Sounds like there might be an issue with your citalopram though that's causing you to need higher doses.

You're in SA and have never seen above 10mg in a pharmacy? They are in every single pharmacy I go into!
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Really? That's odd, I've been to a fair few pharmacies (mostly in the CBD), and they all only seem to have 8mg/10mg. It's hardly a big deal though, it's so cheap that it doesn't matter much.
 
^ Wikipedia says the ceiling dose is calculated at 7mg/kg for males and 6mg/kg for females.

"Example: A 85kg male, bearing a height of 180cm is 5kg overweight, therefore the ceiling dose can be calculated by 7mg x (85-5)kg = 560mg and for a female of the same height and weight, 6mg x (85-5)kg = 480mg."

http://en.wikipedia.org/wiki/Codeine
 
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