Opioids req: BL User experience/ advanced knowledge of Codeine "Ceiling Limit" to dose

[Cartesia]

req: BL User experience/ advanced knowledge of Codeine "Ceiling Limit" to dose

OK I've been doing codeine a long time.... 8 years now? 9? The first few are a blur. I gather I'm one of the lucky ones in terms of metabolism into morphine.

Anyhow, past experience led me to believe there was a ceiling dose to codeine. From what I've read it varied widely, mine seemed to kick in somewhere between 400 - 500 mg. To give you an idea of my conversion rate at the point I was taking 500mg doses of codeine I had to take 80mg oxycodone (no time release) to get to the same place. This isnt an exact comparison due to the difference in feeling, but close enough to give an idea. In neither case was I anywhere near nodding, which I used to do (only in the beginning, and rarely) at just 150-200mg codeine.
I started pushing my dose over time up to a little further than 500ish as my tolerance built, not achieving any enjoyable gains, but noticing a slight improvement up to about 700mg. It was never really 'worth' upping the dose beyond what I thought was the ceiling, but you know.. any tiny gain.

Needless to say at this point I was doing the most efficient CWEs humanly possible.

Now as I understand the metabolism of codeine to morphine is inhibited by morphine itself, but codeine-6-glucuronide which (may) has/have a very mild analgesic/euphoric effect is still metabolised. Or at least this was what people proposed from my readings.

In the neverending quest to get high like the old days, I've started to wonder if it's possible to take a high enough codeine doseage to push the codeine-6-glucuronide levels up to a level that will actually have a strong impact.


Just wondering what people's personal experience with the so called 'ceiling' dose of codeine are - in general and particularly if you've experimented with going way beyond it. My first experiment is 1000mg, minus loss through inneficiency, which - conservatively - I'd say would be no more than 10%, probably more like ~5.

Unfortunately nobody really knows to be able to tell, but it would be great to hear from people who have almost no 2d6 to hear about their experiments with high codeine dose...

Can anyone think of any concerns?
Obviously liver and kidneys cop a beating, but I've had them tested recently and all is fine. so far.
Histamine reaction has never been an issue for me, I've not been itchy/etc. There's certainly no chance of respiration failure.. 750ish mg doesn't get me high anymore so much as it brings my stress down to half the level it would otherwise be at. It looks like alot when put in writing but it's only a 25% increase.

 

[sekio]

In the neverending quest to get high like the old days, I've started to wonder if it's possible to take a high enough codeine doseage to push the codeine-6-glucuronide levels up to a level that will actually have a strong impact.

not really, the other effects of codeine (histamine release etc) will become pretty unbearable at that level.

Obviously liver and kidneys cop a beating,

if you avoid apap usage they take less of a beating than you would expect.

honestly, if 3/4 gram of codeine doesn't do anything more, you need to pick a new drug.

 

[laCster]

^this

the ceiling effect of codeine is usually based on the theory that saturating the 2D6 enzyme inhibits further morphine production; according to wiki, morphine is not the only metabolite to play a significant role in codine base analgesia. rather, glucuronized codeine (C6G) provides most of codeine's pain killing effects. on the other hand like sekio stated, taking too much codeine will produce a major histamine reaction ruining the opiate euphoria from annoying side effects . i agree with sekio, you need to just move on to a stronger opiate like hydrocodone or oxycodone instead of wasting your time with codeine.

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

Codeine is metabolized to codeine-6-glucuronide (C6G) by uridine diphosphate glucuronosyl transferase UGT2B7, and, since only about 5% of codeine is metabolized by cytochrome P450 CYP2D6, the current evidence is that C6G is the primary active compound.[10] Claims about the supposed "ceiling effect" of codeine doses are based on the assumption that high doses of codeine saturate CYP2D6, preventing further conversion of codeine to morphine, however it is now known that C6G is the main metabolite responsible for codeine's analgesia.[11] There is also no evidence that CYP2D6 inhibition is useful in treating codeine dependence,[12] though the metabolism of codeine to morphine (and hence further metabolism to glucuronide morphine conjugates) does have an effect on the abuse potential of codeine.[13] However, CYP2D6 has been implicated in the toxicity and death of neonates when codeine is administered to lactating mothers, particularly those with increased 2D6 activity ("ultra-rapid" metabolizers).[14][15]

 

[Cartesia]

I used to agree with both of you,

but...

my experience over the past few days has been exactly the opposite of what everyone expects. I've been able to get a lot further than I have been in years. I definitely noticed diminished gains back when I went from ~350 up to ~500-750, but this extra bit has significantly increased the euphoria/etc.
Ive been actually *high* for the past few days. Not just 'feeling ok and not withdrawing'.

It's hard to know whats going on technically, unfortunately. I see they've decided now that C6G is an important factor in codeine.. That wasn't the case when I looked many year ago - it was just an idea/ unproven possibility. I'd say given my reaction to codeine compared to that of people I've introduced to it theres a good possibility that I am an ultra-rapid metabolizer through 2d6. Whether that or the prolonged nature of my use has any effect on ceiling dose I have no idea.

Another thought is most people's experience is probably limited to beneath the 'ceiling', and directly above it. I never bothered to push further for a long time because I thought it would be a waste and I imagine most other people think the same, so it may just be a case of having to push beyond it by a lot. Still just guessing but to me it seems like its about the morphine:c6g balance... the lower dose the morphine is doing the work, but then as you get up higher there's no increase in morphine amount due to 2d6 inhibition. c6g is less effective, so it takes a larger dose bump to have a similar strength of effect.

Also like I said, the histamine reaction has never really registered to me. at ~1000mg I'm a little itchy. Not at the point where I *need* to itch, but I do every now and then and find it rather enjoyable. I've seen people itch themselves raw on ~200mg, it just doesn't happen to me.

Oxy/morphine are quite hard to come by here, and waaay outta my price range... As much as I'd love to start doing some real dope I'm going to consider myself lucky that I don't have a source for such things. It's not like the states over here, you can't just drive down to a dodgy area and score from a stranger on the street.

 

[Cartesia]

Another point to mention is I've done a little bit of play with dosing about 300mg 3-4 hours after taking a 1000mg dose. While normally with codeine there is a kind of 6 hour window where redosing is almost completely ineffective, again at this level it seems to work just fine, bringing me at least back to the peak of the experience, or even a little further depending on the timing. IMO this is another indicator that it's C6G doing most of the work in these large doses, and morphine doing the work at low doses.