• BASIC DRUG
    DISCUSSION
    Welcome to Bluelight!
    Posting Rules Bluelight Rules
    Benzo Chart Opioids Chart
    Drug Terms Need Help??
    Drugs 101 Brain & Addiction
    Tired of your habit? Struggling to cope?
    Want to regain control or get sober?
    Visit our Recovery Support Forums
  • BDD Moderators: Keif’ Richards

Do u think there really is a codeine ceiling dose?

A

Anon54

Ex-Bluelighter
Joined
Jun 11, 2010
Messages
861
I found this quoted from wikiepedia which claims there is now evidence that there is no codeine ceilng dose:
Codeine is metabolized to 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 codeine-6-glucuronide (C6G) is the primary active compound.[22] Claims about the supposed "ceiling effect" of codeine doses seemed to rest on the assumption that high doses of codeine saturated CYP2D6, which prevented further conversion of codeine to morphine, which is simply incorrect since we now know that codeine-6-glucuronide (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,[23] 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.[24] 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" metabolisers).
Click to expand...

Ive tried cwe on a pack of panadeine forte before which was 600mg all up & it did feel stronger but I hadnt had any opiates for a while.
I now occationly take 400mg as needed which i can get from one pack but codeine is a little weak.
it also states on the wikipedia codeine page that 200mg of codeine is equal to taking 30mg of morphine so that's not to bad.
would be interesting to know if I were to take 800mg if Id get a better effect.
maybe furter codeine to morphine conversion would stop after approx 450mg but u could still get more from the codeine-6-glucuronide metabolite.
Ofcourse the side effcts would be greater, but I dont get to many from 400mg
So who has tried higher doses than approx 450mg and who thinks they actually got a stronger effect?

Doses can range from 30 mg up to 400 mg. LD50 for codeine is 800 mg in a average nontolerant person. At doses of > 250 mg adverse effects tend to arise, including intense itching, flushed skin, dizziness, sedation, nausea and vomiting
Click to expand...

this is also quoted from erowid which may be something to be concerned about if trying a higher dose. it seems like a very low LD50 imo. This information couldnt be right, could it?
 
Last edited:
That quote from erowid is incorrect. I myself have dosed 1800mg codeine plenty of times.

Also the ceiling dose for codeine is the amount that your liver can metabolise into morphine at any given point. This is not the sole reason for codeine analgesia. So when you go above 400mg the dose response range drops but the effects still increase.
 
^ It's now thought to believe it is more than the morphine that is responsible for codeines affects.. including codeine itself if i'm not mistaken.
 
I think the ceiling dose is highly dependent on the individual, and it isn't an impenatrable ceiling.
 
well I took 600mg today & it felt slightly stronger.
i just obtained some valium. wish i have them before the opiate. that's the proper order to take em.

codeine/valium are such weak drugs. i dont know why i bother with either of them. I mean alcohol is much stronger but i hate waking up with a headache. hmm i guess that's what the valium and codeine are for
 
I find codeine to work above the supposed ceiling dose, but I do find the effects change with higher doses, so my preferred dose is between 400-800mg. I find higher doses more stimulating and doses between 400-800mg more sedating, which I suppose is due to the varying ratios of metabolites at different doses.
 
ok so codeine stops converting to morphine at approx 450mg
the question is how strong are the other metabolites of codeine
400mg of codeine according to the BL converter equals 40mg oc. that's alot & I dont think it's correct.

I had 600mg today & i didnt seem to effect me much at all but I had GFJ which may have made have effected the conversion to morphine negatively.

I was only drinking the GFJ cuz i had 150mf of diaz (I know its alot but i barely feel anything from it even though i only take it a few times a month) might have to switch to xanax to get an effect... anyways...

in the past ive had stronger effects taking up to 600mg.
it would be good to have an equivalence chart which included the metabolites of codeine too.
maybe on wikipedia it has links to the metabolites & gives a fair idea of how it compares to other opiates.

I tolerate even 600mg of codeine with no side effects at all so i could easily tolerate over 1g.

sorry to bump this thread but it's a cheap alternate for when ya dont have stronger opiates like h or oxy but 400mg just doesnt cut it

according to wikipedia
codeine-6-glucuronide (C6G) is the primary active compound. but it doesnt have a link to any info. i'll google it. it doesnt have a dose for example what 400mg of codeine metabolites into codeine-6-glucuronide

If anyone could find out for example how muich 100mg of codeine metabolises to codeine-6-glucuronide & what equivelance it has to other opiates that would be a big help
OK i found Codeine-6-glucuronide (C6G) is a major active metabolite of codeine and may be responsible for as much as 60% of the analgesic effects of codeine. C6G exhibits decreased immunosuppressive effects compared to codeine.[1] During its metabolism, codeine is conjugated with glucuronic acid by the enzyme UDP-Glucuronosyltransferase-2B7 (UGT2B7) to form codeine-6-glucuronide.
Click to expand...
there actually was a wiki page. so probably makes up for 1/2 of codeine's effects.Some sources say up to 70%. now to try to find an opiate conversion chart that includes it
so we can work out the dose. say u have 1g of codeine that would equal about 700mg codeine-6-glucuronide. 1g of codeine would equal 100g morphine. wonder how much morphine codeine-6-glucuronide equals?

can anybody help me find this out because taking doses like 1.2g of codeine may actually work really well
http://onlinelibrary.wiley.com/doi/...+4+Feb+from+10-12+GMT+for+monthly+maintenance
heres what ive found. I dont understand it. maybe this should be in ADD
 
Last edited:
Anon54 said:
now to try to find an opiate conversion chart that includes it
so we can work out the dose. say u have 1g of codeine that would equal about 700mg codeine-6-glucuronide. 1g of codeine would equal 100g morphine. wonder how much morphine codeine-6-glucuronide equals?
Click to expand...
You have all the info you need right there bud. 8)

I did a touch of research to confirm which shows C-6-G is 60% as strong as codeine alone (at least for analgesia in rats by IV haha). link

Unfortunately you have to remember that codeine itself is also thought to be active (not just a prodrug) so you're going to run into a lot of difficult trying to do whatever it is you are trying to do. I'd recommend conservative personal bioassay.
 
Maybe god created codeine that way - otherwise we would see codeine addicts taking grams of codeine a day. Same thing with the fact, that there doesn't seem to be any substances, that would induce codeine's metabolia in a way, that a higher percentage of codeine would transform into morphine in the body. :p
 
If you have elevated liver enzymes (abuse of drugs that induce the livers actions), you can get as high as you want if you have enough...

I always run into the dilemma of not having enough and I am a low level alcoholic. Meaning, I have more than three beers, but less than 10 everyday.

Lifestyle I say, is going to be your biggest determining factor.
 
allegator said:
You have all the info you need right there bud. 8)

I did a touch of research to confirm which shows C-6-G is 60% as strong as codeine alone (at least for analgesia in rats by IV haha). link

Unfortunately you have to remember that codeine itself is also thought to be active (not just a prodrug) so you're going to run into a lot of difficult trying to do whatever it is you are trying to do. I'd recommend conservative personal bioassay.
Click to expand...
so ya saying that any dose higher than the dose of codeine that cant convert to more morphine is 60% as strong. that's still pretty good. for example even if it's half as strong? taking 1.2g of codeine would be twice as strong as a 400mg dose.
if CG6 is up to 70% of codeine metboolites all we would really need to find is an opiate conversion chart which includes CG6 which I dont think there is one.
Ive never tried taking extreme doses of codeine like 2g or anything so i have no idea.
has anyone tried high doses like that?
u'll loose the morphine conversion at 400mg but u'll still get an effect from the CG6. Just dont know how potent an opiate it actually is.
For HR purposes the LD50 for codeine is only 800mg im fairly certain this cant be correct. maybe after 400mg the mechanism of action changes & becomes more dangerous.
I had a break from opiates for a few yrs. i did a cwe on a pack of panadeine forte. that's 600mg. it got me really high actually but i didnt even get sick. I cant imagine 800mg killing half the ppl who took it even if they'd never touched a drug in there life.
the LD50 for oxy is only 55mg. I only took codeine a few times over a year & got my hands on a 80mg OC. i chewed a 1/3 of the pill thinking it was going to be strong. but over the next few hrs ended up chewing the whole pill. I had pretty much no tolerance at that time. I didnt even throw up or anything. Where do they get these LD50s from?
if 55mg of oxy kills half ppl who take it who have no tolerance why did they once have 160mg OCs.
 
Last edited:
i also thought the 800mg ld50 seemed a bit off. the first time i took codeine i did about 350mg and only got a bit nauseous.

Isn't it the case that some potentiators (i think 1st gen antihistamines) block the conversion to morphine (by inhibiting cyp2d6) yet still add to/potentiate the effects of codeine? I did some research and i think this is right. I usually take diphenhydramine before codeine and find it is more euphoric and enjoyable rather than less.
 
http://wikipathways.org/index.php/Pathway:WP1604
Codeine-6-glucuronide has a similar affinity to codeine for the mu opioid receptor
Click to expand...
Between 0-15% of codeine is O-demethylated to morphine, the most active metabolite, which has 200 fold greater affinity for the mu opioid receptor compared to codeine.
Click to expand...
CG6 has a similar affinity to the mu opioid receptor to codeine & morphine is 200 times stronger than morphine
so after the dose which stops the conversion of codeine to morphine & the main active metabolite is CG6 than taking an extra 400mg would only equal 2mg of morphine excluding the other active metabolites.
so basically it would seem that taking more than the ceiling dose it a waste.
although this is quoted from wikipedia.
Codeine is metabolized to 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 codeine-6-glucuronide (C6G) is the primary active compound.[20] Claims about the supposed "ceiling effect" of codeine doses seemed to rest on the assumption that high doses of codeine saturated CYP2D6, which prevented further conversion of codeine to morphine, which is simply incorrect since we now know that codeine-6-glucuronide (C6G) is the main metabolite responsible for codeine's analgesia
Click to expand...
& if CG6 is responsible for most of codeines analgesia it must be stronger than 200 times weaker than morphine.
This site says 80% of codeines analgesia is due to CG6 & says it's responsilbe for codeines effect & has no effect due to its conversion to morphine suggesting there is no ceiling effect
http://www.ncbi.nlm.nih.gov/pubmed/11092114
Abstract

Eighty per cent of codeine is conjugated with glucuronic acid to codeine-6-glucuronide. Only 5% of the dose is O-demethylated to morphine, which in turn is immediately glucuronidated at the 3- and 6-position and excreted renally. Based on the structural requirement of the opiate molecule for interaction with the mu-receptor to result in analgesia, codeine-6-glucuronide in analogy to morphine-6-glucuronide must be the active constituent of codeine. Poor metabolisers of codeine, those who lack the CYP450 2D6 isoenzyme for the O-demethylation to morphine, experience analgesia from codeine-6-glucuronide. Analgesia of codeine does not depend on the formation of morphine and the metaboliser phenotype
Click to expand...
s
o much conflicting information. I know that 50%-%80 of codeine is metabolized into CG6 I just wanna a conversion of CG6 to morphine the site at the top says its 200x weaker than morphine but the next quoted site says it's responsible for most of the effect of codeine. 8(
so that would mean 160mg CG6 equals 30mg of morphine..... ehhh i dont know....
maybe i should just try drinking 800mg of codeine & see if it's twice as fucken strong
 
Last edited:
RobotRipping said:
i also thought the 800mg ld50 seemed a bit off. the first time i took codeine i did about 350mg and only got a bit nauseous.

Isn't it the case that some potentiators (i think 1st gen antihistamines) block the conversion to morphine (by inhibiting cyp2d6) yet still add to/potentiate the effects of codeine? I did some research and i think this is right. I usually take diphenhydramine before codeine and find it is more euphoric and enjoyable rather than less.
Click to expand...
yes dph is a true potentiator of codeine. not just a combo of sedation
http://www.bluelight.ru/vb/threads/191439-Awesome-CYP-450-Chart
 
well Ive got 800mg of codeine in the freezer now. double my dose. i'll edit this post & let u know if it's stronger. twice the dose i should feel something?

OK so Im back. I drank it all in one sip. very very bitter!!!:|
tasted much better than PST though. that stuff takes me 10 mins to skull down.

anyways it defensively feels strong than my usual 400mg dose. I think it stops the 10% conversion to morphine at about 450mg but after than ya still getting the other active metabolites. CG6 for example. & I think actually hydromorphone is actually one too.

Ive had whats listed as the LD50 for codeine but ive got a feeling that nothing going to happen to me. I dont know where they get there LD50 info from but that obviously wrong.

I didnt have codeine for well over a year & i did a cwe on a pack of panadeine forte with 20 pills containing 30mg codeine/500mg apap. so 600mg. I started nodding a bit & felt my eye were heavy so my tolerance had obviously gone down but i was far from ODing. I didnt even feel nausea.
I used 2 out of the 3 packs of codeine today. I could have gone for 1.2 grams. but the soluble apap might be a small concern. but yeah im feeling pretty good.
 
Last edited:
You must log in or register to reply here.
Top